881689-57-2Relevant academic research and scientific papers
Discovery of Tirasemtiv, the First Direct Fast Skeletal Muscle Troponin Activator
Collibee, Scott E.,Bergnes, Gustave,Muci, Alexander,Browne, William F.,Garard, Marc,Hinken, Aaron C.,Russell, Alan J.,Suehiro, Ion,Hartman, James,Kawas, Raja,Lu, Pu-Ping,Lee, Kenneth H.,Marquez, David,Tomlinson, Matthew,Xu, Donghong,Kennedy, Adam,Hwee, Darren,Schaletzky, Julia,Leung, Kwan,Malik, Fady I.,Morgans, David J.,Morgan, Bradley P.
, p. 354 - 358 (2018)
The identification and optimization of the first activators of fast skeletal muscle are reported. Compound 1 was identified from high-throughput screening (HTS) and subsequently found to improve muscle function via interaction with the troponin complex. Optimization of 1 for potency, metabolic stability, and physical properties led to the discovery of tirasemtiv (25), which has been extensively characterized in clinical trials for the treatment of amyotrophic lateral sclerosis.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
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Page/Page column 47-48, (2008/06/13)
Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.
