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Article

Highly Selective Y4 Receptor Antagonist Binds in an Allosteric Binding Pocket.

Journal of medicinal chemistry - 11 Mar 2021

Schüß Corinna, Vu Oanh, Schubert Mario, Du Yu, Mishra Nigam M, Tough Iain R, Stichel Jan, Weaver C David, Emmitte Kyle A, Cox Helen M, Meiler Jens, Beck-Sickinger Annette G

Abstract excerpt

Human neuropeptide Y receptors (Y1R, Y2R, Y4R, and Y5R) belong to the superfamily of G protein-coupled receptors and play an important role in the regulation of food intake and energy metabolism. We identified and characterized the first selective Y4R allosteric antagonist (S)-VU0637120, an important step toward validating Y receptors as therapeutic targets for metabolic diseases. To obtain insight into the...

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PMID: 33595306
DOI: 10.1021/acs.jmedchem.0c02000

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