G protein-coupled receptors: A count of 1001 conformations

Fundamental and Clinical Pharmacology

Volumn 19, Issue 1, 2005, Pages 45-56

  Vauquelin, G ^a   Van Liefde, I ^a  

^a VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

Author keywords

Agonist; Allosterism; Antagonist; Conformation; G protein coupled receptor; Models

Indexed keywords

CELL PROTEIN; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; LIGAND; LIPID;

AGONIST; ALLOSTERISM; BINDING AFFINITY; DRUG RECEPTOR BINDING; DRUG TARGETING; MOLECULAR MODEL; PRIORITY JOURNAL; PROTEIN CONFORMATION; REVIEW; STRUCTURE ANALYSIS;

ALLOSTERIC REGULATION; ANIMALS; HUMANS; MODELS, BIOLOGICAL; MUTATION; PROTEIN CONFORMATION; RECEPTORS, G-PROTEIN-COUPLED;

EID: 13444261019     PISSN: 07673981     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1472-8206.2005.00319.x     Document Type: Review

References (88)

1. Flower D.R. Modelling G-protein-coupled receptors for drug design. Biochim. Biophys. Acta (1999) 1422 207-234.
2. Muller G. Towards 3D structures of G protein-coupled receptors: a multidisciplinary approach. Curr. Med. Chem. (2000) 7 861-888.
3. Gether U. Uncovering molecular mechanisms involved in activation of G protein-coupled receptors. Endocr. Rev. (2000) 21 90-113.
4. Lin S.H., Civelli O. Orphan G protein-coupled receptors: targets for new therapeutic interventions. Ann. Med. (2004) 36 204-214.
5. Henderson R., Baldwin J.M., Ceska T.A., Zemlin F., Beckmann E., Downing K.H. Model for the structure of bacteriorhodopsin based on high-resolution electron cryo-microscopy. J. Mol. Biol. (1990) 213 899-929.
6. Palczewski K., Kumasaka T., Hori T. et al. Crystal structure of rhodopsin: a G protein-coupled receptor. Science (2002) 289 739-745.
7. Wess J. Molecular basis of receptor/G-protein-coupling selectivity. Pharmacol. Ther. (1998) 80 231-264.
8. Hermans E. Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors. Pharmacol. Ther. (2003) 99 25-44.
9. Kenakin T. The classification of seven transmembrane receptors in recombinant expression systems. Pharmacol. Rev. (1996) 48 413-463.
10. 2- Adrenergic and several other G protein-coupled receptors in human atrial membranes activate both Gs and Gi. Circ. Res. (2000) 87 705-709.
11. Laugwitz K.L., Allgeier A., Offermanns S. et al. The human thyrotropin receptor: a heptahelical receptor capable of stimulating members of all four G protein families. Proc. Natl. Acad. Sci. USA (1996) 93 116-120.
12. Gether U., Kobilka B.K. G protein-coupled receptors. II. Mechanism of agonist activation. J. Biol. Chem. (1998) 273 17979-17982.
13. Sheikh S.P., Vilardarga J.P., Baranski T.J. et al. Similar structures and shared switch mechanisms of the beta2-adrenoceptor and the parathyroid hormone receptor. Zn(II) bridges between helices III and VI block activation. J. Biol. Chem. (1999) 274 17033-17041.
14. Hulme E.C., Lu Z.L., Ward S.D., Allman K., Curtis C.A. The conformational switch in 7-transmembrane receptors: the muscarinic receptor paradigm. Eur. J. Pharmacol. (1999) 375 247-260.
15. 2 adrenoceptor. EMBO J. (1997) 16 6737-6747.
16. Pin J.P., Galvez T., Prezeau L. Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors. Pharmacol. Ther. (2003) 98 325-354.
17. Carroll F.Y., Stolle A., Beart P.M. et al. BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. Mol. Pharmacol. (2001) 59 965-973.
18. De Lean A., Stadel J.M., Lefkowitz R.J. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor. J. Biol. Chem. (1980) 255 7108-7117.
