-
1
-
-
42149181885
-
Structural diversity of G protein-coupled receptors and significance for drug discovery
-
Lagerstrom, M.C. and Schioth, H.B. Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat. Rev. Drug Discov. 7, 339-357 (2008).
-
(2008)
Nat. Rev. Drug Discov.
, vol.7
, pp. 339-357
-
-
Lagerstrom, M.C.1
Schioth, H.B.2
-
2
-
-
33751547539
-
How many drug targets are there?
-
Overington, J.P., Al-Lazikani, B., and Hopkins, A.L. How many drug targets are there? Nat. Rev. Drug Discov. 5, 993-996 (2006).
-
(2006)
Nat. Rev. Drug Discov.
, vol.5
, pp. 993-996
-
-
Overington, J.P.1
Al-Lazikani, B.2
Hopkins, A.L.3
-
3
-
-
1642495639
-
Efficacy as a vector: The relative prevalence and paucity of inverse agonism
-
Kenakin, T. Efficacy as a vector: The relative prevalence and paucity of inverse agonism. Mol. Pharmacol. 65, 2-11 (2004).
-
(2004)
Mol. Pharmacol.
, vol.65
, pp. 2-11
-
-
Kenakin, T.1
-
4
-
-
0036490942
-
Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery
-
Christopoulos, A. Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery. Nat. Rev. Drug Discov. 1, 198-210 (2002).
-
(2002)
Nat. Rev. Drug Discov.
, vol.1
, pp. 198-210
-
-
Christopoulos, A.1
-
5
-
-
33847122495
-
Allosteric modulation of G protein-coupled receptors
-
A comprehensive overview of GPCR allosteric modulation
-
May, L.T., Leach, K., Sexton, P.M., and Christopoulos, A. Allosteric modulation of G protein-coupled receptors. Annu. Rev. Pharmacol. Toxicol. 47, 1-51 (2007). A comprehensive overview of GPCR allosteric modulation.
-
(2007)
Annu. Rev. Pharmacol. Toxicol.
, vol.47
, pp. 1-51
-
-
May, L.T.1
Leach, K.2
Sexton, P.M.3
Christopoulos, A.4
-
6
-
-
3042663287
-
G protein-coupled receptor dimerization: Function and ligand pharmacology
-
Milligan, G. G protein-coupled receptor dimerization: Function and ligand pharmacology. Mol. Pharmacol. 66, 1-7 (2004).
-
(2004)
Mol. Pharmacol.
, vol.66
, pp. 1-7
-
-
Milligan, G.1
-
7
-
-
33845903110
-
Functional selectivity and classical concepts of quantitative pharmacology
-
A recent overview on the concepts of stimulusbias and functional selectivity at GPCRs
-
Urban, J.D., Clarke, W.P., von Zastrow, M. et al. Functional selectivity and classical concepts of quantitative pharmacology. J. Pharmacol. Exp. Ther. 320, 1-13 (2007). A recent overview on the concepts of stimulusbias and functional selectivity at GPCRs.
-
(2007)
J. Pharmacol. Exp. Ther.
, vol.320
, pp. 1-13
-
-
Urban, J.D.1
Clarke, W.P.2
Von Zastrow, M.3
-
8
-
-
0017620408
-
ACTH: A short introductory review
-
This is one of the first papers to formalize the "message- address" concept
-
Schwyzer, R. ACTH: A short introductory review. Ann. N.Y. Acad. Sci. 297, 3-26 (1977). This is one of the first papers to formalize the "message-address" concept.
-
(1977)
Ann. N.Y. Acad. Sci.
, vol.297
, pp. 3-26
-
-
Schwyzer, R.1
-
9
-
-
0024405504
-
Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists
-
An early and important review on the utility of bivalent GPCR ligands
-
Portoghese, P.S. Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists. Trends Pharmacol. Sci. 10, 230-235 (1989). An early and important review on the utility of bivalent GPCR ligands.
-
(1989)
Trends Pharmacol. Sci.
, vol.10
, pp. 230-235
-
-
Portoghese, P.S.1
-
10
-
-
3042684536
-
Bivalent ligands for G protein-coupled receptors
-
Messer, W.S., Jr. Bivalent ligands for G protein-coupled receptors. Curr. Pharm. Des. 10, 2015-2020 (2004).
