-
1
-
-
0021058380
-
Operational models of pharmacological agonism
-
Black JW and Leff P (1983) Operational models of pharmacological agonism. Proc R Soc Lond B Biol Sci 220:141-162.
-
(1983)
Proc R Soc Lond B Biol Sci
, vol.220
, pp. 141-162
-
-
Black, J.W.1
Leff, P.2
-
2
-
-
34548487757
-
Stimulation by ghrelin of p42/p44 mitogen-activated protein kinase through the GHS-R1a receptor: Role of G-proteins and beta-arrestins
-
DOI 10.1002/jcp.21109
-
Camiña JP, Lodeiro M, Ischenko O, Martini AC, and Casanueva FF (2007) Stimulation by ghrelin of p42/p44 mitogen-activated protein kinase through the GHS-R1a receptor: role of G-proteins and beta-arrestins. J Cell Physiol 213:187-200. (Pubitemid 47378807)
-
(2007)
Journal of Cellular Physiology
, vol.213
, Issue.1
, pp. 187-200
-
-
Camina, J.P.1
Lodeiro, M.2
Ischenko, O.3
Martini, A.C.4
Casanueva, F.F.5
-
4
-
-
58149193205
-
Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders
-
Conn PJ, Christopoulos A, and Lindsley CW (2009) Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 8:41-54.
-
(2009)
Nat Rev Drug Discov
, vol.8
, pp. 41-54
-
-
Conn, P.J.1
Christopoulos, A.2
Lindsley, C.W.3
-
6
-
-
33845720603
-
Asymmetric conformational changes in a GPCR dimer controlled by G-proteins
-
DOI 10.1038/sj.emboj.7601449, PII 7601449
-
Damian M, Martin A, Mesnier D, Pin JP, and Banères JL (2006) Asymmetric conformational changes in a GPCR dimer controlled by G-proteins. EMBO J 25:5693-5702. (Pubitemid 44967753)
-
(2006)
EMBO Journal
, vol.25
, Issue.24
, pp. 5693-5702
-
-
Damian, M.1
Martin, A.2
Mesnier, D.3
Pin, J.-P.4
Baneres, J.-L.5
-
7
-
-
34548436635
-
2+ signaling and insulin release in islet beta-cells: Novel signal transduction of ghrelin
-
2+ signaling and insulin release in islet beta-cells: novel signal transduction of ghrelin. Diabetes 56:2319-2327.
-
(2007)
Diabetes
, vol.56
, pp. 2319-2327
-
-
Dezaki, K.1
Kakei, M.2
Yada, T.3
-
8
-
-
0023958554
-
Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods
-
Ehlert FJ (1988) Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. Mol Pharmacol 33:187-194.
-
(1988)
Mol Pharmacol
, vol.33
, pp. 187-194
-
-
Ehlert, F.J.1
-
9
-
-
13444274883
-
Evidence for negative binding cooperativity within CCR5-CCR2b heterodimers
-
DOI 10.1124/mol.104.003624
-
El-Asmar L, Springael JY, Ballet S, Andrieu EU, Vassart G, and Parmentier M (2005) Evidence for negative binding cooperativity within CCR5-CCR2b heterodimers. Mol Pharmacol 67:460-469. (Pubitemid 40216739)
-
(2005)
Molecular Pharmacology
, vol.67
, Issue.2
, pp. 460-469
-
-
El-Asmar, L.1
Springael, J.-Y.2
Ballet, S.3
Andrieu, E.U.4
Vassart, G.5
Parmentier, M.6
-
10
-
-
33846030175
-
Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function
-
DOI 10.1074/jbc.M602494200
-
Ellis J, Pediani JD, Canals M, Milasta S, and Milligan G (2006) Orexin-1 receptorcannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. J Biol Chem 281:38812-38824. (Pubitemid 46042008)
-
(2006)
Journal of Biological Chemistry
, vol.281
, Issue.50
, pp. 38812-38824
-
-
Ellis, J.1
Pediani, J.D.2
Canals, M.3
Milasta, S.4
Milligan, G.5
-
11
-
-
15444361604
-
Structural requirements for the activation of the human growth hormone secretagogue receptor by peptide and nonpeptide secretagogues
-
DOI 10.1210/me.12.1.137
-
Feighner SD, Howard AD, Prendergast K, Palyha OC, Hreniuk DL, Nargund R, Underwood D, Tata JR, Dean DC, Tan CP, et al. (1998) Structural requirements for the activation of the human growth hormone secretagogue receptor by peptide and nonpeptide secretagogues. Mol Endocrinol 12:137-145. (Pubitemid 28124786)
-
(1998)
Molecular Endocrinology
, vol.12
