Mechanistic diversity within RLC-dependent myosin ATPase inhibitors differentiates EDG-7500, a diastolic-selective cardiac sarcomere modulator.

doi:10.1172/jci.insight.203086

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Article

Mechanistic diversity within RLC-dependent myosin ATPase inhibitors differentiates EDG-7500, a diastolic-selective cardiac sarcomere modulator.

JCI insight - 22 Sept 2026

Emter Craig A, Henze Marcus, DuVall Mike, Lehman Sarah, Lee Lindsey, Barthel Ben, Hawryluk Natalie A, Madden Molly, Wu Yangsong, Perry Amy, Beyer Martin, Wei Eric, Rupert Cassady, Roof Steve, Peter Angela, DiNatale Emily, Cantrell Sara, Tolley Jessica, Schlachter Stephen, van der Velden Jolanda, Michels Michelle, Seidman Christine, Ma Weikang, Leinwand Leslie, Campbell Stuart, Ochala Julien, Bluemke David, Tharp Darla, Seidman Jonathan, Del Rio Carlos L, Semigran Marc, Evanchik Marc, Koch Kevin, Russell Alan

Abstract excerpt

Small molecules that modulate myofibril ATPase activity via the myosin regulatory light chain (RLC) display a broad spectrum of activity in their ability to enhance relaxation and slow contraction. EDG-7500 exhibits features consistent with a 'diastolic-selective' cardiac sarcomere modulator (d-CSM), and its ability to treat HCM was explored in engineered human tissue (EHT), human HCM cardiac strips, and an R403Q...

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Topics

Animals
Humans
Sarcomeres

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Swine

Myocardial Contraction

Diastole

Myosin Light Chains

Mutation

Calcium

Cardiomyopathy, Hypertrophic

Myofibrils

Myocardium

Source

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Identifiers

PMID: 42770301
DOI: 10.1172/jci.insight.203086
PMCID: PMC13596718

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