-
1
-
-
0031469952
-
Expression cloning and receptor pharmacology of human calcitonin receptors from MCF-7 cells and their relationship to amylin receptors
-
Chen W.-J., Armour S., Way J., Chen G.C., Watson C., Irving P.E., Cobb J., Kadwell S., Beaumont K., Rimele T., Kenakin T.P. Expression cloning and receptor pharmacology of human calcitonin receptors from MCF-7 cells and their relationship to amylin receptors. Mol. Pharmacol. 1997, 52:1164-1175.
-
(1997)
Mol. Pharmacol.
, vol.52
, pp. 1164-1175
-
-
Chen, W.-J.1
Armour, S.2
Way, J.3
Chen, G.C.4
Watson, C.5
Irving, P.E.6
Cobb, J.7
Kadwell, S.8
Beaumont, K.9
Rimele, T.10
Kenakin, T.P.11
-
2
-
-
0017065767
-
Blockade of histamine-induced contractions of intestinal smooth muscle by irreversibly acting agents
-
Kenakin T.P., Cook D.A. Blockade of histamine-induced contractions of intestinal smooth muscle by irreversibly acting agents. Can. J. Physiol. Pharmacol. 1976, 54:386-392.
-
(1976)
Can. J. Physiol. Pharmacol.
, vol.54
, pp. 386-392
-
-
Kenakin, T.P.1
Cook, D.A.2
-
3
-
-
12644296023
-
Agonist potency at the cloned human beta-3 adrenoceptor depends on receptor expression level and nature of assay
-
Wilson S., Chambers J.K., Park J.E., Ladurner A., Cronk D.W., Chapman C.G., Kallender H., Browne M.J., Murphy G.J., Young P.W. Agonist potency at the cloned human beta-3 adrenoceptor depends on receptor expression level and nature of assay. J. Pharmacol. Exp. Ther. 1996, 279:214-221.
-
(1996)
J. Pharmacol. Exp. Ther.
, vol.279
, pp. 214-221
-
-
Wilson, S.1
Chambers, J.K.2
Park, J.E.3
Ladurner, A.4
Cronk, D.W.5
Chapman, C.G.6
Kallender, H.7
Browne, M.J.8
Murphy, G.J.9
Young, P.W.10
-
4
-
-
71749103928
-
Cyclic nucleotides and cell function
-
H. P. Publishing, New York, G. Weissman, R. Claiborne (Eds.)
-
Goldberg N.D. Cyclic nucleotides and cell function. Cell membranes, biochemistry, cell biology, and pathology 1975, 185-202. H. P. Publishing, New York. G. Weissman, R. Claiborne (Eds.).
-
(1975)
Cell membranes, biochemistry, cell biology, and pathology
, pp. 185-202
-
-
Goldberg, N.D.1
-
5
-
-
0018909079
-
Is prenalterol (H 133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from differences in stimulus-response relationships
-
Kenakin T.P., Beek D. Is prenalterol (H 133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from differences in stimulus-response relationships. J. Pharmacol. Exp. Ther. 1980, 213:406-413.
-
(1980)
J. Pharmacol. Exp. Ther.
, vol.213
, pp. 406-413
-
-
Kenakin, T.P.1
Beek, D.2
-
6
-
-
0025783597
-
The relative efficiency of beta-adrenoceptor coupling to myocardial inotropy and diastolic relaxation: Organ-selective treatment of diastolic dysfunction
-
Kenakin T.P., Ambrose J.R., Irving P.E. The relative efficiency of beta-adrenoceptor coupling to myocardial inotropy and diastolic relaxation: Organ-selective treatment of diastolic dysfunction. J. Pharmacol. Exp. Ther. 1991, 257:1189-1197.
-
(1991)
J. Pharmacol. Exp. Ther.
, vol.257
, pp. 1189-1197
-
-
Kenakin, T.P.1
Ambrose, J.R.2
Irving, P.E.3
-
7
-
-
0021172243
-
The measurement of the relative efficacy of agonists by selective potentiation of tissue responses: Studies with isoprenaline and prenalterol in cardiac tissue
-
Kenakin T.P., Beek D. The measurement of the relative efficacy of agonists by selective potentiation of tissue responses: Studies with isoprenaline and prenalterol in cardiac tissue. J. Auton. Pharmacol. 1984, 4:153-159.
-
(1984)
J. Auton. Pharmacol.
, vol.4
, pp. 153-159
-
-
Kenakin, T.P.1
Beek, D.2
-
8
-
-
4444285556
-
The action of acetylcholine and other drugs on the efflux of potassium and rubidium from smooth muscle of the guinea-pig intestine
-
Burgen A.S.V., Spero L. The action of acetylcholine and other drugs on the efflux of potassium and rubidium from smooth muscle of the guinea-pig intestine. Br. J. Pharmacol. 1968, 34:99-115.
-
(1968)
Br. J. Pharmacol.
, vol.34
, pp. 99-115
-
-
Burgen, A.S.V.1
Spero, L.2
-
9
-
-
0031434924
-
Differences between natural and recombinant G-protein coupled receptor systems with varying receptor G-protein stoichiometry
-
Kenakin T.P. Differences between natural and recombinant G-protein coupled receptor systems with varying receptor G-protein stoichiometry. Trends Pharmacol. Sci. 1997, 18:456-464.
-
(1997)
Trends Pharmacol. Sci.
, vol.18
, pp. 456-464
-
-
Kenakin, T.P.1
-
10
-
-
34447636845
-
Collateral efficacy as pharmacological problem applied to new drug discovery
-
Kenakin T.P. Collateral efficacy as pharmacological problem applied to new drug discovery. Expert Opin. Drug Disc. 2006, 1:635-652.
-
(2006)
Expert Opin. Drug Disc.
, vol.1
, pp. 635-652
-
-
Kenakin, T.P.1
-
11
-
-
17644402459
-
Transduction of receptor signals by arrestins
-
Lefkowitz R.J., Shenoy S.K. Transduction of receptor signals by arrestins. Science 2005, 308:512-517.
-
(2005)
Science
, vol.308
, pp. 512-517
-
-
Lefkowitz, R.J.1
Shenoy, S.K.2
-
12
-
-
25844477611
-
Composition and function of G protein-coupled receptor signalsomes controlling mitogen-activated protein kinase activity
-
Luttrell L.M. Composition and function of G protein-coupled receptor signalsomes controlling mitogen-activated protein kinase activity. J. Mol. Neurosci. 2005, 26:253-263.
-
(2005)
J. Mol. Neurosci.
, vol.26
, pp. 253-263
-
-
Luttrell, L.M.1
-
13
-
-
0141593597
-
Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors
-
Azzi M., Charest P.G., Angers S., Rousseau G., Kohout T. arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors. Proc. Natl. Acad. Sci. USA 2003, 100:11406-11411.
-
(2003)
Proc. Natl. Acad. Sci. USA
, vol.100
, pp. 11406-11411
-
-
Azzi, M.1
Charest, P.G.2
Angers, S.3
Rousseau, G.4
Kohout, T.5
-
14
-
-
33751162165
-
2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy
-
2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy. Mol. Pharmacol. 2006, 70:1575-1584.
-
(2006)
Mol. Pharmacol.
, vol.70
, pp. 1575-1584
-
-
Galandrin, S.1
Bouvier, M.2
-
15
-
-
38849136696
-
Pharmacological onomastics: What's in a name?
-
Kenakin T.P. Pharmacological onomastics: What's in a name?. Br. J. Pharmacol. 2008, 153:432-438.
-
(2008)
Br. J. Pharmacol.
, vol.153
, pp. 432-438
-
-
Kenakin, T.P.1
-
16
-
-
0035891883
-
2A receptors by agonists and antagonists
-
2A receptors by agonists and antagonists. Brain Res. Bulletin 2001, 56:441-451.
-
(2001)
Brain Res. Bulletin
, vol.56
, pp. 441-451
-
-
Gray, J.A.1
Roth, B.L.2
-
22
-
-
0034677966
-
Drug discovery: A historical perspective
-
Drews J. Drug discovery: A historical perspective. Science 2000, 287:1960-1964.
-
(2000)
Science
, vol.287
, pp. 1960-1964
-
-
Drews, J.1
-
24
-
-
0002112970
-
General pharmacology
-
Springer, Berlin, Ergansungsweerk band, A. Heffter (Ed.)
-
Clark A.J. General pharmacology. Handbuch der Experimentellen Pharmakologie 1937, 4:165-176. Springer, Berlin, Ergansungsweerk band. A. Heffter (Ed.).
-
(1937)
Handbuch der Experimentellen Pharmakologie
, vol.4
, pp. 165-176
-
-
Clark, A.J.1
-
26
-
-
0000140263
-
Novel GPCR's and their endogenous ligands: Expanding the boundaries of physiology and pharmacology
-
Marchese A., George S.R., Kolakowski L.F., Lynch K.R., O'Dowd B.F. Novel GPCR's and their endogenous ligands: Expanding the boundaries of physiology and pharmacology. Trends Pharmacol. Sci. 1999, 20:370-375.
-
(1999)
Trends Pharmacol. Sci.
, vol.20
, pp. 370-375
-
-
Marchese, A.1
George, S.R.2
Kolakowski, L.F.3
Lynch, K.R.4
O'Dowd, B.F.5
-
27
-
-
0035895505
-
The sequence of the human genome
-
Venter J.C., et al. The sequence of the human genome. Science 2001, 291:1304-1351.
-
(2001)
Science
, vol.291
, pp. 1304-1351
-
-
Venter, J.C.1
-
30
-
-
0033019171
-
Human adrenoceptor polymorphisms: Evolving recognition of clinical importance
-
Buscher R., Hermann V., Insel P.A. Human adrenoceptor polymorphisms: Evolving recognition of clinical importance. Trends Pharmacol. Sci. 1999, 20:94-99.
-
(1999)
Trends Pharmacol. Sci.
, vol.20
, pp. 94-99
-
-
Buscher, R.1
Hermann, V.2
Insel, P.A.3
-
31
-
-
0010673662
-
A modification of receptor theory
-
Stephenson R.P. A modification of receptor theory. Br. J. Pharmacol. 1956, 11:379-393.
-
(1956)
Br. J. Pharmacol.
, vol.11
, pp. 379-393
-
-
Stephenson, R.P.1
-
32
-
-
32844471146
-
Origins of pharmacology
-
Norton S. Origins of pharmacology. Mol. Interventions 2005, 5:144-149.
-
(2005)
Mol. Interventions
, vol.5
, pp. 144-149
-
-
Norton, S.1
-
33
-
-
0022475505
-
Differences in agonist dissociation constant estimates for 5-HT at 5-HT2-receptors: a problem of acute desensitization?
-
Leff P., Martin G.R., Morse J.M. Differences in agonist dissociation constant estimates for 5-HT at 5-HT2-receptors: a problem of acute desensitization?. Br. J. Pharmacol. 1986, 89:493-499.
-
(1986)
Br. J. Pharmacol.
, vol.89
, pp. 493-499
-
-
Leff, P.1
Martin, G.R.2
Morse, J.M.3
-
35
-
-
0019790028
-
Conformational changes and drug action
-
Burgen A.S.V. Conformational changes and drug action. Fed. Proc. 1966, 40:2723-2728.
-
(1966)
Fed. Proc.
, vol.40
, pp. 2723-2728
-
-
Burgen, A.S.V.1
-
36
-
-
0000095559
-
The problem of the haem interaction in haemoglobin and the basis for the Bohr effect
-
Wyman J.J., Allen D.W. The problem of the haem interaction in haemoglobin and the basis for the Bohr effect. J. Polymer Sci. 1951, 7:499-518.
-
(1951)
J. Polymer Sci.
, vol.7
, pp. 499-518
-
-
Wyman, J.J.1
Allen, D.W.2
-
37
-
-
70449143838
-
Interaction at end-plate receptors between different choline derivatives
-
Del Castillo J., Katz B. Interaction at end-plate receptors between different choline derivatives. Proc. Roy. Soc. Lond. B. 1957, 146:369-381.
-
(1957)
Proc. Roy. Soc. Lond. B.
, vol.146
, pp. 369-381
-
-
Del Castillo, J.1
Katz, B.2
-
38
-
-
0034710976
-
Can allosteric regulation be predicted from structure?
-
Freire E. Can allosteric regulation be predicted from structure?. Proc. Natl. Acad. Sci. U.S.A. 2000, 97:11680-11682.
-
(2000)
Proc. Natl. Acad. Sci. U.S.A.
, vol.97
, pp. 11680-11682
-
-
Freire, E.1
-
40
-
-
0001169515
-
Antagonists with negative intrinsic activity at opioid receptors coupled to GTP-binding proteins
-
Costa T., Herz A. Antagonists with negative intrinsic activity at opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. U.S.A. 1989, 86:7321-7325.
-
(1989)
Proc. Natl. Acad. Sci. U.S.A.
, vol.86
, pp. 7321-7325
-
-
Costa, T.1
Herz, A.2
-
41
-
-
0027513982
-
A mutation-induced activated state of the 2-adrenergic receptor: Extending the ternary complex model
-
Samama P., Cotecchia S., Costa T., Lefkowitz R.J. A mutation-induced activated state of the 2-adrenergic receptor: Extending the ternary complex model. J. Biol. Chem. 1993, 268:4625-4636.
-
(1993)
J. Biol. Chem.
, vol.268
, pp. 4625-4636
-
-
Samama, P.1
Cotecchia, S.2
Costa, T.3
Lefkowitz, R.J.4
-
42
-
-
0002112970
-
General pharmacology
-
Springer, Berlin, Ergansungsweerk band, A. Heffter (Ed.)
-
Clark A.J. General pharmacology. Handbuch der Experimentellen Pharmakologie 1937, 4:165-176. Springer, Berlin, Ergansungsweerk band. A. Heffter (Ed.).
-
(1937)
Handbuch der Experimentellen Pharmakologie
, vol.4
, pp. 165-176
-
-
Clark, A.J.1
-
43
-
-
0010673662
-
A modification of receptor theory
-
Stephenson R.P. A modification of receptor theory. Br. J. Pharmacol. 1956, 11:379-393.
-
(1956)
Br. J. Pharmacol.
, vol.11
, pp. 379-393
-
-
Stephenson, R.P.1
-
44
-
-
77049220618
-
Affinity and intrinsic activity in the theory of competitive inhibition
-
Ariens E.J. Affinity and intrinsic activity in the theory of competitive inhibition. Arch. Int. Pharmacodyn. Ther. 1954, 99:32-49.
-
(1954)
Arch. Int. Pharmacodyn. Ther.
, vol.99
, pp. 32-49
-
-
Ariens, E.J.1
-
46
-
-
0001806350
-
A critical survey of receptor theories of drug action
-
Springer-Verlag, Berlin, J.M. Van Rossum (Ed.)
-
MacKay D. A critical survey of receptor theories of drug action. Kinetics of drug action 1977, 255-322. Springer-Verlag, Berlin. J.M. Van Rossum (Ed.).
-
(1977)
Kinetics of drug action
, pp. 255-322
-
-
MacKay, D.1
-
47
-
-
0002355204
-
The use of haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes
-
Academic Press, New York, N.J. Harper, A.B. Simmonds (Eds.)
-
Furchgott R.F. The use of haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Advances in drug research 1966, 21-55. Academic Press, New York. N.J. Harper, A.B. Simmonds (Eds.).
-
(1966)
Advances in drug research
, pp. 21-55
-
-
Furchgott, R.F.1
-
48
-
-
0000328674
-
The classification of adrenoreceptors (adrenergic receptors): An evaluation from the standpoint of receptor theory
-
Springer-Verlag, Berlin, H. Blaschko, E. Muscholl (Eds.)
