Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

发现利什曼原虫 N-肉豆蔻酰转移酶的高亲和力抑制剂

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Abstract

N-Myristoyltransferase (NMT) is a potential drug target in Leishmania parasites. Scaffold-hopping from published inhibitors yielded the serendipitous discovery of a chemotype selective for Leishmania donovani NMT; development led to high affinity inhibitors with excellent ligand efficiency. The binding mode was characterised by crystallography and provides a structural rationale for selectivity.

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