K2P2.1 (TREK-1)–activator complexes reveal a cryptic selectivity filter binding site

Marco Lolicato, Cristina Arrigoni, Takahiro Mori, Yoko Sekioka, Clifford Bryant, Kimberly A. Clark and Daniel L. Minor ()
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Marco Lolicato: Cardiovascular Research Institute, University of California
Cristina Arrigoni: Cardiovascular Research Institute, University of California
Takahiro Mori: Ono Pharmaceutical Co. Ltd
Yoko Sekioka: Ono Pharmaceutical Co. Ltd
Clifford Bryant: Small Molecule Discovery Center, University of California
Kimberly A. Clark: Cardiovascular Research Institute, University of California
Daniel L. Minor: Cardiovascular Research Institute, University of California

Nature, 2017, vol. 547, issue 7663, 364-368

Abstract: Crystal structures of an activated two-pore potassium channel reveal a cryptic binding pocket that binds small-molecule activators that restrict the mobility of the selectivity filter and surrounding structure, stabilizing an active ‘leak-mode’ conformation.

Date: 2017
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DOI: 10.1038/nature22988

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