Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis

Journal of Medicinal Chemistry
Rupesh V ChikhaleMange Ram Yadav

Abstract

Decaprenylphosphoryl-β-d-ribose 2'-epimerase (DprE1), a vital enzyme for cell wall synthesis, plays a crucial role in the formation of lipoarabinomannan and arabinogalactan. It was first reported as a druggable target on the basis of inhibitors discovered in high throughput screening of a drug library. Since then, inhibitors with different types of chemical scaffolds have been reported for their activity against this enzyme. Formation of a covalent or noncovalent bond by the interacting ligand with the enzyme causes loss of its catalytic activity which ultimately leads to the death of the mycobacterium. This Perspective describes various DprE1 inhibitors as anti-TB agents reported to date.

References

Nov 1, 1994·The Journal of Infectious Diseases·V KapurJ M Musser
Mar 1, 1997·Antimicrobial Agents and Chemotherapy·A ScorpioY Zhang
Sep 2, 1997·Proceedings of the National Academy of Sciences of the United States of America·S SreevatsanJ M Musser
Mar 5, 1998·The New England Journal of Medicine·S E ValwayI M Onorato
Jul 10, 1998·Biochimica Et Biophysica Acta·D ChipmanJ V Schloss
Feb 17, 1999·Proceedings of the National Academy of Sciences of the United States of America·E J RubinJ J Mekalanos
Apr 21, 1999·Molecular Microbiology·V Deretic, R A Fratti
Aug 17, 2002·Antimicrobial Agents and Chemotherapy·Corinne J HackbarthZhengyu Yuan
Mar 5, 2003·Journal of Molecular Biology·Michael GrollRobert Huber
Mar 27, 2003·Molecular Microbiology·Christopher M SassettiEric J Rubin
May 23, 2003·Antimicrobial Agents and Chemotherapy·Daiva BakonytePetras Stakenas
May 31, 2003·Proceedings of the National Academy of Sciences of the United States of America·Gyanu LamichhaneWilliam R Bishai
Sep 4, 2003·The Journal of Experimental Medicine·Dirk SchnappingerGary K Schoolnik
Sep 4, 2003·The Journal of Experimental Medicine·Martin I VoskuilGary K Schoolnik
Nov 5, 2003·Journal of Bacteriology·Tanya Parish
Nov 5, 2003·Journal of Bacteriology·Dipti SareenNancy A Buchmeier
Feb 10, 2004·Frontiers in Bioscience : a Journal and Virtual Library·Mary Margaret Wade, Ying Zhang
May 17, 2005·Nature Medicine·Ernesto J Muñoz-Elías, John D McKinney
Jun 2, 2005·Proceedings of the National Academy of Sciences of the United States of America·Jyothi RengarajanEric J Rubin
Oct 5, 2005·PLoS Pathogens·M Cristina GutierrezVeronique Vincent
Jun 9, 2006·Trends in Microbiology·Liem Nguyen, Charles J Thompson
Sep 13, 2006·Antimicrobial Agents and Chemotherapy·Jeanette W P TeoKakoli Mukherjee
Dec 13, 2006·Nature Reviews. Drug Discovery·David J PayneDavid L Pompliano
Mar 8, 2007·Nature Medicine·Stefan H E Kaufmann, Shreemanta K Parida
Mar 27, 2007·Cell·Michael N Alekshun, Stuart B Levy
Mar 31, 2007·Nature Methods·Genee Y LeeMina J Bissell

❮ Previous
Next ❯

Citations

Jun 3, 2020·Archiv der Pharmazie·Gautam KumarSanjay M Jachak
Jun 20, 2020·Chemical Biology & Drug Design·Richard M BeteckLesetja J Legoabe
Feb 11, 2021·Organic & Biomolecular Chemistry·Jian FuStéphane P Vincent
Feb 2, 2021·European Journal of Medicinal Chemistry·Phelelisiwe S DubeRichard M Beteck
Apr 11, 2020·Translational Research : the Journal of Laboratory and Clinical Medicine·Gauri S Shetye SanghyunCho
Sep 9, 2020·European Journal of Medicinal Chemistry·Lingfeng LiuChunhua Qiao
Apr 1, 2021·SAR and QSAR in Environmental Research·H VermaO Silakari
Dec 15, 2020·Journal of Medicinal Chemistry·Gautam KumarShobhna Kapoor
Jun 17, 2021·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·Balungile MadikizelaRüdiger W Seidel
Oct 18, 2019·ACS Medicinal Chemistry Letters·Manjunatha M RPravin S Shirude
Dec 1, 2018·Journal of Medicinal Chemistry·Maciej K RogackiPieter Van der Veken
Sep 20, 2021·Drug Discovery Today·Liu YangTingjun Hou
Sep 6, 2019·The Lancet. Respiratory Medicine·Keertan DhedaUNKNOWN Lancet Respiratory Medicine drug-resistant tuberculosis Commission group

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antitubercular Agents

Antitubercular agents are pharmacologic agents for treatment of tuberculosis. Discover the latest research on antitubercular agents here.

Antitubercular Agents (ASM)

Antitubercular agents are pharmacologic agents for treatment of tuberculosis. Discover the latest research on antitubercular agents here.