Mutation of a highly conserved aspartate residue in the second transmembrane domain of the cannabinoid receptors, CB1 and CB2, disrupts G- protein coupling

Journal of Pharmacology and Experimental Therapeutics

Volumn 285, Issue 2, 1998, Pages 651-658

  Tao, Qing ^a   Abood, Mary E ^a,b  

^a VIRGINIA COMMONWEALTH UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2,3 DIHYDRO 5 METHYL 3 (MORPHOLINOMETHYL) 6 (1 NAPHTHOYL)PYRROLO[1,2,3 DE][1,4]BENZOXAZINE; 4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; ANANDAMIDE; ASPARAGINE; ASPARTIC ACID; CANNABINOID RECEPTOR; CYCLIC AMP; DRONABINOL; GLUTAMIC ACID; GUANINE NUCLEOTIDE BINDING PROTEIN; RIMONABANT;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; CHO CELL; HUMAN; HUMAN CELL; KIDNEY CELL; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; SITE DIRECTED MUTAGENESIS;

ALLOSTERIC REGULATION; ASPARTIC ACID; CELLS, CULTURED; GTP-BINDING PROTEINS; HUMANS; MUTAGENESIS; RECEPTORS, CANNABINOID; RECEPTORS, DRUG; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0031808129     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (34)