-
(2004)
Curr. Pharm. Des.
, vol.10
, pp. 2015-2020
-
-
Messer Jr., W.S.1
-
11
-
-
77049317286
-
Dicholinesters of alpha, omega-dicarboxylic acids and related substances
-
Brucke, F. Dicholinesters of alpha, omega-dicarboxylic acids and related substances. Pharmacol. Rev. 8, 265-335 (1956).
-
(1956)
Pharmacol. Rev.
, vol.8
, pp. 265-335
-
-
Brucke, F.1
-
12
-
-
0019990819
-
Narcotic antagonistic potency of bivalent ligands which contain beta-naltrexamine. Evidence for bridging between proximal recognition sites
-
An early example of the directed design of bivalent GPCR ligands
-
Erez, M., Takemori, A.E., and Portoghese, P.S. Narcotic antagonistic potency of bivalent ligands which contain beta-naltrexamine. Evidence for bridging between proximal recognition sites. J. Med. Chem. 25, 847-849 (1982). An early example of the directed design of bivalent GPCR ligands.
-
(1982)
J. Med. Chem.
, vol.25
, pp. 847-849
-
-
Erez, M.1
Takemori, A.E.2
Portoghese, P.S.3
-
13
-
-
0022902748
-
Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors
-
Portoghese, P.S., Larson, D.L., Sayre, L.M., Yim, C.B., Ronsisvalle, G., Tam, S.W., and Takemori, A.E. Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors. J. Med. Chem. 29, 1855-1861 (1986).
-
(1986)
J. Med. Chem.
, vol.29
, pp. 1855-1861
-
-
Portoghese, P.S.1
Larson, D.L.2
Sayre, L.M.3
Yim, C.B.4
Ronsisvalle, G.5
Tam, S.W.6
Takemori, A.E.7
-
14
-
-
0022251438
-
Stereostructure-activity relationship of opioid agonist and antagonist bivalent ligands. Evidence for bridging between vicinal opioid receptors
-
Portoghese, P.S., Larson, D.L., Yim, C.B., Sayre, L.M., Ronsisvalle, G., Lipkowski, A.W., Takemori, A.E., Rice, K.C., and Tam, S.W. Stereostructure- activity relationship of opioid agonist and antagonist bivalent ligands. Evidence for bridging between vicinal opioid receptors. J. Med. Chem. 28, 1140-1141 (1985).
-
(1985)
J. Med. Chem.
, vol.28
, pp. 1140-1141
-
-
Portoghese, P.S.1
Larson, D.L.2
Yim, C.B.3
Sayre, L.M.4
Ronsisvalle, G.5
Lipkowski, A.W.6
Takemori, A.E.7
Rice, K.C.8
Tam, S.W.9
-
15
-
-
0034883492
-
Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists
-
Christopoulos, A., Grant, M.K., Ayoubzadeh, N., Kim, O.N., Sauerberg, P., Jeppesen, L., and El-Fakahany, E.E. Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists. J. Pharmacol. Exp. Ther. 298, 1260-1268 (2001).
-
(2001)
J. Pharmacol. Exp. Ther.
, vol.298
, pp. 1260-1268
-
-
Christopoulos, A.1
Grant, M.K.2
Ayoubzadeh, N.3
Kim, O.N.4
Sauerberg, P.5
Jeppesen, L.6
El-Fakahany, E.E.7
-
16
-
-
0024472072
-
Polymethylene tetraamines as muscarinic receptor probes
-
Melchiorre, C., Minarini, A., Angeli, P., Giardina, D., Gulini, U., and Quaglia, W. Polymethylene tetraamines as muscarinic receptor probes. Trends Pharmacol. Sci. Suppl. 55-59 (1989).
-
(1989)
Trends Pharmacol. Sci. Suppl.
, pp. 55-59
-
-
Melchiorre, C.1
Minarini, A.2
Angeli, P.3
Giardina, D.4
Gulini, U.5
Quaglia, W.6
-
17
-
-
0035924177
-
Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists
-
Rajeswaran, W.G., Cao, Y., Huang, X.P. et al. Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2, 5-thiadiazole derivatives as selective muscarinic agonists. J. Med. Chem. 44, 4563-4576 (2001).
