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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.
Afiliação
  • Collibee SE; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Bergnes G; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Muci A; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Browne WF; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Garard M; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Hinken AC; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Russell AJ; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Suehiro I; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Hartman J; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Kawas R; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Lu PP; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Lee KH; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Marquez D; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Tomlinson M; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Xu D; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Kennedy A; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Hwee D; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Schaletzky J; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Leung K; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Malik FI; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Morgans DJ; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
  • Morgan BP; Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080, United States.
ACS Med Chem Lett ; 9(4): 354-358, 2018 Apr 12.
Article em En | MEDLINE | ID: mdl-29670700
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.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2018 Tipo de documento: Article