The effect of allosteric modulators on the kinetics of agonist-G protein-coupled receptor interactions in single living cells

Molecular Pharmacology

Volumn 78, Issue 3, 2010, Pages 511-523

  May, Lauren T ^a   Self, Tim J ^a   Briddon, Stephen J ^a   Hill, Stephen J ^a  

^a UNIVERSITY OF NOTTINGHAM   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ABA X BY 630; ABA X BY630; ADENOSINE A1 RECEPTOR; ADENOSINE A3 RECEPTOR; ADENOSINE DERIVATIVE; G PROTEIN COUPLED RECEPTOR; UNCLASSIFIED DRUG; ADENOSINE; BENZAMIDE; BENZAMIDE DERIVATIVE; INDOLE DERIVATIVE; VUF 5455;

ALLOSTERISM; ANIMAL CELL; ARTICLE; DISSOCIATION; DRUG PROTEIN BINDING; DRUG RECEPTOR BINDING; ENZYME KINETICS; EQUILIBRIUM CONSTANT; INTRACELLULAR SIGNALING; NONHUMAN; PERFUSION; PHYSIOLOGICAL PROCESS; PRIORITY JOURNAL; ANALOGS AND DERIVATIVES; ANIMAL; DRUG EFFECTS; DRUG INTERACTION; HAMSTER; KINETICS; METABOLISM;

ADENOSINE; ALLOSTERIC REGULATION; ANIMALS; BENZAMIDES; CRICETINAE; DRUG INTERACTIONS; INDOLES; KINETICS; RECEPTORS, G-PROTEIN-COUPLED;

EID: 77956239484     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.110.064493     Document Type: Article

References (27)

1. Avlani V, May LT, Sexton PM, and Christopoulos A (2004) Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors. J Pharmacol Exp Ther 308:1062-1072.
2. Birdsall NJ, Lazareno S, and Matsui H (1996) Allosteric regulation of muscarinic receptors. Prog Brain Res 109:147-151.
3. Bruns RF and Fergus JH (1990) Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes. Mol Pharmacol 38:939-949.
4. Christopoulos A and Kenakin T (2002) G protein-coupled receptor allosterism and complexing. Pharmacol Rev 54:323-374.
5. Christopoulos A, Lanzafame A, Ziegler A, and Mitchelson F (1997) Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an "infinite dilution" procedure. Biochem Pharmacol 53:795-800.
6. Cohen FR, Lazareno S, and Birdsall NJ (1996a) The affinity of adenosine for the high- and low-affinity states of the human adenosine A1 receptor. Eur J Pharmacol 309:111-114. (Pubitemid 26253025)
7. Cohen FR, Lazareno S, and Birdsall NJ (1996b) The effects of saponin on the binding and functional properties of the human adenosine A1 receptor. Br J Pharmacol 117:1521-1529. (Pubitemid 26116780)
8. Cohen MV and Downey JM (2008) Adenosine: trigger and mediator of cardioprotection. Basic Res Cardiol 103:203-215.
9. Cordeaux Y, Briddon SJ, Alexander SP, Kellam B, and Hill SJ (2008) Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells. FASEB J 22:850-860.
10. Cordeaux Y, Briddon SJ, Megson AE, McDonnell J, Dickenson JM, and Hill SJ (2000) Influence of receptor number on functional responses elicited by agonists acting at the human adenosine A(1) receptor: evidence for signaling pathway-dependent changes in agonist potency and relative intrinsic activity. Mol Pharmacol 58:1075-1084.
11. Dowling MR and Charlton SJ (2006) Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor. Br J Pharmacol 148:927-937. (Pubitemid 44543610)
12. Ellis J, Huyler J, and Brann MR (1991) Allosteric regulation of cloned m1-m5 muscarinic receptor subtypes. Biochem Pharmacol 42:1927-1932.
13. Fredholm BB, IJzerman AP, Jacobson KA, Klotz KN, and Linden J (2001) International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors. Pharmacol Rev 53:527-552.
14. Gao ZG, Van Muijlwijk-Koezen JE, Chen A, Müller CE, IJzerman AP, and Jacobson KA (2001) Allosteric modulation of A(3) adenosine receptors by a series of 3-(2- pyridinyl)isoquinoline derivatives. Mol Pharmacol 60:1057-1063. (Pubitemid 33027441)
15. Han Y, Moreira IS, Urizar E, Weinstein H, and Javitch JA (2009) Allosteric communication between protomers of dopamine class A GPCR dimers modulates activation. Nat Chem Biol 5:688-695.
16. Ilien B, Glasser N, Clamme JP, Didier P, Piemont E, Chinnappan R, Daval SB, Galzi JL, and Mely Y (2009) Pirenzepine promotes the dimerization of muscarinic M1 receptors through a three-step binding process. J Biol Chem 284:19533-19543.
17. Jacobson KA and Gao ZG (2006) Adenosine receptors as therapeutic targets. Nat Rev Drug Discov 5:247-264.
18. Kenakin T (2002) Drug efficacy at G protein-coupled receptors. Annu Rev Pharmacol Toxicol 42:349-379.
19. Lazareno S and Birdsall NJ (1995) Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors. Mol Pharmacol 48:362-378.
20. Lee NH and el-Fakahany EE (1991) Allosteric antagonists of the muscarinic acetylcholine receptor. Biochem Pharmacol 42:199-205.
21. May LT, Avlani VA, Langmead CJ, Herdon HJ, Wood MD, Sexton PM, and Christopoulos A (2007a) Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors. Mol Pharmacol 72:463-476.
22. May LT, Leach K, Sexton PM, and Christopoulos A (2007b) Allosteric modulation of G protein-coupled receptors. Annu Rev Pharmacol Toxicol 47:1-51.
23. Middleton RJ, Briddon SJ, Cordeaux Y, Yates AS, Dale CL, George MW, Baker JG, Hill SJ, and Kellam B (2007) New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells. J Med Chem 50:782-793.
24. Overington JP, Al-Lazikani B, and Hopkins AL (2006) How many drug targets are there? Nat Rev Drug Discov 5:993-996. (Pubitemid 44835126)
25. Rhee SG (2001) Regulation of phosphoinositide-specific phospholipase C. Annu Rev Biochem 70:281-312.
26. Springael JY, Le Minh PN, Urizar E, Costagliola S, Vassart G, and Parmentier M (2006) Allosteric modulation of binding properties between units of chemokine receptor homo- and hetero-oligomers. Mol Pharmacol 69:1652-1661.
27. Swaminath G, Xiang Y, Lee TW, Steenhuis J, Parnot C, and Kobilka BK (2004) Sequential binding of agonists to the beta2 adrenoceptor. Kinetic evidence for intermediate conformational states. J Biol Chem 279:686-691.