PDBsum entry 4c7h

Transferase

PDB id: 4c7h

Contents

Protein chain

411 a.a.

Ligands

EN5

COA-MYA-ENF

DMS ×2

Metals

_MG

Waters ×540

References listed in PDB file

Key reference

• Title: Peptidomimetic inhibitors of n-Myristoyltransferase from human malaria and leishmaniasis parasites.
• Authors: T.O.Olaleye, J.A.Brannigan, S.M.Roberts, R.J.Leatherbarrow, A.J.Wilkinson, E.W.Tate.
• Ref.: Org Biomol Chem, 2014, 12, 8132-8137. [DOI no: 10.1039/c4ob01669f]
• PubMed id: 25230674

Abstract

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.