-
Furchgott R.F. The classification of adrenoreceptors (adrenergic receptors): An evaluation from the standpoint of receptor theory. Handbook of experimental pharmacology, catecholamines 1972, Vol. 33:283-335. Springer-Verlag, Berlin. H. Blaschko, E. Muscholl (Eds.).
-
(1972)
Handbook of experimental pharmacology, catecholamines
, vol.33
, pp. 283-335
-
-
Furchgott, R.F.1
-
49
-
-
0021058380
-
Operational models of pharmacological agonist
-
Black J.W., Leff P. Operational models of pharmacological agonist. Proc. R. Soc. Lond. [Biol.] 1983, 220:141.
-
(1983)
Proc. R. Soc. Lond. [Biol.]
, vol.220
, pp. 141
-
-
Black, J.W.1
Leff, P.2
-
51
-
-
0019137579
-
A ternary complex model explains the agonist-specific binding properties of adenylate cyclase coupled adrenergic receptor
-
DeLean A., Stadel J.M., Lefkowitz R.J. A ternary complex model explains the agonist-specific binding properties of adenylate cyclase coupled adrenergic receptor. J. Biol. Chem. 1980, 255:7108-7117.
-
(1980)
J. Biol. Chem.
, vol.255
, pp. 7108-7117
-
-
DeLean, A.1
Stadel, J.M.2
Lefkowitz, R.J.3
-
52
-
-
0006063198
-
The pharmacologic consequences of modeling synoptic receptor systems
-
CRC Press, Boca Raton, A. Christopoulos (Ed.)
-
Kenakin T.P. The pharmacologic consequences of modeling synoptic receptor systems. Biomedical applications of computer modeling 2000, 1-20. CRC Press, Boca Raton. A. Christopoulos (Ed.).
-
(2000)
Biomedical applications of computer modeling
, pp. 1-20
-
-
Kenakin, T.P.1
-
53
-
-
70449143838
-
Interaction at end-plate receptors between different choline derivatives
-
Del Castillo J., Katz B. Interaction at end-plate receptors between different choline derivatives. Proc. R. Soc. London, B. 1957, 146:369-381.
-
(1957)
Proc. R. Soc. London, B.
, vol.146
, pp. 369-381
-
-
Del Castillo, J.1
Katz, B.2
-
55
-
-
0002060353
-
The relationship between classical and cooperative models for drug action
-
University Park Press, Baltimore, H.P. Rang (Ed.)
-
Colquhoun D. The relationship between classical and cooperative models for drug action. A symposium on drug receptors 1973, 149-182. University Park Press, Baltimore. H.P. Rang (Ed.).
-
(1973)
A symposium on drug receptors
, pp. 149-182
-
-
Colquhoun, D.1
-
56
-
-
0014115893
-
On the application of "a plausible model" of allosteric proteins to the receptor for acetylcholine
-
Karlin A. On the application of "a plausible model" of allosteric proteins to the receptor for acetylcholine. J. Theoret. Biol. 1967, 16:306-320.
-
(1967)
J. Theoret. Biol.
, vol.16
, pp. 306-320
-
-
Karlin, A.1
-
57
-
-
0015535998
-
On the analysis of pharmacological experiments in terms of an allosteric receptor model
-
Thron C.D. On the analysis of pharmacological experiments in terms of an allosteric receptor model. Mol. Pharmacol. 1973, 9:1-9.
-
(1973)
Mol. Pharmacol.
, vol.9
, pp. 1-9
-
-
Thron, C.D.1
-
58
-
-
0018142664
-
The binding of antagonists to brain muscarinic receptors
-
Hulme E.C., Birdsall N.J.M., Burgen A.S.V., Metha P. The binding of antagonists to brain muscarinic receptors. Mol. Pharmacol. 1978, 14:737-750.
-
(1978)
Mol. Pharmacol.
, vol.14
, pp. 737-750
-
-
Hulme, E.C.1
Birdsall, N.J.M.2
Burgen, A.S.V.3
Metha, P.4
-
59
-
-
0017303494
-
Regulation of adrenergic receptors by guanyl-5-yl imidodiphosphate and other purine nucleotides
-
Lefkowitz R.J., Mullikin D., Caron M.G. Regulation of adrenergic receptors by guanyl-5-yl imidodiphosphate and other purine nucleotides. J. Biol. Chem. 1976, 251:4686-4692.
-
(1976)
J. Biol. Chem.
, vol.251
, pp. 4686-4692
-
-
Lefkowitz, R.J.1
Mullikin, D.2
Caron, M.G.3
-
60
-
-
0017280145
-
An agonist-specific effect of guanine nucleotides on the binding of the beta adrenergic receptor
-
MaGuire M.E., Van Arsdale P.M., Gilman A.G. An agonist-specific effect of guanine nucleotides on the binding of the beta adrenergic receptor. Mol. Pharmacol. 1976, 12:335-339.
-
(1976)
Mol. Pharmacol.
, vol.12
, pp. 335-339
-
-
MaGuire, M.E.1
Van Arsdale, P.M.2
Gilman, A.G.3
-
61
-
-
0029935383
-
The cubic ternary complex receptor-occupancy model
-
I. Model description
-
Weiss J.M., Morgan P.H., Lutz M.W., Kenakin T.P. The cubic ternary complex receptor-occupancy model. J. Theroet. Biol. 1996, 178:151-167.
-
(1996)
J. Theroet. Biol.
, vol.178
, pp. 151-167
-
-
Weiss, J.M.1
Morgan, P.H.2
Lutz, M.W.3
Kenakin, T.P.4
-
62
-
-
0029983553
-
The cubic ternary complex receptor-occupancy model
-
II. Understanding apparent affinity
-
Weiss J.M., Morgan P.H., Lutz M.W., Kenakin T.P. The cubic ternary complex receptor-occupancy model. J. Theroet. Biol. 1996, 178:169-182.
-
(1996)
J. Theroet. Biol.
, vol.178
, pp. 169-182
-
-
Weiss, J.M.1
Morgan, P.H.2
Lutz, M.W.3
Kenakin, T.P.4
-
63
-
-
0030596736
-
The cubic ternary complex receptor-occupancy model
-
III. Resurrecting efficacy
-
Weiss J.M., Morgan P.H., Lutz M.W., Kenakin T.P. The cubic ternary complex receptor-occupancy model. J. Theoret. Biol. 1996, 181:381-397.
-
(1996)
J. Theoret. Biol.
, vol.181
, pp. 381-397
-
-
Weiss, J.M.1
Morgan, P.H.2
Lutz, M.W.3
Kenakin, T.P.4
-
64
-
-
0033976851
-
Use of constitutive G-protein-coupled receptor activity for drug discovery
-
Chen G., Way J., Armour S., Watson C., Queen K., Jayawrickreme C., Chen W.-J., Kenakin T.P. Use of constitutive G-protein-coupled receptor activity for drug discovery. Mol. Pharmacol. 1999, 57:125-134.
-
(1999)
Mol. Pharmacol.
, vol.57
, pp. 125-134
-
-
Chen, G.1
Way, J.2
Armour, S.3
Watson, C.4
Queen, K.5
Jayawrickreme, C.6
Chen, W.-J.7
Kenakin, T.P.8
-
65
-
-
0030826705
-
A selective inverse agonist for central cannabinoid receptor inhibits mitogen-activated protein kinase activation stimulated by insulin or insulin-like growth factor
-
Bouaboula M., Perrachon S., Milligan L., Canatt X., Rinaldi-Carmona M., Portier M., Barth F., Calandra B., Pecceu F., Lupker J., Maffrand J.-P., Le Fur G., Casellas P. A selective inverse agonist for central cannabinoid receptor inhibits mitogen-activated protein kinase activation stimulated by insulin or insulin-like growth factor. J. Biol. Chem. 1997, 272:22330-22339.
-
(1997)
J. Biol. Chem.
, vol.272
, pp. 22330-22339
-
-
Bouaboula, M.1
Perrachon, S.2
Milligan, L.3
Canatt, X.4
Rinaldi-Carmona, M.5
Portier, M.6
Barth, F.7
Calandra, B.8
Pecceu, F.9
Lupker, J.10
Maffrand, J.-P.11
Le Fur, G.12
Casellas, P.13
-
66
-
-
0001870572
-
Agonist efficacy and allosteric models of receptor action
-
Onaran H.O., Costa T. Agonist efficacy and allosteric models of receptor action. Ann. N. Y. Acad. Sci. 1997, 812:98-115.
-
(1997)
Ann. N. Y. Acad. Sci.
, vol.812
, pp. 98-115
-
-
Onaran, H.O.1
Costa, T.2
-
67
-
-
0001158926
-
A look at receptor efficacy
-
Springer, Heidelberg, T.P. Kenakin, J.A. Angus (Eds.) From the signaling network of the cell to the intramolecular motion of the receptor
-
Onaran H.O., Scheer A., Cotecchia S., Costa T. A look at receptor efficacy. The pharmacology of functional, biochemical, and recombinant systems handbook of experimental pharmacology 2000, Vol. 148:217-280. Springer, Heidelberg. T.P. Kenakin, J.A. Angus (Eds.).
-
(2000)
The pharmacology of functional, biochemical, and recombinant systems handbook of experimental pharmacology
, vol.148
, pp. 217-280
-
-
Onaran, H.O.1
Scheer, A.2
Cotecchia, S.3
Costa, T.4
-
68
-
-
34447636845
-
Collateral efficacy as pharmacological problem applied to new drug discovery
-
Kenakin T.P. Collateral efficacy as pharmacological problem applied to new drug discovery. Expert Opin. Drug Disc. 2006, 1:635-652.
-
(2006)
Expert Opin. Drug Disc.
, vol.1
, pp. 635-652
-
-
Kenakin, T.P.1
-
72
-
-
0031469952
-
Expression cloning and receptor pharmacology of human calcitonin receptors from MCF-7 cells and their relationship to amylin receptors
-
Chen W.-J., Armour S., Way J., Chen G., Watson C., Irving P., Cobb J., Kadwell S., Beaumont K., Rimele T., Kenakin T.P. Expression cloning and receptor pharmacology of human calcitonin receptors from MCF-7 cells and their relationship to amylin receptors. Mol. Pharmacol. 1997, 52:1164-1175.
-
(1997)
Mol. Pharmacol.
, vol.52
, pp. 1164-1175
-
-
Chen, W.-J.1
Armour, S.2
Way, J.3
Chen, G.4
Watson, C.5
Irving, P.6
Cobb, J.7
Kadwell, S.8
Beaumont, K.9
Rimele, T.10
Kenakin, T.P.11
-
73
-
-
0015861774
-
Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction
-
Cheng Y.C., Prusoff W.H. Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
-
(1973)
Biochem. Pharmacol.
, vol.22
, pp. 3099-3108
-
-
Cheng, Y.C.1
Prusoff, W.H.2
-
74
-
-
0034714211
-
A small molecule antagonist of chemokine receptors CCR1 and CCR3
-
Sabroe I., Peck M.J., Van Keulen B.J., Jorritsma A., Simmons G., Clapham P.R., Williams T.J., Pease J.E. A small molecule antagonist of chemokine receptors CCR1 and CCR3. J. Biol. Chem. 2000, 275:25985-25992.
-
(2000)
J. Biol. Chem.
, vol.275
, pp. 25985-25992
-
-
Sabroe, I.1
Peck, M.J.2
Van Keulen, B.J.3
Jorritsma, A.4
Simmons, G.5
Clapham, P.R.6
Williams, T.J.7
Pease, J.E.8
-
75
-
-
0028972931
-
Positive and negative allosteric interactions on muscarinic receptors
-
Hejnova L., Tucek S., El-Fakahany E.E. Positive and negative allosteric interactions on muscarinic receptors. Eur. J. Pharmacol. 1995, 291:427-430.
-
(1995)
Eur. J. Pharmacol.
, vol.291
, pp. 427-430
-
-
Hejnova, L.1
Tucek, S.2
El-Fakahany, E.E.3
-
76
-
-
1842333847
-
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
-
Jakubic J., El-Fakahany E.E. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 1997, 52:172-177.
-
(1997)
Mol. Pharmacol.
, vol.52
, pp. 172-177
-
-
Jakubic, J.1
El-Fakahany, E.E.2
-
77
-
-
1842333847
-
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
-
Jakubic J., Bacakova L., El-Fakahany E.E., Tucek S. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 1997, 52:172-179.
-
(1997)
Mol. Pharmacol.
, vol.52
, pp. 172-179
-
-
Jakubic, J.1
Bacakova, L.2
El-Fakahany, E.E.3
Tucek, S.4
-
78
-
-
0028231689
-
Mechanisms of steric and cooperative interactions of alcuronium on cardiac muscarinic acetylcholine receptors
-
Proska J., Tucek S. Mechanisms of steric and cooperative interactions of alcuronium on cardiac muscarinic acetylcholine receptors. Mol. Pharmacol. 1994, 45:709-717.
-
(1994)
Mol. Pharmacol.
, vol.45
, pp. 709-717
-
-
Proska, J.1
Tucek, S.2
-
79
-
-
0009196548
-
Quantification of allosteric interactions at G-protein coupled receptors using radioligand assays
-
Wiley and Sons, New York, S.J. Enna (Ed.)
-
Christopoulos A. Quantification of allosteric interactions at G-protein coupled receptors using radioligand assays. Current protocol in pharmacology 2000, 1.22.21-1.22.40. Wiley and Sons, New York. S.J. Enna (Ed.).
-
(2000)
Current protocol in pharmacology
, pp. 1.22.21-1.22.40
-
-
Christopoulos, A.1
-
80
-
-
0029126526
-
Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors
-
Lazareno S., Birdsall N.J.M. Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors. Mol. Pharmacol. 1995, 48:362-378.
-
(1995)
Mol. Pharmacol.
, vol.48
, pp. 362-378
-
-
Lazareno, S.1
Birdsall, N.J.M.2
-
84
-
-
0020324707
-
Mechanisms of hormone-effector coupling: The adrenergic receptor and adenylate cyclase
-
Lefkowitz R.J., Caron M.G., Michel T., Stadel J.M. Mechanisms of hormone-effector coupling: The adrenergic receptor and adenylate cyclase. Fed. Proc. 1982, 41:2664-2670.
-
(1982)
Fed. Proc.
, vol.41
, pp. 2664-2670
-
-
Lefkowitz, R.J.1
Caron, M.G.2
Michel, T.3
Stadel, J.M.4
-
85
-
-
0021336303
-
The kinetics of competitive radioligand binding predicted by the law of mass action
-
Motulsky H.J., Mahan L.C. The kinetics of competitive radioligand binding predicted by the law of mass action. Mol. Pharmacol. 1984, 25:1-9.
-
(1984)
Mol. Pharmacol.
, vol.25
, pp. 1-9
-
-
Motulsky, H.J.1
Mahan, L.C.2
-
86
-
-
0022408262
-
The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium
-
Ehlert F.J. The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium. Mol. Pharmacol. 1985, 28:410-421.
-
(1985)
Mol. Pharmacol.
, vol.28
, pp. 410-421
-
-
Ehlert, F.J.1
-
87
-
-
0028012102
-
Activation of heterologously expressed D3 dopamine receptors: Comparison with D2 dopamine receptors
-
Chio C.L., Lajiness M.E., Huff R.M. Activation of heterologously expressed D3 dopamine receptors: Comparison with D2 dopamine receptors. Mol. Pharmacol 1994, 45:51-60.
-
(1994)
Mol. Pharmacol
, vol.45
, pp. 51-60
-
-
Chio, C.L.1
Lajiness, M.E.2
Huff, R.M.3
-
88
-
-
0030993594
-
Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor
-
Roettger B.F., Ghanekar D., Rao R., Toledo C., Yingling J., Pinon D., Miller L.J. Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor. Mol. Pharmacol 1997, 51:357-362.
