-
1
-
-
3042798261
-
Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: Molecular modeling and mutagenesis approaches to receptor structure and function
-
Kristiansen, K. Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: Molecular modeling and mutagenesis approaches to receptor structure and function. Pharmacol. Ther. 103, 21-80 (2004).
-
(2004)
Pharmacol. Ther.
, vol.103
, pp. 21-80
-
-
Kristiansen, K.1
-
2
-
-
33947356279
-
G protein-coupled receptor structure and activation
-
Kobilka, B.K. G protein-coupled receptor structure and activation. Biochim. Biophys. Acta 1768, 794-807 (2007).
-
(2007)
Biochim. Biophys. Acta
, vol.1768
, pp. 794-807
-
-
Kobilka, B.K.1
-
3
-
-
42149181885
-
Structural diversity of G protein-coupled receptors and significance for drug discovery
-
Lagerström, M.C. & Schiöth, 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
-
-
Lagerström, M.C.1
Schiöth, H.B.2
-
4
-
-
0026629249
-
Tethered ligand agonist peptides Structural requirements for thrombin receptor activation reveal mechanism of proteolytic unmasking of agonist function
-
Scarborough, R.M. et al. Tethered ligand agonist peptides. Structural requirements for thrombin receptor activation reveal mechanism of proteolytic unmasking of agonist function. J. Biol. Chem. 267, 13146-13149 (1992).
-
(1992)
J. Biol. Chem.
, vol.267
, pp. 13146-13149
-
-
Scarborough, R.M.1
-
5
-
-
1542316313
-
A molecular dissection of the glycoprotein hormone receptors
-
Vassart, G., Pardo, L. & Costagliola, S. A molecular dissection of the glycoprotein hormone receptors. Trends Biochem. Sci. 29, 119-126 (2004).
-
(2004)
Trends Biochem. Sci.
, vol.29
, pp. 119-126
-
-
Vassart, G.1
Pardo, L.2
Costagliola, S.3
-
6
-
-
78650273555
-
Alternative G protein coupling and biased agonism: New insights into melanocortin-4 receptor signalling
-
Breit, A. et al. Alternative G protein coupling and biased agonism: New insights into melanocortin-4 receptor signalling. Mol. Cell. Endocrinol. 331, 232-240 (2011).
-
(2011)
Mol. Cell. Endocrinol.
, vol.331
, pp. 232-240
-
-
Breit, A.1
-
7
-
-
70349334681
-
In silico mutagenesis: A case study of the melanocortin 4 receptor
-
Bromberg, Y., Overton, J., Vaisse, C., Leibel, R.L. & Rost, B. In silico mutagenesis: A case study of the melanocortin 4 receptor. FASEB J. 23, 3059-3069 (2009).
-
(2009)
FASEB J.
, vol.23
, pp. 3059-3069
-
-
Bromberg, Y.1
Overton, J.2
Vaisse, C.3
Leibel, R.L.4
Rost, B.5
-
8
-
-
9644279627
-
Constitutive activity of the melanocortin-4 receptor is maintained by its N-terminal domain and plays a role in energy homeostasis in humans
-
Srinivasan, S. et al. Constitutive activity of the melanocortin-4 receptor is maintained by its N-terminal domain and plays a role in energy homeostasis in humans. J. Clin. Invest. 114, 1158-1164 (2004).
-
(2004)
J. Clin. Invest.
, vol.114
, pp. 1158-1164
-
-
Srinivasan, S.1
-
9
-
-
0036033424
-
Constitutive activity of G-protein-coupled receptors: Cause of disease and common property of wild-type receptors
-
Seifert, R. & Wenzel-Seifert, K. Constitutive activity of G-protein-coupled receptors: Cause of disease and common property of wild-type receptors. Naunyn Schmiedebergs Arch. Pharmacol. 366, 381-416 (2002).
-
(2002)
Naunyn Schmiedebergs Arch. Pharmacol.
