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Cardiac Myosin Inhibitors: Expanding the Horizon for Hypertrophic Cardiomyopathy Management

Annals of Pharmacotherapy, 2023
Objective: To review the current literature on the efficacy and safety of cardiac myosin inhibitors (CMIs) for the treatment of hypertrophic cardiomyopathy (HCM). Data Sources: A literature search was conducted on PubMed from origin to April 2023, using the search terms “MYK-461,” “mavacamten,” “CK-3773274,” and “aficamten.” Studies were limited to ...
Alyssa Sykuta   +5 more
openaire   +2 more sources

A small-molecule inhibitor of skeletal muscle myosin II

Nature Cell Biology, 2001
We screened a small-molecule library for inhibitors of rabbit muscle myosin II subfragment 1 (S1) actin-stimulated ATPase activity. The best inhibitor, N-benzyl-p-toluene sulphonamide (BTS), an aryl sulphonamide, inhibited the Ca2+-stimulated S1 ATPase, and reversibly blocked gliding motility.
A, Cheung   +6 more
openaire   +2 more sources

2,3-Butanedione monoxime (BDM) as a myosin inhibitor

Journal of Muscle Research & Cell Motility, 2002
2,3-Butanedione monoxime (BDM) is the well-characterized, low-affinity, non-competitive inhibitor of skeletal muscle myosin-II. It has been widely used at millimolar concentrations in cell biological experiments with the assumption that it is an ATPase inhibitor of the myosin superfamily. To determine the usefulness of BDM as a general myosin inhibitor,
openaire   +2 more sources

Aficamten—A Second in Class Cardiac Myosin Inhibitor for Hypertrophic Cardiomyopathy

Cardiology in Review, 2023
Hypertrophic cardiomyopathy is an under-recognized disease with a genetic component that results in abnormal and often asymmetric thickening of the left ventricle in addition to decreased compliance and progressive fibrosis of the myocardium. It further poses significant complications related to dynamic left ventricular outflow obstruction over time in
Jay, Patel   +4 more
openaire   +2 more sources

Myosin Inhibitors

Journal of the American College of Cardiology, 2023
Ajith Nair   +2 more
openaire   +1 more source

Blebbistatin, a Myosin II Inhibitor, Is Photoinactivated by Blue Light

Biochemistry, 2004
Blebbistatin is a small molecule inhibitor discovered in a screen for inhibitors of nonmuscle myosin IIA. Blebbistatin inhibits the actin-activated MgATPase activity and in vitro motility of class II myosins. In cells, it has been shown to inhibit contraction of the cytokinetic ring.
Takeshi, Sakamoto   +4 more
openaire   +2 more sources

Small peptide inhibitors of smooth muscle myosin light chain kinase

Journal of Medicinal Chemistry, 1990
The pentapeptide Ser-Asn-Val-Phe-Ala-OBzl has been identified as the smallest inhibitory peptide of myosin light chain kinase (MLCK) derived from the primary sequence of the light chain phosphorylation site. The specific contributions of individual amino acid side chains and backbone elements of this pentapeptide toward the stabilization of the enzyme ...
F C, Gaeta   +5 more
openaire   +2 more sources

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