, Issue.1
, pp. 137-145
-
-
Feighner, S.D.1
Howard, A.D.2
Prendergast, K.3
Palyha, O.C.4
Hreniuk, D.L.5
Nargund, R.6
Underwood, D.7
Tata, J.R.8
Dean, D.C.9
Tan, C.P.10
McKee, K.K.11
Woods, J.W.12
Patchett, A.A.13
Smith, R.G.14
Van Der Ploeg, L.H.T.15
-
13
-
-
33644658516
-
Ghrelin receptor mutations - Too little height and too much hunger
-
DOI 10.1172/JCI27999
-
Holst B and Schwartz TW (2006) Ghrelin receptor mutations-too little height and too much hunger. J Clin Invest 116:637-641. (Pubitemid 43326872)
-
(2006)
Journal of Clinical Investigation
, vol.116
, Issue.3
, pp. 637-641
-
-
Holst, B.1
Schwartz, T.W.2
-
14
-
-
24344479915
-
Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling
-
DOI 10.1210/me.2005-0059
-
Holst B, Brandt E, Bach A, Heding A, and Schwartz TW (2005) Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling. Mol Endocrinol 19:2400-2411. (Pubitemid 41252832)
-
(2005)
Molecular Endocrinology
, vol.19
, Issue.9
, pp. 2400-2411
-
-
Holst, B.1
Brandt, E.2
Bach, A.3
Heding, A.4
Schwartz, T.W.5
-
15
-
-
0242330291
-
High Constitutive Signaling of the Ghrelin Receptor - Identification of a Potent Inverse Agonist
-
DOI 10.1210/me.2003-0069
-
Holst B, Cygankiewicz A, Jensen TH, Ankersen M, and Schwartz TW (2003) High constitutive signaling of the ghrelin receptor-identification of a potent inverse agonist. Mol Endocrinol 17:2201-2210. (Pubitemid 37352532)
-
(2003)
Molecular Endocrinology
, vol.17
, Issue.11
, pp. 2201-2210
-
-
Holst, B.1
Cygankiewicz, A.2
Jensen, T.H.3
Ankersen, M.4
Schwartz, T.W.5
-
16
-
-
58849138430
-
Overlapping binding site for the endogenous agonist, smallmolecule agonists, and ago-allosteric modulators on the ghrelin receptor
-
Holst B, Frimurer TM, Mokrosinski J, Halkjaer T, Cullberg KB, Underwood CR, and Schwartz TW (2009) Overlapping binding site for the endogenous agonist, smallmolecule agonists, and ago-allosteric modulators on the ghrelin receptor. Mol Pharmacol 75:44-59.
-
(2009)
Mol Pharmacol
, vol.75
, pp. 44-59
-
-
Holst, B.1
Frimurer, T.M.2
Mokrosinski, J.3
Halkjaer, T.4
Cullberg, K.B.5
Underwood, C.R.6
Schwartz, T.W.7
-
17
-
-
33747603675
-
Ghrelin receptor inverse agonists: Identification of an active peptide core and its interaction epitopes on the receptor
-
DOI 10.1124/mol.106.024422
-
Holst B, Lang M, Brandt E, Bach A, Howard A, Frimurer TM, Beck-Sickinger A, and Schwartz TW (2006) Ghrelin receptor inverse agonists: identification of an active peptide core and its interaction epitopes on the receptor. Mol Pharmacol 70:936-946. (Pubitemid 44268450)
-
(2006)
Molecular Pharmacology
, vol.70
, Issue.3
, pp. 936-946
-
-
Holst, B.1
Lang, M.2
Brandt, E.3
Bach, A.4
Howard, A.5
Frimurer, T.M.6
Beck-Sickinger, A.7
Schwartz, T.W.8
-
18
-
-
9444246501
-
A receptor in pituitary and hypothalamus that functions in growth hormone release
-
Howard AD, Feighner SD, Cully DF, Arena JP, Liberator PA, Rosenblum CI, Hamelin M, Hreniuk DL, Palyha OC, Anderson J, et al. (1996) A receptor in pituitary and hypothalamus that functions in growth hormone release. Science 273:974-977. (Pubitemid 26275178)
-
(1996)
Science
, vol.273
, Issue.5277
, pp. 974-977
-
-
Howard, A.D.1
Feighner, S.D.2
Cully, D.F.3
Arena, J.P.4
Liberator, P.A.5
Rosenblum, C.I.6
Hamelin, M.7
Hreniuk, D.L.8
Palyha, O.C.9
Anderson, J.10
Paress, P.S.11
Diaz, C.12
Chou, M.13
Liu, K.K.14
McKee, K.K.15
Pong, S.-S.16
Chaung, L.-Y.17
Elbrecht, A.18
Dashkevicz, M.19
Heavens, R.20
Rigby, M.21
Sirinathsinghji, D.J.S.22
Dean, D.C.23
Melillo, D.G.24
Patchett, A.A.25
Nargund, R.26
Griffin, P.R.27
Demartino, J.A.28
Gupta, S.K.29
Schaeffer, J.M.30
Smith, R.G.31
Van Der Ploeg, L.H.T.32
more..