-
(1997)
Mol. Pharmacol
, vol.51
, pp. 357-362
-
-
Roettger, B.F.1
Ghanekar, D.2
Rao, R.3
Toledo, C.4
Yingling, J.5
Pinon, D.6
Miller, L.J.7
-
89
-
-
0036841022
-
A pH-sensitive fluor CypHer 5, used to monitor agonist-induced G-protein coupled receptor internalization in live cells.
-
Adie E.J., Kalinka S., Smith L., Francis M.J., Marenghi A., Cooper M.E., Briggs M., Michael N.P., Milligan G., Game S. A pH-sensitive fluor CypHer 5, used to monitor agonist-induced G-protein coupled receptor internalization in live cells. Biotechniques 2002, 33:1152-1157.
-
(2002)
Biotechniques
, vol.33
, pp. 1152-1157
-
-
Adie, E.J.1
Kalinka, S.2
Smith, L.3
Francis, M.J.4
Marenghi, A.5
Cooper, M.E.6
Briggs, M.7
Michael, N.P.8
Milligan, G.9
Game, S.10
-
90
-
-
0033976851
-
Use of constitutive G protein-coupled receptor activity for drug discovery
-
Chen G., Way J., Armour S., Watson C., Queen K., Jayawrickreme C., Chen W.-J., Kenakin T.P. Use of constitutive G protein-coupled receptor activity for drug discovery. Mol. Pharmacol 1999, 57:125-134.
-
(1999)
Mol. Pharmacol
, vol.57
, pp. 125-134
-
-
Chen, G.1
Way, J.2
Armour, S.3
Watson, C.4
Queen, K.5
Jayawrickreme, C.6
Chen, W.-J.7
Kenakin, T.P.8
-
91
-
-
0030006847
-
2-adrenergic receptors in rat C6 glioma cells: Functional interactions between closely related subtypes
-
2-adrenergic receptors in rat C6 glioma cells: Functional interactions between closely related subtypes. Mol. Pharmacol 1996, 50:175-184.
-
(1996)
Mol. Pharmacol
, vol.50
, pp. 175-184
-
-
Zhong, H.1
Guerrero, S.W.2
Esbenshade, T.A.3
Minneman, K.P.4
-
92
-
-
0028981057
-
16 couple a wide variety of receptors to phospholipase C
-
16 couple a wide variety of receptors to phospholipase C. J. Biol. Chem 1995, 270:15175-15180.
-
(1995)
J. Biol. Chem
, vol.270
, pp. 15175-15180
-
-
Offermanns, S.1
Simon, M.I.2
-
93
-
-
8644252687
-
Discovery of the positive allosteric modulators of the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1-H-pyrazol-5-yl)benzamides that potentiate receptor function
-
Johnson M.P., Wisnoski D.D., Leister W.H., O'Brien J.A., Lemaire W., Williams D.L., Burno M., Sur C., Kinney G.G., Pettibone D.J., Tiller P.R., Smith S., Duggan M.E., Hartman G.D., Conn P.J., Huff J.R. Discovery of the positive allosteric modulators of the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1-H-pyrazol-5-yl)benzamides that potentiate receptor function. J. Med. Chem 2004, 47:5825-5828.
-
(2004)
J. Med. Chem
, vol.47
, pp. 5825-5828
-
-
Johnson, M.P.1
Wisnoski, D.D.2
Leister, W.H.3
O'Brien, J.A.4
Lemaire, W.5
Williams, D.L.6
Burno, M.7
Sur, C.8
Kinney, G.G.9
Pettibone, D.J.10
Tiller, P.R.11
Smith, S.12
Duggan, M.E.13
Hartman, G.D.14
Conn, P.J.15
Huff, J.R.16
-
94
-
-
0031434924
-
Differences between natural and recombinant G-protein coupled receptor systems with varying receptor/G-protein stoichiometry
-
Kenakin T.P. Differences between natural and recombinant G-protein coupled receptor systems with varying receptor/G-protein stoichiometry. Trends Pharmacol. Sci 1997, 18:456-464.
-
(1997)
Trends Pharmacol. Sci
, vol.18
, pp. 456-464
-
-
Kenakin, T.P.1
-
95
-
-
8044237686
-
An attempt to study the effects of chemical structure on the affinity and efficacy of compounds related to acetylcholine
-
Barlow R.B., Scott K.A., Stephenson R.P. An attempt to study the effects of chemical structure on the affinity and efficacy of compounds related to acetylcholine. Br. J. Pharmacol 1967, 21:509-522.
-
(1967)
Br. J. Pharmacol
, vol.21
, pp. 509-522
-
-
Barlow, R.B.1
Scott, K.A.2
Stephenson, R.P.3
-
96
-
-
0019182114
-
N,N-Diethyl-2-(1-pyridyl)ethylamine, a partial agonist for the histamine receptor in guinea pig ileum
-
Kenakin T.P., Cook D.A. N,N-Diethyl-2-(1-pyridyl)ethylamine, a partial agonist for the histamine receptor in guinea pig ileum. Can. J. Physiol. Pharmacol 1980, 58:1307-1310.
-
(1980)
Can. J. Physiol. Pharmacol
, vol.58
, pp. 1307-1310
-
-
Kenakin, T.P.1
Cook, D.A.2
-
97
-
-
0002355204
-
The use of haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes
-
Academic Press, London, New York, N.J. Harper, A.B. Simmonds (Eds.)
-
Furchgott R.F. The use of haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Advances in drug research 1966, Vol. 3:21-55. Academic Press, London, New York. N.J. Harper, A.B. Simmonds (Eds.).
-
(1966)
Advances in drug research
, vol.3
, pp. 21-55
-
-
Furchgott, R.F.1
-
99
-
-
0021355975
-
The relative contribution of affinity and efficacy to agonist activity: Organ selectivity of noradrenaline and oxymetazoline
-
Kenakin T.P. The relative contribution of affinity and efficacy to agonist activity: Organ selectivity of noradrenaline and oxymetazoline. Br. J. Pharmacol 1984, 81:131-141.
-
(1984)
Br. J. Pharmacol
, vol.81
, pp. 131-141
-
-
Kenakin, T.P.1
-
100
-
-
78651175536
-
The uptake of atropine and related drugs by intestinal smooth muscle of the guinea pig in relation to acetylcholine receptors
-
Paton W.D.M., Rang H.P. The uptake of atropine and related drugs by intestinal smooth muscle of the guinea pig in relation to acetylcholine receptors. Proc. R. Soc. Lond. [Biol.] 1965, 163:1-44.
-
(1965)
Proc. R. Soc. Lond. [Biol.]
, vol.163
, pp. 1-44
-
-
Paton, W.D.M.1
Rang, H.P.2
-
101
-
-
0002177268
-
The quantitative effects of antagonistic drugs
-
Gaddum J.H. The quantitative effects of antagonistic drugs. J. Physiol. Lond. 1937, 89:7P-9P.
-
(1937)
J. Physiol. Lond.
, vol.89
, pp. 7P-9P
-
-
Gaddum, J.H.1
-
102
-
-
0002293829
-
Quantitative studies of antagonists for 5-hydroxytryptamine
-
Gaddum J.H., Hameed K.A., Hathway D.E., Stephens F.F. Quantitative studies of antagonists for 5-hydroxytryptamine. Q. J. Exp. Physiol. 1955, 40:49-74.
-
(1955)
Q. J. Exp. Physiol.
, vol.40
, pp. 49-74
-
-
Gaddum, J.H.1
Hameed, K.A.2
Hathway, D.E.3
Stephens, F.F.4
-
103
-
-
0009644628
-
Some quantitative uses of drug antagonists
-
Arunlakshana O., Schild H.O. Some quantitative uses of drug antagonists. Br. J. Pharmacol. 1959, 14:48-58.
-
(1959)
Br. J. Pharmacol.
, vol.14
, pp. 48-58
-
-
Arunlakshana, O.1
Schild, H.O.2
-
104
-
-
0024446412
-
Pharmacologic discrimination between receptor heterogeneity and allosteric interaction: Resultant analysis of gallamine and pirenzeipine antagonism of muscarinic responses in rat trachea
-
Kenakin T.P., Boselli C. Pharmacologic discrimination between receptor heterogeneity and allosteric interaction: Resultant analysis of gallamine and pirenzeipine antagonism of muscarinic responses in rat trachea. J. Pharmacol. Exp. Ther. 1989, 250:944-952.
-
(1989)
J. Pharmacol. Exp. Ther.
, vol.250
, pp. 944-952
-
-
Kenakin, T.P.1
Boselli, C.2
-
105
-
-
0020053249
-
The Schild regression in the process of receptor classification
-
Kenakin T.P. The Schild regression in the process of receptor classification. Can. J. Physiol. Pharmacol. 1982, 60:249-265.
-
(1982)
Can. J. Physiol. Pharmacol.
, vol.60
, pp. 249-265
-
-
Kenakin, T.P.1
-
106
-
-
0010673662
-
A modification of receptor theory
-
Stephenson R.P. A modification of receptor theory. Br. J. Pharmacol. 1956, 11:379-393.
-
(1956)
Br. J. Pharmacol.
, vol.11
, pp. 379-393
-
-
Stephenson, R.P.1
-
107
-
-
33745833578
-
On equilibrium dissociation constants for complexes of drug receptor subtypes: Selective and nonselective interactions of partial agonists with two adrenoceptor subtypes mediating positive chronotropic effects of isoprenaline in kitten atria
-
Kaumann A.J., Marano M. On equilibrium dissociation constants for complexes of drug receptor subtypes: Selective and nonselective interactions of partial agonists with two adrenoceptor subtypes mediating positive chronotropic effects of isoprenaline in kitten atria. Naunyn Schmiedebeberg's Arch. Pharmacol. 1982, 219:216-221.
-
(1982)
Naunyn Schmiedebeberg's Arch. Pharmacol.
, vol.219
, pp. 216-221
-
-
Kaumann, A.J.1
Marano, M.2
-
108
-
-
0018095505
-
The pharmacological classification of practolol and choropractolol
-
Kenakin T.P., Black J.W. The pharmacological classification of practolol and choropractolol. Mol. Pharmacol. 1978, 14:607-623.
-
(1978)
Mol. Pharmacol.
, vol.14
, pp. 607-623
-
-
Kenakin, T.P.1
Black, J.W.2
-
110
-
-
0029094516
-
Analysis of competitive agonist-antagonist interactions by nonlinear regression
-
Lew M.J., Angus J.A. Analysis of competitive agonist-antagonist interactions by nonlinear regression. Trends Pharmacol. Sci. 1996, 16:328-337.
-
(1996)
Trends Pharmacol. Sci.
, vol.16
, pp. 328-337
-
-
Lew, M.J.1
Angus, J.A.2
-
111
-
-
0021990306
-
An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation
-
Black J.W., Leff P., Shankley N.P., Wood J. An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation. Br. J. Pharmacol. 1985, 84:561-571.
-
(1985)
Br. J. Pharmacol.
, vol.84
, pp. 561-571
-
-
Black, J.W.1
Leff, P.2
Shankley, N.P.3
Wood, J.4
-
112
-
-
0027260718
-
Estimation of partial agonist affinity by interaction with a full agonist: A direct operational model-fit approach
-
Leff P., Dougall I.G., Harper D. Estimation of partial agonist affinity by interaction with a full agonist: A direct operational model-fit approach. Br. J. Pharmacol. 1993, 110:239-244.
-
(1993)
Br. J. Pharmacol.
, vol.110
, pp. 239-244
-
-
Leff, P.1
Dougall, I.G.2
Harper, D.3
-
113
-
-
1842333847
-
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
-
Jakubic J, Bacakova I, El-Fakahany E.E, Tucek S Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol 1997, 52:172-179.
-
(1997)
Mol. Pharmacol
, vol.52
, pp. 172-179
-
-
Jakubic, J.1
Bacakova, I.2
El-Fakahany, E.E.3
Tucek, S.4
-
114
-
-
0002449434
-
The active site of enzyme action
-
Koshland D.E. The active site of enzyme action. Adv. Enzymol 1960, 22:45-97.
-
(1960)
Adv. Enzymol
, vol.22
, pp. 45-97
-
-
Koshland, D.E.1
-
115
-
-
0026689405
-
Modulation by certain conserved aspartate residues of the allosteric interaction of gallamine and the ml muscarinic receptor
-
Lee N.H., Hu J., El-Fakahany E.E. Modulation by certain conserved aspartate residues of the allosteric interaction of gallamine and the ml muscarinic receptor. J. Pharmacol. Exp. Ther 1992, 262:312-316.
-
(1992)
J. Pharmacol. Exp. Ther
, vol.262
, pp. 312-316
-
-
Lee, N.H.1
Hu, J.2
El-Fakahany, E.E.3
-
116
-
-
0028271687
-
Structure of the binding site for nonnucleoside inhibitors of the reverse transcriptase of human immunodeficiency virus type 1
-
Smerdon S.J., Jager J., Wang J., Kohlstaedt L.A., Chirino A.J., Friedman J.M., Rice P.A., Steitz T.A. Structure of the binding site for nonnucleoside inhibitors of the reverse transcriptase of human immunodeficiency virus type 1. Proc. Natl. Acad. Sci. USA 1994, 91:3911-3915.
-
(1994)
Proc. Natl. Acad. Sci. USA
, vol.91
, pp. 3911-3915
-
-
Smerdon, S.J.1
Jager, J.2
Wang, J.3
Kohlstaedt, L.A.4
Chirino, A.J.5
Friedman, J.M.6
Rice, P.A.7
Steitz, T.A.8
-
117
-
-
1242294467
-
Allosteric inhibition through core disruption
-
Horn J.R, Shoichet B.K. Allosteric inhibition through core disruption. J. Mol. Biol 2004, 336:1283-1291.
-
(2004)
J. Mol. Biol
, vol.336
, pp. 1283-1291
-
-
Horn, J.R.1
Shoichet, B.K.2
-
118
-
-
0034660681
-
A new allosteric site in glycogen phosphorylase b as a target for drug interactions
-
Oikonomakos N.G., Skamnaki V.T., Tsitsanou K.E., Gavalas N.G., Johnson L. A new allosteric site in glycogen phosphorylase b as a target for drug interactions. Structure 2000, 8:575-584.
-
(2000)
Structure
, vol.8
, pp. 575-584
-
-
Oikonomakos, N.G.1
Skamnaki, V.T.2
Tsitsanou, K.E.3
Gavalas, N.G.4
Johnson, L.5
-
119
-
-
3142781225
-
Small-molecule inhibitors of protein-protein interactions: progressing towards the dream
-
Arkin M.R., Wells J.A. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nature Rev. Drug Disc 2004, 3:301-317.
-
(2004)
Nature Rev. Drug Disc
, vol.3
, pp. 301-317
-
-
Arkin, M.R.1
Wells, J.A.2
-
120
-
-
0037666888
-
Implications of protein flexibility for drug discovery
-
Teague S.J. Implications of protein flexibility for drug discovery. Nature Reviews Drug Discovery 2003, 2:527-541.
-
(2003)
Nature Reviews Drug Discovery
, vol.2
, pp. 527-541
-
-
Teague, S.J.1
-
121
-
-
15744391870
-
The CCR5 receptor-based mechanism of action of 873140, a potent allosteric non-competitive HIV entry-inhibitor
-
Watson C., Jenkinson S., Kazmierski W., Kenakin T.P. The CCR5 receptor-based mechanism of action of 873140, a potent allosteric non-competitive HIV entry-inhibitor. Mol. Pharmacol 2005, 67:1268-1282.
-
(2005)
Mol. Pharmacol
, vol.67
, pp. 1268-1282
-
-
Watson, C.1
Jenkinson, S.2
Kazmierski, W.3
Kenakin, T.P.4
-
122
-
-
18344395134
-
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site
-
Tong C., Churchill L, Cirillo P.F., Gilmore T, Graham A.G., Grob P.M., Hickey E.R., Moss N., Pav S., Regan F. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nature Sturctural Mol. Biol. 2002, 9:268-272.
