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Article

Structural implications of hERG K+ channel block by a high-affinity minimally structured blocker.

The Journal of biological chemistry - 4 May 2018

Helliwell Matthew V, Zhang Yihong, El Harchi Aziza, Du Chunyun, Hancox Jules C, Dempsey Christopher E

Abstract excerpt

Cardiac potassium channels encoded by human ether-à-go-go-related gene (hERG) are major targets for structurally diverse drugs associated with acquired long QT syndrome. This study characterized hERG channel inhibition by a minimally structured high-affinity hERG inhibitor, Cavalli-2, composed of three phenyl groups linked by polymethylene spacers around a central amino group, chosen to probe the spatial...

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Source

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Identifiers

PMID: 29545312
DOI: 10.1074/jbc.RA117.000363
PMCID: PMC5936838

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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