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Discovery of Tirasemtiv, the First Direct Fast Skeletal Muscle Troponin Activator.

ABSTRACT: 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.

SUBMITTER: Collibee SE 

PROVIDER: S-EPMC5900333 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature

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The identification and optimization of the first activators of fast skeletal muscle are reported. Compound <b>1</b> was identified from high-throughput screening (HTS) and subsequently found to improve muscle function via interaction with the troponin complex. Optimization of <b>1</b> for potency, metabolic stability, and physical properties led to the discovery of tirasemtiv (<b>25</b>), which has been extensively characterized in clinical trials for the treatment of amyotrophic lateral scleros  ...[more]

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