Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase

Victor Goncalves; James A. Brannigan; Alice Laporte; Andrew S. Bell; Shirley M. Roberts; Anthony J. Wilkinson; Robin J. Leatherbarrow; Edward W. Tate

doi:10.1039/C6MD00531D

Article dans une revue

Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase

Victor Goncalves ^{1, *} James A. Brannigan ² Alice Laporte ¹ Andrew S. Bell ¹ Shirley M. Roberts ² Anthony J. Wilkinson ² Robin J. Leatherbarrow ¹ Edward W. Tate ^{1, *}

* Auteur correspondant

1 Department of Chemistry [Imperial College London]

2 Structural Biology Laboratory, Department of Chemistry, University of York

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).

Keywords : potential-drug target myristoyl-coa selective inhibitors vivax malaria discovery design ligand leishmaniasis falciparum parasites

Type de document :

Article dans une revue

Domaine :

Sciences du Vivant [q-bio] / Biochimie, Biologie Moléculaire

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https://hal-univ-bourgogne.archives-ouvertes.fr/hal-01496799
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Soumis le : lundi 27 mars 2017 - 19:09:17
Dernière modification le : mardi 18 janvier 2022 - 14:26:05

Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase

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Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase

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