Critical amino acid residues of the common allosteric site on the M 2 muscarinic acetylcholine receptor: More similarities than differences between the structurally divergent agents gallamine and bis(ammonio)alkane-type hexamethylene-bis-[dimethyl-(3-phthalimidopropyl) ammonium]dibromide

Molecular Pharmacology

Volumn 68, Issue 3, 2005, Pages 769-778

  Huang, Xi Ping ^a   Prilla, Stefanie ^b   Mohr, Klaus ^b   Ellis, John ^a  

^a PENN STATE MILTON S HERSHEY MEDICAL CENTER   (United States)

^b UNIVERSITY OF BONN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

1,6 HEXAMETHYLENEBIS[DIMETHYL(3 PHTHALIMIDOPROPYL)AMMONIUM BROMIDE]; AMINO ACID; ASPARAGINE; GALLAMINE; MUSCARINIC M2 RECEPTOR; MUTANT PROTEIN; THREONINE; TYROSINE;

ALLOSTERISM; AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG COMPETITION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN STRUCTURE; STRUCTURE ANALYSIS;

ALLOSTERIC SITE; AMINO ACID SEQUENCE; GALLAMINE TRIETHIODIDE; HUMANS; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; PHTHALIMIDES; PROTEIN CONFORMATION; RECEPTOR, MUSCARINIC M2; SEQUENCE HOMOLOGY, AMINO ACID; THREONINE; TYROSINE;

EID: 23944472444     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.105.014043     Document Type: Article

References (33)

