Bacterial Transferase MraY, a Source of Inspiration towards New Antibiotics

Mickaël Fer 1 Laurent Le Corre 1 Nicolas Pietrancosta 1, 2 Nathalie Evrard-Todeschi 1 Samir Olatunji 3, 4 Ahmed Bouhss 3, 5 Sandrine Calvet-Vitale 1 Christine Gravier-Pelletier 1
1 LCBPT - UMR 8601 - Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques
2 CBMIT - Modélisation et Immunologie pour la Thérapie
3 I2BC - Institut de Biologie Intégrative de la Cellule
4 Trinity College Dublin
5 SABNP - Structure et activité des biomolécules normales et pathologiques
Abstract : The bacterial resistance to antibiotics constitutes more than ever a severe public health problem. The enzymes involved in bacterial peptidoglycan biosynthesis are pertinent targets for developing new antibiotics, notably the MraY transferase that is not targeted by any marketed drug. Many research groups are currently working on the study or the inhibition of this enzyme. After a concise overview of the role, mechanism and inhibition of MraY, the structure-activity relationships of 5'-triazole-containing aminoribosyluridine inhibitors, we previously synthetized, will be presented. The recently published MraY X-ray structures allowed us to achieve a molecular virtual high-throughput screening of commercial databases and our in-house library resulting in the identification of promising compounds for the further development of new antibiotics.
Keywords : MraY biological evaluations docking molecular modelling mutagenesis nucleoside antibiotics triazoles
Document type :
Journal articles
Complete list of metadatas
https://hal-univ-evry.archives-ouvertes.fr/hal-02173143
Contributor : Olek Maciejak <>
Submitted on : Thursday, July 4, 2019 - 11:56:42 AM
Last modification on : Thursday, July 18, 2019 - 2:54:10 PM

Identifiers

Collections

UNIV-EVRY | CEA | CEA-UPSAY | UNIV-PARIS5 | I2BC | CEA-DRF | SABNP | USPC | UNIV-PARIS-SACLAY | JOLIOT

Citation

Mickaël Fer, Laurent Le Corre, Nicolas Pietrancosta, Nathalie Evrard-Todeschi, Samir Olatunji, et al.. Bacterial Transferase MraY, a Source of Inspiration towards New Antibiotics. Current Medicinal Chemistry, Bentham Science Publishers, 2019, 25 (42), pp.6013-6029. ⟨10.2174/0929867325666180330095154⟩. ⟨hal-02173143⟩

Export

BibTeX TEI DC DCterms EndNote

Share

Metrics

Record views

37

Université d'Évry-Val-d'Essonne

Boulevard François Mitterrand
91025 Evry Cedex
www.univ-evry.fr

Les gènes de la connaissance