-
(2002)
Nature Sturctural Mol. Biol.
, vol.9
, pp. 268-272
-
-
Tong, C.1
Churchill, L.2
Cirillo, P.F.3
Gilmore, T.4
Graham, A.G.5
Grob, P.M.6
Hickey, E.R.7
Moss, N.8
Pav, S.9
Regan, F.10
-
123
-
-
0030986787
-
HIV-1 induced cell fusion is mediated by multiple regions within both the viral envelope and the CCR-5 co-receptor
-
Bieniassz P.D., Fridell R.A., Aramori I., Ferguson S.S., Caron M.G., Cullen B.R. HIV-1 induced cell fusion is mediated by multiple regions within both the viral envelope and the CCR-5 co-receptor. EMBO J 1997, 16:2599-2609.
-
(1997)
EMBO J
, vol.16
, pp. 2599-2609
-
-
Bieniassz, P.D.1
Fridell, R.A.2
Aramori, I.3
Ferguson, S.S.4
Caron, M.G.5
Cullen, B.R.6
-
124
-
-
0032543307
-
Structure of an HIV gp120 envelope glycoprotein in complex with the CD4 receptor and a neutralizing human antibody
-
Kwong P.D., Wyatt R., Robinson J., Sweet R.W., Sodroski J., Hendricks W.A. Structure of an HIV gp120 envelope glycoprotein in complex with the CD4 receptor and a neutralizing human antibody. Nature 1998, 393:648-659.
-
(1998)
Nature
, vol.393
, pp. 648-659
-
-
Kwong, P.D.1
Wyatt, R.2
Robinson, J.3
Sweet, R.W.4
Sodroski, J.5
Hendricks, W.A.6
-
125
-
-
0030861238
-
Two distinct CCR5 domains can mediate coreceptor usage by human immunodeficiency virus type 1
-
Doranz B.J, Lu Z.-H, Rucker J, Zhang T.-Y, Sharron M, Cen Y.-H, Wang Z.-X, Guo H.-H, Du J.-D, Accavitti M.A, Doms R.W, Peiper S.C Two distinct CCR5 domains can mediate coreceptor usage by human immunodeficiency virus type 1. J. Virol 1997, 71:6305-6314.
-
(1997)
J. Virol
, vol.71
, pp. 6305-6314
-
-
Doranz, B.J.1
Lu, Z.-H.2
Rucker, J.3
Zhang, T.-Y.4
Sharron, M.5
Cen, Y.-H.6
Wang, Z.-X.7
Guo, H.-H.8
Du, J.-D.9
Accavitti, M.A.10
Doms, R.W.11
Peiper, S.C.12
-
126
-
-
0035220578
-
Gp120: Biologic aspects of structural features
-
Poignard P., Saphire E.O., Parren P.W., Burton D.R. gp120: Biologic aspects of structural features. Annu. Rev. Immunol 2001, 19:253-274.
-
(2001)
Annu. Rev. Immunol
, vol.19
, pp. 253-274
-
-
Poignard, P.1
Saphire, E.O.2
Parren, P.W.3
Burton, D.R.4
-
127
-
-
0032546844
-
The HIV-1 envelope glycoproteins: Fusogens, antigens, and immunogens
-
Wyatt R., Sodroski J. The HIV-1 envelope glycoproteins: Fusogens, antigens, and immunogens. Science 1998, 280:1884-1888.
-
(1998)
Science
, vol.280
, pp. 1884-1888
-
-
Wyatt, R.1
Sodroski, J.2
-
128
-
-
0037039380
-
HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use
-
Trkola A., Kuhmann S.E., Strizki J.M., Maxwell E., Ketas T., Morgan T., Pugach P., Xu S., Wojcik L., Tagat J., Palani A., Shapiro S., Clader J.W., McCombie S., Reyes G.R., Baroudy B.M., Moore J.P. HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use. Proc. Natl. Acad. Sci. USA 2002, 99:395-400.
-
(2002)
Proc. Natl. Acad. Sci. USA
, vol.99
, pp. 395-400
-
-
Trkola, A.1
Kuhmann, S.E.2
Strizki, J.M.3
Maxwell, E.4
Ketas, T.5
Morgan, T.6
Pugach, P.7
Xu, S.8
Wojcik, L.9
Tagat, J.10
Palani, A.11
Shapiro, S.12
Clader, J.W.13
McCombie, S.14
Reyes, G.R.15
Baroudy, B.M.16
Moore, J.P.17
-
129
-
-
12144289333
-
Genetic and phenotypic analyses of human immunodeficiency virus type 1 escape from small-molecule CCR inhibitor
-
Korber B.T., Wolinsky S.M., Moore J.P., Kuhmann S.E, Pugach P, Kunstman K.J, Taylor J, Stanfield R.L, Snyder A, Strizki J.M, Riley J, Baroudy B.M, Wilson I.A, et al. Genetic and phenotypic analyses of human immunodeficiency virus type 1 escape from small-molecule CCR inhibitor. J. Virol 2004, 78:2790-2807.
-
(2004)
J. Virol
, vol.78
, pp. 2790-2807
-
-
Korber, B.T.1
Wolinsky, S.M.2
Moore, J.P.3
Kuhmann, S.E.4
Pugach, P.5
Kunstman, K.J.6
Taylor, J.7
Stanfield, R.L.8
Snyder, A.9
Strizki, J.M.10
Riley, J.11
Baroudy, B.M.12
Wilson, I.A.13
-
130
-
-
0029758113
-
Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1
-
Nagasaw T, Hirota S, Tachibana K, Takakura N, Nishikawa S, Kitamura Y, Yoshida N, Kikutani H, Kishimoto T Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1. Nature 1996, 382:635-638.
-
(1996)
Nature
, vol.382
, pp. 635-638
-
-
Nagasaw, T.1
Hirota, S.2
Tachibana, K.3
Takakura, N.4
Nishikawa, S.5
Kitamura, Y.6
Yoshida, N.7
Kikutani, H.8
Kishimoto, T.9
-
131
-
-
0032508033
-
The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract
-
Tachibana K., Hirota S., Iizasa H., Yoshida H., Kawabata K., Kataoka Y., Kitamura Y., Matsushima K., Yoshida N., Nishikawa S., Kishimoto T., Nagasawa T. The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract. Nature 1998, 393:591-594.
-
(1998)
Nature
, vol.393
, pp. 591-594
-
-
Tachibana, K.1
Hirota, S.2
Iizasa, H.3
Yoshida, H.4
Kawabata, K.5
Kataoka, Y.6
Kitamura, Y.7
Matsushima, K.8
Yoshida, N.9
Nishikawa, S.10
Kishimoto, T.11
Nagasawa, T.12
-
132
-
-
0032507962
-
Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development
-
Zou Y.R., Kottmann A.H., Kuroda M., Taniuchi I., Littman D.R. Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature 1998, 393:595-599.
-
(1998)
Nature
, vol.393
, pp. 595-599
-
-
Zou, Y.R.1
Kottmann, A.H.2
Kuroda, M.3
Taniuchi, I.4
Littman, D.R.5
-
133
-
-
0037428443
-
Indentification of allosteric peptide agonists of CXCR4
-
Sachpatzidis A., Benton B.K., Manfredis J.P., Wang H., Hamilton A., Dohlman H.G., Lolis E. Indentification of allosteric peptide agonists of CXCR4. J. Biol. Chem 2003, 278:896-907.
-
(2003)
J. Biol. Chem
, vol.278
, pp. 896-907
-
-
Sachpatzidis, A.1
Benton, B.K.2
Manfredis, J.P.3
Wang, H.4
Hamilton, A.5
Dohlman, H.G.6
Lolis, E.7
-
134
-
-
0032568336
-
Dissociation of the signalling and antiviral properties of SDF-1-derived small peptides
-
Heveker N., Montes M., Germeroth L., Amara A., Trautmann A., Alizon M., Schneider-Mergener J. Dissociation of the signalling and antiviral properties of SDF-1-derived small peptides. Current Biology 1998, 8:369-376.
-
(1998)
Current Biology
, vol.8
, pp. 369-376
-
-
Heveker, N.1
Montes, M.2
Germeroth, L.3
Amara, A.4
Trautmann, A.5
Alizon, M.6
Schneider-Mergener, J.7
-
135
-
-
0019972810
-
The cholinergic hypothesis of geriatric memory dysfunction
-
Bartus R.T., Dean R.L., Beer B., Lippa A.S. The cholinergic hypothesis of geriatric memory dysfunction. Science 1982, 217:408-417.
-
(1982)
Science
, vol.217
, pp. 408-417
-
-
Bartus, R.T.1
Dean, R.L.2
Beer, B.3
Lippa, A.S.4
-
136
-
-
0029055030
-
Allosteric modulation of muscarinic acetylcholine receptors
-
Tucek S., Proska J. Allosteric modulation of muscarinic acetylcholine receptors. Trends Pharmacol. Sci 1995, 16:205-212.
-
(1995)
Trends Pharmacol. Sci
, vol.16
, pp. 205-212
-
-
Tucek, S.1
Proska, J.2
-
137
-
-
0033528461
-
Acetylcholinesterase inhibitors for Alzheimer's disease
-
Flicker L. Acetylcholinesterase inhibitors for Alzheimer's disease. Br. Med. J 1999, 318:615-616.
-
(1999)
Br. Med. J
, vol.318
, pp. 615-616
-
-
Flicker, L.1
-
138
-
-
0002567031
-
New approach to drug therapy of Alzheimer's dementia
-
Maelicke A, Albuquerque E.X New approach to drug therapy of Alzheimer's dementia. Drug Discovery Today 1996, 1:53-59.
-
(1996)
Drug Discovery Today
, vol.1
, pp. 53-59
-
-
Maelicke, A.1
Albuquerque, E.X.2
-
139
-
-
0031887759
-
Ivermectin: A positive allosteric effector of the a7 neuronal nicotinic acetylcholine receptor
-
Krause R.M, Buisson B, Bertrand S, Corringer P.-J, Galzi J.-L, Changeux J.-P, Bertrand D Ivermectin: A positive allosteric effector of the a7 neuronal nicotinic acetylcholine receptor. Mol. Pharmacol 1998, 53:283-294.
-
(1998)
Mol. Pharmacol
, vol.53
, pp. 283-294
-
-
Krause, R.M.1
Buisson, B.2
Bertrand, S.3
Corringer, P.-J.4
Galzi, J.-L.5
Changeux, J.-P.6
Bertrand, D.7
-
140
-
-
0023958554
-
Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods
-
Ehlert F.J. Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. Mol. Pharmacol 1988, 33:187-194.
-
(1988)
Mol. Pharmacol
, vol.33
, pp. 187-194
-
-
Ehlert, F.J.1
-
141
-
-
0021990306
-
An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation
-
Black J.W., Leff P., Shankley N.P., Wood J. An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation. Br. J. Pharmacol 1985, 84:561-571.
-
(1985)
Br. J. Pharmacol
, vol.84
, pp. 561-571
-
-
Black, J.W.1
Leff, P.2
Shankley, N.P.3
Wood, J.4
-
142
-
-
27844519281
-
New concepts in durg discovery: Collateral efficacy and permissive antagonism
-
Kenakin T.P. New concepts in durg discovery: Collateral efficacy and permissive antagonism. Nature Rev. Durg Disc 2005, 4:919-927.
-
(2005)
Nature Rev. Durg Disc
, vol.4
, pp. 919-927
-
-
Kenakin, T.P.1
-
143
-
-
33751183557
-
Determining the potency and molecular mechanism of action of insurmountable antagonists
-
Kenakin T.P., Jenkinson S., Watson C. Determining the potency and molecular mechanism of action of insurmountable antagonists. J. Pharmacol. Exp. Ther 2006, 319:710-723.
-
(2006)
J. Pharmacol. Exp. Ther
, vol.319
, pp. 710-723
-
-
Kenakin, T.P.1
Jenkinson, S.2
Watson, C.3
-
144
-
-
24044539957
-
Allosteric modulation of the cannabinoid CB1 receptor
-
Price M.R., Baillie G.L., Thomas A., Stevenson L.A., Easson M., Goodwin R., McLean A., Mclntosh L., Goodwin G., Walker G., Westwood P., Marrs J., Thomson F., Cowley P., Chistopoulos A., Pertwee R.G., Ross R.A. Allosteric modulation of the cannabinoid CB1 receptor. Mol. Pharm 2005, 68:1484-1495.
-
(2005)
Mol. Pharm
, vol.68
, pp. 1484-1495
-
-
Price, M.R.1
Baillie, G.L.2
Thomas, A.3
Stevenson, L.A.4
Easson, M.5
Goodwin, R.6
McLean, A.7
Mclntosh, L.8
Goodwin, G.9
Walker, G.10
Westwood, P.11
Marrs, J.12
Thomson, F.13
Cowley, P.14
Chistopoulos, A.15
Pertwee, R.G.16
Ross, R.A.17
-
145
-
-
0009196548
-
Overview of receptor allosterism
-
John Wiley and Sons, New York
-
Christopoulos A. Overview of receptor allosterism. Current protocols in pharmacology 2000, Vol 1:1.21.21-1.21.45. John Wiley and Sons, New York.
-
(2000)
Current protocols in pharmacology
, vol.1
, pp. 1.21.21-1.21.45
-
-
Christopoulos, A.1
-
146
-
-
0002293829
-
Quantitative studies of antagonists for 5-hydroxytryptamine
-
Gaddum J.H., Hameed K.A., Hathway D.E., Stephens F.F. Quantitative studies of antagonists for 5-hydroxytryptamine. Q. J. Exp. Physiol 1955, 40:49-74.
-
(1955)
Q. J. Exp. Physiol
, vol.40
, pp. 49-74
-
-
Gaddum, J.H.1
Hameed, K.A.2
Hathway, D.E.3
Stephens, F.F.4
-
147
-
-
0029776693
-
Activation of muscarinic acetylcholine receptors via their allosteric binding sites
-
Jakubic J., Bacakova L., Lisá V., El-Fakahany E.E., Tucek S. Activation of muscarinic acetylcholine receptors via their allosteric binding sites. Proc. Natl. Acad. Sci. USA 1996, 93:8705-8709.
-
(1996)
Proc. Natl. Acad. Sci. USA
, vol.93
, pp. 8705-8709
-
-
Jakubic, J.1
Bacakova, L.2
Lisá, V.3
El-Fakahany, E.E.4
Tucek, S.5
-
148
-
-
0031024171
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
Lipinski C., Lombardo F., Dominy B., Feeney P. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug. Deliv. Rev. 2001, 23:3-25.
-
(2001)
Adv. Drug. Deliv. Rev.
, vol.23
, pp. 3-25
-
-
Lipinski, C.1
Lombardo, F.2
Dominy, B.3
Feeney, P.4
-
149
-
-
0021812342
-
Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs
-
Richardson B.P., Engel G., Donatsch P., Stadler P.A. Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs. Nature 1985, 316:126-131.
-
(1985)
Nature
, vol.316
, pp. 126-131
-
-
Richardson, B.P.1
Engel, G.2
Donatsch, P.3
Stadler, P.A.4
-
150
-
-
0018611577
-
Symbiotic approach to drug design: Antihypertensive adrenergic blocking agents
-
Baldwin J.J., Lumma W.C., Lundell G.F., Ponticello G.S., Raab A.W., Engelhardt E.L., Hirschmann E.L., Sweet C.S., Scriabine A. Symbiotic approach to drug design: Antihypertensive adrenergic blocking agents. J. Med. Chem. 1979, 22:1284-1290.
