Recent advances in the discovery of N-myristoyltransferase inhibitors.

作者: Can Zhao , Shutao Ma

DOI: 10.1002/CMDC.201402174

关键词:

摘要: N-Myristoyltransferase (NMT) is a cytosolic monomeric enzyme present in eukaryotes such as fungi and protozoa, but not found prokaryotes. The attachment of 14-carbon saturated fatty acid, myristate, from myristoyl-CoA (14:0 CoA) to the N-terminal glycine residue specific set cellular proteins commonly called protein N-myristoylation. myristoylation reaction catalyzed by myristoyl CoA:NMT both necessary for growth various organisms conclusive proliferation. Therefore, NMT has been identified novel promising target antifungal, antiparasitic, anticancer agents, large number potent inhibitors with activities have reported. Herein we describe recent advances discovery inhibitors. We introduce only functions NMT, also some representative natural synthetic inhibitors, focus on their biological activity, selectivity, structure-activity relationship (SAR) information. In particular, inspiration inhibitor structures future direction these compounds are highlighted.

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