Discovery of Tirasemtiv, the First Direct Fast Skeletal Muscle Troponin Activator. Academic Article uri icon

Overview

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.

publication date

  • February 13, 2018

Identity

PubMed Central ID

  • PMC5900333

Scopus Document Identifier

  • 85045344878

Digital Object Identifier (DOI)

  • 10.1021/acsmedchemlett.7b00546

PubMed ID

  • 29670700

Additional Document Info

volume

  • 9

issue

  • 4