-
(1979)
J. Med. Chem.
, vol.22
, pp. 1284-1290
-
-
Baldwin, J.J.1
Lumma, W.C.2
Lundell, G.F.3
Ponticello, G.S.4
Raab, A.W.5
Engelhardt, E.L.6
Hirschmann, E.L.7
Sweet, C.S.8
Scriabine, A.9
-
151
-
-
0034461768
-
Drug-like properties and the causes of poor solubility and poor permeability
-
Lipinski C.A. Drug-like properties and the causes of poor solubility and poor permeability. J. Pharmacol. Tox. Meth. 2000, 44:235-249.
-
(2000)
J. Pharmacol. Tox. Meth.
, vol.44
, pp. 235-249
-
-
Lipinski, C.A.1
-
152
-
-
1842333847
-
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
-
Jakubic J., Bacakova I., El-Fakahany E.E., Tucek S. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 1997, 52:172-179.
-
(1997)
Mol. Pharmacol.
, vol.52
, pp. 172-179
-
-
Jakubic, J.1
Bacakova, I.2
El-Fakahany, E.E.3
Tucek, S.4
-
153
-
-
17944365465
-
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure-Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes
-
Finke P.E., Oates B., Mills S.G., MacCoss M., Malkowitz L., Springer M.S., Gould S.L., DeMartino J.A., Carella A., Carver G., et al. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure-Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. 2001, 11:2475-2479.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2475-2479
-
-
Finke, P.E.1
Oates, B.2
Mills, S.G.3
MacCoss, M.4
Malkowitz, L.5
Springer, M.S.6
Gould, S.L.7
DeMartino, J.A.8
Carella, A.9
Carver, G.10
-
154
-
-
0033003760
-
A simple statistical parameter for use in evaluation and validation of high throughput screening assays
-
Zhang J.-H., Chung T.D.Y., Oldenburg K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J. Biomeolecular Screening 1999, 4:67-72.
-
(1999)
J. Biomeolecular Screening
, vol.4
, pp. 67-72
-
-
Zhang, J.-H.1
Chung, T.D.Y.2
Oldenburg, K.R.3
-
155
-
-
0021745755
-
Functional group contributions to drug-receptor interactions
-
Andrews P.R., Craik D.J., Martin J.L. Functional group contributions to drug-receptor interactions. J. Med. Chem. 1984, 27:1648-1657.
-
(1984)
J. Med. Chem.
, vol.27
, pp. 1648-1657
-
-
Andrews, P.R.1
Craik, D.J.2
Martin, J.L.3
-
156
-
-
1942453243
-
Ligand efficiency: A useful metric for lead selection
-
Hopkins A.L., Groom C.R., Alex A. Ligand efficiency: A useful metric for lead selection. Drug Disc. Today 2004, 9:430-431.
-
(2004)
Drug Disc. Today
, vol.9
, pp. 430-431
-
-
Hopkins, A.L.1
Groom, C.R.2
Alex, A.3
-
157
-
-
0033621044
-
The maximal affinity of ligands
-
Kuntz I.D., Chen K., Sharp K.A., Kollman P.A. The maximal affinity of ligands. Proc. Natl. Acad. Sci. USA 1999, 96:9997-10002.
-
(1999)
Proc. Natl. Acad. Sci. USA
, vol.96
, pp. 9997-10002
-
-
Kuntz, I.D.1
Chen, K.2
Sharp, K.A.3
Kollman, P.A.4
-
158
-
-
0030993594
-
Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor
-
Roettger B.F., Ghanekar D., Rao R., Toledo C., Yingling J., Pinon D., Miller L.J. Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor. Mol. Pharmacol. 1997, 51:357-362.
-
(1997)
Mol. Pharmacol.
, vol.51
, pp. 357-362
-
-
Roettger, B.F.1
Ghanekar, D.2
Rao, R.3
Toledo, C.4
Yingling, J.5
Pinon, D.6
Miller, L.J.7
-
159
-
-
14644420930
-
Interfacial inhibition of macromolecular interactions: Nature's paradigm for drug discovery
-
Pommier Y., Cherfils J. Interfacial inhibition of macromolecular interactions: Nature's paradigm for drug discovery. Trend. Pharmacol. Sci. 2005, 26:138-145.
-
(2005)
Trend. Pharmacol. Sci.
, vol.26
, pp. 138-145
-
-
Pommier, Y.1
Cherfils, J.2
-
160
-
-
0001870572
-
Agonist efficacy and allosteric models of receptor action
-
Onaran H.O., Costa T. Agonist efficacy and allosteric models of receptor action. Ann. N. Y. Acad. Sci. 1997, 812:98-115.
-
(1997)
Ann. N. Y. Acad. Sci.
, vol.812
, pp. 98-115
-
-
Onaran, H.O.1
Costa, T.2
-
161
-
-
0001158926
-
A look at receptor efficacy. From the signaling network of the cell to the intramolecular motion of the receptor
-
Springer, Heidelberg, Vol. 148, T.P. Kenakin, J.A. Angus (Eds.)
-
Onaran H.O., Scheer A., Cotecchia S., Costa T. A look at receptor efficacy. From the signaling network of the cell to the intramolecular motion of the receptor. The pharmacology of functional, biochemical, and recombinant systems handbook of experimental pharmacology 2000, 217-280. Springer, Heidelberg, Vol. 148. T.P. Kenakin, J.A. Angus (Eds.).
-
(2000)
The pharmacology of functional, biochemical, and recombinant systems handbook of experimental pharmacology
, pp. 217-280
-
-
Onaran, H.O.1
Scheer, A.2
Cotecchia, S.3
Costa, T.4
-
162
-
-
0036591660
-
The ligand paradox between affinity and efficacy: Can you be there and not make a difference?
-
Kenakin T.P., Onaran O. The ligand paradox between affinity and efficacy: Can you be there and not make a difference?. Trends Pharmacol. Sci. 2002, 23:275-280.
-
(2002)
Trends Pharmacol. Sci.
, vol.23
, pp. 275-280
-
-
Kenakin, T.P.1
Onaran, O.2
-
163
-
-
34447645129
-
Resonance energy transfer approaches in molecular pharmacology and beyond
-
Marullo S., Bouvier M. Resonance energy transfer approaches in molecular pharmacology and beyond. Trends Pharmacol. Sci. 2007, 28:362-365.
-
(2007)
Trends Pharmacol. Sci.
, vol.28
, pp. 362-365
-
-
Marullo, S.1
Bouvier, M.2
-
164
-
-
20844434337
-
A FLASH-based approach to determine G protein-coupled receptor activation in living cells
-
Hoffmann C., Gaietta G., Bünemann M., Adams S., Oberdorff-Maass S., Behr B., et al. A FLASH-based approach to determine G protein-coupled receptor activation in living cells. Nat. Methods 2005, 2:171-176.
-
(2005)
Nat. Methods
, vol.2
, pp. 171-176
-
-
Hoffmann, C.1
Gaietta, G.2
Bünemann, M.3
Adams, S.4
Oberdorff-Maass, S.5
Behr, B.6
-
165
-
-
0141593597
-
Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors
-
Azzi M., Charest P.G., Angers S., Rousseau G., Kohout T. arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors. Proc. Natl. Acad. Sci. USA 2003, 100:11406-11411.
-
(2003)
Proc. Natl. Acad. Sci. USA
, vol.100
, pp. 11406-11411
-
-
Azzi, M.1
Charest, P.G.2
Angers, S.3
Rousseau, G.4
Kohout, T.5
-
166
-
-
10644230013
-
Using confidence intervals around individual means to assess statistical significance between two means
-
Julious S.A. Using confidence intervals around individual means to assess statistical significance between two means. Pharmaceut. Stat. 2004, 3:217-222.
-
(2004)
Pharmaceut. Stat.
, vol.3
, pp. 217-222
-
-
Julious, S.A.1
-
167
-
-
9344269434
-
Structure-based design of estrogen receptor-selective ligands
-
Manas E.S., Unwalla R.J., Xu Z.B., Malamas M.S., Miller C.P., Harris H.A., Hsiao C., Akopian T., Hum W.-T., Malakian K., Wolfrom S., Bapat A., Bhat R.A., Stahl M.L., Somers M.S., Alvarez J.C. Structure-based design of estrogen receptor-selective ligands. J. Amer. Chem. Soc. 2004, 126:15106-15119.
-
(2004)
J. Amer. Chem. Soc.
, vol.126
, pp. 15106-15119
-
-
Manas, E.S.1
Unwalla, R.J.2
Xu, Z.B.3
Malamas, M.S.4
Miller, C.P.5
Harris, H.A.6
Hsiao, C.7
Akopian, T.8
Hum, W.-T.9
Malakian, K.10
Wolfrom, S.11
Bapat, A.12
Bhat, R.A.13
Stahl, M.L.14
Somers, M.S.15
Alvarez, J.C.16
-
168
-
-
27344435806
-
Quantitative risk modeling for new pharmaceutical compounds
-
Tang Z., Taylor M.J., Lisboa P., Dyas M. Quantitative risk modeling for new pharmaceutical compounds. Drug Disc. Today 2005, 22:1520-1526.
-
(2005)
Drug Disc. Today
, vol.22
, pp. 1520-1526
-
-
Tang, Z.1
Taylor, M.J.2
Lisboa, P.3
Dyas, M.4
-
169
-
-
0033576601
-
The design of leadlike combinatorial libraries
-
Teague S.J., Davis A.M., Leeson P.D., Oprea T.J. The design of leadlike combinatorial libraries. Angewandte Chemie International Edition 1999, 38:3743-3748.
-
(1999)
Angewandte Chemie International Edition
, vol.38
, pp. 3743-3748
-
-
Teague, S.J.1
Davis, A.M.2
Leeson, P.D.3
Oprea, T.J.4
-
170
-
-
0027336957
-
(.+-.)-3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: A conformationally restricted analog of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor
-
King F.D., Brown A.M., Gaster L.M., Kaumann A.J., Medhurst A.D., Parker S.G., Parsons A.A., Patch T.L., Raval P. (.+-.)-3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: A conformationally restricted analog of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor. J. Med. Chem. 1993, 36:1918.
-
(1993)
J. Med. Chem.
, vol.36
, pp. 1918
-
-
King, F.D.1
Brown, A.M.2
Gaster, L.M.3
Kaumann, A.J.4
Medhurst, A.D.5
Parker, S.G.6
Parsons, A.A.7
Patch, T.L.8
Raval, P.9
-
171
-
-
0023883194
-
Synthesis and anti-ulcer activities of sodium alkylazulene sulfonates
-
Yanagisawa T., Wakabayashi S., Tomiyama T., Yasunami M., Takase K. Synthesis and anti-ulcer activities of sodium alkylazulene sulfonates. Chem. Pharm. Bull. 1988, 36:641.
-
(1988)
Chem. Pharm. Bull.
, vol.36
, pp. 641
-
-
Yanagisawa, T.1
Wakabayashi, S.2
Tomiyama, T.3
Yasunami, M.4
Takase, K.5
-
172
-
-
0023751351
-
6-Methylenandrosta-1,4-diene-3,17-dione (FCE 24304): A new irreversible aromatase inhibitor
-
Giudici D., Ornati G., Briatico G., Buzzetti F., Lombardi P., di Salle E. 6-Methylenandrosta-1,4-diene-3,17-dione (FCE 24304): A new irreversible aromatase inhibitor. J. Steroid. Biochem. 1988, 30:391.
-
(1988)
J. Steroid. Biochem.
, vol.30
, pp. 391
-
-
Giudici, D.1
Ornati, G.2
Briatico, G.3
Buzzetti, F.4
Lombardi, P.5
di Salle, E.6
-
174
-
-
0023886910
-
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines
-
Krapcho J., Turk C., Cushman D.W., Powell J.R., DeForrest J.M., Spitzmiller E.R., Karanewsky D.S., Duggan M., Rovnyak G., Schwartz J., Natarajan S., Godfrey J.D., Ryono D.E., Neubeck R., Atwal K.S., Petrillo E.W. Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines. J. Med. Chem. 1988, 31:1148.
-
(1988)
J. Med. Chem.
, vol.31
, pp. 1148
-
-
Krapcho, J.1
Turk, C.2
Cushman, D.W.3
Powell, J.R.4
DeForrest, J.M.5
Spitzmiller, E.R.6
Karanewsky, D.S.7
Duggan, M.8
Rovnyak, G.9
Schwartz, J.10
Natarajan, S.11
Godfrey, J.D.12
Ryono, D.E.13
Neubeck, R.14
Atwal, K.S.15
Petrillo, E.W.16
-
175
-
-
0031788930
-
ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease
-
Sham H.L., Kempf D.J., Molla A., Marsh K.C., Kumar G.N., Chen C.-M., Kati W., Stewart K., Lal R., Hsu A., Betebenner D., Korneyeva M., Vasavanonda S., McDonald E., Saldivar A., Wideburg N., Chen X., Niu P., Park C., Jayanti V., Grabowski B., Granneman G.R., Sun E., Japour A.J., Leonard J.M., Plattner J.J., Norbeck D.W. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob. Agents Chemother. 1998, 42:3218.
-
(1998)
Antimicrob. Agents Chemother.
, vol.42
, pp. 3218
-
-
Sham, H.L.1
Kempf, D.J.2
Molla, A.3
Marsh, K.C.4
Kumar, G.N.5
Chen, C.-M.6
Kati, W.7
Stewart, K.8
Lal, R.9
Hsu, A.10
Betebenner, D.11
Korneyeva, M.12
Vasavanonda, S.13
McDonald, E.14
Saldivar, A.15
Wideburg, N.16
Chen, X.17
Niu, P.18
Park, C.19
Jayanti, V.20
Grabowski, B.21
Granneman, G.R.22
Sun, E.23
Japour, A.J.24
Leonard, J.M.25
Plattner, J.J.26
Norbeck, D.W.27
more..
-
176
-
-
0037124196
-
Drugs, leads, and drug-likeness: An analysis of some recently launched drugs
-
Proudfoot J.R. Drugs, leads, and drug-likeness: An analysis of some recently launched drugs. Bioogan. Med. Chem. Lett. 2002, 12:1647-1650.
-
(2002)
Bioogan. Med. Chem. Lett.
, vol.12
, pp. 1647-1650
-
-
Proudfoot, J.R.1
-
178
-
-
26944446576
-
In vitro safety pharmacology profiling: An essential tool for successful drug development
-
Whitebread S., Hamon J., Bojanic D., Urban L. In vitro safety pharmacology profiling: An essential tool for successful drug development. Drug Disc. Today 2005, 10:1421-1433.
-
(2005)
Drug Disc. Today
, vol.10
, pp. 1421-1433
-
-
Whitebread, S.1
Hamon, J.2
Bojanic, D.3
Urban, L.4
-
179
-
-
22944438384
-
Research on adverse drug events: Muscarinic m3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes
-
Silvetre J.S., Prous J. Research on adverse drug events: Muscarinic m3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes. Meth. Find. Exp. Clin. Pharmacol. 2005, 27:289-304.
-
(2005)
Meth. Find. Exp. Clin. Pharmacol.
, vol.27
, pp. 289-304
-
-
Silvetre, J.S.1
Prous, J.2
-
180
-
-
27644596457
-
Predicting in vivo drug interactions from in vitro drug discovery data
-
Wienkers L.C., Heath T.G. Predicting in vivo drug interactions from in vitro drug discovery data. Nature Rev. Drug Discovery 2005, 4:825-833.
-
(2005)
Nature Rev. Drug Discovery
, vol.4
, pp. 825-833
-
-
Wienkers, L.C.1
Heath, T.G.2
-
181
-
-
21044451732
-
GPCR antitarget modeling: Pharmacophore models for biogenic amine binding GPCRs to avoid GPCR-mediated side effect
-
Klabunde T., Evers A. GPCR antitarget modeling: Pharmacophore models for biogenic amine binding GPCRs to avoid GPCR-mediated side effect. Chem. Bio. Chem. 2005, 6:876-889.
