Application of receptor theory to allosteric modulation of receptors

Progress in Molecular Biology and Translational Science

Volumn 115, Issue , 2013, Pages 217-290

  Hall, David A ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Constitutive activity; Cubic ternary complex model; Intrinsic efficacy; Keywords; Operational model; Protean agonism; Receptor inactivation; Two state model

Indexed keywords

EID: 84873906998     PISSN: 18771173     EISSN: None     Source Type: Book Series    
DOI: 10.1016/B978-0-12-394587-7.00006-3     Document Type: Chapter

References (38)

1. A. Christopoulos, and T.P. Kenakin G-protein-coupled receptor allosterism and complexing Pharmacol Rev 54 2002 323 374
2. D.A. Hall Predicting dose-response curve behaviour: mathematical models of allosteric receptor-ligand interactions N.G. Bowery, Allosteric receptor modulation in drug targeting 2006 Taylor & Francis New York 39 78
3. K. Leach, P.M. Sexton, and A. Christopoulos Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology Trends Pharmacol Sci 28 2007 382 389
4. K.J. Gregory, P.M. Sexton, and A. Christopoulos Overview of receptor allosterism Curr Protoc Pharmacol 51 2010 1.21.1 1.21.34
5. L.M. Luttrell, and T.P. Kenakin Refining efficacy: allosterism and bias in G-protein coupled receptor signalling Methods Mol Biol 756 2011 3 35
6. D.A. Hall Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation Mol Pharmacol 58 2000 1412 1423
7. T. Kenakin, and O. Onaran The ligand paradox between affinity and efficacy: can you be there and not make a difference? Trends Pharmacol Sci 23 2002 275 289
8. H.O. Onaran, A. Scheer, S. Cotecchia, and T. Costa A look at receptor efficacy. From the signalling network of the cell to the intramolecular motion of the receptor Handb Exp Pharmacol 148 2000 217 259
9. H.O. Onaran, and T. Costa Agonist efficacy and allosteric models of receptor action Ann N Y Acad Sci 812 1997 98 115
10. R.J. Slack, and D.A. Hall Development of operational models of receptor activation including constitutive receptor activity and their use to determine the efficacy of the chemokine TARC at the CC-chemokine receptor CCR4 Br J Pharmacol 166 2012 1774 1792
11. A. De Léan, J.M. Stadel, and R.J. Lefkowitz A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-Adrenergic receptor J Biol Chem 255 1980 7108 7117
12. J.M. Weiss, P.H. Morgan, M.W. Lutz, and T.P. Kenakin The cubic ternary complex receptor-occupancy model I. Model description J Theor Biol 178 1996 151 167
13. J.M. Weiss, P.H. Morgan, M.W. Lutz, and T.P. Kenakin The cubic ternary complex receptor-occupancy model II. Understanding apparent affinity J Theor Biol 178 1996 169 182
14. J.M. Weiss, P.H. Morgan, M.W. Lutz, and T.P. Kenakin The cubic ternary complex receptor-occupancy model III. Resurrecting efficacy J Theor Biol 181 1996 381 397
15. T. Kenakin Pharmacological proteus? Trends Pharmacol Sci 16 1995 256 257
16. S. Lazareno, and N.J. Birdsall Detection, quantification and verification of allosteric interactions with labelled and unlabelled ligands at G-protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors Mol Pharmacol 48 1995 362 378
17. F.J. Ehlert Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods Mol Pharmacol 33 1988 187 194
18. T. Costa, and A. Herz Antagonists with negative intrinsic activity at δ opioid receptors coupled to GTP-binding proteins Proc Natl Acad Sci USA 86 1989 7321 7325
19. M. Corsi, P. Fina, and D.A. Trist Co-Agonism in drug-receptor interaction: illustrated by the NMDA receptor Trends Pharmacol Sci 17 1996 220 222
20. 2 muscarinic receptor J Pharmacol Exp Ther 325 2008 1039 1060
21. J.M. Stockton, N.J.M. Birdsall, A.S.V. Burgen, and E.C. Hulme Modification of the binding properties of muscarinic receptors by gallamine Mol Pharmacol 23 1983 551 558
22. A. Karlin On the application of a "plausible model" of allosteric proteins to the receptor for acetylcholine J Theor Biol 16 1967 306 320
23. C.D. Thron On the analysis of pharmacological experiments in terms of an allosteric model Mol Pharmacol 9 1972 1 9
24. D. Colquhoun The relation between classical and cooperative models for drug action H.P. Rang, Drug receptors 1973 The Macmillan Company London 149 182
25. V.K. Balakrishnan Schaum's outline of graph theory 1997 McGraw-Hill Companies Inc. USA
26. S. Lazareno, P. Gharagozloo, D. Kuonen, A. Popham, and N.J.M. Birdsall Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies Mol Pharmacol 53 1998 573 589
27. J. Jakubík, L. Bačáková, E.E. El-Fakahany, and S. Tuček Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors Mol Pharmacol 52 1998 172 179
28. F.J. Ehlert, H. Suga, and M.T. Griffin Analysis of agonism and inverse agonism in functional assays with constitutive activity: estimation of orthosteric ligand affinity constants for active and inactive receptor states J Pharmacol Exp Ther 338 2011 671 686
29. N. Bindslev A homotropic two-state model and auto-Antagonism BMC Pharmacol 4 2004 11
30. T. Kenakin Agonist-receptor efficacy II: agonist trafficking of receptor signals Trends Pharmacol Sci 16 1995 232 238
31. P. Leff, C. Scaramellini, C. Law, and K. McKechnie A three-state receptor model of agonist action Trends Pharmacol Sci 18 1997 355 362
32. T. Kenakin New concepts in drug discovery: collateral efficacy and permissive agonism Nat Rev Drug Discov 4 2005 919 927
33. J.W. Black, and P. Leff Operational models of pharmacological agonism Proc R Soc Lond B Biol Sci 220 1983 141 162
34. R.F. Furchgott The use of β-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-Agonist complexes N.J. Harper, A.B. Simmonds, Advances in drug research vol. 3 1966 Academic Press New York 21 25
35. D.S. Riggs The mathematical approach to physiological problems 1963 The Williams and Wilkins Company Baltimore
36. i3 Mol Pharmacol 71 2007 1349 1359
37. 2A-Adrenoceptors Mol Pharmacol 53 1998 963 968
38. J.R. Lane, B. Powney, A. Wise, S. Rees, and G. Milligan G protein coupling and ligand selectivity of the D2L and D3 dopamine receptors J Pharmacol Exp Ther 325 2008 319 330