Diarylquinoline

Diarylquinolines (DARQs) is a chemical class of drugs that treat tuberculosis, e.g. bedaquiline. The drug targets the subunit c of mycobacterial ATP synthase,[1] inhibiting the enzyme so mycobacterium tuberculosis cannot synthesise ATP. This effectively kills the bacteria. As of 2014, the only licensed indication of the drug bedaquiline is in the treatment of multi-drug-resistant tuberculosis, primarily due to concerns about safety.

Although ATP synthase in bacteria is similar to its eukaryotic analogue, diarylquinoline agents are very specific to the bacterial enzyme,[2] so are safe for use in humans and other eukaryotes. This also suggests that ATP synthase inhibition is an attractive therapeutic target[2]

References

  1. ↑ Koul, Anil; Dendouga, Najoua; Vergauwen, Karen; Molenberghs, Brenda; Vranckx, Luc; Willebrords, Rudy; Ristic, Zorica; Lill, Holger; Dorange, Ismet; Guillemont, Jerome; Bald, Dirk; Andries, Koen (2007). "Diarylquinolines target subunit c of mycobacterial ATP synthase". Nature Chemical Biology 3 (6): 323–324. doi:10.1038/nchembio884. ISSN 1552-4450.
  2. 1 2 Haagsma, A. C.; Abdillahi-Ibrahim, R.; Wagner, M. J.; Krab, K.; Vergauwen, K.; Guillemont, J.; Andries, K.; Lill, H.; Koul, A.; Bald, D. (2008). "Selectivity of TMC207 towards Mycobacterial ATP Synthase Compared with That towards the Eukaryotic Homologue". Antimicrobial Agents and Chemotherapy 53 (3): 1290–2. doi:10.1128/AAC.01393-08. PMC 2650532. PMID 19075053.
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