19. Samama P., Cotecchia S., Costa T., Lefkowitz R.J. A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model. J. Biol. Chem. (1993) 268 4625-4636.
20. Milligan G. Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective. Mol. Pharmacol. (2003) 64 1271-1276.
21. Weiss J.M., Morgan P.M., Lutz M.W., Kenakin T.P. The cubic ternary complex receptor-occupancy model. I. Model description. J. Theor. Biol. (1996) 178 151-167.
22. Weiss J.M., Morgan P.H., Lutz M.W., Kenakin T.P. The cubic ternary complex receptor-occupancy model. II. Understanding apparent affinity. J. Theor. Biol. (1996) 178 169-182.
23. Parnot C., Bardin S., Miserey-Lenkei S., Guedin D., Corvol P., Clauser E. Systematic identification of mutations that constitutively activate the angiotensin II type 1A receptor by screening a randomly mutated cDNA library with an original pharmacological bioassay. Proc. Natl. Acad. Sci. USA (2000) 97 7615-7620.
24. Kjelsberg M.A., Cotecchia S., Ostrowski J., Caron M.G., Lefkowitz R.J. Constitutive activation of the alpha 1B-adrenergic receptor by all amino acid substitutions at a single site. Evidence for a region which constrains receptor activation. J. Biol. Chem. (1992) 267 1430-1433.
25. 1A angiotensin II receptor induces its constitutive activation. J. Biol. Chem. (1997) 272 1822-1826.
26. 1 receptor activation is dependent upon two juxtaposed asparagine residues on transmembrane helices III and VII. J. Biol. Chem. (1997) 272 4245-4251.
27. Hunyady L., Vauquelin G., Vanderheyden P. Agonist induction and conformational selection during activation of a G-protein-coupled receptor. Trends Pharmacol. Sci. (2003) 24 81-86.
28. 1 receptor activation. J. Biol. Chem. (2002) 277 23107-23110.
29. 1 receptors. Biochem. Pharmacol. (2003) 65 1329-1335.
30. Parnot C., Miserey-Lenkei S., Bardin S., Corvol P., Clauser E. Lessons from constitutively active mutants of G protein-coupled receptors. Trends Endocrinol. Metab. (2002) 13 336-343.
31. Giraldo J. Agonist induction, conformational selection, and mutant receptors. FEBS Lett. (2004) 556 13-18.
32. Ghanouni P., Gryczynski Z., Steenhuis J.J. et al. Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptor. J. Biol. Chem. (2001) 276 24433-24436.
33. Swaminath G., Xiang Y., Lee T.W., Steenhuis J., Parnot C., Kobilka B.K. Sequential binding of agonists to the beta2 adrenoceptor. Kinetic evidence for intermediate conformational states. J. Biol. Chem. (2004) 279 686-691.
34. Ferguson S.S. Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signaling. Pharmacol. Rev. (2001) 53 1-24.
35. Luttrell L.M., Lefkowitz R.J. The role of beta-arrestins in the termination and transduction of G-protein-coupled receptor signals. J. Cell. Sci. (2002) 115 455-465.
36. Palanche T., Ilien B., Zoffmann S. et al. The neurokinin A receptor activates calcium and cAMP responses through distinct conformational states. J. Biol. Chem. (2001) 276 34853-34861.
37. Holloway A.C., Qian H., Pipolo L. et al. Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, and phosphorylation of type 1A angiotensin receptors. Mol. Pharmacol. (2002) 61 768-777.
38. Devi L.A. Heterodimerization of G-protein-coupled receptors: pharmacology, signaling and trafficking. Trends Pharmacol. Sci. (2001) 22 532-537.
39. Rios C.D., Jordan B.A., Gomes I., Devi L.A. G-protein-coupled receptor dimerization: modulation of receptor function. Pharmacol. Ther. (2001) 92 71-87.
40. Kobilka B.K. The role of cytosolic and membrane factors in processing of the human beta-2 adrenergic receptor following translocation and glycosylation in a cell-free system. J. Biol. Chem. (1990) 265 7610-7618.