-
(2001)
J. Med. Chem.
, vol.44
, pp. 4563-4576
-
-
Rajeswaran, W.G.1
Cao, Y.2
Huang, X.P.3
-
18
-
-
10544224535
-
Serotonin dimers: Application of the bivalent ligand approach to the design of new potent and selective 5-HT1B/1D agonists
-
Halazy, S., Perez, M., Fourrier, C. et al. Serotonin dimers: Application of the bivalent ligand approach to the design of new potent and selective 5-HT1B/1D agonists. J. Med. Chem. 39, 4920-4927 (1996).
-
(1996)
J. Med. Chem.
, vol.39
, pp. 4920-4927
-
-
Halazy, S.1
Perez, M.2
Fourrier, C.3
-
19
-
-
26444449975
-
Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies
-
Soulier, J.L., Russo, O., Giner, M. et al. Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies. J. Med. Chem. 48, 6220-6228 (2005).
-
(2005)
J. Med. Chem.
, vol.48
, pp. 6220-6228
-
-
Soulier, J.L.1
Russo, O.2
Giner, M.3
-
20
-
-
34249685481
-
Synthesis and evaluation of homo-bivalent GnRHR ligands
-
Bonger, K.M., van den Berg, R.J., Heitman, L.H., IJzerman, A.P., Oosterom, J., Timmers, C.M., Overkleeft, H.S., and van der Marel, G.A. Synthesis and evaluation of homo-bivalent GnRHR ligands. Bioorg. Med. Chem. 15, 4841-4856 (2007).
-
(2007)
Bioorg. Med. Chem.
, vol.15
, pp. 4841-4856
-
-
Bonger, K.M.1
Van Den Berg, R.J.2
Heitman, L.H.3
IJzerman, A.P.4
Oosterom, J.5
Timmers, C.M.6
Overkleeft, H.S.7
Van Der Marel, G.A.8
-
21
-
-
0035927440
-
Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5′- to 6′-position of naltrindole
-
Sharma, S.K., Jones, R.M., Metzger, T.G., Ferguson, D.M., and Portoghese, P.S. Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5′- to 6′-position of naltrindole. J. Med. Chem. 44, 2073-2079 (2001).
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2073-2079
-
-
Sharma, S.K.1
Jones, R.M.2
Metzger, T.G.3
Ferguson, D.M.4
Portoghese, P.S.5
-
22
-
-
21144446486
-
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers
-
This paper outlines the discovery of a heterodimer selective GPCR ligand that was originally designed based on the message-address concept
-
Waldhoer, M., Fong, J., Jones, R.M., Lunzer, M.M., Sharma, S.K., Kostenis, E., Portoghese, P.S., and Whistler, J.L. A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. Proc. Natl. Acad. Sci. U.S.A. 102, 9050-9055 (2005). This paper outlines the discovery of a heterodimer selective GPCR ligand that was originally designed based on the message-address concept.
-
(2005)
Proc. Natl. Acad. Sci. U.S.A.
, vol.102
, pp. 9050-9055
-
-
Waldhoer, M.1
Fong, J.2
Jones, R.M.3
Lunzer, M.M.4
Sharma, S.K.5
Kostenis, E.6
Portoghese, P.S.7
Whistler, J.L.8
-
25
-
-
0030989997
-
Chimeric strategies for the rational design of bioactive analogs of small peptide hormones
-
Howl, J., Langel, U., Hawtin, S.R., Valkna, A., Yarwood, N.J., Saar, K., and Wheatley, M. Chimeric strategies for the rational design of bioactive analogs of small peptide hormones. FASEB J. 11, 582-590 (1997).
-
(1997)
FASEB J.
, vol.11
, pp. 582-590
-
-
Howl, J.1
Langel, U.2
Hawtin, S.R.3
Valkna, A.4
Yarwood, N.J.5
Saar, K.6
Wheatley, M.7
-
26
-
-
0032474283
-
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes
-
Perez, M., Jorand-Lebrun, C., Pauwels, P.J., Pallard, I., and Halazy, S. Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes. Bioorg. Med. Chem. Lett. 8, 1407-1412 (1998).
