Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors

British Journal of Pharmacology

Volumn 153, Issue 7, 2008, Pages 1353-1363

  Strange, P G ^a  

^a UNIVERSITY OF READING   (United Kingdom)

Author keywords

Agonist affinity; Agonist binding; Agonist efficacy; G protein coupled receptors

Indexed keywords

ASPARTIC ACID; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE; LIGAND; MUSCARINIC RECEPTOR; SODIUM ION;

ACCURACY; AGONIST; BINDING AFFINITY; DISSOCIATION CONSTANT; DRUG EFFICACY; DRUG MECHANISM; DRUG TARGETING; LIGAND BINDING; MUTAGENESIS; PRIORITY JOURNAL; REVIEW;

BINDING SITES; DRUG AGONISM; DRUG DESIGN; HUMANS; LIGANDS; MODELS, BIOLOGICAL; PROTEIN BINDING; RECEPTORS, G-PROTEIN-COUPLED;

EID: 41849132178     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707672     Document Type: Review

References (72)

1. Alder JT, Hacksell U, Strange PG (2003). Analysis of molecular determinants of affinity and relative efficacy of a series of R- and S-2-(dipropylamino)tetralins at the 5-HT1A serotonin receptor. Br J Pharmacol 138: 1129-1139.
2. Avalos M, Mak C, Randall PK, Trzeciakowski JP, Abell C, Kwan SW et al. (2001). Nonlinear analysis of partial dopamine agonist effects on cAMP in C6 glioma cells. J Pharmacol Toxicol Methods 45: 17-37.
3. Barlow RB, Scott NC, Stephenson RP (1967). The affinity and efficacy of onium salts on the frog rectus abdominis. Br J Pharmacol Chemother 31: 188-196.
4. Besse JC, Furchgott RF (1976). Dissociation constants and relative efficacies of agonists acting on alpha adrenergic receptors in rabbit aorta. J Pharmacol Exp Ther 197: 66-78.
5. Black JW, Leff P (1983). Operational models of pharmacological agonism. Proc R Soc London B Biol Sci 220: 141-162.
6. Black JW, Shankley NP (1990). Interpretation of agonist affinity estimations: the question of distributed receptor states. Proc R Soc London B Biol Sci 240: 503-518.
7. Ceresa BP, Limbird LE (1994). Mutation of an aspartate residue highly conserved among G-protein-coupled receptors results in nonreciprocal disruption of alpha 2-adrenergic receptor-G-protein interactions. A negative charge at amino acid residue 79 forecasts alpha 2A-adrenergic receptor sensitivity to allosteric modulation by monovalent cations and fully effective receptor/-G-protein coupling. J Biol Chem 269: 29557-29564.
8. Chung FZ, Wang CD, Potter PC, Venter JC, Fraser CM (1988). Site-directed mutagenesis and continuous expression of human beta-adrenergic receptors. Identification of a conserved aspartate residue involved in agonist binding and receptor activation. J Biol Chem 263: 4052-4055.
9. Colquhoun D (1998). Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors. Br J Pharmacol 125: 924-947.
10. Costa T, Lang J, Gless C, Herz A (1990). Spontaneous association between opioid receptors and GTP-binding regulatory proteins in native membranes: specific regulation by antagonists and sodium ions. Mol Pharmacol 37: 383-394.
11. De Lean A, Stadel JM, Lefkowitz RJ (1980). A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor. J Biol Chem 255: 7108-7117.
12. Del Castillo J, Katz B (1957). Interaction at end-plate receptors between different choline derivatives. Proc R Soc London B Biol Sci 146: 369-381.
13. Donnelly D, Maudsley S, Gent JP, Moser RN, Hurrell CR, Findlay JB (1999). Conserved polar residues in the transmembrane domain of the human tachykinin NK2 receptor: functional roles and structural implications. Biochem J 339 (Part 1): 55-61.
