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Recent advances in the discovery of N-myristoyltransferase inhibitors
1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012 (P.R. China), Fax: (+86) 531-88382548.
Abstract:
N-Myristoyltransferase (NMT) is a cytosolic monomeric enzyme present in eukaryotes such as fungi and protozoa, but is not found in prokaryotes. The attachment of a 14-carbon saturated fatty acid, myristate, from myristoyl-CoA (14:0 CoA) to the N-terminal glycine residue in a specific set of cellular proteins is commonly called protein N-myristoylation. The myristoylation reaction catalyzed by the enzyme myristoyl CoA:NMT is both necessary for the growth of various organisms and conclusive for cellular proliferation. Therefore, NMT has been identified as a novel and promising target for antifungal, antiparasitic, and anticancer agents, and a large number of potent NMT inhibitors with antifungal, antiparasitic, and anticancer activities have been reported. Herein we describe recent advances in the discovery of NMT inhibitors. We introduce not only the functions of NMT, but also some representative natural and synthetic inhibitors, with a focus on their biological activity, selectivity, and structure-activity relationship (SAR) information. In particular, inspiration from NMT inhibitor structures and the future direction of these compounds are highlighted.
Insights
N-Myristoyltransferase (NMT) is crucial for cell growth and proliferation. Recent research highlights NMT inhibitors as promising antifungal, antiparasitic, and anticancer agents, focusing on their activity and structure-activity relationships.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Molecular Biology
Background:
- N-Myristoyltransferase (NMT) is a key enzyme in eukaryotes, catalyzing protein N-myristoylation.
- This process involves attaching a myristate fatty acid to N-terminal glycine residues of proteins.
- NMT is essential for organism growth and cellular proliferation, making it a significant drug target.
Purpose of the Study:
- To review recent advancements in the discovery of NMT inhibitors.
- To discuss the functions of NMT and its role in various biological processes.
- To highlight promising natural and synthetic NMT inhibitors, including their biological activity, selectivity, and SAR.
Main Methods:
- Literature review of recent studies on NMT inhibitors.
- Analysis of reported biological activities, selectivity profiles, and structure-activity relationships (SAR).
- Focus on natural and synthetic compounds targeting NMT.
Main Results:
- NMT inhibitors show significant potential as antifungal, antiparasitic, and anticancer agents.
- Various natural and synthetic inhibitors have been identified with potent activities.
- Structure-activity relationship (SAR) studies provide insights for further inhibitor design.
Conclusions:
- NMT is a validated and promising target for developing novel therapeutic agents.
- Continued research into NMT inhibitors, inspired by existing structures, is crucial for future drug discovery.
- Understanding SAR is key to optimizing inhibitor efficacy and selectivity for therapeutic applications.
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