-
(1998)
Bioorg. Med. Chem. Lett.
, vol.8
, pp. 1407-1412
-
-
Perez, M.1
Jorand-Lebrun, C.2
Pauwels, P.J.3
Pallard, I.4
Halazy, S.5
-
27
-
-
58149193205
-
Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders
-
Conn, P.J., Christopoulos, A., and Lindsley, C.W. Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders. Nat. Rev. Drug Discov. 8, 41-54 (2009).
-
(2009)
Nat. Rev. Drug Discov.
, vol.8
, pp. 41-54
-
-
Conn, P.J.1
Christopoulos, A.2
Lindsley, C.W.3
-
28
-
-
24044539957
-
1 receptor
-
This paper provides a striking example of divergent effects on orthosteric ligand affinity versus efficacy by an allosteric GPCR modulator
-
1 receptor. Mol. Pharmacol. 68, 1484-1495 (2005). This paper provides a striking example of divergent effects on orthosteric ligand affinity versus efficacy by an allosteric GPCR modulator.
-
(2005)
Mol. Pharmacol.
, vol.68
, pp. 1484-1495
-
-
Price, M.R.1
Baillie, G.L.2
Thomas, A.3
-
29
-
-
33747181100
-
Allosteric agonists of 7TM receptors: Expanding the pharmacological toolbox
-
Langmead, C.J. and Christopoulos, A. Allosteric agonists of 7TM receptors: Expanding the pharmacological toolbox. Trends Pharmacol. Sci. 27, 475-481 (2006).
-
(2006)
Trends Pharmacol. Sci.
, vol.27
, pp. 475-481
-
-
Langmead, C.J.1
Christopoulos, A.2
-
31
-
-
52949115240
-
New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug)
-
Nawaratne, V., Leach, K., Suratman, N., Loiacono, R.E., Felder, C.C., Armbruster, B.N., Roth, B.L., Sexton, P.M., and Christopoulos, A. New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug). Mol. Pharmacol. 74, 1119-1131 (2008).
-
(2008)
Mol. Pharmacol.
, vol.74
, pp. 1119-1131
-
-
Nawaratne, V.1
Leach, K.2
Suratman, N.3
Loiacono, R.E.4
Felder, C.C.5
Armbruster, B.N.6
Roth, B.L.7
Sexton, P.M.8
Christopoulos, A.9
-
32
-
-
0036258990
-
G Protein-coupled receptor allosterism and complexing
-
Christopoulos, A. and Kenakin, T. G Protein-coupled receptor allosterism and complexing. Pharmacol. Rev. 54, 323-374 (2002).
-
(2002)
Pharmacol. Rev.
, vol.54
, pp. 323-374
-
-
Christopoulos, A.1
Kenakin, T.2
-
33
-
-
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. 33, 187-194 (1988).
-
(1988)
Mol. Pharmacol.
, vol.33
, pp. 187-194
-
-
Ehlert, F.J.1
-
34
-
-
0033669603
-
Modeling the functional effects of allosteric modulators at pharmacological receptors: An extension of the two-state model of receptor activation
-
Hall, D.A. Modeling the functional effects of allosteric modulators at pharmacological receptors: An extension of the two-state model of receptor activation. Mol. Pharmacol. 58, 1412-1423 (2000).
-
(2000)
Mol. Pharmacol.
, vol.58
, pp. 1412-1423
-
-
Hall, D.A.1
-
35
-
-
27844519281
-
New concepts in drug discovery: Collateral efficacy and permissive antagonism
-
Kenakin, T. New concepts in drug discovery: Collateral efficacy and permissive antagonism. Nat. Rev. Drug Discov. 4, 919-927 (2005).
-
(2005)
Nat. Rev. Drug Discov.
, vol.4
, pp. 919-927
-
-
Kenakin, T.1
-
36
-
-
34447632041
-
Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology
-
This review provides examples of allosteric modulator-engendered functional selectivity
-
Leach, K., Sexton, P.M., and Christopoulos, A. Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology. Trends Pharmacol. Sci. 28, 382-389 (2007). This review provides examples of allosteric modulator-engendered functional selectivity.
