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癸异戊二烯基磷酸核糖2'-表异构酶(DprE1):抗结核药物研发的挑战性靶点。

Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1): challenging target for antitubercular drug discovery.

作者信息

Gawad Jineetkumar, Bonde Chandrakant

机构信息

Department of Pharmaceutical Chemistry, SVKM's NMIMS School of Pharmacy & Technology Management, Shirpur Dist, Dhule, Maharashtra, 425 405, India.

出版信息

Chem Cent J. 2018 Jun 23;12(1):72. doi: 10.1186/s13065-018-0441-2.

Abstract

Tuberculosis has proved harmful to the entire history of mankind from past several decades. Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1) is a recent target which was identified in 2009 but unfortunately it is neither explored nor crossed phase II. In past several decades few targets were identified for effective antitubercular drug discovery. Resistance is the major problem for effective antitubercular drug discovery. Arabinose is constituent of mycobacterium cell wall. Biosynthesis of arabinose is FAD dependant two step epimerisation reaction which is catalysed by DprE1 and DprE2 flavoprotein enzymes. The current review is mainly emphases on DprE1 as a perspective challenge for further research.

摘要

在过去几十年里,结核病已被证明对整个人类历史有害。癸异戊二烯基磷酸核糖2'-表异构酶(DprE1)是2009年确定的一个新靶点,但遗憾的是,它既未得到深入研究,也未进入二期试验阶段。在过去几十年里,有效抗结核药物研发的靶点很少。耐药性是有效抗结核药物研发的主要问题。阿拉伯糖是分枝杆菌细胞壁的组成成分。阿拉伯糖的生物合成是一个依赖黄素腺嘌呤二核苷酸(FAD)的两步表异构化反应,由DprE1和DprE2黄素蛋白酶催化。本综述主要强调DprE1作为进一步研究的一个潜在挑战。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/b04553a59202/13065_2018_441_Fig1_HTML.jpg

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