Preclinical drug discovery study demonstrates the identification of tirasemtiv for troponin activation in fast skeletal muscle, highlighting potential therapy for amyotrophic lateral sclerosis.
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.
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Collibee et al. (2018) studied this question.
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