Back to search

Article

Structure-based identification and characterisation of novel inhibitors of K <sub>Na</sub> 1.1 potassium channels, a stratified target for <i>KCNT1</i> -related epilepsy

2019-09-26

Abstract excerpt

Several types of drug-resistant epileptic encephalopathies of infancy have been associated with mutations in the KCNT1 gene, which encodes the sodium-activated potassium channel subunit K Na 1.1. These mutations are commonly gain-of-function, increasing channel activity, therefore inhibition by drugs is proposed as a stratified approach to treat disorders. To date, quinidine therapy has been trialled with severa...

Topics

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

Identifiers and source

Literature Corpus work
6fc696a3-f360-54f8-bf2f-1fdc10858bcf
DOI
10.1101/779975
Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest
Interactive article relationship graphSelect a related publication card to move it into the centre and load its closest explainable connections. Solid lines are source-backed structured connections. Dashed lines are semantic discovery signals and are not scientific evidence.
Structure-based identification and characterisation of novel inhibitors of K <sub>Na</sub> 1.1 potassium channels, a stratified target for <i>KCNT1</i> -related epilepsyDOI 10.1101/779975
Targeting KNa1.1 channels in KCNT1-associated epilepsy.Semantic proximity
Large-Scale Structure-Based Virtual Screening Identifies Diverse K <sub>Na</sub> 1.1 (KCNT1) Potassium Channel InhibitorsSemantic proximity
Approaches for the discovery of drugs that target K Na 1.1 channels in KCNT1-associated epilepsy.Semantic proximity
New use for an old drug: quinidine in KCNT1-related epilepsy therapy.Semantic proximity
Identification of new KCNT1-epilepsy drugs by <i>in silico,</i> cell and <i>Drosophila</i> modellingSemantic proximity
Discovery of Potent and Selective Blockers Targeting the Epilepsy-Associated KNa1.1 Channel.Semantic proximity
Structural basis for pore blockade of the human cardiac sodium channel Na <sub>v</sub> 1.5 by tetrodotoxin and quinidineSemantic proximity
CryoEM reveals unprecedented binding site for Na <sub>V</sub> 1.7 inhibitors enabling rational design of potent hybrid inhibitorsSemantic proximity
The Functional Properties, Physiological Roles, Channelopathy and Pharmacological Characteristics of the Slack (KCNT1) Channel.Semantic proximity
A molecular switch in RCK2 triggers sodium-dependent activation of K <sub>Na</sub> 1.1 (KCNT1) potassium channelsSemantic proximity
Epilepsy-causing <i>KCNT1</i> variants increase K <sub>Na</sub> 1.1 channel activity by disrupting the activation gateSemantic proximity
Discovery of the First Orally Available, Selective KNa1.1 Inhibitor: In Vitro and In Vivo Activity of an Oxadiazole SeriesSemantic proximity
Select a neighboring publication to make it the new centre.