Article

An Activator Locks Kv7.1 Channels Open by Electro-Mechanical Uncoupling and Allosterically Modulates its Pore

2021-02-11

Abstract excerpt

Loss-of-function mutations in K v 7.1 often lead to long QT syndrome (LQTS), a cardiac repolarization disorder associated with increased risk of arrhythmia and subsequent sudden cardiac death. The discovery of agonistic I Ks modulators may offer a new potential strategy in pharmacological treatment of this disorder. The benzodiazepine ( R )-L3 potently activates K v 7.1 channels and shortens action potential...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 18a3767d-f9f0-569a-b8eb-b72526e16da5
DOI: 10.1101/2021.02.11.430741

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

An Activator Locks Kv7.1 Channels Open by Electro-Mechanical Uncoupling and Allosterically Modulates its PoreDOI 10.1101/2021.02.11.430741Read

A benzodiazepine activator locks Kv7.1 channels open by electro-mechanical uncoupling.Semantic proximity Read

Pharmacological activation of normal and arrhythmia-associated mutant KCNQ1 potassium channels.Semantic proximity Read

Molecular determinants of KCNQ1 channel block by a benzodiazepine.Semantic proximity Read

A generic binding pocket for small molecule <i> I <sub>Ks</sub> </i> activators at the extracellular inter-subunit interface of KCNQ1 and KCNE1 channel complexesSemantic proximity Read

Molecular simulations reveal a mechanism for enhanced allosteric coupling between voltage-sensor and pore domains in KCNQ1 explaining its activation by ML277Semantic proximity Read

Site and Mechanism of ML252 Inhibition of Kv7 Voltage-Gated Potassium Channels.Semantic proximity Read

Kinetic model for NS1643 drug activation of WT and L529I variants of Kv11.1 (hERG1) potassium channel.Semantic proximity Read

ML277 specifically enhances pore opening of KCNQ1 with VSD at the activated state by modulating VSD-pore couplingSemantic proximity Read

KCNQ-Encoded Potassium Channels as Therapeutic Targets.Semantic proximity Read

Functional screen for subtype specificity of voltage sensor-targeted Kv7 potentiators.Semantic proximity Read

Stereoselectivity and functional plasticity of a common ligand-binding pocket in TRPM3Semantic proximity Read

Structural basis for pharmacological modulation of the TRPC6 channel.Semantic proximity Read