二芳基喹啉靶向分枝杆菌ATP合酶的c亚基。
Diarylquinolines target subunit c of mycobacterial ATP synthase.
作者信息
Koul Anil, Dendouga Najoua, Vergauwen Karen, Molenberghs Brenda, Vranckx Luc, Willebrords Rudy, Ristic Zorica, Lill Holger, Dorange Ismet, Guillemont Jerome, Bald Dirk, Andries Koen
机构信息
Department of Antimicrobial Research, Tibotec BVBA, Johnson & Johnson, Turnhoutseweg 30, B-2340 Beerse, Belgium.
出版信息
Nat Chem Biol. 2007 Jun;3(6):323-4. doi: 10.1038/nchembio884. Epub 2007 May 13.
The diarylquinoline R207910 (TMC207) is a promising candidate in clinical development for the treatment of tuberculosis. Though R207910-resistant mycobacteria bear mutations in ATP synthase, the compound's precise target is not known. Here we establish by genetic, biochemical and binding assays that the oligomeric subunit c (AtpE) of ATP synthase is the target of R207910. Thus targeting energy metabolism is a new, promising approach for antibacterial drug discovery.
二芳基喹啉R207910（TMC207）是结核病临床治疗中一个很有前景的候选药物。尽管对R207910耐药的分枝杆菌在ATP合酶中存在突变，但该化合物的确切靶点尚不清楚。在此，我们通过遗传学、生物化学和结合分析确定，ATP合酶的寡聚c亚基（AtpE）是R207910的靶点。因此，靶向能量代谢是抗菌药物研发的一种新的、有前景的方法。
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