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

Computer-aided Discovery of Aromatic L-α-Amino Acids as Agonists of the Orphan G Protein-Coupled Receptor GPR139

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Computer-aided Discovery of Aromatic L-α-Amino Acids as Agonists of the Orphan G Protein-Coupled Receptor GPR139

Vignir Isberg et al. J Chem Inf Model. .

Abstract

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-α-amino acids, L-tryptophan and l-phenylalanine were found to have EC50 values of 220 and 320 μM, respectively, making them the first putative endogenous agonists for GPR139.

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