Effects of D3.49A, R3.50A, and A6.34E mutations on ligand binding and activation of the cannabinoid-2 (CB2) receptor

Biochemical Pharmacology

Volumn 65, Issue 7, 2003, Pages 1077-1085

  Feng, Wenke ^a   Song, Z H ^a  

^a University of Louisville School of Medicine   (United States)

Author keywords

Cannabinoid receptor; G protein coupled receptor; Ligand binding; Marijuana; Signal transduction; Site directed mutagenesis

Indexed keywords

ASPARTYLARGINYLTYROSINE; CANNABINOID 2 RECEPTOR; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; MUTANT PROTEIN; TRIPEPTIDE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DNA TRANSFECTION; EMBRYO; HUMAN; HUMAN CELL; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN MOTIF; SIGNAL TRANSDUCTION; SITE DIRECTED MUTAGENESIS; WILD TYPE;

EID: 0037377593     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(03)00005-4     Document Type: Article

References (35)

1. Gaoni Y., Mechoulam R. Isolation, structure and partial synthesis of an active constituent of hashish. J. Am. Chem. Soc. 86:1964;1646-1647.
2. Matsuda L.A., Lolait S.J., Brownstein M.J., Young A.C., Bonner T.I. Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature. 346:1990;561-564.
3. 2 receptors. Pharmacol. Ther. 74:1997;129-180.
4. 1 cannabinoid receptor in the brain. Neurobiol. Dis. 5:1998;405-416.
5. 2 receptor messenger RNAs during embryonic development in the rat. Neuroscience. 82:1998;1131-1149.
6. Khanolkar A.D., Palmer S.L., Makriyannis A. Molecular probes for the cannabinoid receptors. Chem. Phys. Lipids. 108:2000;37-52.
7. Munro S., Thomas K.L., Abu-Shaar M. Molecular characterization of a peripheral receptor for cannabinoids. Nature. 365:1993;61-65.
8. i in the inhibition of adenylate cyclase by cannabimimetic drugs. Mol. Pharmacol. 29:1986;307-313.
9. Felder C.C., Veluz J.S., Williams H.L., Briley E.M., Matsuda L.A. Cannabinoid agonists stimulate both receptor- and non-receptor-mediated signal transduction pathways in cells transfected with and expressing cannabinoid receptor clones. Mol. Pharmacol. 42:1992;838-845.
10. nY motif and the cysteines in the C-terminal juxtamembrane region of the CB2 cannabinoid receptor. FEBS Lett. 501:2001;166-170.
11. 2-adrenergic receptor: how structure elucidates function. Annu. Rev. Pharmacol. Toxicol. 32:1992;167-183.
12. Strader C.D., Fong T.M., Tota M.R., Underwood D., Dixon R.A. Structure and function of G protein-coupled receptors. Annu. Rev. Biochem. 63:1994;101-132.
13. Garcia D.E., Brown S., Hille B., Mackie K. Protein kinase C disrupts cannabinoid actions by phosphorylation of the CB1 cannabinoid receptor. J. Neurosci. 18:1998;2834-2841.
14. 2 adrenoceptor. EMBO J. 16:1997;6737-6747.
15. Gether U., Kobilka B.K. G protein-coupled receptors. II. Mechanism of agonist activation. J. Biol. Chem. 273:1998;17979-17982.
16. Zhu S.Z., Wang S.Z., Hu J., el Fakahany E.E. An arginine residue conserved in most G protein-coupled receptors is essential for the function of the m1 muscarinic receptor. Mol. Pharmacol. 45:1994;517-523.
17. Oliveira L., Paiva A.C., Sander C., Vriend G. A common step for signal transduction in G protein-coupled receptors. Trends Pharmacol. Sci. 15:1994;170-172.
18. van Rhee A.M., Jacobson K.A. Molecular architecture of G protein-coupled receptors. Drug Dev. Res. 37:1996;1-38.
19. 1B-adrenergic receptor: role of highly conserved polar amino acids in receptor activation. EMBO J. 15:1996;3566-3578.
20. 1B-adrenergic receptor by all amino acid substitutions at a single site. Evidence for a region which constrains receptor activation. J. Biol. Chem. 267:1992;1430-1433.
21. Ballesteros JA, Weinstein HW. Integrated methods for the construction of three-dimensional models and computational probing of structure-function relationships in G-protein coupled receptors. In: Sealfon SC, editor. Methods in neuroscience. San Diego: Academic Press; 1995. p. 366-428.
22. Bramblett R.D., Panu A.M., Ballesteros J.A., Reggio P.H. Construction of a 3D model of the cannabinoid CB1 receptor: determination of helix ends and helix orientation. Life Sci. 56:1995;1971-1982.
23. 2. Mol. Pharmacol. 56:1999;834-840.
24. Chen C., Okayama H. High-efficiency transformation of mammalian cells by plasmid DNA. Mol. Cell Biol. 7:1987;2745-2752.
25. 35S ]thio)triphosphate binding in rat brain membranes Life Sci. 59:1996;659-668.
26. 50) of an enzymatic reaction. Biochem. Pharmacol. 22:1973;3099-3108.
27. Di Marzo V. 'Endocannabinoids' and other fatty acid derivatives with cannabimimetic properties: biochemistry and possible physiopathological relevance. Biochim. Biophys Acta. 392:1998;153-175.
28. Mechoulam R., Fride E., Di Marzo V. Endocannabinoids. Eur. J. Pharmacol. 359:1998;1-18.
29. 2 cannabinoid receptor. FEBS Lett. 466:2000;300-304.
30. Lu Z.-L., Curtis C.A., Jones P.G., Pavia J., Hulme E.C. 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. 51:1997;234-241.
31. 2 adrenergic receptor: constitutive activation, structural instability, and conformational rearrangement of transmembrane segment 6. Mol. Pharmacol. 56:1999;175-184.
32. i protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: implication for intracellular signalization cross-regulation. Mol. Pharmacol. 55:1999;473-480.
33. Portier M., Rinaldi-Carmona M., Pecceu F., Combes T., Poinot-Chazel C., Calandra B., Barth F., le Fur G., Casellas P. SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist. J. Pharmacol. Exp. Ther. 288:1999;582-589.
34. Chiu T.T., Yung L.Y., Wong Y.H. Inverse agonistic effect of ICI-174,864 on the cloned δ-opioid receptor: role of G protein and adenylyl cyclase activation. Mol. Pharmacol. 50:1996;1651-1657.
35. 1b-adrenergic receptor: effects on receptor isomerization and activation. Mol. Pharmacol. 57:2000;219-231.