Article
'Tethering' fragment-based drug discovery to identify inhibitors of the essential respiratory membrane protein type II NADH dehydrogenase.
Bioorganic & medicinal chemistry letters - 15 Jul 2018
Heikal Adam, Nakatani Yoshio, Jiao Wanting, Wilson Chris, Rennison David, Weimar Marion R, Parker Emily J, Brimble Margaret A, Cook Gregory M
Abstract excerpt
Energy generation is a promising area of drug discovery for both bacterial pathogens and parasites. Type II NADH dehydrogenase (NDH-2), a vital respiratory membrane protein, has attracted attention as a target for the development of new antitubercular and antimalarial agents. To date, however, no potent, specific inhibitors have been identified. Here, we performed a site-directed screening technique,...
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