, vol.366
, pp. 381-416
-
-
Seifert, R.1
Wenzel-Seifert, K.2
-
10
-
-
38449087113
-
In vivo evidence for inverse agonism of Agouti-related peptide in the central nervous system of proopiomelanocortin-deficient mice
-
Tolle, V. & Low, M.J. In vivo evidence for inverse agonism of Agouti-related peptide in the central nervous system of proopiomelanocortin- deficient mice. Diabetes 57, 86-94 (2008).
-
(2008)
Diabetes
, vol.57
, pp. 86-94
-
-
Tolle, V.1
Low, M.J.2
-
11
-
-
34447558562
-
Antibodies against the melanocortin-4 receptor act as inverse agonists in vitro and in vivo
-
Peter, J.C. et al. Antibodies against the melanocortin-4 receptor act as inverse agonists in vitro and in vivo. Am. J. Physiol. Regul. Integr. Comp. Physiol. 292, R2151-R2158 (2007).
-
(2007)
Am. J. Physiol. Regul. Integr. Comp. Physiol.
, vol.292
-
-
Peter, J.C.1
-
12
-
-
0030764741
-
Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein
-
Ollmann, M.M. et al. Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein. Science 278, 135-138 (1997).
-
(1997)
Science
, vol.278
, pp. 135-138
-
-
Ollmann, M.M.1
-
13
-
-
0030614331
-
Role of melanocortinergic neurons in feeding and the agouti obesity syndrome
-
Fan, W., Boston, B.A., Kesterson, R.A., Hruby, V.J. & Cone, R.D. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature 385, 165-168 (1997).
-
(1997)
Nature
, vol.385
, pp. 165-168
-
-
Fan, W.1
Boston, B.A.2
Kesterson, R.A.3
Hruby, V.J.4
Cone, R.D.5
-
14
-
-
0035130843
-
AgRP 83-132) acts as an inverse agonist on the human-melanocortin-4 receptor
-
Nijenhuis, W.A., Oosterom, J. & Adan, R.A. AgRP(83-132) acts as an inverse agonist on the human-melanocortin-4 receptor. Mol. Endocrinol. 15, 164-171 (2001).
-
(2001)
Mol. Endocrinol.
, Issue.15
, pp. 164-171
-
-
Nijenhuis, W.A.1
Oosterom, J.2
Adan, R.A.3
-
15
-
-
10744221862
-
Inverse agonist activity of agouti and agouti-related protein
-
Chai, B.X. et al. Inverse agonist activity of agouti and agouti-related protein. Peptides 24, 603-609 (2003).
-
(2003)
Peptides
, vol.24
, pp. 603-609
-
-
Chai, B.X.1
-
16
-
-
0001169515
-
Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins
-
Costa, T. & Herz, A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. USA 86, 7321-7325 (1989).
-
(1989)
Proc. Natl. Acad. Sci. USA
, vol.86
, pp. 7321-7325
-
-
Costa, T.1
Herz, A.2
-
17
-
-
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
-
18
-
-
78049429422
-
Loop-swapped chimeras of the agouti-related protein and the agouti signaling protein identify contacts required for melanocortin 1 receptor selectivity and antagonism
-
Patel, M.P. et al. Loop-swapped chimeras of the agouti-related protein and the agouti signaling protein identify contacts required for melanocortin 1 receptor selectivity and antagonism. J. Mol. Biol. 404, 45-55 (2010).
-
(2010)
J. Mol. Biol.
, vol.404
, pp. 45-55
-
-
Patel, M.P.1
-
19
-
-
77957055780
-
Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors
-
Ballesteros, J.A. & Weinstein, H. Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors. Methods Neurosci. 25, 366-428 (1995).
-
(1995)
Methods Neurosci.
, vol.25
, pp. 366-428
-
-
Ballesteros, J.A.1
Weinstein, H.2
-
20
-
-
33646404622
-
Melanocortin 4 receptor mutations in a large cohort of severely obese adults: Prevalence, functional classification, genotype-phenotype relationship, and lack of association with binge eating
-
Lubrano-Berthelier, C. et al. Melanocortin 4 receptor mutations in a large cohort of severely obese adults: Prevalence, functional classification, genotype-phenotype relationship, and lack of association with binge eating. J. Clin. Endocrinol. Metab. 91, 1811-1818 (2006).
