Mycobacterium tuberculosis KasA as a drug target: Structure-based inhibitor design

Reshma S. Rudraraju, Samer S. Daher, Ricardo Gallardo-Macias, Xin Wang, Matthew B. Neiditch, Joel S. Freundlich

Research output: Contribution to journalReview articlepeer-review

4 Scopus citations


Recent studies have reported the β-ketoacyl-acyl carrier protein KasA as a druggable target for Mycobacterium tuberculosis. This review summarizes the current status of major classes of KasA inhibitors with an emphasis on significant contributions from structure-based design methods leveraging X-ray crystal structures of KasA alone and in complex with inhibitors. The issues addressed within each inhibitor class are discussed while detailing the characterized interactions with KasA and structure-activity relationships. A critical analysis of these findings should lay the foundation for new KasA inhibitors to study the basic biology of M. tuberculosis and to form the basis of new antitubercular molecules of clinical significance with activity against drug-sensitive and drug-resistant infections.

Original languageEnglish (US)
Article number1008213
JournalFrontiers in Cellular and Infection Microbiology
StatePublished - Sep 15 2022
Externally publishedYes

Bibliographical note

Publisher Copyright:
Copyright © 2022 Rudraraju, Daher, Gallardo-Macias, Wang, Neiditch and Freundlich.


  • KasA
  • medicinal chemistry
  • mycobacterium tuberculosis
  • structure-based drug discovery
  • β-ketoacyl synthase

PubMed: MeSH publication types

  • Journal Article
  • Review
  • Research Support, N.I.H., Extramural


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