14. Ehlert FJ (1987). Coupling of muscarinic receptors to adenylate cyclase in the rabbit myocardium: effects of receptor inactivation. J Pharmacol Exp Ther 240: 23-30.
15. Ehlert FJ (2001). The ternary complex model. In: Christopoulos A (ed). Biomedical Applications of Computer Modelling. CRC Press LLC: Danvers. pp 21-85.
16. Ehlert FJ, Griffin MT, Sawyer GW, Bailon R (1999). A simple method for estimation of agonist activity at receptor subtypes: comparison of native and cloned M3 muscarinic receptors in guinea pig ileum and transfected cells. J Pharmacol Exp Ther 289: 981-992.
17. Fersht A (1999). Structure and Mechanism in Protein Science. W H Freeman: New York.
18. Fraser CM, Wang CD, Robinson DA, Gocayne JD, Venter JC (1989). Site-directed mutagenesis of m1 muscarinic acetylcholine receptors: conserved aspartic acids play important roles in receptor function. Mol Pharmacol 36: 840-847.
19. Furchgott RF (1966). The use of beta-haloalkylamines in the determination of dissociation constants of receptor-agonist complexes. In: Harper NJ, Simmonds AB (eds). Advances in Drug Research, vol. 3. Academic Press: New York. pp 21-55.
20. Furchgott RF, Bursztyn P (1967). Comparison of dissociation constants and of relative efficacies of selected agonists acting on parasympathetic receptors. Ann NY Acad Sci 144: 882-898.
21. Gardner BR, Hall DA, Strange PG (1997). Agonist action at D2(short) dopamine receptors determined in ligand binding and functional assays. J Neurochem 69: 2589-2598.
22. 15. J Pharmacol Exp Ther 321: 1193-1207.
23. Horstman DA, Brandon S, Wilson AL, Guyer CA, Cragoe Jr EJ, Limbird LE (1990). An aspartate conserved among G-protein receptors confers allosteric regulation of alpha 2-adrenergic receptors by sodium. J Biol Chem 265: 21590-21595.
24. Hulme EC, Curtis CA, Page KM, Jones PG (1995). The role of charge interactions in muscarinic agonist binding, and receptor-response coupling. Life Sci 56: 891-898.
25. Hulme EC, Lu ZL (1998). Scanning mutagenesis of transmembrane domain 3 of the M1 muscarinic acetylcholine receptor. J Physiol Paris 92: 269-274.
26. Jinnah HA, Page T, Friedmann T (1993). Brain purines in a genetic mouse model of Lesch-Nyhan disease. J Neurochem 60: 2036-2045.
27. Kenakin T (2005). New concepts in drug discovery: collateral efficacy and permissive antagonism. Nat Rev Drug Discov 4: 919-927.
28. + regulation of agonist binding but does not alter receptor-G protein association. Mol Pharmacol 44: 380-384.
29. Kong H, Raynor K, Yasuda K, Moe ST, Portoghese PS, Bell GI et al. (1993b). A single residue, aspartic acid 95, in the delta opioid receptor specifies selective high affinity agonist binding. J Biol Chem 268: 23055-23058.
30. Leff P (1995). The two-state model of receptor activation. Trends Pharmacol Sci 16: 89-97.
31. Leff P, Dougall IG, Harper DH, Dainty IA (1990a). Errors in agonist affinity estimation: do they and should they occur in isolated tissue experiments? Trends Pharmacol Sci 11: 64-67.
32. Leff P, Harper D, Dainty IA, Dougall IG (1990b). Pharmacological estimation of agonist affinity: detection of errors that may be caused by the operation of receptor isomerisation or ternary complex mechanisms. Br J Pharmacol 101: 55-60.