-
19
-
-
0029162109
-
Pharmacological proteus?
-
Kenakin T (1995) Pharmacological proteus? Trends Pharmacol Sci 16:256-258.
-
(1995)
Trends Pharmacol Sci
, vol.16
, pp. 256-258
-
-
Kenakin, T.1
-
20
-
-
15544385058
-
Ghrelin: Structure and function
-
Kojima M and Kangawa K (2005) Ghrelin: structure and function. Physiol Rev 85:495-522.
-
(2005)
Physiol Rev
, vol.85
, pp. 495-522
-
-
Kojima, M.1
Kangawa, K.2
-
21
-
-
33747181100
-
Allosteric agonists of 7TM receptors: Expanding the pharmacological toolbox
-
Langmead CJ and Christopoulos A (2006) Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. Trends Pharmacol Sci 27:475-481.
-
(2006)
Trends Pharmacol Sci
, vol.27
, pp. 475-481
-
-
Langmead, C.J.1
Christopoulos, A.2
-
22
-
-
34447632041
-
Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology
-
DOI 10.1016/j.tips.2007.06.004, PII S0165614707001496, Allosterism and Collateral Efficacy
-
Leach K, Sexton PM, and Christopoulos A (2007) Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. Trends Pharmacol Sci 28:382-389. (Pubitemid 47087967)
-
(2007)
Trends in Pharmacological Sciences
, vol.28
, Issue.8
, pp. 382-389
-
-
Leach, K.1
Sexton, P.M.2
Christopoulos, A.3
-
23
-
-
33947536063
-
Physiological, pathological and potential therapeutic roles of ghrelin
-
DOI 10.1016/j.drudis.2007.02.009, PII S1359644607000827
-
Leite-Moreira AF and Soares JB (2007) Physiological, pathological and potential therapeutic roles of ghrelin. Drug Discov Today 12:276-288. (Pubitemid 46467484)
-
(2007)
Drug Discovery Today
, vol.12
, Issue.7-8
, pp. 276-288
-
-
Leite-Moreira, A.F.1
Soares, J.-B.2
-
24
-
-
0344394262
-
Intracellular signaling mechanisms mediating ghrelin-stimulated growth hormone release in somatotropes
-
Malagón MM, Luque RM, Ruiz-Guerrero E, Rodríguez-Pacheco F, García-Navarro S, Casanueva FF, Gracia-Navarro F, and Castaño JP (2003) Intracellular signaling mechanisms mediating ghrelin-stimulated growth hormone release in somatotropes. Endocrinology 144:5372-5380.
-
(2003)
Endocrinology
, vol.144
, pp. 5372-5380
-
-
Malagón, M.M.1
Luque, R.M.2
Ruiz-Guerrero, E.3
Rodríguez-Pacheco, F.4
García-Navarro, S.5
Casanueva, F.F.6
Gracia-Navarro, F.7
Castaño, J.P.8
-
25
-
-
35548953701
-
Ligand-directed signaling: 50 ways to find a lover
-
Michel MC and Alewijnse AE (2007) Ligand-directed signaling: 50 ways to find a lover. Mol Pharmacol 72:1097-1099.
-
(2007)
Mol Pharmacol
, vol.72
, pp. 1097-1099
-
-
Michel, M.C.1
Alewijnse, A.E.2
-
26
-
-
0347627709
-
Constitutive activity and inverse agonists of G protein-coupled receptors: A current perspective
-
Milligan G (2003) Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective. Mol Pharmacol 64:1271-1276.