-
(2005)
Chem. Bio. Chem.
, vol.6
, pp. 876-889
-
-
Klabunde, T.1
Evers, A.2
-
182
-
-
12144257810
-
Derivation and validation of toxicophores for mutagenicity prediction
-
Kazius J., Bursi R. Derivation and validation of toxicophores for mutagenicity prediction. J. Med. Chem. 2005, 48:312-320.
-
(2005)
J. Med. Chem.
, vol.48
, pp. 312-320
-
-
Kazius, J.1
Bursi, R.2
-
183
-
-
0014104395
-
Effect of polymorphism on the absorption of chloramphenicol from chloramphenicol palmitate
-
Aguiar A.J., Krc J., Kinkel A.W., Samyn A.C. Effect of polymorphism on the absorption of chloramphenicol from chloramphenicol palmitate. J. Pharm. Sci. 1967, 56(7):847-853.
-
(1967)
J. Pharm. Sci.
, vol.56
, Issue.7
, pp. 847-853
-
-
Aguiar, A.J.1
Krc, J.2
Kinkel, A.W.3
Samyn, A.C.4
-
184
-
-
0001787724
-
Absorption of drugs from the rat small intestine
-
Schanker L.S., Tocco D.T., Brodie B.B., Hogben C.A.M. Absorption of drugs from the rat small intestine. J. Pharmacol. Exp. Ther. 1958, 123:81-88.
-
(1958)
J. Pharmacol. Exp. Ther.
, vol.123
, pp. 81-88
-
-
Schanker, L.S.1
Tocco, D.T.2
Brodie, B.B.3
Hogben, C.A.M.4
-
186
-
-
84971199691
-
Calculation of drug solubilities by pharmacy students
-
Cates I.A. Calculation of drug solubilities by pharmacy students. Amer. J. Pharm. Ed. 1981, 45:11-13.
-
(1981)
Amer. J. Pharm. Ed.
, vol.45
, pp. 11-13
-
-
Cates, I.A.1
-
187
-
-
0003409952
-
-
Lippincott, Williams, Wilkins, New York
-
Williams D.A., Lemke T.L. Foye's principle of medicinal chemistry 2002, Lippincott, Williams, Wilkins, New York. 5.
-
(2002)
Foye's principle of medicinal chemistry
-
-
Williams, D.A.1
Lemke, T.L.2
-
188
-
-
0001334658
-
Design principles for orally bioavailable drugs
-
Navia M.A., Chaturvedi P.R. Design principles for orally bioavailable drugs. Drug Disc. Today 1996, 1:179-199.
-
(1996)
Drug Disc. Today
, vol.1
, pp. 179-199
-
-
Navia, M.A.1
Chaturvedi, P.R.2
-
189
-
-
2642527944
-
Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery
-
Kerns E.H., Di L., Petusky S., Farris M., Ley R., Jupp P. Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery. J. Pharm. Sci. 2004, 93:1440-1453.
-
(2004)
J. Pharm. Sci.
, vol.93
, pp. 1440-1453
-
-
Kerns, E.H.1
Di, L.2
Petusky, S.3
Farris, M.4
Ley, R.5
Jupp, P.6
-
190
-
-
14644398632
-
Cell culture-based models of intestinal permeability: A critique
-
Balimane P.V., Chong S. Cell culture-based models of intestinal permeability: A critique. Drug. Disc. Today 2005, 10:335-343.
-
(2005)
Drug. Disc. Today
, vol.10
, pp. 335-343
-
-
Balimane, P.V.1
Chong, S.2
-
191
-
-
34247492532
-
The pivotal role of hepatocytes in drug discovery
-
Soars M.G., McGinnity D.F., Grime K., Riley R.J. The pivotal role of hepatocytes in drug discovery. Chemico-Biol. Interactions 2007, 168:2-15.
-
(2007)
Chemico-Biol. Interactions
, vol.168
, pp. 2-15
-
-
Soars, M.G.1
McGinnity, D.F.2
Grime, K.3
Riley, R.J.4
-
192
-
-
34247510665
-
Hepatocytes-the choice to investigate drug metabolism and toxicity in man: In vitro variability as a reflection of in vivo
-
Gomez-Lechon M., Castell J.V., Donato M.T. Hepatocytes-the choice to investigate drug metabolism and toxicity in man: In vitro variability as a reflection of in vivo. Chemico-Biol. Interactions 2007, 168:30-50.
-
(2007)
Chemico-Biol. Interactions
, vol.168
, pp. 30-50
-
-
Gomez-Lechon, M.1
Castell, J.V.2
Donato, M.T.3
-
193
-
-
0014056670
-
Metabolism, blood levels and rate of excretion of acetohexamide in human subjects
-
Galloway J.A., McMahon R.E., Culp H.W., Marshall F., Young E.C. Metabolism, blood levels and rate of excretion of acetohexamide in human subjects. Diabetes 1965, 16:118-127.
-
(1965)
Diabetes
, vol.16
, pp. 118-127
-
-
Galloway, J.A.1
McMahon, R.E.2
Culp, H.W.3
Marshall, F.4
Young, E.C.5
-
194
-
-
0030438721
-
Prediction of the human pharmacokinetics of troglitazone, a new and extensively metabolized antidiabetic agent, after oral administration, with an animal scale-up approach
-
Izumi T., Enomoto S., Hosiyama K., Sasahara K., Shibukawa A., Nakagawa T., Suguyama Y. Prediction of the human pharmacokinetics of troglitazone, a new and extensively metabolized antidiabetic agent, after oral administration, with an animal scale-up approach. J. Pharmacol. Exp. Ther. 1996, 277:1630-1641.
-
(1996)
J. Pharmacol. Exp. Ther.
, vol.277
, pp. 1630-1641
-
-
Izumi, T.1
Enomoto, S.2
Hosiyama, K.3
Sasahara, K.4
Shibukawa, A.5
Nakagawa, T.6
Suguyama, Y.7
-
195
-
-
0032951239
-
Pharmacokinetics of 8-methoxyquinoloe, moxifloxacin: A comparison in humans and other mammalian species
-
Siefert H.M., Domdey-Bette A., Henninger K., Hucke F., Kohlsdorfer C., Stass H.H. Pharmacokinetics of 8-methoxyquinoloe, moxifloxacin: A comparison in humans and other mammalian species. J. Antimicrob. Chemother. 1999, 43(Suppl. B):69-76.
-
(1999)
J. Antimicrob. Chemother.
, vol.43
, pp. 69-76
-
-
Siefert, H.M.1
Domdey-Bette, A.2
Henninger, K.3
Hucke, F.4
Kohlsdorfer, C.5
Stass, H.H.6
-
196
-
-
0037364162
-
ADMET in silico modeling: Towards prediction paradise?
-
van de Waterbeemd H., Gifford E. ADMET in silico modeling: Towards prediction paradise?. Nature Rev. Drug Disc. 2003, 2:192-204.
-
(2003)
Nature Rev. Drug Disc.
, vol.2
, pp. 192-204
-
-
van de Waterbeemd, H.1
Gifford, E.2
-
198
-
-
2342444862
-
A return to the fundamentals of drug discovery
-
Williams M. A return to the fundamentals of drug discovery. Curr. Opin. Investigational Drugs 2004, 5:29-33.
-
(2004)
Curr. Opin. Investigational Drugs
, vol.5
, pp. 29-33
-
-
Williams, M.1
-
199
-
-
4644339418
-
Functional pharmacology: The drug discovery bottleneck?
-
Walker M.J.A., Barrett T., Guppy L.J. Functional pharmacology: The drug discovery bottleneck?. Drug Disc. Today 2004, 3:208-215.
-
(2004)
Drug Disc. Today
, vol.3
, pp. 208-215
-
-
Walker, M.J.A.1
Barrett, T.2
Guppy, L.J.3
-
200
-
-
20844449415
-
A pathophysiological paradigm for the therapy of psychiatric disease
-
Spedding M., Jay T., Cost de Silva J., Perret L. A pathophysiological paradigm for the therapy of psychiatric disease. Nature Rev. Drug. Disc. 2005, 4:467-476.
-
(2005)
Nature Rev. Drug. Disc.
, vol.4
, pp. 467-476
-
-
Spedding, M.1
Jay, T.2
Cost de Silva, J.3
Perret, L.4
-
202
-
-
0035895513
-
What if there were only 30,000 human genes?
-
Claverie J.-M. What if there were only 30,000 human genes?. Science 2001, 291:1255-1257.
-
(2001)
Science
, vol.291
, pp. 1255-1257
-
-
Claverie, J.-M.1
-
203
-
-
0034677966
-
Drug discovery: A historical perspective
-
Drews J. Drug discovery: A historical perspective. Science 2000, 287:1960-1964.
-
(2000)
Science
, vol.287
, pp. 1960-1964
-
-
Drews, J.1
-
204
-
-
0032509889
-
Mechanisms of disease: Chemokines-Chemotactic cytokines that mediate inflammation
-
Luster A.D. Mechanisms of disease: Chemokines-Chemotactic cytokines that mediate inflammation. N. Eng. J. Med. 1998, 338:436-445.
-
(1998)
N. Eng. J. Med.
, vol.338
, pp. 436-445
-
-
Luster, A.D.1
-
205
-
-
0031466811
-
Expression and function of CCR5 and CXCR4 on human langerhans cells and macrophages: Implications for HIV primary infection
-
Zaitseva M., Blauvelt A., Lee S., Lapham C.K., Klaus-Kovtun V., Mostowski H., Manischewitz J., Golding H. Expression and function of CCR5 and CXCR4 on human langerhans cells and macrophages: Implications for HIV primary infection. Nature Medicine 1997, 3:1369-1375.
-
(1997)
Nature Medicine
, vol.3
, pp. 1369-1375
-
-
Zaitseva, M.1
Blauvelt, A.2
Lee, S.3
Lapham, C.K.4
Klaus-Kovtun, V.5
Mostowski, H.6
Manischewitz, J.7
Golding, H.8
-
206
-
-
0033811703
-
Downregulation of the CCRS beta-chemokine receptor and inhibition of HIV-1 infection by stable VA1-ribozyme chimeric transcripts
-
Cagnon L., Rossi J.J. Downregulation of the CCRS beta-chemokine receptor and inhibition of HIV-1 infection by stable VA1-ribozyme chimeric transcripts. Antisense & Nucleic Acid Drug Development 2000, 10:251-261.
-
(2000)
Antisense & Nucleic Acid Drug Development
, vol.10
, pp. 251-261
-
-
Cagnon, L.1
Rossi, J.J.2
-
207
-
-
13044256383
-
A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity
-
Baba M., Nishimura O., Kanzaki N., Okamoto M., Sawada H., Iizawa Y., Shiraishi M., Aramaki Y., Okonogi K., Ogawa Y., Meguro K., Fujino M. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc. Natl. Acad. Sci. USA 1999, 96:5698-5703.
-
(1999)
Proc. Natl. Acad. Sci. USA
, vol.96
, pp. 5698-5703
-
-
Baba, M.1
Nishimura, O.2
Kanzaki, N.3
Okamoto, M.4
Sawada, H.5
Iizawa, Y.6
Shiraishi, M.7
Aramaki, Y.8
Okonogi, K.9
Ogawa, Y.10
Meguro, K.11
Fujino, M.12
-
209
-
-
17944365465
-
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure: Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes
-
Finke P.E., Oates B., Mills S.G., MacCoss M., Malkowitz L., Springer M.S., Gould S.L., DeMartino J.A., Carella A., Carver G., et al. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure: Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. 2001, 11:2475-2479.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2475-2479
-
-
Finke, P.E.1
Oates, B.2
Mills, S.G.3
MacCoss, M.4
Malkowitz, L.5
Springer, M.S.6
Gould, S.L.7
DeMartino, J.A.8
Carella, A.9
Carver, G.10
-
210
-
-
0032550337
-
Aminooxypentane-RANTES induces CCR5 internalization but inhibits recycling: A novel inhibitory mechanism of HIV infectivity
-
Mack M., Luckow B., Nelson P.J., Cihak J., Simmons G., Clapham P.R., Signoret N., Marsh M., Stangassinger M., Borlat F., Wells T.N.C., Schlondorff D., Proudfoot A.E.I. Aminooxypentane-RANTES induces CCR5 internalization but inhibits recycling: A novel inhibitory mechanism of HIV infectivity. J. Exp. Med. 1998, 187:1215-1224.
-
(1998)
J. Exp. Med.
, vol.187
, pp. 1215-1224
-
-
Mack, M.1
Luckow, B.2
Nelson, P.J.3
Cihak, J.4
Simmons, G.5
Clapham, P.R.6
Signoret, N.7
Marsh, M.8
Stangassinger, M.9
Borlat, F.10
Wells, T.N.C.11
Schlondorff, D.12
Proudfoot, A.E.I.13
-
211
-
-
0030951442
-
Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist
-
Simmons G., Clapham P.R., Picard L., Offord R.E., Rosenkilde M.M., Schwartz T.W., Buser R., Wells T.N.C., Proudfoot A.E.I. Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist. Science 1997, 276:276-279.
-
(1997)
Science
, vol.276
, pp. 276-279
-
-
Simmons, G.1
Clapham, P.R.2
Picard, L.3
Offord, R.E.4
Rosenkilde, M.M.5
Schwartz, T.W.6
Buser, R.7
Wells, T.N.C.8
Proudfoot, A.E.I.9
-
212
-
-
0032692850
-
Spontaneous and antigen-induced production of HIV-inhibitory-chemokines are associated with AIDS-free status
-
Garzino-Demo A., Moss R.B., Margolick J.B., Cleghorn F., Sill A., Blattner W.A., Cocchi F., Carlo D.J., DeVico A.L., Gallo R.C. Spontaneous and antigen-induced production of HIV-inhibitory-chemokines are associated with AIDS-free status. Proc. Natl. Acad. Sci. USA 1999, 96:11986-11991.
-
(1999)
Proc. Natl. Acad. Sci. USA
, vol.96
, pp. 11986-11991
-
-
Garzino-Demo, A.1
Moss, R.B.2
Margolick, J.B.3
Cleghorn, F.4
Sill, A.5
Blattner, W.A.6
Cocchi, F.7
Carlo, D.J.8
DeVico, A.L.9
Gallo, R.C.10
-
213
-
-
0031908542
-
Production of beta-chemokines in human immunodeficiency virus (HIV) infection: Evidence that high levels of macrophage in inflammatory protein-1-beta are associated with a decreased risk of HIV progression
-
Ullum H., Lepri A.C., Victor J., Aladdin H., Phillips A.N., Gerstoft J., Skinhoj P., Klarlund Pedersen B.K. Production of beta-chemokines in human immunodeficiency virus (HIV) infection: Evidence that high levels of macrophage in inflammatory protein-1-beta are associated with a decreased risk of HIV progression. J. Infect. Dis. 1998, 177:331-336.
-
(1998)
J. Infect. Dis.
, vol.177
, pp. 331-336
-
-
Ullum, H.1
Lepri, A.C.2
Victor, J.3
Aladdin, H.4
Phillips, A.N.5
Gerstoft, J.6
Skinhoj, P.7
Klarlund Pedersen, B.K.8
-
214
-
-
0035168719
-
Suppression of CCR5-but not CXCR4-tropic HIV-1 in lymphoid tissue by human herpesvirus 6
-
Grivel J.-C., Ito Y., Faga G., Santoro F., Shaheen F., Malnati M.S., Fitzgerald W., Lusso P., Margolis L. Suppression of CCR5-but not CXCR4-tropic HIV-1 in lymphoid tissue by human herpesvirus 6. Nature Med. 2001, 7:1232.
