Literature DB >> 22439843

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

Victor Goncalves1, James A Brannigan, David Whalley, Keith H Ansell, Barbara Saxty, Anthony A Holder, Anthony J Wilkinson, Edward W Tate, Robin J Leatherbarrow.   

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.
© 2012 American Chemical Society

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Year:  2012        PMID： 22439843      PMCID： PMC3863987          DOI： 10.1021/jm300040p

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  15 in total

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3.  Association of NMT2 with the acyl-CoA carrier ACBD6 protects the N-myristoyltransferase reaction from palmitoyl-CoA.

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4.  Novel Thienopyrimidine Inhibitors of Leishmania N-Myristoyltransferase with On-Target Activity in Intracellular Amastigotes.

Authors:  Andrew S Bell; Zhiyong Yu; Jennie A Hutton; Megan H Wright; James A Brannigan; Daniel Paape; Shirley M Roberts; Charlotte L Sutherell; Markus Ritzefeld; Anthony J Wilkinson; Deborah F Smith; Robin J Leatherbarrow; Edward W Tate
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Review 7.  Post-translational protein modifications in malaria parasites.

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Journal:  Nat Rev Microbiol       Date:  2015-02-09       Impact factor: 60.633

8.  Validation of N-myristoyltransferase as an antimalarial drug target using an integrated chemical biology approach.

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Journal:  Nat Chem       Date:  2013-12-22       Impact factor: 24.427

9.  Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery.

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Journal:  J Med Chem       Date:  2012-10-15       Impact factor: 7.446

10.  Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase.

Authors:  Mark D Rackham; James A Brannigan; David K Moss; Zhiyong Yu; Anthony J Wilkinson; Anthony A Holder; Edward W Tate; Robin J Leatherbarrow
Journal:  J Med Chem       Date:  2012-12-17       Impact factor: 7.446
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