Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 20, Pages 8879-8890Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm301160h
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Funding
- Wellcome Trust [087792]
- Medical Research Council [0900278, U117532067]
- EU F97 project MALSIG [HEALTH-F3-2009-223044]
- Biotechnology and Biological Sciences Research Council [BB/D02014X/1] Funding Source: researchfish
- Medical Research Council [MC_U117532067, G0900278] Funding Source: researchfish
- BBSRC [BB/D02014X/1] Funding Source: UKRI
- MRC [MC_U117532067, G0900278] Funding Source: UKRI
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Design of inhibitors for N-myristoyltransferase (NMT), an enzyme responsible for protein trafficking in Plasmodium falciparum, the most lethal species of parasites that cause malaria, is described. Chemistry-driven optimization of compound 1 from a focused NMT inhibitor library led to the identification of two early lead compounds 4 and 25, which showed good enzyme and cellular potency and excellent selectivity over human NMT. These molecules provide a valuable starting point for further development.
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