Constitutive activation of chimeric m2/m5 muscarinic receptors and delineation of G-protein coupling selectivity domains

Biochemical Pharmacology

Volumn 51, Issue 4, 1996, Pages 539-544

  Burstein, Ethan S ^a   Spalding, Tracy A ^a   Brann, Mark R ^a,b  

^a UNIVERSITY OF VERMONT COLLEGE OF MEDICINE   (United States)

^b ACADIA PHARMACEUTICALS INC   (United States)

Author keywords

chimera; constitutive activity; G protein; receptor; signal transduction; structure function

Indexed keywords

ADENYLATE CYCLASE; ATROPINE; CARBACHOL; CHIMERIC PROTEIN; GUANINE NUCLEOTIDE BINDING PROTEIN; METHYLSCOPOLAMINE; MUSCARINIC AGENT; MUSCARINIC M2 RECEPTOR; MUSCARINIC M5 RECEPTOR; MUSCARINIC RECEPTOR; PHOSPHATIDYLINOSITOL; RADIOLIGAND;

ANIMAL CELL; ARTICLE; CELL LINE; CELL PROLIFERATION; CELL STRAIN 3T3; CELL TRANSFORMATION; CONTROLLED STUDY; GENETIC TRANSFECTION; MOUSE; NONHUMAN; PHOSPHOINOSITIDE METABOLISM; PRIORITY JOURNAL; PROTEIN DOMAIN; RECEPTOR BINDING; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; TURNOVER TIME;

EID: 0030060858     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/0006-2952(95)02234-1     Document Type: Article

References (31)