-
(2003)
Mol Pharmacol
, vol.64
, pp. 1271-1276
-
-
Milligan, G.1
-
27
-
-
33947369500
-
G protein-coupled receptor dimerisation: Molecular basis and relevance to function
-
DOI 10.1016/j.bbamem.2006.09.021, PII S0005273606003804
-
Milligan G (2007) G protein-coupled receptor dimerisation: molecular basis and relevance to function. Biochim Biophys Acta 1768:825-835. (Pubitemid 46452542)
-
(2007)
Biochimica et Biophysica Acta - Biomembranes
, vol.1768
, Issue.4
, pp. 825-835
-
-
Milligan, G.1
-
28
-
-
40349085622
-
A day in the life of a G protein-coupled receptor: The contribution to function of G protein-coupled receptor dimerization
-
Milligan G (2008) A day in the life of a G protein-coupled receptor: the contribution to function of G protein-coupled receptor dimerization. Br J Pharmacol 153 (Suppl 1):S216-S229.
-
(2008)
Br J Pharmacol
, vol.153
, Issue.SUPPL. 1
-
-
Milligan, G.1
-
29
-
-
36448968578
-
Allosteric modulation of heterodimeric G-protein-coupled receptors
-
DOI 10.1016/j.tips.2007.11.001, PII S0165614707002581
-
Milligan G and Smith NJ (2007) Allosteric modulation of heterodimeric G-proteincoupled receptors. Trends Pharmacol Sci 28:615-620. (Pubitemid 350166577)
-
(2007)
Trends in Pharmacological Sciences
, vol.28
, Issue.12
, pp. 615-620
-
-
Milligan, G.1
Smith, N.J.2
-
30
-
-
13244253556
-
Fitting models to biological data using linear and nonlinear regression
-
Oxford University Press, New York
-
Motulsky HJ and Christopoulos A (2004) Fitting models to biological data using linear and nonlinear regression. A Practical Guide to Curve Fitting, Oxford University Press, New York.
-
(2004)
A Practical Guide to Curve Fitting
-
-
Motulsky, H.J.1
Christopoulos, A.2
-
31
-
-
0035072228
-
125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland
-
Muccioli G, Papotti M, Locatelli V, Ghigo E, and Deghenghi R (2001) Binding of 125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland. J Endocrinol Invest 24:RC7-RC9. (Pubitemid 32293633)
-
(2001)
Journal of Endocrinological Investigation
, vol.24
, Issue.3
-
-
Muccioli, G.1
Papotti, M.2
Locatelli, V.3
Ghigo, E.4
Deghenghi, R.5
-
32
-
-
33644653308
-
Loss of constitutive activity of the growth hormone secretagogue receptor in familial short stature
-
DOI 10.1172/JCI25303
-
Pantel J, Legendre M, Cabrol S, Hilal L, Hajaji Y, Morisset S, Nivot S, Vie-Luton MP, Grouselle D, de Kerdanet M, et al. (2006) Loss of constitutive activity of the growth hormone secretagogue receptor in familial short stature. J Clin Invest 116:760-768. (Pubitemid 43326885)
-
(2006)
Journal of Clinical Investigation
, vol.116
, Issue.3
, pp. 760-768
-
-
Pantel, J.1
Legendre, M.2
Cabrol, S.3
Hilal, L.4
Hajaji, Y.5
Morisset, S.6
Nivot, S.7
Vie-Luton, M.-P.8
Grouselle, D.9
De Kerdanet, M.10
Kadiri, A.11
Epelbaum, J.12
Le Bouc, Y.13
Amselem, S.14
-
33
-
-
44449175613
-
CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2-DOP receptor heterodimer
-
DOI 10.1042/BJ20071689
-
Parenty G, Appelbe S, and Milligan G (2008) CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2- DOP receptor heterodimer. Biochem J 412:245-256. (Pubitemid 351758230)
-
(2008)
Biochemical Journal
, vol.412
, Issue.2
, pp. 245-256
-
-
Parenty, G.1
Appelbe, S.2
Milligan, G.3
-
34
-
-
34447562579
-
2-adrenoceptor
-
DOI 10.1016/j.cellsig.2007.05.002, PII S0898656807001301
-
Sartania N, Appelbe S, Pediani JD, and Milligan G (2007) Agonist occupancy of a single monomeric element is sufficient to cause internalization of the dimeric beta2-adrenoceptor. Cell Signal 19:1928-1938. (Pubitemid 47081383)
-
(2007)
Cellular Signalling
, vol.19
, Issue.9
, pp. 1928-1938
-
-
Sartania, N.1
Appelbe, S.2
Pediani, J.D.3
Milligan, G.4
-
35
-
-
33645796458
-
Ago-allosteric modulation and other types of allostery in dimeric 7TM receptors
-
Schwartz TW and Holst B (2006) Ago-allosteric modulation and other types of allostery in dimeric 7TM receptors. J Recept Signal Transduct Res 26:107-128.
