Structural insights into TRPV2 activation by small molecules

Ruth A. Pumroy; Anna D. Protopopova; Tabea C. Fricke; Iris U. Lange; Ferdinand M. Haug; Phuong T. Nguyen; Pamela N. Gallo; Bárbara B. Sousa; Gonçalo J. L. Bernardes; Vladimir Yarov-Yarovoy; Andreas Leffler; Vera Y. Moiseenkova-Bell

doi:10.1038/s41467-022-30083-3

Nature Communications (Apr 2022)

Structural insights into TRPV2 activation by small molecules

Ruth A. Pumroy,
Anna D. Protopopova,
Tabea C. Fricke,
Iris U. Lange,
Ferdinand M. Haug,
Phuong T. Nguyen,
Pamela N. Gallo,
Bárbara B. Sousa,
Gonçalo J. L. Bernardes,
Vladimir Yarov-Yarovoy,
Andreas Leffler,
Vera Y. Moiseenkova-Bell

Affiliations

Ruth A. Pumroy: Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania
Anna D. Protopopova: Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania
Tabea C. Fricke: Department of Anesthesiology and Intensive Care Medicine, Hannover Medical School
Iris U. Lange: Department of Anesthesiology and Intensive Care Medicine, Hannover Medical School
Ferdinand M. Haug: Department of Anesthesiology and Intensive Care Medicine, Hannover Medical School
Phuong T. Nguyen: Department of Physiology and Membrane Biology, University of California
Pamela N. Gallo: Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania
Bárbara B. Sousa: Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa
Gonçalo J. L. Bernardes: Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa
Vladimir Yarov-Yarovoy: Department of Physiology and Membrane Biology, University of California
Andreas Leffler: Department of Anesthesiology and Intensive Care Medicine, Hannover Medical School
Vera Y. Moiseenkova-Bell: Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania

DOI: https://doi.org/10.1038/s41467-022-30083-3
Journal volume & issue: Vol. 13, no. 1
pp. 1 – 12

Abstract

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A non-selective calcium channel transient receptor potential vanilloid 2 (TRPV2) is a potential drug target. Here, the authors employ cryo-electron microscopy, in silico docking, and electrophysiology to identify a binding site for an activator 2-aminoethoxydiphenyl borate (2-APB) in this channel.

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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