Ontology highlight
ABSTRACT:
SUBMITTER: Mercier RW
PROVIDER: S-EPMC3023919 | biostudies-literature | 2010 Oct
REPOSITORIES: biostudies-literature
Mercier Richard W RW Pei Ying Y Pandarinathan Lakshmipathi L Janero David R DR Zhang Jing J Makriyannis Alexandros A
Chemistry & biology 20101001 10
The human cannabinoid 2 GPCR (hCB2) is a prime therapeutic target. To define potential cysteine-related binding motifs critical to hCB2-ligand interaction, a library of hCB2 cysteine-substitution mutants and a novel, high-affinity biarylpyrazole hCB2 antagonist/inverse agonist (AM1336) functionalized to serve as a covalent affinity probe to target cysteine residues within (or in the microenvironment of) its hCB2 binding pocket were generated. The data provide direct experimental demonstration th ...[more]