An allosteric ligand-binding site in the extracellular cap of K2P channels

Qichao Luo; Liping Chen; Xi Cheng; Yuqin Ma; Xiaona Li; Bing Zhang; Li Li; Shilei Zhang; Fei Guo; Yang Li; Huaiyu Yang

doi:10.1038/s41467-017-00499-3

Nature Communications (Aug 2017)

An allosteric ligand-binding site in the extracellular cap of K2P channels

Qichao Luo,
Liping Chen,
Xi Cheng,
Yuqin Ma,
Xiaona Li,
Bing Zhang,
Li Li,
Shilei Zhang,
Fei Guo,
Yang Li,
Huaiyu Yang

Affiliations

Qichao Luo: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Liping Chen: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Xi Cheng: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Yuqin Ma: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Xiaona Li: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Bing Zhang: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Li Li: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Shilei Zhang: Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases & Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Soochow University
Fei Guo: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Yang Li: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Huaiyu Yang: State Key Laboratory of Drug Research and Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences

DOI: https://doi.org/10.1038/s41467-017-00499-3
Journal volume & issue: Vol. 8, no. 1
pp. 1 – 9

Abstract

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TREKs are members of the two-pore domain potassium (K2P) channels, being important clinical targets. Here the authors identify inhibitors of K2P that bind to an allosteric site located in their extracellular cap, suggesting that it might be a promising drug target for these channels.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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