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Cryo-EM structure of K+-bound hERG channel in the presence of astemizole

ABSTRACT:

SUBMITTER: Naruhiko Adachi

PROVIDER: EMPIAR-10629 | biostudies-other |

REPOSITORIES: biostudies-other

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Cryo-EM Structure of K<sup>+</sup>-Bound hERG Channel Complexed with the Blocker Astemizole.

Asai Tatsuki T Adachi Naruhiko N Moriya Toshio T Oki Hideyuki H Maru Takamitsu T Kawasaki Masato M Suzuki Kano K Chen Sisi S Ishii Ryohei R Yonemori Kazuko K Igaki Shigeru S Yasuda Satoshi S Ogasawara Satoshi S Senda Toshiya T Murata Takeshi T

Structure (London, England : 1993) 20210114 3

The hERG channel is a voltage-gated potassium channel involved in cardiac repolarization. Off-target hERG inhibition by drugs has become a critical issue in the pharmaceutical industry. The three-dimensional structure of the hERG channel was recently reported at 3.8-Å resolution using cryogenic electron microscopy (cryo-EM). However, the drug inhibition mechanism remains unclear because of the scarce structural information regarding the drug- and potassium-bound hERG channels. In this study, we ...[more]

PMID: 33450182

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