Article
Aficamten is a small-molecule cardiac myosin inhibitor designed to treat hypertrophic cardiomyopathy.
Nature cardiovascular research - 1 Aug 2024
Hartman James J, Hwee Darren T, Robert-Paganin Julien, Chuang Chihyuan, Chin Eva R, Edell Samantha, Lee Ken H, Madhvani Roshni, Paliwal Preeti, Pernier Julien, Sarkar Saswata Sankar, Schaletzky Julia, Schauer Kristine, Taheri Khanha D, Wang Jingying, Wehri Eddie, Wu Yangsong, Houdusse Anne, Morgan Bradley P, Malik Fady I
Abstract excerpt
Hypertrophic cardiomyopathy (HCM) is an inherited disease of the sarcomere resulting in excessive cardiac contractility. The first-in-class cardiac myosin inhibitor, mavacamten, improves symptoms in obstructive HCM. Here we present aficamten, a selective small-molecule inhibitor of cardiac myosin that diminishes ATPase activity by strongly slowing phosphate release, stabilizing a weak actin-binding state. Binding...
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