-
(2001)
Nature Med.
, vol.7
, pp. 1232
-
-
Grivel, J.-C.1
Ito, Y.2
Faga, G.3
Santoro, F.4
Shaheen, F.5
Malnati, M.S.6
Fitzgerald, W.7
Lusso, P.8
Margolis, L.9
-
215
-
-
0001633495
-
Genetic restriction of HIV-1 infection and progression to AIDS by a deletion allele of the CKR5 structural gene
-
Dean M., Carrington M., Winkler C., Huttley G.A., Smith M.W., Allikmets R., Goedert J.J., Buchbinder S.P., Vittinghoff E., Gomperts E., Donfield S., Vlahov D., Kaslow R., Saah A., Rinaldo C., Detels R. Genetic restriction of HIV-1 infection and progression to AIDS by a deletion allele of the CKR5 structural gene. Science 1996, 273:1856-1862.
-
(1996)
Science
, vol.273
, pp. 1856-1862
-
-
Dean, M.1
Carrington, M.2
Winkler, C.3
Huttley, G.A.4
Smith, M.W.5
Allikmets, R.6
Goedert, J.J.7
Buchbinder, S.P.8
Vittinghoff, E.9
Gomperts, E.10
Donfield, S.11
Vlahov, D.12
Kaslow, R.13
Saah, A.14
Rinaldo, C.15
Detels, R.16
-
216
-
-
16044367526
-
The role of a mutant CCR5 allele in HIV-1 transmission and disease progression
-
Huang Y., Paxton W.A., Wolinsky S.M., Neumann A.U., Zhang L., He T., Kang S., Ceradini D., Jin Z., Yazdanbakhsh K., Kunstman K., Erickson D., Dragon E., Landau N.R., Phair J., Ho D.D., Koup R.A. The role of a mutant CCR5 allele in HIV-1 transmission and disease progression. Nature Med. 1996, 2:1240-1243.
-
(1996)
Nature Med.
, vol.2
, pp. 1240-1243
-
-
Huang, Y.1
Paxton, W.A.2
Wolinsky, S.M.3
Neumann, A.U.4
Zhang, L.5
He, T.6
Kang, S.7
Ceradini, D.8
Jin, Z.9
Yazdanbakhsh, K.10
Kunstman, K.11
Erickson, D.12
Dragon, E.13
Landau, N.R.14
Phair, J.15
Ho, D.D.16
Koup, R.A.17
-
217
-
-
15844388931
-
Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection
-
Liu R., Paxton W.A., Choe S., Ceradini D., Martin S.R., Horuk R., MacDonald M.I., Stuhlmann H., Koup R.A., Landau N.R. Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection. Cell 1996, 86:367-377.
-
(1996)
Cell
, vol.86
, pp. 367-377
-
-
Liu, R.1
Paxton, W.A.2
Choe, S.3
Ceradini, D.4
Martin, S.R.5
Horuk, R.6
MacDonald, M.I.7
Stuhlmann, H.8
Koup, R.A.9
Landau, N.R.10
-
218
-
-
12644274812
-
Relative resistance to HIV-1 infection of CD4 lymphocytes from persons who remain uninfected despite multiple high-risk sexual exposures
-
Paxton W.A., Martin S.R., Tse D., O'Brien T.R., Skurnick J., VanDevanter N.L., Padian N., Braun J.F., Kotler D.P., Wolinsky S.M., Koup R.A. Relative resistance to HIV-1 infection of CD4 lymphocytes from persons who remain uninfected despite multiple high-risk sexual exposures. Nature Med. 1996, 2:412-417.
-
(1996)
Nature Med.
, vol.2
, pp. 412-417
-
-
Paxton, W.A.1
Martin, S.R.2
Tse, D.3
O'Brien, T.R.4
Skurnick, J.5
VanDevanter, N.L.6
Padian, N.7
Braun, J.F.8
Kotler, D.P.9
Wolinsky, S.M.10
Koup, R.A.11
-
219
-
-
16044373004
-
Resistance to HIV-1 infection in Caucasian individuals bearing mutant alleles to the CCR-5 chemokine receptor gene
-
Samson M., Libert F., Doranz B.J., Rucker J., Liesnard C., Farber C.M., Saragosti S., Lapoumerouilie C., Cognaux J., Forceille C., Muyldermans G., Verhofstede C., Collman R.G., Doms R.W., Vassart G., Parmentier M. Resistance to HIV-1 infection in Caucasian individuals bearing mutant alleles to the CCR-5 chemokine receptor gene. Nature 1996, 382:722-725.
-
(1996)
Nature
, vol.382
, pp. 722-725
-
-
Samson, M.1
Libert, F.2
Doranz, B.J.3
Rucker, J.4
Liesnard, C.5
Farber, C.M.6
Saragosti, S.7
Lapoumerouilie, C.8
Cognaux, J.9
Forceille, C.10
Muyldermans, G.11
Verhofstede, C.12
Collman, R.G.13
Doms, R.W.14
Vassart, G.15
Parmentier, M.16
-
220
-
-
0028979682
-
Requirement of MIP-1 for an inflammatory response to viral infection
-
Cook D.N., Beck M.A., Coffman T.M., Kirby S.L., Sheridan J.F., Pragnell I.B., Smithies O. Requirement of MIP-1 for an inflammatory response to viral infection. Science 1995, 269:1583-1585.
-
(1995)
Science
, vol.269
, pp. 1583-1585
-
-
Cook, D.N.1
Beck, M.A.2
Coffman, T.M.3
Kirby, S.L.4
Sheridan, J.F.5
Pragnell, I.B.6
Smithies, O.7
-
221
-
-
0034800634
-
Adverse effect of the CCR5 promoter -2459A allele on HIV-1 disease progression
-
Knudsen T.B., Kristiansen T.B., Katsenstein T.L., Eugen-Olsen J. Adverse effect of the CCR5 promoter -2459A allele on HIV-1 disease progression. J. Med. Virol. 2001, 65:441.
-
(2001)
J. Med. Virol.
, vol.65
, pp. 441
-
-
Knudsen, T.B.1
Kristiansen, T.B.2
Katsenstein, T.L.3
Eugen-Olsen, J.4
-
222
-
-
0036490096
-
Regulators of G-protein signaling as new central nervous system drug targets
-
Neubig R.R., Siderovski D.P. Regulators of G-protein signaling as new central nervous system drug targets. Nature Rev. Drug Disc. 2002, 1:187-196.
-
(2002)
Nature Rev. Drug Disc.
, vol.1
, pp. 187-196
-
-
Neubig, R.R.1
Siderovski, D.P.2
-
223
-
-
1342303482
-
Of mice and not men: Differences between mouse and human immunology
-
Mestas J., Hughes C.C. Of mice and not men: Differences between mouse and human immunology. J. Immunol. 2004, 172:2731-2738.
-
(2004)
J. Immunol.
, vol.172
, pp. 2731-2738
-
-
Mestas, J.1
Hughes, C.C.2
-
224
-
-
0034214841
-
NK1 (Substance P) receptor antagonists: Why are they not analgesic in humans?
-
Hill R. NK1 (Substance P) receptor antagonists: Why are they not analgesic in humans?. Trends Pharmacol. Sci. 2000, 21:244-246.
-
(2000)
Trends Pharmacol. Sci.
, vol.21
, pp. 244-246
-
-
Hill, R.1
-
225
-
-
0035940445
-
SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo
-
Strizki J.M., Xu S., Wagner N.E., Wojcik L., Liu J., Hou Y., Endres M., Palani A., Shapiro S., Clader J.W., et al. SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo. Proc. Natl. Acad. Sci. USA 2001, 98:12718-12723.
-
(2001)
Proc. Natl. Acad. Sci. USA
, vol.98
, pp. 12718-12723
-
-
Strizki, J.M.1
Xu, S.2
Wagner, N.E.3
Wojcik, L.4
Liu, J.5
Hou, Y.6
Endres, M.7
Palani, A.8
Shapiro, S.9
Clader, J.W.10
-
227
-
-
0036532579
-
Recombinant baculoviruses as mammalian cell gene-delivery vectors
-
Kost T.A., Condreay J.P. Recombinant baculoviruses as mammalian cell gene-delivery vectors. Trends Biotechnol. 2002, 20:173-180.
-
(2002)
Trends Biotechnol.
, vol.20
, pp. 173-180
-
-
Kost, T.A.1
Condreay, J.P.2
-
228
-
-
1942517818
-
Techniques: Cardiovascular pharmacology and drug discovery in the 21st century
-
Douglas S.A., Ohlstein E.H., Johns D.G. Techniques: Cardiovascular pharmacology and drug discovery in the 21st century. Trends Pharmacol. Sci. 2004, 25:225-233.
-
(2004)
Trends Pharmacol. Sci.
, vol.25
, pp. 225-233
-
-
Douglas, S.A.1
Ohlstein, E.H.2
Johns, D.G.3
-
229
-
-
0028838012
-
Dimerization of cell surface receptors in signal transduction
-
Heldin C.H. Dimerization of cell surface receptors in signal transduction. Cell 1995, 80:213-223.
-
(1995)
Cell
, vol.80
, pp. 213-223
-
-
Heldin, C.H.1
-
230
-
-
0036780743
-
G-protein-coupled receptor oligomerization and its potential for drug discovery
-
George S.R., O'Dowd B.F., Lee S.P. G-protein-coupled receptor oligomerization and its potential for drug discovery. Nature Rev. Drug Disc. 2002, 1:808-820.
-
(2002)
Nature Rev. Drug Disc.
, vol.1
, pp. 808-820
-
-
George, S.R.1
O'Dowd, B.F.2
Lee, S.P.3
-
231
-
-
0034618268
-
At1-receptor heterodimers show enhanced G-protein activation and altered receptor sequestration
-
AbdAlla S., Lother H., Quitterer U. At1-receptor heterodimers show enhanced G-protein activation and altered receptor sequestration. Nature 2000, 407:94-98.
-
(2000)
Nature
, vol.407
, pp. 94-98
-
-
AbdAlla, S.1
Lother, H.2
Quitterer, U.3
-
232
-
-
0034785580
-
Increased AT(1) receptor dimers in preeclampsia mediate enhanced angiotensin II responsiveness
-
AbdAla S., Lother H., el Massiery A., Quitterer U. Increased AT(1) receptor dimers in preeclampsia mediate enhanced angiotensin II responsiveness. Nature Med. 2001, 7:1003-1009.
-
(2001)
Nature Med.
, vol.7
, pp. 1003-1009
-
-
AbdAla, S.1
Lother, H.2
el Massiery, A.3
Quitterer, U.4
-
233
-
-
17144473106
-
Chemokine receptor homo- or heterodimerization activates distinct signaling pathways
-
Mellado M., Rodríguez-Frade J.M., Vila-Coro A.J., Fernández S., Martín de Ana A., Jones D.R., Torán J.L., Martínez-Aet C. Chemokine receptor homo- or heterodimerization activates distinct signaling pathways. EMBO J. 2001, 20:2497-2507.
-
(2001)
EMBO J.
, vol.20
, pp. 2497-2507
-
-
Mellado, M.1
Rodríguez-Frade, J.M.2
Vila-Coro, A.J.3
Fernández, S.4
Martín de Ana, A.5
Jones, D.R.6
Torán, J.L.7
Martínez-Aet, C.8
-
234
-
-
21144446486
-
A heterodimer-selective agonist shows in vivo relevance of G-protein coupled receptor dimers
-
Wildoer M., Fong J., Jones R.M., Lunzer M.M., Sharma S.K., Kostensis E., Portoghese P.S., Whistler J.L. A heterodimer-selective agonist shows in vivo relevance of G-protein coupled receptor dimers. Proc. Nat. Acad. Sci. USA 2005, 102:9050-9055.
-
(2005)
Proc. Nat. Acad. Sci. USA
, vol.102
, pp. 9050-9055
-
-
Wildoer, M.1
Fong, J.2
Jones, R.M.3
Lunzer, M.M.4
Sharma, S.K.5
Kostensis, E.6
Portoghese, P.S.7
Whistler, J.L.8
-
235
-
-
0242269463
-
GPCR dimerization
-
Milligan G., Ramsay D., Pascal G., Carrillo J.J. GPCR dimerization. Life Sci. 2003, 74:181-188.
-
(2003)
Life Sci.
, vol.74
, pp. 181-188
-
-
Milligan, G.1
Ramsay, D.2
Pascal, G.3
Carrillo, J.J.4
-
236
-
-
0043069489
-
Drug research: Myths, hype, and reality
-
Kubinyi H. Drug research: Myths, hype, and reality. Nature Rev. Drug Disc. 2003, 2:665-668.
-
(2003)
Nature Rev. Drug Disc.
, vol.2
, pp. 665-668
-
-
Kubinyi, H.1
-
237
-
-
0033303252
-
Pharmacological characterization of receptor-activity-modifying proteins (RAMPs) and the human calcitonin receptor
-
Armour S.L., Foord S., Kenakin T., Chen W.-J. Pharmacological characterization of receptor-activity-modifying proteins (RAMPs) and the human calcitonin receptor. J. Pharmacol. Toxicol. Meth. 1999, 42:217-224.
-
(1999)
J. Pharmacol. Toxicol. Meth.
, vol.42
, pp. 217-224
-
-
Armour, S.L.1
Foord, S.2
Kenakin, T.3
Chen, W.-J.4
-
238
-
-
0033054409
-
RAMPS: Accessory proteins for seven transmembrane domain receptors
-
Foord S.M., Marshall F.H. RAMPS: Accessory proteins for seven transmembrane domain receptors. Trends Pharmacol. Sci. 1999, 20:184-187.
-
(1999)
Trends Pharmacol. Sci.
, vol.20
, pp. 184-187
-
-
Foord, S.M.1
Marshall, F.H.2
-
239
-
-
0033013790
-
The amino terminus of receptor activity modifying proteins is a critical determinant of glycosylation state and ligand binding of calcitonin-like receptor
-
Fraser N.J., Wise A., Brown J., McLatchie L.M., Main M.J., Foord S.M. The amino terminus of receptor activity modifying proteins is a critical determinant of glycosylation state and ligand binding of calcitonin-like receptor. Mol. Pharmacol. 1999, 55:1054-1059.
-
(1999)
Mol. Pharmacol.
, vol.55
, pp. 1054-1059
-
-
Fraser, N.J.1
Wise, A.2
Brown, J.3
McLatchie, L.M.4
Main, M.J.5
Foord, S.M.6
-
240
-
-
4644264129
-
An integrative biology approach for analysis of drug action in models of human vascular inflammation
-
Kunkel E.J., Dea M., Ebens A., Hytopoulos E., Melrose J., Nguyen D., Ota K.S., Plavec I., Wang Y., Watson S.R., Butcher E.C., Berg E.L. An integrative biology approach for analysis of drug action in models of human vascular inflammation. FASEB J. 2004, 18:1279-1301.
-
(2004)
FASEB J.
, vol.18
, pp. 1279-1301
-
-
Kunkel, E.J.1
Dea, M.2
Ebens, A.3
Hytopoulos, E.4
Melrose, J.5
Nguyen, D.6
Ota, K.S.7
Plavec, I.8
Wang, Y.9
Watson, S.R.10
Butcher, E.C.11
Berg, E.L.12
-
241
-
-
4644356849
-
Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMap analysis in complex human primary cell-based models
-
Kunkel E.J., Plavec I., Nguyen D., Melrose J., Rosler E.S., Kao L.T., Wang Y., Hytopoulos E., Bishop A.C., Bateman R., Shokat K.M., Butcher E.C., Berg E.L. Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMap analysis in complex human primary cell-based models. ASSAY Drug. Dev. Technol. 2004, 2:431-441.
-
(2004)
ASSAY Drug. Dev. Technol.
