Synergistic Lethality of a Binary Inhibitor of <named-content content-type="genus-species">Mycobacterium tuberculosis</named-content> KasA

Synergistic Lethality of a Binary Inhibitor of <named-content content-type="genus-species">Mycobacterium tuberculosis</named-content> KasA

ABSTRACT We report GSK3011724A (DG167) as a binary inhibitor of β-ketoacyl-ACP synthase (KasA) in Mycobacterium tuberculosis. Genetic and biochemical studies established KasA as the primary target. The X-ray crystal structure of the KasA-DG167 complex refined to 2.0-Å resolution revealed two interac...

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Main Authors: Pradeep Kumar, Glenn C. Capodagli, Divya Awasthi, Riju Shrestha, Karishma Maharaja, Paridhi Sukheja, Shao-Gang Li, Daigo Inoyama, Matthew Zimmerman, Hsin Pin Ho Liang, Jansy Sarathy, Marizel Mina, George Rasic, Riccardo Russo, Alexander L. Perryman, Todd Richmann, Aditi Gupta, Eric Singleton, Sheetal Verma, Seema Husain, Patricia Soteropoulos, Zhe Wang, Roxanne Morris, Gene Porter, Gautam Agnihotri, Padmini Salgame, Sean Ekins, Kyu Y. Rhee, Nancy Connell, Véronique Dartois, Matthew B. Neiditch, Joel S. Freundlich, David Alland
Format: article
Language:EN
Published: American Society for Microbiology 2018
Subjects:
antitubercular
DG167
KasA
Mycobacterium tuberculosis
mycolic acid biosynthesis
drug development
Microbiology
QR1-502
Online Access:https://doaj.org/article/8d6c465583e4410c8afdd48c4a9a3287
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https://doaj.org/article/8d6c465583e4410c8afdd48c4a9a3287

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