First small molecular inhibitors of T. brucei dolicholphosphate mannose synthase (DPMS), a validated drug target in African sleeping sickness

…, BL Young, H Denton, DL Hughes, GK Wagner

Index: Smith, Terry K.; Young, Benjamin L.; Denton, Helen; Hughes, David L.; Wagner, Gerd K. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 6 p. 1749 - 1752

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Citation Number: 33

Abstract

Drug-like molecules with activity against Trypanosoma brucei are urgently required as potential therapeutics for the treatment of African sleeping sickness. Starting from known inhibitors of other glycosyltransferases, we have developed the first small molecular inhibitors of dolicholphosphate mannose synthase (DPMS), a mannosyltransferase critically involved in glycoconjugate biosynthesis in T. brucei. We show that these DPMS inhibitors ...