Discovery of Plasmodium vivax N-myristoyltransferase inhibitors - Research Database, The University of York

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Discovery of Plasmodium vivax N-myristoyltransferase inhibitors: screening, synthesis, and structural characterization of their binding mode

Research output: Contribution to journal › Article › peer-review

Published copy (DOI)

10.1021/jm300040p

Author(s)

Victor Goncalves
James A Brannigan
David Whalley
Keith H Ansell
Barbara Saxty
Anthony A Holder
Anthony J Wilkinson
Edward W Tate
Robin J Leatherbarrow

Department/unit(s)

Chemistry

Publication details

Journal	JOURNAL OF MEDICINAL CHEMISTRY
Date	Published - 12 Apr 2012
Issue number	7
Volume	55
Number of pages	5
Pages (from-to)	3578-82
Original language	English

Abstract

N-Myristoyltransferase (NMT) is a prospective drug target against parasitic protozoa. Herein we report the successful discovery of a series of Plasmodium vivax NMT inhibitors by high-throughput screening. A high-resolution crystal structure of the hit compound in complex with NMT was obtained, allowing understanding of its novel binding mode. A set of analogues was designed and tested to define the chemical groups relevant for activity and selectivity.

Projects

N-Myristol Transferase as a drug target for anti-malarial therapy
Project: Research project (funded) › Research

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