Discovery of Tirasemtiv, the First Direct Fast Skeletal Muscle Troponin Activator.
ACS Med Chem Lett
; 9(4): 354-358, 2018 Apr 12.
Article
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| 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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Base de datos:
MEDLINE
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En
Revista:
ACS Med Chem Lett
Año:
2018
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Article
País de afiliación:
Estados Unidos