Mickaël J. Fer, Laurent Le Corre, Nicolas Pietrancosta, Nathalie Evrard-Todeschi , Samir Olatunji, Ahmed Bouhss, Sandrine Calvet-Vitale* and Christine Gravier-Pelletier* Pages 6013 - 6029 ( 17 )
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.
MraY, nucleoside antibiotics, triazoles, molecular modelling, docking, biological evaluations, mutagenesis.
Universite Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Peres 75006 Paris, Universite Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Peres 75006 Paris, Universite Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Peres 75006 Paris, Universite Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Peres 75006 Paris, Institute for Integrative Biology of the Cell (I2BC), CEA, CNRS, Univ Paris-Sud, Universite Paris-Saclay, Gif-sur-Yvette 91198, Institute for Integrative Biology of the Cell (I2BC), CEA, CNRS, Univ Paris-Sud, Universite Paris-Saclay, Gif-sur-Yvette 91198, Universite Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Peres 75006 Paris, Universite Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Peres 75006 Paris