, vol.2
, pp. 431-441
-
-
Kunkel, E.J.1
Plavec, I.2
Nguyen, D.3
Melrose, J.4
Rosler, E.S.5
Kao, L.T.6
Wang, Y.7
Hytopoulos, E.8
Bishop, A.C.9
Bateman, R.10
Shokat, K.M.11
Butcher, E.C.12
Berg, E.L.13
-
242
-
-
0242499448
-
Cytostatic and apoptotic actions of TGF in homeostasis and cancer
-
Siegel P.M., Massague J. Cytostatic and apoptotic actions of TGF in homeostasis and cancer. Nature Rev. Cancer 2003, 3:807-821.
-
(2003)
Nature Rev. Cancer
, vol.3
, pp. 807-821
-
-
Siegel, P.M.1
Massague, J.2
-
243
-
-
0020035442
-
The effects of MDL 17,043 on cardiac inotropy in the anaesthetized dog
-
Dage R.C., Roebel L.E., Hsieh C.P., Weiner D.L., Woodward J.K. The effects of MDL 17,043 on cardiac inotropy in the anaesthetized dog. J. Cardiovasc. Pharmacol. 1982, 4:500-512.
-
(1982)
J. Cardiovasc. Pharmacol.
, vol.4
, pp. 500-512
-
-
Dage, R.C.1
Roebel, L.E.2
Hsieh, C.P.3
Weiner, D.L.4
Woodward, J.K.5
-
244
-
-
0023612341
-
A method to assess concomitant cardiac phosphodiesterase inhibition and positive inotropy
-
Kenakin T.P., Scott D.L. A method to assess concomitant cardiac phosphodiesterase inhibition and positive inotropy. J. Cardiovasc. Pharmacol. 1987, 10:658-666.
-
(1987)
J. Cardiovasc. Pharmacol.
, vol.10
, pp. 658-666
-
-
Kenakin, T.P.1
Scott, D.L.2
-
245
-
-
0023108279
-
An in vivo analysis of purine-mediated renal vasoconstriction in rat isolated kidney
-
Kenakin T.P., Pike N.B. An in vivo analysis of purine-mediated renal vasoconstriction in rat isolated kidney. Br. J. Pharmacol. 1987, 90:373-381.
-
(1987)
Br. J. Pharmacol.
, vol.90
, pp. 373-381
-
-
Kenakin, T.P.1
Pike, N.B.2
-
246
-
-
0002370296
-
Drug and organ selectivity: Similarities and differences
-
Academic Press, New York
-
Kenakin T.P. Drug and organ selectivity: Similarities and differences. Advances in drug research 1985, Vol. 15:71-109. Academic Press, New York.
-
(1985)
Advances in drug research
, vol.15
, pp. 71-109
-
-
Kenakin, T.P.1
-
247
-
-
23844474716
-
The ultimate model organism: Progress in experimental medicine
-
Littman B.H., Williams S.A. The ultimate model organism: Progress in experimental medicine. Nature Rev. Drug Disc. 2005, 4:631-638.
-
(2005)
Nature Rev. Drug Disc.
, vol.4
, pp. 631-638
-
-
Littman, B.H.1
Williams, S.A.2
-
250
-
-
1642401467
-
Pharmaceutical productivity: The imperative for new paradigms
-
Milne G.M. Pharmaceutical productivity: The imperative for new paradigms. Annu. Rep. Med. Chem. 2003, 38:383-396.
-
(2003)
Annu. Rep. Med. Chem.
, vol.38
, pp. 383-396
-
-
Milne, G.M.1
-
251
-
-
0037107019
-
Surrogate endpoints in cancer drug development
-
Sikora K. Surrogate endpoints in cancer drug development. Drug Disc. Today 2002, 7:951-956.
-
(2002)
Drug Disc. Today
, vol.7
, pp. 951-956
-
-
Sikora, K.1
-
252
-
-
0034666653
-
Antiarrhythmic and electrophysiological effects of GYK-16638, a novel N-(phenoxyalkyl)-N-phenylalkylamine, in rabbits
-
Baczko I., El-Reyani N.E., Farkas A., Virág L., Iost N., Leprán I., Mátyus P., Varró A., Papp J.G. Antiarrhythmic and electrophysiological effects of GYK-16638, a novel N-(phenoxyalkyl)-N-phenylalkylamine, in rabbits. Eur. J. Pharmacol. 2000, 404:181-190.
-
(2000)
Eur. J. Pharmacol.
, vol.404
, pp. 181-190
-
-
Baczko, I.1
El-Reyani, N.E.2
Farkas, A.3
Virág, L.4
Iost, N.5
Leprán, I.6
Mátyus, P.7
Varró, A.8
Papp, J.G.9
-
253
-
-
27144449695
-
Designed multiple ligands: An emerging drug discovery paradigm
-
Morphy R., Rankovic Z. Designed multiple ligands: An emerging drug discovery paradigm. J. Med. Chem. 2005, 48:6523-6543.
-
(2005)
J. Med. Chem.
, vol.48
, pp. 6523-6543
-
-
Morphy, R.1
Rankovic, Z.2
-
254
-
-
0032539780
-
Dimerization of sumitryptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist
-
Perez M., Pauwels P.J., Fourrier C., Chopin P., Valentin J.-P., John G.W., Marien M., Halazy S. Dimerization of sumitryptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist. Bioorg. Med. Chem. Lett. 1998, 8:675-680.
-
(1998)
Bioorg. Med. Chem. Lett.
, vol.8
, pp. 675-680
-
-
Perez, M.1
Pauwels, P.J.2
Fourrier, C.3
Chopin, P.4
Valentin, J.-P.5
John, G.W.6
Marien, M.7
Halazy, S.8
-
256
-
-
0031051342
-
Combined antagonism of leukotrienes and histamine produces predominant inhibition of allergen-induced early and late phase airway obstruction in asthmatics
-
Zhang M., van de Stolpe A., Zuiderveld O., Timmermans H. Combined antagonism of leukotrienes and histamine produces predominant inhibition of allergen-induced early and late phase airway obstruction in asthmatics. Eur. J. Med. Chem. 1997, 32:95-102.
-
(1997)
Eur. J. Med. Chem.
, vol.32
, pp. 95-102
-
-
Zhang, M.1
van de Stolpe, A.2
Zuiderveld, O.3
Timmermans, H.4
-
257
-
-
0021857696
-
The importance of adrenoceptor agonist activity of dobutamine to inotropic selectivity in the anaesthetized cat
-
Kenakin T.P., Johnson S.F. The importance of adrenoceptor agonist activity of dobutamine to inotropic selectivity in the anaesthetized cat. Eur. J. Pharmacol. 1985, 111:347-354.
-
(1985)
Eur. J. Pharmacol.
, vol.111
, pp. 347-354
-
-
Kenakin, T.P.1
Johnson, S.F.2
-
258
-
-
8444238556
-
Beta-blockers in heart failure: Are pharmacological differences clinically important?
-
Metra M., Dei Cas L., di Lenarda A., Poole-Wilson P. Beta-blockers in heart failure: Are pharmacological differences clinically important?. Heart Fail. Rev. 2004, 9:123-130.
-
(2004)
Heart Fail. Rev.
, vol.9
, pp. 123-130
-
-
Metra, M.1
Dei Cas, L.2
di Lenarda, A.3
Poole-Wilson, P.4
-
259
-
-
0021058380
-
Operational models of pharmacological agonist
-
Black J.W., Leff P. Operational models of pharmacological agonist. Proc. R. Soc. Lond. [Biol.] 1983, 220:141.
-
(1983)
Proc. R. Soc. Lond. [Biol.]
, vol.220
, pp. 141
-
-
Black, J.W.1
Leff, P.2
-
260
-
-
0010673662
-
A modification of receptor theory
-
Stephenson R.P. A modification of receptor theory. Br. J. Pharmacol. 1956, 11:379-393.
-
(1956)
Br. J. Pharmacol.
, vol.11
, pp. 379-393
-
-
Stephenson, R.P.1
-
262
-
-
0018909079
-
Is prenalterol (H 133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from difference in stimulus-response relationships
-
Kenakin T.P., Beek D. Is prenalterol (H 133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from difference in stimulus-response relationships. J. Pharmacol. Exp. Ther.. 1980, 213:406-413.
-
(1980)
J. Pharmacol. Exp. Ther..
, vol.213
, pp. 406-413
-
-
Kenakin, T.P.1
Beek, D.2
-
263
-
-
34548853458
-
Allosteric agonist modulators
-
Kenakin T.P. Allosteric agonist modulators. J. Recept. Signal. Transd. 2007, 27:247-259.
-
(2007)
J. Recept. Signal. Transd.
, vol.27
, pp. 247-259
-
-
Kenakin, T.P.1
-
264
-
-
0015861774
-
Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction
-
Cheng Y.C., Prusoff W.H. Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
-
(1973)
Biochem. Pharmacol.
, vol.22
, pp. 3099-3108
-
-
Cheng, Y.C.1
Prusoff, W.H.2
-
265
-
-
0027522536
-
Further concerns over Cheng-Prusoff analysis
-
Leff P., Dougall I.G. Further concerns over Cheng-Prusoff analysis. Trends Pharmacol. Sci. 1993, 14:110-112.
-
(1993)
Trends Pharmacol. Sci.
, vol.14
, pp. 110-112
-
-
Leff, P.1
Dougall, I.G.2
-
266
-
-
34447624153
-
Collateral efficacy in drug discovery: Taking advantage of the good (allosteric) nature of 7TM receptors
-
Kenakin T.P. Collateral efficacy in drug discovery: Taking advantage of the good (allosteric) nature of 7TM receptors. Trends Pharmacol. Sci.. 2007, 28:407-415.
-
(2007)
Trends Pharmacol. Sci..
, vol.28
, pp. 407-415
-
-
Kenakin, T.P.1
-
267
-
-
0030450983
-
A novel mechanism of activity-dependent NMDA receptor antagonism describes the effect of ifenprodil in rat cultured cortical neurons
-
Kew J.N.C., Trube G., Kemp J.A. A novel mechanism of activity-dependent NMDA receptor antagonism describes the effect of ifenprodil in rat cultured cortical neurons. J. Physiol. 1996, 497:761-772.
-
(1996)
J. Physiol.
, vol.497
, pp. 761-772
-
-
Kew, J.N.C.1
Trube, G.2
Kemp, J.A.3
-
268
-
-
33748325882
-
Drug target residence time and its implications for lead optimization
-
Copeland R.A., Pompliano D.L., Meek T.D. Drug target residence time and its implications for lead optimization. Nat. Rev. Drug Disc. 2006, 5::730-739.
-
(2006)
Nat. Rev. Drug Disc.
, pp. 730-739
-
-
Copeland, R.A.1
Pompliano, D.L.2
Meek, T.D.3
-
269
-
-
33751183557
-
Determining the potency and molecular mechanism of action of insurmountable antagonists
-
Kenakin T.P., Jenkinson S., Watson C. Determining the potency and molecular mechanism of action of insurmountable antagonists. J. Pharmacol. Exp. Ther. 2006, 319:710-723.
-
(2006)
J. Pharmacol. Exp. Ther.
, vol.319
, pp. 710-723
-
-
Kenakin, T.P.1
Jenkinson, S.2
Watson, C.3
-
270
-
-
0002177268
-
The quantitative effects of antagonistic drugs
-
Gaddum J.H. The quantitative effects of antagonistic drugs. J. Physiol. Lond. 1937, 89:7P-9P.
-
(1937)
J. Physiol. Lond.
, vol.89
, pp. 7P-9P
-
-
Gaddum, J.H.1
-
272
-
-
84882062420
-
-
SAS Institute, Cary, North Carolina, R.J. Freund, C.R. Litell (Eds.)
-
Non-linear models: SAS system recognition 1991, SAS Institute, Cary, North Carolina. R.J. Freund, C.R. Litell (Eds.).
-
(1991)
Non-linear models: SAS system recognition
-
-
-
273
-
-
0035993439
-
Assessing the (a)symmetry of concentration-effect curves: Empirical versus mechanistic models
-
Giraldo J., Vivas N.M., Vila E., Badia A. Assessing the (a)symmetry of concentration-effect curves: Empirical versus mechanistic models. Pharmacol. Therap 2002, 95:21-45.
-
(2002)
Pharmacol. Therap
, vol.95
, pp. 21-45
-
-
Giraldo, J.1
Vivas, N.M.2
Vila, E.3
Badia, A.4
-
274
-
-
0033303265
-
Development of scintillation-proximity assays for alpha adrenoceptors
-
Gobel J., Saussy D.L., Goetiz A.S. Development of scintillation-proximity assays for alpha adrenoceptors. J. Pharmacol. Toxicol. Meth 1999, 42:2-7.
-
(1999)
J. Pharmacol. Toxicol. Meth
, vol.42
, pp. 2-7
-
-
Gobel, J.1
Saussy, D.L.2
Goetiz, A.S.3
-
275
-
-
0003293418
-
On the nature of the function expressive of the law of human mortality
-
Gompertz B. On the nature of the function expressive of the law of human mortality. Philo. Trans. R. Soc. Lond 1825, 36:513-585.
-
(1825)
Philo. Trans. R. Soc. Lond
, vol.36
, pp. 513-585
-
-
Gompertz, B.1
-
276
-
-
0019402921
-
The measurement of antagonist potency and the importance of selective inhibition of agonist uptake processes
-
Kenakin T.P., Beek D. The measurement of antagonist potency and the importance of selective inhibition of agonist uptake processes. J. Pharmacol. Exp. Ther 1981, 219:112-120.
-
(1981)
J. Pharmacol. Exp. Ther
, vol.219
, pp. 112-120
-
-
Kenakin, T.P.1
Beek, D.2
-
277
-
-
4043147979
-
A flexible growth function for empirical use
-
Richards F.J. A flexible growth function for empirical use. J. Exp. Bot 1959, 10:290-300.
-
(1959)
J. Exp. Bot
, vol.10
, pp. 290-300
-
-
Richards, F.J.1
-
279
-
-
0033663775
-
The use of stimulus-biased assay systems to detect agonist-specific receptor active states: Implications for the trafficking of receptor stimulus by agonists
-
Watson C., Chen G., Irving P.E., Way J., Chen W.-J., Kenakin T.P. The use of stimulus-biased assay systems to detect agonist-specific receptor active states: Implications for the trafficking of receptor stimulus by agonists. Mol. Pharmacol 2000, 58:1230-1238.
-
(2000)
Mol. Pharmacol
, vol.58
, pp. 1230-1238
-
-
Watson, C.1
Chen, G.2
Irving, P.E.3
Way, J.4
Chen, W.-J.5
Kenakin, T.P.6
-
280
-
-
0015861774
-
Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction
-
Cheng Y.C., Prusoff W.H. Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
-
(1973)
Biochem. Pharmacol.
, vol.22
, pp. 3099-3108
-
-
Cheng, Y.C.1
Prusoff, W.H.2
-
281
-
-
0021947834
-
Self-cancellation of drug properties as a mode of organ selectivity: The antimuscarinic effects of ambenonium
-
Kenakin T.P., Beek D. Self-cancellation of drug properties as a mode of organ selectivity: The antimuscarinic effects of ambenonium. J. Pharmacol. Exp. Ther. 1985, 232:732-740.
-
(1985)
J. Pharmacol. Exp. Ther.
, vol.232
, pp. 732-740
-
-
Kenakin, T.P.1
Beek, D.2
-
282
-
-
1842333847
-
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
-
Jakubic J., Bacakova L., Lisa V., El-Fakahany E.E., Tucek S. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 1997, 52:172-179.
-
(1997)
Mol. Pharmacol.
, vol.52
, pp. 172-179
-
-
Jakubic, J.1
Bacakova, L.2
Lisa, V.3
El-Fakahany, E.E.4
Tucek, S.5
|