دورية
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function
| العنوان: | Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function |
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| المؤلفون: | Collibee, Scott E., Bergnes, Gustave, Chuang, Chihyuan, Ashcraft, Luke, Gardina, Jeffrey, Garard, Marc, Jamison, Chris R., Lu, Kevin, Lu, Pu-Ping, Muci, Alexander, Romero, Antonio, Valkevich, Ellen, Wang, Wenyue, Warrington, Jeffrey, Yao, Bing, Durham, Nickie, Hartman, James, Marquez, Anna, Hinken, Aaron, Schaletzky, Julia, Xu, Donghong, Hwee, Darren T., Morgans, David, Malik, Fady I., Morgan, Bradley P. |
| المصدر: | Journal of Medicinal Chemistry; October 2021, Vol. 64 Issue: 20 p14930-14941, 12p |
| مستخلص: | The discovery of reldesemtiv, a second-generation fast skeletal muscle troponin activator (FSTA) that increases force production at submaximal stimulation frequencies, is reported. Property-based optimization of high throughput screening hit 1led to compounds with improved free exposure and in vivomuscle activation potency compared to the first-generation FSTA, tirasemtiv. Reldesemtiv demonstrated increased muscle force generation in a phase 1 clinical trial and is currently being evaluated in clinical trials for the treatment of amyotrophic lateral sclerosis. |
| قاعدة البيانات: | Supplemental Index |
| تدمد: | 00222623 15204804 |
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| DOI: | 10.1021/acs.jmedchem.1c01067 |