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Diarylquinoline information


Diaryl quinolines (DARQs) are a chemical class of drugs that treat tuberculosis. They target subunit c of mycobacterial ATP synthase,[1] inhibiting the enzyme so mycobacterium tuberculosis cannot synthesise ATP. This effectively kills the bacteria.

Although ATP synthase in bacteria is similar to its eukaryotic analogue, diarylquinoline agents (such as TMC207) are very specific to the bacterial enzyme,[2] so were expected to be safe for use in humans and other eukaryotes. This also suggests that bacterial ATP synthase inhibition is an attractive therapeutic target.[2]

  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. PMID 17496888.
  2. ^ a b 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" (PDF). Antimicrobial Agents and Chemotherapy. 53 (3): 1290–2. doi:10.1128/AAC.01393-08. PMC 2650532. PMID 19075053.

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