Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 7, Pages 3578-3582Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm300040p
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Funding
- Medical Research Council (MRC) [G0900278, U117532067]
- Wellcome Trust [087792]
- Biotechnology and Biological Sciences Research Council [BB/D02014X/1]
- Biotechnology and Biological Sciences Research Council [BB/D02014X/1] Funding Source: researchfish
- Medical Research Council [MC_U117532067, MC_G1000806, G0900278] Funding Source: researchfish
- BBSRC [BB/D02014X/1] Funding Source: UKRI
- MRC [MC_U117532067, G0900278, MC_G1000806] Funding Source: UKRI
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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.
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