-
(2006)
J Recept Signal Transduct Res
, vol.26
, pp. 107-128
-
-
Schwartz, T.W.1
Holst, B.2
-
36
-
-
33845903110
-
Functional selectivity and classical concepts of quantitative pharmacology
-
DOI 10.1124/jpet.106.104463
-
Urban JD, Clarke WP, von Zastrow M, Nichols DE, Kobilka B, Weinstein H, Javitch JA, Roth BL, Christopoulos A, Sexton PM, et al. (2007) Functional selectivity and classical concepts of quantitative pharmacology. J Pharmacol Exp Ther 320:1-13. (Pubitemid 46025713)
-
(2007)
Journal of Pharmacology and Experimental Therapeutics
, vol.320
, Issue.1
, pp. 1-13
-
-
Urban, J.D.1
Clarke, W.P.2
Von Zastrow, M.3
Nichols, D.E.4
Kobilka, B.5
Weinstein, H.6
Javitch, J.A.7
Roth, B.L.8
Christopoulos, A.9
Sexton, P.M.10
Miller, K.J.11
Spedding, M.12
Mailman, R.B.13
-
37
-
-
2942528459
-
Biological, physiological, pathophysiological, and pharmacological aspects of ghrelin
-
DOI 10.1210/er.2002-0029
-
van der Lely AJ, Tschöp M, Heiman ML, and Ghigo E (2004) Biological, physiological, pathophysiological, and pharmacological aspects of ghrelin. Endocr Rev 25:426-457. (Pubitemid 38780667)
-
(2004)
Endocrine Reviews
, vol.25
, Issue.3
, pp. 426-457
-
-
Van Der Lely, A.J.1
Tschop, M.2
Heiman, M.L.3
Ghigo, E.4
-
38
-
-
34250666273
-
A monomeric G protein-coupled receptor isolated in a high-density lipoprotein particle efficiently activates its G protein
-
DOI 10.1073/pnas.0611448104
-
Whorton MR, Bokoch MP, Rasmussen SG, Huang B, Zare RN, Kobilka B, and Sunahara RK (2007) A monomeric G protein-coupled receptor isolated in a highdensity lipoprotein particle efficiently activates its G protein. Proc Natl Acad Sci U S A 104:7682-7687. (Pubitemid 47185966)
-
(2007)
Proceedings of the National Academy of Sciences of the United States of America
, vol.104
, Issue.18
, pp. 7682-7687
-
-
Whorton, M.R.1
Bokoch, M.P.2
Rasmussen, S.G.F.3
Huang, B.4
Zare, R.N.5
Kobilka, B.6
Sunahara, R.K.7
-
39
-
-
42949164679
-
Efficient coupling of transducin to monomeric rhodopsin in a phospholipid bilayer
-
Whorton MR, Jastrzebska B, Park PS, Fotiadis D, Engel A, Palczewski K, and Sunahara RK (2008) Efficient coupling of transducin to monomeric rhodopsin in a phospholipid bilayer. J Biol Chem 283:4387-4394.
-
(2008)
J Biol Chem
, vol.283
, pp. 4387-4394
-
-
Whorton, M.R.1
Jastrzebska, B.2
Park, P.S.3
Fotiadis, D.4
Engel, A.5
Palczewski, K.6
Sunahara, R.K.7
-
40
-
-
0031058751
-
Interactions of the alpha(2A)-adrenoceptor with multiple G(i) family G-proteins: Studies with pertussis toxin-resistant G-protein mutants
-
Wise A, Watson-Koken MA, Rees S, Lee M, and Milligan G (1997) Interactions of the alpha2A-adrenoceptor with multiple Gi-family G-proteins: studies with pertussis toxin-resistant G-protein mutants. Biochem J 321:721-728. (Pubitemid 27084881)
-
(1997)
Biochemical Journal
, vol.321
, Issue.3
, pp. 721-728
-
-
Wise, A.1
Watson-Koken, M.-A.2
Rees, S.3
Lee, M.4
Milligan, G.5
|