191932-98-6Relevant academic research and scientific papers
Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites
Olaleye, Tayo O.,Brannigan, James A.,Roberts, Shirley M.,Leatherbarrow, Robin J.,Wilkinson, Anthony J.,Tate, Edward W.
, p. 8132 - 8137 (2014)
N-Myristoyltransferase (NMT) has been shown to be essential in Leishmania and subsequently validated as a drug target in Plasmodium. Herein, we discuss the use of antifungal NMT inhibitors as a basis for inhibitor development resulting in the first sub-micromolar peptidomimetic inhibitors of Plasmodium and Leishmania NMTs. High-resolution structures of these inhibitors with Plasmodium and Leishmania NMTs permit a comparative analysis of binding modes, and provide the first crystal structure evidence for a ternary NMT-Coenzyme A/myristoylated peptide product complex. This journal is
