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Drugging the Sarcomere, a Delicate Balance: Position of N-Terminal Charge of the Inhibitor W7

Authors :
Fangze Cai
Thomas Kampourakis
Kieran T. Cockburn
Brian D. Sykes
Source :
ACS Chemical Biology. 17:1495-1504
Publication Year :
2022
Publisher :
American Chemical Society (ACS), 2022.

Abstract

W7 is a sarcomere inhibitor that decreases the calcium sensitivity of force development in cardiac muscle. W7 binds to the interface of the regulatory domain of cardiac troponin C (cNTnC) and the switch region of troponin I (cTnI), decreasing the binding of cTnI to cNTnC, presumably by electrostatic repulsion between the -NH

Details

ISSN :
15548937 and 15548929
Volume :
17
Database :
OpenAIRE
Journal :
ACS Chemical Biology
Accession number :
edsair.doi.dedup.....d7562c78ec1ec47b1b78f23411441dcf