Bedaquiline
Antituberculosis / SARS-CoV2 3CLpro inhibitor / Bedaquiline is a clinically useful antituberculosis agent that is active (MIC’s 0.030 to 0.120 µg/mL) against multi-drug resistant strains.1 It interferes with mycobacterial energy metabolism via binding to the oligomeric subunit c (AtpE)2 and subunit 3 of ATP synthase inhibiting ATP production.4 Bedaquiline has recently been found to be an inhibitor (IC50 = 18.7 µM) of the SARS-CoV-2 main protease, 3CLpro.5
Biochemicals & reagents
843663-66-1
TMC207; R207910
1) Andries et al. (2005), A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis; Science, 307 223 2) Koul et al. (2007), Diarylquinolines target subunit c of mycobacterial ATP synthase; Nat. Chem. Biol., 3 323 3) Biukovic et al. (2013), Variations of subunit {varepsilon} of the Mycobacterium tuberculosis F1F0 ATP synthase and a novel model for mechanism of action of the tuberculosis drug TMC207; Antimicrob. Agents Chemother., 57 168 4) Sarathy et al. (2019), Re-Understanding the Mechanisms of Action of the Anti-Mycobacterial Drug Bedaquiline; Antibiotics (Basel), 8 261 5) Ghahremanpour et al. (2020), Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2; ACS Med. Chem. Lett., 11 2526
RT
TARGET: Protease; Cytochrome/MDR -- PATHWAY: Mitochondrial function -- DISEASE AREA: Infectious disease