Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library.

doi:10.1073/pnas.1620645114

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Article

Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library.

Proceedings of the National Academy of Sciences of the United States of America - 14 Feb 2017

Ahn Seungkirl, Kahsai Alem W, Pani Biswaranjan, Wang Qin-Ting, Zhao Shuai, Wall Alissa L, Strachan Ryan T, Staus Dean P, Wingler Laura M, Sun Lillian D, Sinnaeve Justine, Choi Minjung, Cho Ted, Xu Thomas T, Hansen Gwenn M, Burnett Michael B, Lamerdin Jane E, Bassoni Daniel L, Gavino Bryant J, Husemoen Gitte, Olsen Eva K, Franch Thomas, Costanzi Stefano, Chen Xin, Lefkowitz Robert J

Abstract excerpt

The β2-adrenergic receptor (β2AR) has been a model system for understanding regulatory mechanisms of G-protein-coupled receptor (GPCR) actions and plays a significant role in cardiovascular and pulmonary diseases. Because all known β-adrenergic receptor drugs target the orthosteric binding site of the receptor, we set out to isolate allosteric ligands for this receptor by panning DNA-encoded small-molecule...

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PMID: 28130548
DOI: 10.1073/pnas.1620645114
PMCID: PMC5321036

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