33. Liapakis G, Chan WC, Papadokostaki M, Javitch JA (2004). Synergistic contributions of the functional groups of epinephrine to its affinity and efficacy at the beta2 adrenergic receptor. Mol Pharmacol 65: 1181-1190.
34. Lin H, Saisch SG, Strange PG (2006). Assays for enhanced activity of low efficacy partial agonists at the D(2) dopamine receptor. Br J Pharmacol 149: 291-299.
35. Mackay D (1988). Continuous variation of agonist affinity constants. Trends Pharmacol Sci 9: 156-157.
36. Mackay D (1990). Agonist potency and apparent affinity: interpretation using classical and steady-state ternary-complex models. Trends Pharmacol Sci 11: 17-22.
37. Mak CK, Avalos M, Randall PK, Kwan SW, Abell CW, Neumeyer JL et al. (1996). Improved models for pharmacological null experiments: calculation of drug efficacy at recombinant D1A dopamine receptors stably expressed in clonal cell lines. Neuropharmacology 35: 549-570.
38. Martin S, Botto JM, Vincent JP, Mazella J (1999). Pivotal role of an aspartate residue in sodium sensitivity and coupling to G proteins of neurotensin receptors. Mol Pharmacol 55: 210-215.
39. McKinney M, Miller JH, Gibson VA, Nickelson L, Aksoy S (1991). Interactions of agonists with M2 and M4 muscarinic receptor subtypes mediating cyclic AMP inhibition. Mol Pharmacol 40: 1014-1022.
40. McLoughlin DJ, Strange PG (2000). Mechanisms of agonism and inverse agonism at serotonin 5-HT1A receptors. J Neurochem 74: 347-357.
41. Moya PR, Berg KA, Gutierrez-Hernandez MA, Saez-Briones P, Reyes-Parada M, Cassels BK et al. (2007). Functional selectivity of hallucinogenic phenethylamine and phenylisopropylamine derivatives at human 5-hydroxytryptamine (5-HT)2A and 5-HT2C receptors. J Pharmacol Exp Ther 321: 1054-1061.
42. Neve KA (1991). Regulation of dopamine D2 receptors by sodium and pH. Mol Pharmacol 39: 570-578.
43. Neve KA, Cox BA, Henningsen RA, Spanoyannis A, Neve RL (1991). Pivotal role for aspartate-80 in the regulation of dopamine D2 receptor affinity for drugs and inhibition of adenylyl cyclase. Mol Pharmacol 39: 733-739.
44. Otero AD (1990). Transphosphorylation and G protein activation. Biochem Pharmacol 39: 1399-1404.
45. Perlman JH, Nussenzveig DR, Osman R, Gershengorn MC (1992). Thyrotropin-releasing hormone binding to the mouse pituitary receptor does not involve ionic interactions. A model for neutral peptide binding to G protein-coupled receptors. J Biol Chem 267: 24413-24417.
46. Rang HP (2006). The receptor concept: pharmacology's big idea. Br J Pharmacol 147 (Suppl 1): S9-S16.
47. Roberts DJ, Lin H, Strange PG (2004). Mechanisms of agonist action at D2 dopamine receptors. Mol Pharmacol 66: 1573-1579.
48. Ruffolo Jr RR, Dillard RD, Yaden EL, Waddell JE (1979a). Receptor interactions of imidazolines. II. Affinities and efficacies of hydroxy-substituted tolazoline derivatives in rat aorta. J Pharmacol Exp Ther 211: 74-79.
49. Ruffolo Jr RR, Rosing EL, Waddell JE (1979b). Receptor interactions of imidazolines. I. Affinity and efficacy for alpha adrenergic receptors in rat aorta. J Pharmacol Exp Ther 209: 429-436.
50. Ruffolo Jr RR, Waddell JE (1982). Receptor interactions of imidazolines: alpha-adrenoceptors of rat and rabbit aortae differentiated by relative potencies, affinities and efficacies of imidazoline agonists. Br J Pharmacol 77: 169-176.
51. Ruffolo Jr RR, Waddell JE (1983). Aromatic and benzylic hydroxyl substitution of imidazolines and phenethylamines: differences in activity at alpha-1 and alpha-2 adrenergic receptors. J Pharmacol Exp Ther 224: 559-566.