-
(2006)
J. Clin. Endocrinol. Metab.
, vol.91
, pp. 1811-1818
-
-
Lubrano-Berthelier, C.1
-
21
-
-
61849161252
-
Association of functionally significant Melanocortin-4 but not Melanocortin-3 receptor mutations with severe adult obesity in a large North American case-control study
-
Calton, M.A. et al. Association of functionally significant Melanocortin-4 but not Melanocortin-3 receptor mutations with severe adult obesity in a large North American case-control study. Hum. Mol. Genet. 18, 1140-1147 (2009).
-
(2009)
Hum. Mol. Genet.
, vol.18
, pp. 1140-1147
-
-
Calton, M.A.1
-
22
-
-
0035918601
-
Structure activity studies of the melanocortin-4 receptor by in vitro mutagenesis: Identification of agouti-related protein (AGRP), melanocortin agonist and synthetic peptide antagonist interaction determinants
-
Haskell-Luevano, C., Cone, R.D., Monck, E.K. & Wan, Y.P. Structure activity studies of the melanocortin-4 receptor by in vitro mutagenesis: Identification of agouti-related protein (AGRP), melanocortin agonist and synthetic peptide antagonist interaction determinants. Biochemistry 40, 6164-6179 (2001).
-
(2001)
Biochemistry
, vol.40
, pp. 6164-6179
-
-
Haskell-Luevano, C.1
Cone, R.D.2
Monck, E.K.3
Wan, Y.P.4
-
23
-
-
26444467486
-
Linking ligand binding to histamine H1 receptor activation
-
Jongejan, A. et al. Linking ligand binding to histamine H1 receptor activation. Nat. Chem. Biol. 1, 98-103 (2005).
-
(2005)
Nat. Chem. Biol.
, vol.1
, pp. 98-103
-
-
Jongejan, A.1
-
24
-
-
63849323943
-
Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-HT4 receptors
-
Pellissier, L.P. et al. Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-HT4 receptors. Mol. Pharmacol. 75, 982-990 (2009).
-
(2009)
Mol. Pharmacol.
, vol.75
, pp. 982-990
-
-
Pellissier, L.P.1
-
25
-
-
77950505038
-
A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors
-
Holst, B. et al. A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors. J. Biol. Chem. 285, 3973-3985 (2010).
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 3973-3985
-
-
Holst, B.1
-
26
-
-
79953234218
-
Crystal structure of metarhodopsin II
-
Choe, H.W. et al. Crystal structure of metarhodopsin II. Nature 471, 651-655 (2011).
-
(2011)
Nature
, vol.471
, pp. 651-655
-
-
Choe, H.W.1
-
27
-
-
79953242234
-
The structural basis of agonist-induced activation in constitutively active rhodopsin
-
Standfuss, J. et al. The structural basis of agonist-induced activation in constitutively active rhodopsin. Nature 471, 656-660 (2011).
-
(2011)
Nature
, vol.471
, pp. 656-660
-
-
Standfuss, J.1
-
28
-
-
79954782236
-
Structure of an agonist-bound human A2A adenosine receptor
-
Xu, F. et al. Structure of an agonist-bound human A2A adenosine receptor. Science 332, 322-327 (2011).
-
(2011)
Science
, vol.332
, pp. 322-327
-
-
Xu, F.1
-
29
-
-
78651405537
-
The structural basis for agonist and partial agonist action on a β1-adrenergic receptor
-
Warne, T. et al. The structural basis for agonist and partial agonist action on a β1-adrenergic receptor. Nature 469, 241-244 (2011).
-
(2011)
Nature
, vol.469
, pp. 241-244
-
-
Warne, T.1
-
30
-
-
78651411166
-
Structure of a nanobody-stabilized active state of the β2 adrenoceptor
-
Rasmussen, S.G. et al. Structure of a nanobody-stabilized active state of the β2 adrenoceptor. Nature 469, 175-180 (2011).