-
(2007)
Trends Pharmacol. Sci.
, vol.28
, pp. 382-389
-
-
Leach, K.1
Sexton, P.M.2
Christopoulos, A.3
-
37
-
-
0141593597
-
β-Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors
-
This paper provides one of the earliest and most striking examples of reversals of efficacy of an orthosteric ligand depending on the signal pathway being investigated
-
Azzi, M., Charest, P.G., Angers, S., Rousseau, G., Kohout, T., Bouvier, M., and Piñeyro, G. β-Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Proc. Natl. Acad. Sci. U.S.A. 100, 11406-11411 (2003). This paper provides one of the earliest and most striking examples of reversals of efficacy of an orthosteric ligand depending on the signal pathway being investigated.
-
(2003)
Proc. Natl. Acad. Sci. U.S.A.
, vol.100
, pp. 11406-11411
-
-
Azzi, M.1
Charest, P.G.2
Angers, S.3
Rousseau, G.4
Kohout, T.5
Bouvier, M.6
Piñeyro, G.7
-
38
-
-
0345735773
-
2-adrenoceptor provide evidence for agonist-directed signaling
-
2-adrenoceptor provide evidence for agonist-directed signaling. Mol. Pharmacol. 64, 1357-1369 (2003).
-
(2003)
Mol. Pharmacol.
, vol.64
, pp. 1357-1369
-
-
Baker, J.G.1
Hall, I.P.2
Hill, S.J.3
-
39
-
-
34447642715
-
The evasive nature of drug efficacy: Implications for drug discovery
-
Galandrin, S., Oligny-Longpre, G., and Bouvier, M. The evasive nature of drug efficacy: Implications for drug discovery. Trends Pharmacol. Sci. 28, 423-430 (2007).
-
(2007)
Trends Pharmacol. Sci.
, vol.28
, pp. 423-430
-
-
Galandrin, S.1
Oligny-Longpre, G.2
Bouvier, M.3
-
40
-
-
40849102720
-
A conservative, single-amino acid substitution in the second cytoplasmic domain of the human serotonin 2C receptor alters both ligand-dependent and -independent receptor signaling
-
Berg, K.A., Dunlop, J., Sanchez, T., Silva, M., and Clarke, W.P. A conservative, single-amino acid substitution in the second cytoplasmic domain of the human serotonin 2C receptor alters both ligand-dependent and -independent receptor signaling. J. Pharmacol. Exp. Ther. 324, 1084-1092 (2008).
-
(2008)
J. Pharmacol. Exp. Ther.
, vol.324
, pp. 1084-1092
-
-
Berg, K.A.1
Dunlop, J.2
Sanchez, T.3
Silva, M.4
Clarke, W.P.5
-
41
-
-
59649112659
-
Dualsteric GPCR targeting: A novel route to binding and signaling pathway selectivity
-
This is an excellent example of the design, synthesis and validation of the bitopic ligand approach, including engendering receptor selectivity in native tissues
-
Antony, J., Kellershohn, K., Mohr-Andra, M. et al. Dualsteric GPCR targeting: A novel route to binding and signaling pathway selectivity. FASEB J. 23, 442-450 (2009). This is an excellent example of the design, synthesis and validation of the bitopic ligand approach, including engendering receptor selectivity in native tissues.
-
(2009)
FASEB J.
, vol.23
, pp. 442-450
-
-
Antony, J.1
Kellershohn, K.2
Mohr-Andra, M.3
-
42
-
-
30444436744
-
Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors
-
This is the first publication describing the empirical design of a bitopic GPCR orthosteric/allosteric ligand
-
Disingrini, T., Muth, M., Dallanoce, C., Barocelli, E., Bertoni, S., Kellershohn, K., Mohr, K., De Amici, M., and Holzgrabe, U. Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors. J. Med. Chem. 49, 366-372 (2006). This is the first publication describing the empirical design of a bitopic GPCR orthosteric/allosteric ligand.
