Discovery of Plasmodium vivax N-Myristoyltransferase Inhibitors: Screening, Synthesis, and Structural Characterization of their Binding Mode
File(s)
Accepted version
Author(s)
Type
Journal Article
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.
Date Issued
2012-04-12
Date Acceptance
2012-03-22
Citation
Journal of Medicinal Chemistry, 2012, 55 (7), pp.3578-3582
ISSN
0022-2623
Publisher
American Chemical Society
Start Page
3578
End Page
3582
Journal / Book Title
Journal of Medicinal Chemistry
Volume
55
Issue
7
Copyright Statement
This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://dx.doi.org/10.1021/jm300040p
Subjects
Science & Technology
Life Sciences & Biomedicine
Chemistry, Medicinal
Pharmacology & Pharmacy
CHEMISTRY, MEDICINAL
DRUG TARGET
DERIVATIVES
ANTAGONISTS
PARASITES
MALARIA
Publication Status
Published