Computer-aided discovery of aromatic l-Î±-amino acids as agonists of the orphan G protein-coupled receptor GPR139.

J Chem Inf Model. 2014 Jun 23;54(6):1553-7. doi:10.1021/ci500197a. Epub 2014 May 30

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摘要

GPR139 is an orphan G protein-coupled receptor expressed mainly in the central nervous system. We developed a pharmacophore model based on known GPR139 surrogate agonists which led us to propose aromatic-containing dipeptides as potential ligands. Upon testing, the dipeptides demonstrated agonism in the Gq pathway. Next, in testing all 20 proteinogenic l-Î±-amino acids, L-tryptophan and l-phenylalanine were found to have EC50 values of 220 and 320 Î¼M, respectively, making them the first putative endogenous agonists for GPR139.

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Computer-aided discovery of aromatic l-Î±-amino acids as agonists of the orphan G protein-coupled receptor GPR139.

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