期刊
FEBS LETTERS
卷 466, 期 2-3, 页码 300-304出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/S0014-5793(00)01094-2
关键词
cannabinoid CB2 receptor; G protein; site-directed mutagenesis
The DRY motif, at the junction of transmembrane helix 3 and intracellular loop 2 of G protein-coupled receptors, is highly conserved. Mutations were introduced into the CB2 cannabinoid receptor to studs the role of this motif in CB2 signaling, D mutations (DPY130-132AAA and D130A) markedly reduced binding of cannabinoid agonists, while no significant reduction was observed sith R131A or Y132A. Mutating a (R131A) only partially reduced, and mutating Y (Y132A) more efficiently reduced the cannabinoid-induced inhibition of adenylyl cyclase. Thus, in CB2, D130 is involved in agonist binding, whereas Y seems to have a role in receptor downstream signaling, (C) 2000 Federation of European Biochemical Societies.
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