41. Gether U., Ballesteros J.A., Seifert R., Sanders-Bush E., Weinstein H., Kobilka B.K. Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility. J. Biol. Chem. (1997) 272 2587-2590.
42. 1 receptor subtype. Br. J. Pharmacol. (1993) 110 761-771.
43. 1 subtype angiotensin II receptor antagonist. J. Pharmacol. Exp. Ther. (1993) 265 826-834.
44. Noda M., Shibouta Y., Inada Y. et al. Inhibition of rabbit aortic angiotensin II (AII) receptor by CV-11974, a new neuropeptide AII antagonist. Biochem. Pharmacol. (1993) 46 311-318.
45. Mochizuki S., Sato T., Furata K. et al. Pharmacological properties of KT3-671, a novel nonpeptide angiotensin II receptor antagonist. Cardiovasc. Pharmacol. (1995) 25 22-29.
46. 1 receptors. Br. J. Pharmacol. (1999) 126 1057-1065.
47. Verheilen I., Fierens F.L.P., De Backer J.-P., Vauquelin G., Vanderheyden P.M.L. Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors. Fundam. Clin. Pharmacol. (2001) 14 577-585.
48. 1 receptor antagonists: the role of tight antagonist binding. Eur. J. Pharmacol. (1999) 372 199-206.
49. 1 cells. Biochem. Pharmacol. (2000) 59 927-935.
50. Vauquelin G., Van Liefde I., Birzbier B.B., Vanderheyden P.M.L. New insights in insurmountable antagonism. Fundam. Clin. Pharmacol. (2002) 16 262-272.
51. Vauquelin G., Van Liefde I., Vanderheyden P.M.L. Models and methods for studying insurmountable antagonism. Trends Pharmacol. Sci. (2002) 23 514-518.
52. 3H]-irbesartan to human recombinant angiotensin II type 1 receptors. J. Renin Angiotensin Aldosterone Syst. (2000) 1 159-165.
53. 1 receptors and their non-peptide antagonists. Biochem. Pharmacol. (2001) 61 277-284.
54. 1 receptor antagonism: the need for different antagonist binding states of the receptor. Trends Pharmacol. Sci. (2001) 22 343-344.
55. 1 receptor antagonists. J. Renin Angiotensin Aldosterone Syst. (2001) 2 S24-S31.
56. 1 receptor differently affects the binding of surmountable and insurmountable non-peptide antagonists. J. Renin Angiotensin Aldosterone Syst. (2000) 1 283-288.
57. Kenakin T. Agonist-receptor efficacy. II. Agonist trafficking of receptor signals. Trends Pharmacol. Sci. (1995) 16 232-238.
58. Kenakin T. Ligand-selective receptor conformations revisited: the promise and the problem. Trends Pharmacol. Sci. (2003) 24 346-354.
59. 2A-adrenergic receptor signaling in Chinese hamster ovary cells: 1-isoproterenol selectively activates Gs. J. Pharmacol. Exp. Ther. (2000) 294 539-547.
60. Berg K.A., Maayani S., Goldfarb J., Scaramellini C., Leff P., Clarke W.P. Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: evidence for agonist-directed trafficking of receptor stimulus. Mol. Pharmacol. (1998) 54 94-104.
61. Spengler D., Waeber C., Pantaloni C. et al. Differential signal transduction by five splice variants of the PACAP receptor. Nature (1993) 365 170-175.
62. Pommier B., Da Nascimento S., Dumont S. et al. The cholecystokininB receptor is coupled to two effector pathways through pertussis toxin-sensitive and -insensitive G proteins. J. Neurochem. (1999) 73 281-288.
63. Leff P., Scaramellini C., Law C., McKechnie K. A three-state receptor model of agonist action. Trends Pharmacol. Sci. (1997) 18 355-362.
64. Pike L.J. Lipid rafts: bringing order to chaos. J. Lipid Res. (2003) 44 655-667.
65. Ostrom R.S., Insel P.A. The evolving role of lipid rafts and caveolae in G protein-coupled receptor signaling: implications for molecular pharmacology. Br. J. Pharmacol. (2004) 143 235-245.
