Results 1 to 10 of about 26,699 (253)

Aficamten is a small-molecule cardiac myosin inhibitor designed to treat hypertrophic cardiomyopathy [PDF]

Nature Cardiovascular Research
AbstractHypertrophic 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 ...
James J Hartman, Julien Robert-Paganin, Anne Houdusse   +2 more
exaly   +6 more sources

Novel cardiac myosin inhibitor for hypertrophic cardiomyopathy. [PDF]

J Gen Physiol
New RLC-1 small-molecule inhibits actomyosin interactions, reduces contractile force, and speeds up myosin cross-bridge kinetics.
Szczesna-Cordary D.
europepmc   +4 more sources

Pharmacokinetics, disposition, and biotransformation of the cardiac myosin inhibitor aficamten in humans [PDF]

Pharmacology Research & Perspectives
Aficamten, a cardiac myosin inhibitor, is being developed for the treatment of patients with symptomatic hypertrophic cardiomyopathy (HCM). The purpose of this study was to determine the absorption, metabolism, and excretion of aficamten.
Donghong Xu, Punag Divanji, Adrienne Griffith, Rajaa Sukhun, Kathleen Cheplo, Jianlin Li, Polina German   +6 more
doaj   +4 more sources

Mechanisms of a novel regulatory light chain–dependent cardiac myosin inhibitor [PDF]

Journal of General Physiology
Hypertrophic cardiomyopathy (HCM) is a genetic disease of the heart characterized by thickening of the left ventricle (LV), hypercontractility, and impaired relaxation. HCM is caused primarily by heritable mutations in sarcomeric proteins, such as β myosin heavy chain.
Michael Regnier, Farid Moussavi-Harami, Thomas C Irving   +2 more
exaly   +4 more sources

Cardiac Myosin Inhibitors in the Treatment of Hypertrophic Cardiomyopathy: Clinical Trials and Future Challenges

Biomolecules
Hypertrophic cardiomyopathy (HCM) is a prevalent and often underdiagnosed genetic cardiac disorder characterized by left ventricular hypertrophy and, in many cases, dynamic left ventricular outflow tract obstruction (LVOTO).
Arnold Kukowka, Marek Droździk
doaj   +4 more sources

Cardiac myosin inhibitor, CK-586, minimally reduces systolic function and ameliorates obstruction in feline hypertrophic cardiomyopathy [PDF]

Scientific Reports
Hypertrophic cardiomyopathy (HCM) remains the most common cardiomyopathy in humans and cats with few preclinical pharmacologic interventional studies. Small-molecule sarcomere inhibitors are promising novel therapeutics for the management of obstructive ...
Victor N. Rivas, Amanda E. Crofton, Carina E. Jauregui, Jalena R. Wouters, Betty S. Yang, Luke A. Wittenburg, Joanna L. Kaplan, Darren T. Hwee, Anne N. Murphy, Bradley P. Morgan, Fady I. Malik, Samantha P. Harris, Joshua A. Stern   +12 more
doaj   +3 more sources

Discovery of a novel cardiac-specific myosin modulator using artificial intelligence-based virtual screening

Nature Communications, 2023
Direct modulation of cardiac myosin function has emerged as a therapeutic target for both heart disease and heart failure. However, the development of myosin-based therapeutics has been hampered by the lack of targeted in vitro screening assays.
Priyanka Parijat, Seetharamaiah Attili, Zoe Hoare, Michael Shattock, Victor Kenyon, Thomas Kampourakis   +5 more
doaj   +2 more sources

Angiotensin II Facilitates Matrix Metalloproteinase-9-Mediated Myosin Light Chain Kinase Degradation in Pressure Overload-Induced Cardiac Hypertrophy

Cellular Physiology and Biochemistry, 2017
Background/Aims: Angiotensin II (Ang II) has been shown to promote cardiac remodeling during the process of hypertrophy. Myosin light chain kinase (MLCK), a specific kinase for the phosphorylation of myosin light chain 2 (MLC2), plays an important role ...
Shun Wang, Mian Cheng, Zhengqing Hu, Shan Hu, Qiang Zou, Xin Lai, Beilei Liu, Hong Jiang, Congxin Huang, Gang Wu   +9 more
doaj   +2 more sources

Mavacamten Cardiac Myosin Inhibitor: Clinical Applications and Future Perspectives. [PDF]

Cureus
Mavacamten is a first-in-class, selective allosteric inhibitor of cardiac myosin adenosine triphosphatase (ATPase) that has emerged as a novel therapeutic option for patients with symptomatic hypertrophic obstructive cardiomyopathy (HOCM) who remain refractory to conventional therapy, such as beta-blockers and calcium channel blockers.
Ramadan MM, Al-Najjar RA, Abady RS, Obaid HA, Mostafa YA, Al-Obeid MT, Elmahal M.   +6 more
europepmc   +3 more sources

Effects of Aficamten on cardiac contractility in a feline translational model of hypertrophic cardiomyopathy [PDF]

Scientific Reports, 2023
Hypertrophic cardiomyopathy (HCM) is the most prevalent inherited cardiac disease in humans and cats and lacks efficacious pharmacologic interventions in the preclinical phase of disease.
Ashley N. Sharpe, Maureen S. Oldach, Victor N. Rivas, Joanna L. Kaplan, Ashley L. Walker, Samantha L. Kovacs, Darren T. Hwee, Peadar Cremin, Bradley P. Morgan, Fady I. Malik, Samantha P. Harris, Joshua A. Stern   +11 more
doaj   +2 more sources