A tale of two inhibitors: diarylquinolines and squaramides

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.