-
(2006)
J. Med. Chem.
, vol.49
, pp. 366-372
-
-
Disingrini, T.1
Muth, M.2
Dallanoce, C.3
Barocelli, E.4
Bertoni, S.5
Kellershohn, K.6
Mohr, K.7
De Amici, M.8
Holzgrabe, U.9
-
43
-
-
34547208823
-
A novel multivalent ligand that bridges the allosteric and orthosteric binding sites of the M2 muscarinic receptor
-
Steinfeld, T., Mammen, M., Smith, J.A., Wilson, R.D., and Jasper, J.R. A novel multivalent ligand that bridges the allosteric and orthosteric binding sites of the M2 muscarinic receptor. Mol. Pharmacol. 72, 291-302 (2007).
-
(2007)
Mol. Pharmacol.
, vol.72
, pp. 291-302
-
-
Steinfeld, T.1
Mammen, M.2
Smith, J.A.3
Wilson, R.D.4
Jasper, J.R.5
-
44
-
-
57649170953
-
A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand
-
This is the first paper identifying a bitopic mechanism as the basis of selectivity of a previously known functionally selective GPCR agonist
-
Valant, C., Gregory, K.J., Hall, N.E., Scammells, P.J., Lew, M.J., Sexton, P.M., and Christopoulos, A. A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. J. Biol. Chem. 283, 29312-29321 (2008). This is the first paper identifying a bitopic mechanism as the basis of selectivity of a previously known functionally selective GPCR agonist.
-
(2008)
J. Biol. Chem.
, vol.283
, pp. 29312-29321
-
-
Valant, C.1
Gregory, K.J.2
Hall, N.E.3
Scammells, P.J.4
Lew, M.J.5
Sexton, P.M.6
Christopoulos, A.7
-
45
-
-
45749136445
-
Allosteric modulation of muscarinic acetylcholine receptors
-
Gregory, K.J., Sexton, P.M., and Christopoulos, A. Allosteric modulation of muscarinic acetylcholine receptors. Curr. Neuropharmacol. 5, 157-167 (2007).
-
(2007)
Curr. Neuropharmacol.
, vol.5
, pp. 157-167
-
-
Gregory, K.J.1
Sexton, P.M.2
Christopoulos, A.3
-
46
-
-
0031774720
-
International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors
-
Caulfield, M.P. and Birdsall, N.J. International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors. Pharmacol. Rev. 50, 279-290 (1998).
-
(1998)
Pharmacol. Rev.
, vol.50
, pp. 279-290
-
-
Caulfield, M.P.1
Birdsall, N.J.2
-
47
-
-
0020691525
-
The effect of McN-A-343 on muscarinic receptors in the cerebral cortex and heart
-
Birdsall, N.J.M., Burgen, A.S.V., Hulme, E.C., Stockton, J.M., and Zigmond, M.J. The effect of McN-A-343 on muscarinic receptors in the cerebral cortex and heart. Br. J. Pharmacol. 78, 257-259 (1983).
-
(1983)
Br. J. Pharmacol.
, vol.78
, pp. 257-259
-
-
Birdsall, N.J.M.1
Burgen, A.S.V.2
Hulme, E.C.3
Stockton, J.M.4
Zigmond, M.J.5
-
48
-
-
34547187191
-
Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors
-
May, L.T., Avlani, V.A., Langmead, C.J., Herdon, H.J., Wood, M.D., Sexton, P.M., and Christopoulos, A. Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors. Mol. Pharmacol. 72, 463-476 (2007).
-
(2007)
Mol. Pharmacol.
, vol.72
, pp. 463-476
-
-
May, L.T.1
Avlani, V.A.2
Langmead, C.J.3
Herdon, H.J.4
Wood, M.D.5
Sexton, P.M.6
Christopoulos, A.7
-
49
-
-
0028062082
-
Identification of drugs competing with d-tubocurarine for an allosteric site on cardiac muscarinic receptors
-
Waelbroeck, M. Identification of drugs competing with d-tubocurarine for an allosteric site on cardiac muscarinic receptors. Mol. Pharmacol. 46, 685-692 (1994).
-
(1994)
Mol. Pharmacol.
, vol.46
, pp. 685-692
-
-
Waelbroeck, M.1
-
50
-
-
34248560933
-
Estimation of agonist activity at G protein-coupled receptors: Analysis of M2 muscarinic receptor signaling through Gi/o, Gs, and G15
-
Griffin, M.T., Figueroa, K.W., Liller, S., and Ehlert, F.J. Estimation of agonist activity at G protein-coupled receptors: Analysis of M2 muscarinic receptor signaling through Gi/o, Gs, and G15. J. Pharmacol. Exp. Ther. 321, 1193-1207 (2007).
