A tale of two inhibitors: diarylquinolines and squaramides

EMBO J. 2023 Aug 1;42(15):e114912. doi: 10.15252/embj.2023114912. Epub 2023 Jul 12.

Abstract

The diarylquinoline bedaquiline (BDQ) is an FDA-approved drug for the treatment of multidrug-resistant tuberculosis that targets the mycobacterial adenosine triphosphate (ATP) synthase, a key enzyme in cellular respiration. In a recent study, Courbon et al (2023) examine the interaction between Mycobacterium smegmatis ATP synthase with the second generation diarylquinoline TBAJ-876 and the squaramide inhibitor SQ31f, showing that both drugs prevent the rotatory motions needed for enzymatic function.

Publication types

  • Comment

MeSH terms

  • Adenosine Triphosphate
  • Antitubercular Agents / pharmacology
  • Antitubercular Agents / therapeutic use
  • Diarylquinolines* / pharmacology
  • Diarylquinolines* / therapeutic use
  • Mycobacterium tuberculosis*

Substances

  • Diarylquinolines
  • Antitubercular Agents
  • squaramide
  • Adenosine Triphosphate