title: Antituberculars which target decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1: state of art.
abstract: Multidrug resistance is a major barrier in the battle against tuberculosis and still a leading cause of death worldwide. In order to fight this pathogen, two routes are practicable: vaccination or drug treatment. Vaccination against Mycobacterium tuberculosis with the current vaccine Mycobacterium bovis Bacillus Calmette-Guerin is partially successful, being its efficacy variable. A few new tuberculosis vaccines are now in various phases of clinical trials. The emergence of multidrug-resistant strains of M. tuberculosis gave the impulse to discover new effective antitubercular drugs, a few of which are in clinical development. Here we focus on three different classes of very promising antitubercular drugs recently discovered (benzothiazinones, dinitrobenzamides, and benzoquinoxalines) that share the same cellular target: a subunit of the heteromeric decaprenylphosphoryl-β-D: -ribose 2'-epimerase, encoded by the dprE1 (or Rv3790) gene. This enzyme is involved in the biosynthesis of D: -arabinose which is crucial for the synthesis of the mycobacterial cell wall and essential for the pathogen's survival.
authors.affiliation: Dipartimento di Biologia e Biotecnologie Lazzaro Spallanzani, Università degli Studi di Pavia, Via Ferrata 9, Pavia, Italy. silvia.buroni@unipv.it
authors.forename: Silvia
authors.initials: S
authors.lastname: Buroni
authors.forename: Maria Rosalia
authors.initials: MR
authors.lastname: Pasca
authors.forename: Ana Luisa
authors.initials: AL
authors.lastname: de Jesus Lopes Ribeiro
authors.forename: Giulia
authors.initials: G
authors.lastname: Degiacomi
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Molteni
authors.forename: Giovanna
authors.initials: G
authors.lastname: Riccardi
mesh_terms: D000995:Antitubercular Agents / Q000494:pharmacology*; D001089:Arabinose / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D009163:Mycobacterium bovis; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000201:enzymology* / Q000378:metabolism; D010088:Oxidoreductases / Q000037:antagonists & inhibitors*; D011810:Quinoxalines / Q000494:pharmacology; D019998:Racemases and Epimerases / Q000037:antagonists & inhibitors*
chemical_list: D000995:Antitubercular Agents; D004791:Enzyme Inhibitors; D011810:Quinoxalines; C032931:benzoquinoxaline; D001089:Arabinose; D010088:Oxidoreductases; D019998:Racemases and Epimerases