52. Samama P, Cotecchia S, Costa T, Lefkowitz RJ (1993). A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model. J Biol Chem 268: 4625-4636.
53. Smit MJ, Vischer HF, Bakker RA, Jongejan A, Timmerman H, Pardo L et al. (2007). Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity. Annu Rev Pharmacol Toxicol 47: 53-87.
54. 35S]GTP gamma S binding. Eur J Pharmacol 320: 267-275.
55. Strader CD, Sigal IS, Candelore MR, Rands E, Hill WS, Dixon RA (1988). Conserved aspartic acid residues 79 and 113 of the beta-adrenergic receptor have different roles in receptor function. J Biol Chem 263: 10267-10271.
56. Strader CD, Sigal IS, Register RB, Candelore MR, Rands E, Dixon RA (1987). Identification of residues required for ligand binding to the beta-adrenergic receptor. Proc Natl Acad Sci USA 84: 4384-4388.
57. Strange PG (1998). Three-state and two-state models. Trends Pharmacol Sci 19: 85-86.
58. Strange PG (1999). G-protein coupled receptors: conformations and states. Biochem Pharmacol 58: 1081-1088.
59. Strange PG (2000). Agonist binding to G-protein coupled receptors. Br J Pharmacol 129: 820-821.
60. 3H]spiperone discriminates between the G-protein-coupled and -uncoupled forms. Biochem Pharmacol 45: 1003-1009.
61. Trzeciakowski JP (1999a). Stimulus amplification, efficacy, and the operational model. Part I - binary complex occupancy mechanisms. J Theor Biol 198: 329-346.
62. Trzeciakowski JP (1999b). Stimulus amplification, efficacy, and the operational model. Part II - ternary complex occupancy mechanisms. J Theor Biol 198: 347-374.
63. Umland SP, Wan Y, Shah H, Billah M, Egan RW, Hey JA (2001). Receptor reserve analysis of the human alpha(2C)-adrenoceptor using. Eur J Pharmacol 411: 211-221.
64. Urizar E, Claeysen S, Deupi X, Govaerts C, Costagliola S, Vassart G et al. (2005). An activation switch in the rhodopsin family of G protein-coupled receptors: the thyrotropin receptor. J Biol Chem 280: 17135-17141.
65. Wade SM, Lan K, Moore DJ, Neubig RR (2001). Inverse agonist activity at the alpha(2A)-adrenergic receptor. Mol Pharmacol 59: 532-542.
66. Wang CD, Buck MA, Fraser CM (1991). Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists. Mol Pharmacol 40: 168-179.
67. Wang CD, Gallaher TK, Shih JC (1993). Site-directed mutagenesis of the serotonin 5-hydroxytrypamine2 receptor: identification of amino acids necessary for ligand binding and receptor activation. Mol Pharmacol 43: 931-940.
68. Ward SD, Curtis CA, Hulme EC (1999). Alanine-scanning mutagenesis of transmembrane domain 6 of the M(1) muscarinic acetylcholine receptor suggests that Tyr381 plays key roles in receptor function. Mol Pharmacol 56: 1031-1041.
69. Waud DR (1969). On the measurement of the affinity of partial agonists for receptors. J Pharmacol Exp Ther 170: 117-122.
70. 35S]guanosine-5′-O-(3-thio)triphosphate binding: agonist potencies and the influence of sodium chloride on intrinsic activity. Mol Pharmacol 51: 1060-1069.
71. Williams C, Sewing A (2005). G-protein coupled receptor assays: to measure affinity or efficacy that is the question. Comb Chem High Throughput Screen 8: 285-292.
72. Wilson J, Lin H, Fu D, Javitch JA, Strange PG (2001). Mechanisms of inverse agonism of antipsychotic drugs at the D(2) dopamine receptor: use of a mutant D(2) dopamine receptor that adopts the activated conformation. J Neurochem 77: 493-504.