A Preclinical Candidate Targeting Mycobacterium tuberculosis KasA

Published Mycobacterium tuberculosis β-ketoacyl-ACP synthase KasA inhibitors lack sufficient potency and/or pharmacokinetic properties. A structure-based approach was used to optimize existing KasA inhibitor DG167. This afforded indazole JSF-3285 with a 30-fold increase in mouse plasma exposure. Bio...

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Vydáno v:Cell Chem Biol
Hlavní autoři: Inoyama, Daigo, Awasthi, Divya, Capodagli, Glenn C., Tsotetsi, Kholiswa, Sukheja, Paridhi, Zimmerman, Matthew, Li, Shao-Gang, Jadhav, Ravindra, Russo, Riccardo, Wang, Xin, Grady, Courtney, Richmann, Todd, Shrestha, Riju, Li, Liping, Ahn, Yong-Mo, Liang, Hsin Pin Ho, Mina, Marizel, Park, Steven, Perlin, David S., Connell, Nancy, Dartois, Véronique, Alland, David, Neiditch, Matthew B., Kumar, Pradeep, Freundlich, Joel S.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2020
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Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC7245553/
https://ncbi.nlm.nih.gov/pubmed/32197094
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.chembiol.2020.02.007
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