000201082 001__ 201082
000201082 005__ 20181203023556.0
000201082 022__ $$a1381-6128
000201082 02470 $$2ISI$$a000338509300006
000201082 037__ $$aARTICLE
000201082 245__ $$aDprE1-from the Discovery to the Promising Tuberculosis Drug Target
000201082 260__ $$aSharjah$$bBentham Science Publ Ltd$$c2014
000201082 269__ $$a2014
000201082 300__ $$a25
000201082 336__ $$aJournal Articles
000201082 520__ $$aSeveral groups working in the field of the development of new antituberculosis drugs have recently reported active compounds targeting mycobacterial enzyme DprE1. Along with its counterpart, DprE2, it catalyses a unique epimerization reaction resulting in the synthesis of decaprenylphosphoryl arabinose, the single donor of arabinosyl residues for the build-up of arabinans, fundamental components of the mycobacterial cell wall. This review presents the historical background leading to the discovery of DprE1, focusing on the biochemical and structural characterization of this important emerging target and introducing the molecules acting on DprE1 including the development of the most successful series - the benzothiazinones, currently in late pre-clinical development, which turned to be suicide inhibitors of DprE1.
000201082 6531_ $$aTuberculosis
000201082 6531_ $$adrug target
000201082 6531_ $$aDprE1
000201082 6531_ $$astructure
000201082 6531_ $$ainhibitors
000201082 6531_ $$aSAR
000201082 6531_ $$abenzothiazinones
000201082 700__ $$aMikusova, Katarina$$uComenius Univ, Fac Nat Sci, Dept Biochem, Bratislava 84215, Slovakia
000201082 700__ $$aMakarov, Vadim$$uRAS, AN Bakh Biochem Inst, Moscow 119071, Russia
000201082 700__ $$0242076$$aNeres, Joao$$g196878
000201082 773__ $$j20$$k27$$q4379-4403$$tCurrent Pharmaceutical Design
000201082 909C0 $$0252302$$pUPCOL$$xU11742
000201082 909CO $$ooai:infoscience.tind.io:201082$$pSV$$particle
000201082 917Z8 $$x217823
000201082 937__ $$aEPFL-ARTICLE-201082
000201082 973__ $$aEPFL$$rREVIEWED$$sPUBLISHED
000201082 980__ $$aARTICLE