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

Recent studies have reported the beta-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.

Automated summary

This review summarizes the current research progress on the druggable target KasA in Mycobacterium tuberculosis, focusing on structure-based design methods using X-ray crystal structures. The discussed inhibitor classes and their interactions with KasA provide insights into the development of new KasA inhibitors for studying the basic biology of M. tuberculosis and combating drug-sensitive and drug-resistant infections.