TB Research

Therapeutic Potential of Coumestan Pks13 Inhibitors for Tuberculosis

Shichun Lun, Shiqi Xiao, Wei Zhang, Shuangshuang Wang, Hendra Gunosewoyo, Li-Fang Yu, William R. Bishai

Antimicrobial Agents and Chemotherapy · 2021-02

Abstract

Polyketide synthase 13 (Pks13) is an important enzyme found in Mycobacterium tuberculosis that condenses two fatty acyl chains to produce α-alkyl β-ketoesters, which in turn serve as the precursors for the synthesis of mycolic acids that are essential building blocks for maintaining the cell wall integrity of M. tuberculosis . Coumestan derivatives have recently been identified in our group as a new chemotype that exerts its antitubercular effects via targeting of Pks13.

MeSH terms

  • Mycobacterium tuberculosis
  • Tuberculosis
  • Bioavailability
  • Pharmacology
  • Cytotoxicity
  • Antibiotics
  • Microbiology
  • Polyketide
  • Drug
  • Pharmacokinetics
  • Drug resistance
  • Chemistry
  • Enzyme
  • Biology