66. Lelkowitz R.J., Pierce K.L., Luttrell L.M. Dancing with different partners: protein kinase a phosphorylation of seven membrane-spanning receptors regulates their G protein-coupling specificity. Mol. Pharmacol. (2002) 62 971-974.
67. 2 adrenergic receptor-Src protein kinase complexes. Science (1999) 283 655-661.
68. DeFea K.A., Zalevsky J., Thoma M.S., Dery O., Mullins R.D., Bunnett N.W. β-Arrestin-dependent endocytosis of proteinase-activated receptor 2 is required for intracellular targeting of activated ERK1/2. J. Cell. Biol. (2000) 148 1267-1281.
69. Schwartz T.W., Gether U., Schambye H., Hjorth S.A. Molecular mechanism of action of non-peptide ligands for peptide receptors. Curr. Pharm. Des. (1995) 1 325-342.
70. Monod J., Changeux J.-P., Jacob F. Allosteric proteins and cellular control systems. J. Mol. Biol. (1963) 6 306-329.
71. Lebesgue D., Wallukat G., Mijares A., Granier C., Argibay J., Hoebeke J. An agonist-like monoclonal antibody against the human beta2-adrenoceptor. Eur. J. Pharmacol. (1998) 348 123-133.
72. Christopoulos A. Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat. Rev. Drug. Discov. (2002) 1 198-210.
73. Christopoulos A., Kenakin T. G protein-coupled receptor allosterism and complexing. Pharmacol. Rev. (2003) 54 323-374.
74. Koshland D.E. Jr. Nemethy G., Filmer D. Comparison of experimental binding data and theoretical models in proteins containing subunits. Biochemistry (1966) 5 365-385.
75. Chen J., Hage D.S. Quantitative analysis of allosteric drug-protein binding by biointeraction chromatography. Nat. Biotechnol. (1994) 22 1445-1448.
76. Milligan G., White J.H. Protein-protein interactions at G-protein-coupled receptors. Trends Pharmacol. Sci. (2001) 22 513-518.
77. Hur E.M., Kim K.T. G protein-coupled receptor signalling and cross-talk: achieving rapidity and specificity. Cell. Signal. (2002) 14 397-405.
78. Brady A.E., Limbird L.E. G protein-coupled receptor interacting proteins: emerging roles in localization and signal transduction. Cell Signal. (2002) 14 297-309.
79. Morfis M., Christopoulos A., Sexton P.M. RAMPs: 5 years on. where to now? Trends Pharmacol. Sci. (2003) 24 596-601.
80. George S.R., Fan T., Xie Z. et al. Oligomerization of mu- and delta-opioid receptors. Generation of novel functional properties. J. Biol. Chem. (2000) 275 26128-26135.
81. McLatchie L.M., Fraser N.J., Main M.J. et al. RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor. Nature (1998) 393 333-339.
82. Juaneda C., Dumont Y., Quirion R. The molecular pharmacology of CGRP and related peptide receptor subtypes. Trends Pharmacol. Sci. (2000) 21 432-438.
83. Hay D.L., Howitt S.G., Conner A.C., Schindler M., Smith D.M., Poyner D.R. CL/Ramp2 and CL/Ramp3 produce pharmacologically distinct adrenomedullin receptors: a comparison of effects of adrenomedullin 22-52. CGRP 8-37 and BIBN4096BS. Br. J. Pharmacol. (2003) 140 477-486.
84. Mallee J.J., Salvatore C.A., Lebourdelles B. et al. Ramp1 determines the species selectivity of non-peptide CGRP receptor antagonists. J. Biol. Chem. (2002) 277 14294-14298.
85. 3H]candesartan to intact cells and membrane preparations. Biochem. Pharmacol. (2002) 63 1273-1279.
86. 1 receptors in intact cells. Biochem. Pharmacol. (2004) 67 1601-1606.
87. Klein U., Gimpl G., Fahrenholz F. Alteration of the myometrial plasma membrane cholesterol content with beta-cyclodextrin modulates the binding affinity of the oxytocin receptor. Biochemistry (1995) 34 13784-13793.
88. Krumins A.M., Barber R. The stability of the agonist beta2-adrenergic receptor-Gs complex: evidence for agonist-specific states. Mol. Pharmacol. (1997) 52 144-154.