Mh. Rhee et al., Role of the highly conserved Asp-Arg-Tyr motif in signal transduction of the CB2 cannabinoid receptor, FEBS LETTER, 466(2-3), 2000, pp. 300-304
The DRY motif, at the junction of transmembrane helix 3 and intracellular l
oop 2 of G protein-coupled receptors, is highly conserved. Mutations were i
ntroduced into the CB2 cannabinoid receptor to studs the role of this motif
in CB2 signaling, D mutations (DPY130-132AAA and D130A) markedly reduced b
inding of cannabinoid agonists, while no significant reduction was observed
sith R131A or Y132A. Mutating a (R131A) only partially reduced, and mutati
ng Y (Y132A) more efficiently reduced the cannabinoid-induced inhibition of
adenylyl cyclase. Thus, in CB2, D130 is involved in agonist binding, where
as Y seems to have a role in receptor downstream signaling, (C) 2000 Federa
tion of European Biochemical Societies.