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Functional roles of the tyrosine within the NP(X) n Y motif and the cysteines in the C‐terminal juxtamembrane region of the CB2 cannabinoid receptor
Author(s) -
Feng Wenke,
Song Z.H
Publication year - 2001
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(01)02642-4
Subject(s) - transmembrane domain , cannabinoid receptor type 2 , site directed mutagenesis , receptor , alanine , cannabinoid , g protein coupled receptor , biology , forskolin , tyrosine , chemistry , agonist , biochemistry , microbiology and biotechnology , cannabinoid receptor , amino acid , gene , mutant
In G protein‐coupled receptors, a NP(X) n Y motif in the seventh transmembrane domain and cysteine residues in the C‐terminal juxtamembrane region are conserved. In the current study, the roles of Y299 within the NPVIY motif and C313 and C320 in the C‐terminal juxtamembrane region of the human CB2 cannabinoid receptor were investigated by site‐directed mutagenesis. Replacing Y299 with alanine resulted in a complete loss of ligand binding and a severe impairment of cannabinoid‐induced inhibition of forskolin‐stimulated cAMP accumulation. The C313A and C320A mutations markedly reduced functional coupling to adenylate cyclase, but had no effect on ligand binding and agonist‐induced receptor desensitization.