Role of the highly conserved Asp-Arg-Tyr motif in signal transduction of the CB2 cannabinoid receptor |
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Authors: | Rhee M H Nevo I Levy R Vogel Z |
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Institution: | Department of Neurobiology, The Weizmann Institute of Science, Rehovot, Israel. |
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Abstract: | 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 study the role of this motif in CB2 signaling. D mutations (DRY130-132AAA and D130A) markedly reduced binding of cannabinoid agonists, while no significant reduction was observed with R131A or Y132A. Mutating R (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. |
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