-
(2007)
J. Pharmacol. Exp. Ther.
, vol.321
, pp. 1193-1207
-
-
Griffin, M.T.1
Figueroa, K.W.2
Liller, S.3
Ehlert, F.J.4
-
51
-
-
55249118679
-
Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats
-
Jones, C.K., Brady, A.E., Davis, A.A. et al. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J. Neurosci. 28, 10422-10433 (2008).
-
(2008)
J. Neurosci.
, vol.28
, pp. 10422-10433
-
-
Jones, C.K.1
Brady, A.E.2
Davis, A.A.3
-
52
-
-
46249084634
-
Characterization of a CNS penetrant, selective M1 muscarinic receptor agonist, 77-LH-28-1
-
Langmead, C.J., Austin, N.E., Branch, C.L. et al. Characterization of a CNS penetrant, selective M1 muscarinic receptor agonist, 77-LH-28-1. Br. J. Pharmacol. 154, 1104-1115 (2008).
-
(2008)
Br. J. Pharmacol.
, vol.154
, pp. 1104-1115
-
-
Langmead, C.J.1
Austin, N.E.2
Branch, C.L.3
-
53
-
-
59449090754
-
Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors
-
Lebon, G., Langmead, C.J., Tehan, B.G., and Hulme, E.C. Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors. Mol. Pharmacol. 75, 331-341 (2009).
-
(2009)
Mol. Pharmacol.
, vol.75
, pp. 331-341
-
-
Lebon, G.1
Langmead, C.J.2
Tehan, B.G.3
Hulme, E.C.4
-
54
-
-
33751072945
-
Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: Evidence for three distinct modes of receptor activation
-
Spalding, T.A., Ma, J.N., Ott, T.R., Friberg, M., Bajpai, A., Bradley, S.R., Davis, R.E., Brann, M.R., and Burstein, E.S. Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: Evidence for three distinct modes of receptor activation. Mol. Pharmacol. 70, 1974-1983 (2006).
-
(2006)
Mol. Pharmacol.
, vol.70
, pp. 1974-1983
-
-
Spalding, T.A.1
Ma, J.N.2
Ott, T.R.3
Friberg, M.4
Bajpai, A.5
Bradley, S.R.6
Davis, R.E.7
Brann, M.R.8
Burstein, E.S.9
-
55
-
-
0036259109
-
Discovery of an ectopic activation site on the M1 muscarinic receptor
-
Spalding, T.A., Trotter, C., Skjaerbaek, N., Messier, T.L., Currier, E.A., Burstein, E.S., Li, D., Hacksell, U., and Brann, M.R. Discovery of an ectopic activation site on the M1 muscarinic receptor. Mol. Pharmacol. 61, 1297-1302 (2002).
-
(2002)
Mol. Pharmacol.
, vol.61
, pp. 1297-1302
-
-
Spalding, T.A.1
Trotter, C.2
Skjaerbaek, N.3
Messier, T.L.4
Currier, E.A.5
Burstein, E.S.6
Li, D.7
Hacksell, U.8
Brann, M.R.9
-
56
-
-
10744223983
-
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-daspartate receptor activity
-
Sur, C., Mallorga, P.J., Wittmann, M. et al. N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-daspartate receptor activity. Proc. Natl. Acad. Sci. U.S.A. 100, 13674-13679 (2003).
-
(2003)
Proc. Natl. Acad. Sci. U.S.A.
, vol.100
, pp. 13674-13679
-
-
Sur, C.1
Mallorga, P.J.2
Wittmann, M.3
-
57
-
-
20444499405
-
2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists
-
2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists. J. Biol. Chem. 280, 22165-22171 (2005).
-
(2005)
J. Biol. Chem.
, vol.280
, pp. 22165-22171
-
-
Swaminath, G.1
Deupi, X.2
Lee, T.W.3
Zhu, W.4
Thian, F.S.5
Kobilka, T.S.6
Kobilka, B.7
|