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Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase
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![]() | Accepted version | 6.1 MB | Microsoft Word | View/Open |
![]() | Published version | 1.23 MB | Adobe PDF | View/Open |
Title: | Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase |
Authors: | Goncalves, V Brannigan, JA Laporte, A Bell, AS Roberts, SM Wilkinson, AJ Leatherbarrow, RJ Tate, EW |
Item Type: | Journal Article |
Abstract: | The parasite Plasmodium vivax is the most widely distributed cause of recurring malaria. N-myristoyltransferase (NMT), an enzyme that catalyses the covalent attachment of myristate to the N-terminal glycine of substrate proteins, has been described as a potential target for the treatment of this disease. Herein, we report the synthesis and the structure-guided optimization of a series of quinolines with balanced activity against both Plasmodium vivax and Plasmodium falciparum N-myristoyltransferase (NMT). |
Issue Date: | 11-Nov-2016 |
Date of Acceptance: | 9-Nov-2016 |
URI: | http://hdl.handle.net/10044/1/43036 |
DOI: | https://dx.doi.org/10.1039/C6MD00531D |
ISSN: | 2040-2511 |
Publisher: | Royal Society of Chemistry |
Start Page: | 191 |
End Page: | 197 |
Journal / Book Title: | MedChemComm |
Volume: | 8 |
Copyright Statement: | This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. |
Sponsor/Funder: | Wellcome Trust Medical Research Council (MRC) |
Funder's Grant Number: | 087792/B/08/Z G0900278 |
Keywords: | Science & Technology Life Sciences & Biomedicine Biochemistry & Molecular Biology Chemistry, Medicinal Pharmacology & Pharmacy POTENTIAL-DRUG TARGET MYRISTOYL-COA SELECTIVE INHIBITORS VIVAX MALARIA DISCOVERY DESIGN LIGAND LEISHMANIASIS FALCIPARUM PARASITES 0304 Medicinal And Biomolecular Chemistry 0305 Organic Chemistry 1115 Pharmacology And Pharmaceutical Sciences |
Notes: | crosscheck: This document is CrossCheck deposited related_data: Supplementary Information identifier: Victor Goncalves (ResearcherID) copyright_licence: The Royal Society of Chemistry has an exclusive publication licence for this journal history: Received 20 September 2016; Accepted 9 November 2016; Accepted Manuscript published 11 November 2016; Advance Article published 18 November 2016 |
Publication Status: | Published |
Appears in Collections: | Chemistry Biological and Biophysical Chemistry Faculty of Natural Sciences |