-
(2011)
Nature
, vol.469
, pp. 175-180
-
-
Rasmussen, S.G.1
-
31
-
-
78651399683
-
Structure and function of an irreversible agonist-β2 adrenoceptor complex
-
Rosenbaum, D.M. et al. Structure and function of an irreversible agonist-β2 adrenoceptor complex. Nature 469, 236-240 (2011).
-
(2011)
Nature
, vol.469
, pp. 236-240
-
-
Rosenbaum, D.M.1
-
32
-
-
0037174606
-
β 2 adrenergic receptor activation modulation of the proline kink in transmembrane 6 by a rotamer toggle switch
-
Shi, L. et al. β2 adrenergic receptor activation. Modulation of the proline kink in transmembrane 6 by a rotamer toggle switch. J. Biol. Chem. 277, 40989-40996 (2002).
-
(2002)
J. Biol. Chem.
, vol.277
, pp. 40989-40996
-
-
Shi, L.1
-
33
-
-
20444499405
-
Probing the 2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists
-
Swaminath, G. et al. Probing the 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
-
34
-
-
11144246968
-
GPCR deorphanizations: The novel, the known and the unexpected transmitters
-
Civelli, O. GPCR deorphanizations: The novel, the known and the unexpected transmitters. Trends Pharmacol. Sci. 26, 15-19 (2005).
-
(2005)
Trends Pharmacol. Sci.
, vol.26
, pp. 15-19
-
-
Civelli, O.1
-
35
-
-
31844446495
-
Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery
-
Bond, R.A. & Ijzerman, A.P. Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery. Trends Pharmacol. Sci. 27, 92-96 (2006).
-
(2006)
Trends Pharmacol. Sci.
, vol.27
, pp. 92-96
-
-
Bond, R.A.1
Ijzerman, A.P.2
-
36
-
-
0033976851
-
Use of constitutive G protein-coupled receptor activity for drug discovery
-
Chen, G. et al. Use of constitutive G protein-coupled receptor activity for drug discovery. Mol. Pharmacol. 57, 125-134 (2000).
-
(2000)
Mol. Pharmacol.
, vol.57
, pp. 125-134
-
-
Chen, G.1
-
37
-
-
0034812072
-
The use of constitutively active receptors for drug discovery at the G protein-coupled receptor gene pool
-
Behan, D.P. & Chalmers, D.T. The use of constitutively active receptors for drug discovery at the G protein-coupled receptor gene pool. Curr. Opin. Drug Discov. Devel. 4, 548-560 (2001).
-
(2001)
Curr. Opin. Drug Discov. Devel.
, vol.4
, pp. 548-560
-
-
Behan, D.P.1
Chalmers, D.T.2
-
38
-
-
65549087559
-
The N-terminal domain of GPR61, an orphan G-protein-coupled receptor, is essential for its constitutive activity
-
Toyooka, M., Tujii, T. & Takeda, S. The N-terminal domain of GPR61, an orphan G-protein-coupled receptor, is essential for its constitutive activity. J. Neurosci. Res. 87, 1329-1333 (2009).
-
(2009)
J. Neurosci. Res.
, vol.87
, pp. 1329-1333
-
-
Toyooka, M.1
Tujii, T.2
Takeda, S.3
-
39
-
-
0037439274
-
Intracellular retention is a common characteristic of childhood obesity-associated MC4R mutations
-
Lubrano-Berthelier, C. et al. Intracellular retention is a common characteristic of childhood obesity-associated MC4R mutations. Hum. Mol. Genet. 12, 145-153 (2003).
-
(2003)
Hum. Mol. Genet.
, vol.12
, pp. 145-153
-
-
Lubrano-Berthelier, C.1
-
40
-
-
0033927916
-
Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity
-
Vaisse, C. et al. Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity. J. Clin. Invest. 106, 253-262 (2000).
-
(2000)
J. Clin. Invest.
, vol.106
, pp. 253-262
-
-
Vaisse, C.1
|