1. Abood ME, Ditto KA, Noel MA, Showalter VM and Tao Q (1997) Isolation and expression of mouse CB1 cannabinoid receptor gene: comparison of binding properties with those of native CB1 receptors in mouse brain and N18TG2 neuroblastoma cells. Biochem Pharmacol 53:207-214.
2. Abood ME and Tao Q (1995) Characterization of a delta opioid receptor in rat pheochromocytoma cells. J Pharmacol Exp Ther 274:1566-1573.
3. Adams IB, Ryan W, Singer M, Thomas BF, Compton DR, Razdan RK and Martin BR (1995) Evaluation of cannabinoid receptor binding and in vivo activities for anandamide analogs. J Pharmacol Exp Ther 273:1172-1181.
4. Ceresa BP and Limbird LE (1994) Mutation of an aspartate residue highly conserved among G-protein coupled receptors results in non-reciprocal disruption of α2- adrenergic receptor-G-protein interactions. J Biol Chem 269:29557-29564.
5. Cheng YC and Prusoff WH (1973) Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (IC50) on an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
6. Compton DR, Rice KC, De Costa BR, Razdan RK, Melvin LS, Johnson MR and Martin BR (1993) Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities. J Pharmacol Exp Ther 265:218-226.
7. Costa T, Lang J, Gless C and Herz A (1989) Spontaneous association between opioid receptors and GTP-binding regulatory proteins in native membranes: specific regulation by antagonists and sodium ions. Mol Pharmacol 37:383-394.
8. Devane WA, Dysarz IFA, Johnson MR, Melvin LS and Hewlett AC (1988) Determination and characterization of a cannabinoid receptor in rat brain. Mol Pharmacol 34:605-613.
9. Devane WA, Hanus L, Breuer A, Pertwee RG, Stevenson LA, Griffin G, Gibson D, Mandelbaum A, Etinger A and Mechoulam R (1992) Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 258:1946-1949.
10. Felder CC, Joyce KE, Briley EM, Mansouri J, Mackie K, Blond O, Lai Y, Ma AL and Mitchell RL (1995) Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors. Mol Pharmacol 48:443-450.
11. Gerard CM, Mollereau C, Vassart G and Parmentier M (1991) Molecular cloning of a human cannabinoid receptor which is also expressed in testis. Biochem J 279: 129-134.
12. Herkenham M, Lynn AB, Johnson MR, Melvin LS, de Costa BR and Rice KC (1991) Characterization and localization of cannabinoid receptors in rat brain: A quantitative in vitro autoradiographic study. J Neurosci 11:563-583.
13. Herkenham M, Lynn AB, Little MD, Johnson MR, Melvin LS, DeCosta BR and Rice KC (1990) Cannabinoid receptor localization in the brain. Proc Natl Acad Sci USA 87:1932-1936.
14. Hewlett AC and Fleming RM (1984) Cannabinoid inhibition of adenylate cyclase. Pharmacology of the response in neuroblastoma cell membranes. Mol Pharmacol 26:532-538.
15. Kong H, Raynor K, Yasuda K, Moe ST, Portoghese PS, Bell GI and Reisine T (1993a) A single residue, aspartic acid 95, in the δ-opioid receptor specifies selective high affinity agonist binding. J Biol Chem 268:23055-23058.
16. Kong H, Raynor K, Yasuda K, Bell GI and Reisine T (1993b) Mutation of an Aspartate at Residue 89 in Somatostatin receptor subtype 2 prevents Na+ regulation of agonist binding but does not alter receptor-G protein association. Mol Pharmacol. 44:380-384.
17. Kuster JE, Stevenson JI, Ward SJ, D'Ambra TE and Haycock DA (1993) Aminoal- kylindole binding in rat cerebellum: selective displacement by natural and synthetic cannabinoids. J Pharmacol Exp Ther 264:1352-1363.
18. 2a-adrenergic receptor subtype. Science 273:801-803.
19. Martin BR (1986) Cellular effects of cannabinoids. Pharmacol Rev 38:45-74.
20. Matsuda LA, Lolait SJ, Brownstein MJ, Young AC and Bonner TI (1990) Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature 346:561-564.
21. Munro S, Thomas KL and Abu-Shaar M (1993) Molecular characterization of a peripheral receptor for cannabinoids. Nature 365:61-65.
22. Neve KA, Cox BA, Henningsen RA, Spanoyannis A and Neve RL (1991) Pivotal role for aspartate-80 in the regulation of dopamine D2 receptor affinity for drugs and inhibition of adenylyl cyclase. Mol Pharmacol 39:733-739.
23. Papworth C, Bauer J, Braman J and Wright D (1996) Site-directed mutagenesis in one day with >80% efficiency. Strategies 9:3-4.
24. Rinaldi-Carmona M, Earth F, Heaulme M, Shire D, Calandra B, Congy C, Martinez S, Maruani J, Neliat G, Caput D, Ferrar P, Soubrie P, Breliere JC and Fur GL (1994) SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 350:240-244.
25. Rosenthal HE (1967) A graphic method for the determination and presentation of binding parameters in a complex system. Anal Biochem 20:525-537.
26. Scatchard G (1951) The attractions of proteins for small molecules and ions. Ann N Y Acad Sci 51:670-672.
27. Schatz AR, Lee M, Condie RB, Pulaski JT and Kaminski NE (1997) Cannabinoid receptors CB1 and CB2: a characterization of expression and adenylate cyclase modulation within the immune system. Toxicol Appl Pharmacol 142:278-287.
28. 2A receptor. J Biol Chem 270:16683-16688.
29. Showalter VM, Compton DR, Martin BR and Abood ME (1996) Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): Identification of cannabinoid receptor subtype selective ligands. J Pharmacol Exp Ther 278:989-999.
30. Slipetz DM, O'Neill GP, Favreau L, Dufresne C, Gallant M, Gareau Y, Guay D, Labelle M and Metters KM (1995) Activation of the human peripheral cannabinoid receptor results in inhibition of adenylyl cyclase. Mol Pharmacol 48:352-361.
31. Song Z-H and Bonner TI (1996) A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN55212-2. Mol Pharmacol 49:891-896.
32. Surprenant A, Horstman DA, Akbarali H and Limbird LE (1992) A point mutation of the alpha 2-adrenoceptor that blocks coupling to potassium but not calcium currents. Science 257:977-980.
33. Suryanarayana SD, VonZastrow M and Kobilka BK (1992) Identification of intramo-lecular interactions in adrenergic receptors. J Biol Chem 267:21991-21994.
34. Zhou W, Flanagan C, Ballasteros JA, Konvica K, Davidson JS, Weinstein H, Millar RP and Sealfon SC (1994) A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-releasing hormone receptor. Mol Pharmacol 45:165-170.