1. Baba A, Yoshikawa T, Fukuda Y, Sugiyama T, Shimada M, Akaishi M, Tsuchimoto K, Ogawa S, and Fu M (2004) Autoantibodies against M2-muscarinic acetylcholine receptors: new upstream targets in atrial fibrillation in patients with dilated cardiomyopathy. Eur Heart J 25:1108-1115.
2. Birdsall NJ, Lazareno S, Popham A, and Saldanha J (2001) Multiple allosteric sites on muscarinic receptors. Life Sci 68:2517-2524.
3. Buller S, Zlotos DP, Mohr K, and Ellis J (2002) Allosteric site on muscarinic acetylcholine receptors: a single amino acid in transmembrane region 7 is critical to the subtype selectivities of caracurine V derivatives and alkane-bisammonium ligands. Mol Pharmacol 61:160-168.
4. Christopoulos A and Kenakin T (2002) G protein-coupled receptor allosterism and complexing. Pharmacol Rev 54:323-374.
5. Clark AL and Mitchelson F (1976) The inhibitory effect of gallamine on muscarinic receptors. Br J Pharmacol 58:323-331.
6. Ellis J (1997) Allosteric binding sites on muscarinic receptors. Drug Dev Res 40:193-204.
7. Ellis J (2002) Muscarinic receptors, in Understanding G Protein-Coupled Receptors and their Role in the CNS (Davies CH, Pangalos MN eds) pp 349-371, Oxford University Press, Oxford.
8. Ellis J, Huyler J, and Brann MR (1991) Allosteric regulation of cloned m1-m5 muscarinic receptor subtypes. Biochem Pharmacol 42:1927-1932.
9. Ellis J and Seidenberg M (1989) Gallamine exerts biphasic allosteric effects at muscarinic receptors. Mol Pharmacol 35:173-176.
10. Ellis J and Seidenberg M (1992) Two allosteric modulators interact at a common site on cardiac muscarinic receptors. Mol Pharmacol 42:638-641.
11. Ellis J and Seidenberg M (2000) Interactions of alcuronium, TMB-8 and other allosteric ligands with muscarinic acetylcholine receptors: studies with chimeric receptors. Mol Pharmacol 58:1451-1460.
12. Ellis J, Seidenberg M, and Brann MR (1993) Use of chimeric muscarinic receptors to investigate epitopes involved in allosteric interactions. Mol Pharmacol 44:583-588.
13. Ford DJ, Essex A, Spalding TA, Burstein ES, and Ellis J (2002) Homologous mutations near the junction of the sixth transmembrane domain and the third extracellular loop lead to constitutive activity and enhanced agonist affinity at all muscarinic receptor subtypes. J Pharmacol Exp Ther 300:810-817.
14. Gnagey AL, Seidenberg M, and Ellis J (1999) Site-directed mutagenesis reveals two epitopes involved in the subtype selectivity of the allosteric interactions of gallamine at muscarinic acetylcholine receptors. Mol Pharmacol 56:1245-1253.
15. 2 muscarinic cholinoceptor activation by human chagasic autoantibodies: association with bradycardia. Heart 82:273-278.
16. Jakubik J, Krejci A, and Dolezal V (2005) Asparagine, valine and threonine in the third extracellular loop of muscarinic receptor have essential roles in the positive cooperativity of strychnine-like allosteric modulators. J Pharmacol Exp Ther 313:688-696.
17. 3 receptors. Mol Pharmacol 60:761-767.
18. Lazareno S and Birdsall NJ (1995) Detection, quantitation and verification of allosteric interactions of agents with labeled and unlabeled ligands at G proteincoupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors. Mol Pharmacol 48:362-378.
19. Lazareno S, Popham A, and Birdsall NJ (2002) Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors. Mol Pharmacol 62:1492-1505.
20. Lee NH and el-Fakahany EE (1991) Allosteric interactions at the m1, m2 and m3 muscarinic receptor subtypes. J Pharmacol Exp Ther 256:468-479.
21. Leppik RA, Miller RC, Eck M, and Paquet JL (1994) Role of acidic amino acids in the allosteric modulation by gallamine of antagonist binding at the m2 muscarinic acetylcholine receptor. Mol Pharmacol 45:983-990.
22. Liu J, Schoneberg T, van Rhee M, and Wess J (1995) Mutational analysis of the relative orientation of transmembrane helices I and VII in G protein-coupled receptors. J Biol Chem 270:19532-19539.
23. Lullmann H, Ohnesorge FK, Schauwecker GC, and Wassermann O (1969) Inhibition of the actions of carbachol and DFP on guinea pig isolated atria by alkane-bisammonium compounds. Eur J Pharmacol 6:241-247.
24. Matsui H, Lazareno S, and Birdsall NJ (1995) Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis. Mol Pharmacol 47:88-98.
25. Palczewski K, Kumasha T, Hori T, Behnke CS, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, et al. (2000) Crystal structure of rhodopsin: a G-protein-coupled receptor. Science (Wash DC) 289:739-745.
26. Peter JC, Wallukat G, Tugler J, Maurice D, Roegel JC, Briand JP, and Hoebeke J (2004) Modulation of the M2 muscarinic acetylcholine receptor activity with monoclonal anti-M2 receptor antibody fragments. J Biol Chem 279:55697-55706.
27. Potter LT, Ferrendelli CA, Hanchett HE, Hollifield MA, and Lorenzi MV (1989) Tetrahydroaminoacridine and other allosteric antagonists of hippocampal M1 muscarine receptors. Mol Pharmacol 35:652-660.
28. Spalding TA, Burstein ES, Brauner-Osborne H, Hill-Eubanks D, and Brann MR (1995) Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis. J Pharmacol Exp Ther 275:1274-1279.
29. Spalding TA, Burstein ES, Wells JW, and Brann MR (1997) Constitutive activation of the m5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6. Biochemistry 36:10109-10116.
30. Trankle C, Andresen I, Lambrecht G, and Mohr K (1998) M2 receptor binding of the selective antagonist AF-DX 384: possible involvement of the common allosteric site. Mol Pharmacol 53:304-312.
31. Trankle C and Mohr K (1997) Divergent modes of action among cationic allosteric modulators of muscarinic M2 receptors. Mol Pharmacol 51:674-682.
32. 2 receptors. Mol Pharmacol 64:180-190.
33. 5 subtype selectivities of some structurally diverse allosteric ligands in N-methylscopolamine-occupied receptors. Mol Pharmacol 64:21-31.