1. Dohlman HG, Thorner J, Caron MG and Lefkowitz RJ, Model systems for the study of seven-transmembrane-segment receptors. Annu Rev Biochem 60: 653-688, 1991.
2. Brann MR (Ed.), Molecular Biology of G-Protein-Coupled Receptors. Birkhauser, Boston, 1992.
3. Kubo T, Fukuda K, Mikami A, Maeda A, Takahashi H, Mishina M, Haga T, Haga K, Ichiyama A, Kangawa K, Kojima M, Matsuo H, Hirose T and Numa S, Cloning, sequencing and expression of complementary DNA encoding the muscarinic acethylcholine receptor. Nature 323: 411-416, 1986.
4. Peralta EG, Winslow JW, Peterson GL, Smith DH, Ashkenazi A, Ramachandran J, Schimerlink MI and Capon DJ, Primary structure and biochemical properties of an m2 muscarinic receptor. Science 236: 600-605, 1987.
5. Bonner TI, Buckley NJ, Young AC and Brann MR, Identification of a family of muscarinic acetylcholine receptor genes. Science 237: 527-532, 1987.
6. Bonner TI, Young AC, Brann MR and Buckley NJ, Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes. Neuron 1: 403-410, 1988.
7. Jones SVP, Levey AI, Weiner DM, Ellis J, Novotny E, Yu S, Dorje F, Wess J and Brann MR, Muscarinic acetylcholine receptors. In: Molecular Biology of G-Protein-Coupled Receptors (Ed. Brann MR), pp. 170-197. Birkhauser, Boston, 1992.
8. Hulme EC, Birdsall NJM and Buckley NJ, Muscarinic receptor subtypes. Annu Rev Pharmacol Toxicol 30: 633-673, 1990.
9. Johnson GL, Gardner AM, Lange-Carter C, Qian NX, Russell M and Winitz S, How does the G-protein, Gi2, transduce mitogenic signals? J Cell Biochem 54: 415-422, 1994.
10. Burstein ES, Spalding TA, Hill-Eubanks D, and Brann MR, Structure-function of muscarinic receptor coupling to G proteins. Random saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins. J Biol Chem 270: 3141-3146, 1995.
11. q. FEBS Lett 363: 261-263, 1995.
12. Wigler M, Silverstein S, Lee L-S, Pellicer A, Cheng Y-C and Axel R, Transfer of purified herpes virus thymidine kinase gene to cultured mouse cells. Cell 11: 223-232, 1977.
13. Okayama H and Berg P, A cDNA cloning vector that permits expression of cDNA inserts in mammalian cells. Mol Cell Biol 3: 280-289, 1983.
14. Lim K and Chae C-B, A simple assay for DNA transfection by incubation of the cells in culture dishes with substrates for β-galactosidase. Biotechniques 7: 576-579, 1989.
15. Bräuner-Osborne H and Brann MR, Pharmacology of muscarinic acetylcholine receptor subtypes (m1-m5): High throughput assays in mammalian cells. Eur J Pharmacol, in press.
16. Wess J, Gdula D and Brann MR, Site-directed mutagenesis of the m3 muscarinic receptor: Identification of a series of threonine and tyrosine residues involved in agonist but not antagonist binding. EMBO J 10: 3729-3734, 1991.
17. Wess J, Gdula D and Brann MR, Structural basis of the subtype selectivity of muscarinic antagonists: A study with chimeric m2/ m5 muscarinic receptors. Mol Pharmacol 41: 369-374, 1992.
18. Gutkind JS, Novotny EA, Brann MR and Robbins KC, Muscarinic acetylcholine receptor subtypes as agonist-dependent oncogenes. Proc Natl Acad Sci USA 88: 4703-4707, 1991.
19. Spalding TA, Burstein ES, Jørgensen HB, Hill-Eubanks D and Brann MR, Pharmacology of a constitutively activated receptor generated by random mutagenesis. J Pharmacol Exp Ther 275: 1274-1279, 1995.
20. Kubo T, Bujo H, Akiba I, Nakai J, Mishina M and Numa S, Location of a region of the muscarinic acetylcholine receptor involved in selective effector coupling. FEBS Lett 241: 119-125, 1988.
21. Wess J, Brann MR and Bonner TI, Identification of a small intracellular region of the muscarinic m3 receptor as a determinant of selective coupling to PI turnover. FEBS Lett 258: 133-136, 1989.
22. Wess J, Bonner TI and Brann MR, Delineation of muscarinic receptor domains conferring selectivity of coupling to guanine nucleotide-binding proteins and second messengers. Mol Pharmacol 38: 517-523, 1990.
23. Lechleiter J, Helmiss R, Duerson K, Ennulat D, David N, Clapham D and Peralta E, Distinct sequence elements control the specificity of G protein activation by muscarinic acetylcholine receptor subtypes. EMBO J 9: 4381-4390, 1990.
24. Shapiro RA and Nathanson NM, Deletion analysis of the mouse m1 muscarinic acetylcholine receptor: Effects on phosphoinositide metabolism and down-regulation. Biochemistry 28: 8946-8950, 1989.
25. Lameh J, Philip M, Sharma YK, Moro O, Ramachandran J and Sadee W, Hm1 muscarinic cholinergic receptor internalization requires a domain in the third cytoplasmic loop. J Biol Chem 267: 13406-13412, 1992.
26. Arden JR, Nagata O, Shockley MS, Philip M, Lameh J and Sadee W, Mutational analysis of third cytoplasmic loop domains in G-protein coupling of the Hm1 muscarinic receptor. Biochem Biophys Res Commun 188: 1111-1115, 1992.
27. Kunkel MT and Peralta EG, Charged amino acids required for signal transduction by the m3 muscarinic acetylcholine receptor. EMBO J 12: 3809-3815, 1993.
28. s in response to muscarinic agonists. J. Biol Chem 265: 6219-6224, 1990.
29. Wong SKF and Ross EM, Chimeric muscarinic cholinergic: β-adrenergic receptors that are functionally promiscuous among G proteins. J Biol Chem 269: 18968-18976, 1994.
30. Schwartz TW, Locating ligand binding sites in 7TM receptors by protein engineering. Curr Opin Biotechnol 5: 434-444, 1994.
31. 1B-adrenergic receptor by all amino acid substitutions at a single site. J Biol Chem 267: 1430-1433, 1992.