Multiple allosteric sites on muscarinic receptors

Life Sciences

Volumn 68, Issue 22-23, 2001, Pages 2517-2524

  Birdsall, Nigel J M ^a   Lazareno, Sebastian ^b   Popham, Angela ^b   Saldanha, Jose ^a  

^a NATIONAL INSTITUTE FOR MEDICAL RESEARCH   (United Kingdom)

^b MEDICAL RESEARCH COUNCIL   (United Kingdom)

Author keywords

Acetylcholine; Allosterism; Muscarinic receptor; Receptor model

Indexed keywords

ACETYLCHOLINE; BRUCINE; G PROTEIN COUPLED RECEPTOR; GALLAMINE; KT 5720; LIGAND; METHYLSCOPOLAMINE; MUSCARINIC RECEPTOR; STAUROSPORINE;

ALLOSTERISM; ARTICLE; BINDING KINETICS; BINDING SITE; DISSOCIATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; EXPERIMENTAL MODEL; LIGAND BINDING; PROTEIN BINDING; PROTEIN STRUCTURE;

EID: 0035957549     PISSN: 00243205     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0024-3205(01)01047-5     Document Type: Conference Paper

References (32)

1. Birdsall NJM, Cohen F, Lazareno S, Matsui H. Allosteric regulation of G-protein-linked receptors. Biochem Soc Trans 1995; 23:108-111
2. Lazareno S, Gharagozloo P, Kuonen D, Popham A, Birdsall NJM. Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: Radioligand binding studies. Mol Pharmacol 1998; 53:573-589
3. Birdsall NJM, Farries T, Gharagozloo P, Kobayashi S, Lazareno S and Sugimoto, M. Subtype selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: Functional studies. Mol Pharmacol 1999; 54:778-787
4. Palcewski K., Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M. Crystal structure of rhodopsin: A G-protein-coupled receptor. Science 2000; 289:739-745.
5. Gurevich VV, Pals-Rylaarsdam R, Benovic JL, Hosey MM, Onorato JJ. Agonist-receptor-arrestin, an alternative ternary complex with high agonist affinity. J Biol Chem 1997; 272:28849-28852
6. + exchange. Nature 1998; 392:626-630
7. Mellado M, Rodriguez-Frade JM, Aragay A, del Real G, Martin AM, Vila-Coro AJ, Serrano A, Mayor F, Marinez-A, C. The chemokine monocyte chemotactic protein 1 triggers Janus kinase 2 activation and tyrosine phosphorylation of the CCRB2 receptor. J Immunol 1998; 161:805-813
8. Corset V, Nguyen-Ba-Charvet KT, Forcet C, Moyse E, Chedotal A, Mehlen P. Netrin-1-mediated axon outgrowth and cAMP production requires interaction with the adenosine A2b receptor. Nature 2000; 407:747-750
9. Fryer AD, Jacoby DB. Effect of inflammatory cell mediators on M2 muscarinic receptors in the lungs. Life Sci 1993; 52:529-536.
10. Jacoby DB et al., Life Sci 2001 These proceedings
11. Devi, LA. G-protein-coupled receptor dimers in the limelight. Trends Pharmacol. Sci 2000; 21:324-326
12. 5 and γ-aminobutyric acid A receptors. Nature 2000; 403:274-280
13. Clark AL, Mitchelson F. The inhibitory effect of gallamine on muscarinic receptors. Br J Pharmacol 1976; 58:323-331
14. Stockton JM, Birdsall NJM, Burgen ASV, Hulme EC. Modification of the binding properties of muscarinic receptors by gallamine. Mol Pharmacol 1983; 23:551-557
15. Tucek S, Musilkova J, Nedoma J, Proska J, Shelkovnikov S, Vorlicek J. Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors. Mol Pharmacol 1990;38:674-680.
16. Lazareno S, Birdsall NJM 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 1995; 48:362-378
17. Birdsall NJM, Farries T, Gharagozloo P, Kobayashi S, Kuonen D, Lazareno S, Popham A, Sugimoto M. Selective allosteric enhancement of the binding and actions of acetylcholine at muscarinic receptor subtypes. Life Sci 1997; 60:1047-1052
18. Gharagozloo P, Lazareno S, Popham A, Birdsall NJM. Allosteric interactions of quaternary strychnine and brucine derivatives with muscarinic acetylcholine receptors. J Med Chem 1999; 42:438-445
19. Ellis J, Seidenberg M Two allosteric modulators interact at a common site on cardiac muscarinic receptors. Mol Pharmacol 1992; 42:638-641
20. Waelbroeck M. Identification of drugs competing with D-tubocurarine for an allosteric site on cardiac muscarinic receptors. Mol Pharmacol 1994; 46:685-692
21. 2 receptors. J Pharmacol Exp Ther 1997; 282:278-285.
22. Ellis J, Huyler J, Brann MR. Allosteric regulation of cloned m1-m5 muscarinic receptor subtypes. Biochem Pharmacol 1991; 42:1927-1932
23. Potter LT, Ferrendelli CA, Hanchett HE, Hollifield MA, Lorenzi MV. Tetrahydroaminoacridine and other allosteric antagonists of hippocampal M1 muscarine receptors. Mol Pharmacol 1989; 35:652-660
24. 2 receptors. Mol Pharmacol 1997; 51:674-682
25. Lazareno S, Popham A, Birdsall NJM. Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-3H]scopolamine and acetylcholine at muscarinic receptor subtypes: Identification of a second allosteric site. Mol Pharmacol 2000; 58:194-207
26. Lazareno S, Popham A, Birdsall NJM. Muscarinic interactions of bisindolylmaleimide analogues. Eur J Pharmacol 1998; 360:281-284
27. Matsui H, Lazareno S, Birdsall NJM. Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis. Mol Pharmacol 1995; 47: 88-98
28. Leppik RA, Miller RC, Eck M, Paquet JL. Role of acidic amino acids in the allosteric modulation by gallamine of antagonist binding at the m2 muscarinic acetylcholine receptor. Mol Pharmacol 1994; 45: 983-990
29. Gnagey AL., Seidenberg 1M, Ellis J. Site-directed mutagenesis reveals two epitopes involved in the subtype selectivity of the allosteric interactions of gallamine at muscarinic acetylcholine receptors Mol Pharmacol 1999; 56:1245-1253.
30. Spalding TA, Burstein ES, Wells JW, Brann MR. Constitutive activation of the m5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6. Biochemistry 1997; 36:10109-10116
31. Hulme EC, Lu Z-L, Curtis CAM, Saldanha J. The conformational switch in muscarinic acetylcholine receptors. Life Sci. 2001; these proceedings
32. Lu Z-L, Curtis CAM, Jones PG, Pavia J, Hulme EC. The role of the aspartate-arginine-tyrosine triad in the m1 muscarinic receptor: Mutations of aspartate 122 and tyrosine 124 decrease receptor expression but do not abolish signaling. Mol. Pharmacol 1997; 51:234-241.