• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

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.

DOI:10.1186/s13065-018-0441-2
PMID:29936616
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6015584/
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/0136/6015584/56d6c71554ac/13065_2018_441_Fig15_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/b04553a59202/13065_2018_441_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/6c6a8acb36dd/13065_2018_441_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/1abfb2a949c5/13065_2018_441_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/b3718ff8a47e/13065_2018_441_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/d91c72c64b2f/13065_2018_441_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/0337ebfbedcd/13065_2018_441_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/932ba7fdc767/13065_2018_441_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/8bace14a61fe/13065_2018_441_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/cfc2039ac54c/13065_2018_441_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/9ba6eb462627/13065_2018_441_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/88b9c72ae880/13065_2018_441_Fig11_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/f8a56a442364/13065_2018_441_Fig12_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/975bfac364b6/13065_2018_441_Fig13_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/70cf87a97bea/13065_2018_441_Fig14_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/56d6c71554ac/13065_2018_441_Fig15_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/b04553a59202/13065_2018_441_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/6c6a8acb36dd/13065_2018_441_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/1abfb2a949c5/13065_2018_441_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/b3718ff8a47e/13065_2018_441_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/d91c72c64b2f/13065_2018_441_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/0337ebfbedcd/13065_2018_441_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/932ba7fdc767/13065_2018_441_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/8bace14a61fe/13065_2018_441_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/cfc2039ac54c/13065_2018_441_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/9ba6eb462627/13065_2018_441_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/88b9c72ae880/13065_2018_441_Fig11_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/f8a56a442364/13065_2018_441_Fig12_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/975bfac364b6/13065_2018_441_Fig13_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/70cf87a97bea/13065_2018_441_Fig14_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0136/6015584/56d6c71554ac/13065_2018_441_Fig15_HTML.jpg

相似文献

1
Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1): challenging target for antitubercular drug discovery.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。
Chem Cent J. 2018 Jun 23;12(1):72. doi: 10.1186/s13065-018-0441-2.
2
Insights into development of Decaprenyl-phosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitors as antitubercular agents: A state of the art review.深入了解去甲二氢愈创木酸磷酸酯β-D-核糖 2'-差向异构酶(DprE1)抑制剂作为抗结核药物的作用机制:最新研究进展综述。
Indian J Tuberc. 2022 Oct;69(4):404-420. doi: 10.1016/j.ijtb.2021.09.003. Epub 2021 Sep 10.
3
Structure-activity relationship mediated molecular insights of DprE1 inhibitors: A Comprehensive Review.DprE1 抑制剂的构效关系介导的分子见解:全面综述。
J Biomol Struct Dyn. 2024 Aug;42(12):6472-6522. doi: 10.1080/07391102.2023.2230312. Epub 2023 Jul 3.
4
Current Affairs, Future Perspectives of Tuberculosis and Antitubercular Agents.结核病及抗结核药物的时事与未来展望
Indian J Tuberc. 2018 Jan;65(1):15-22. doi: 10.1016/j.ijtb.2017.08.011. Epub 2017 Aug 14.
5
Structure based pharmacophore modelling approach for the design of azaindole derivatives as DprE1 inhibitors for tuberculosis.基于结构的药效团建模方法用于设计氮杂吲哚衍生物作为结核分枝杆菌DprE1抑制剂
J Mol Graph Model. 2020 Dec;101:107718. doi: 10.1016/j.jmgm.2020.107718. Epub 2020 Aug 21.
6
Structure, dynamics, and interaction of Mycobacterium tuberculosis (Mtb) DprE1 and DprE2 examined by molecular modeling, simulation, and electrostatic studies.通过分子建模、模拟和静电研究对结核分枝杆菌(Mtb)DprE1和DprE2的结构、动力学及相互作用进行研究。
PLoS One. 2015 Mar 19;10(3):e0119771. doi: 10.1371/journal.pone.0119771. eCollection 2015.
7
Virtual Screening of Small Molecular Inhibitors against DprE1.DprE1 小分子抑制剂的虚拟筛选
Molecules. 2018 Feb 27;23(3):524. doi: 10.3390/molecules23030524.
8
Biosynthesis of D-arabinose in mycobacteria - a novel bacterial pathway with implications for antimycobacterial therapy.分枝杆菌中D-阿拉伯糖的生物合成——一种对抗分枝杆菌治疗有影响的新型细菌途径。
FEBS J. 2008 Jun;275(11):2691-711. doi: 10.1111/j.1742-4658.2008.06395.x. Epub 2008 Apr 15.
9
Functional investigation of the antitubercular drug target Decaprenylphosphoryl-β-D-ribofuranose-2-epimerase DprE1/DprE2 complex.抗结核药物靶点癸异戊烯基磷酸化-β-D-呋喃核糖-2-表异构酶DprE1/DprE2复合物的功能研究
Biochem Biophys Res Commun. 2022 Jun 4;607:49-53. doi: 10.1016/j.bbrc.2022.03.091. Epub 2022 Mar 28.
10
DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization.由于其细胞壁定位,DprE1是一个易受攻击的结核病药物靶点。
ACS Chem Biol. 2015 Jul 17;10(7):1631-6. doi: 10.1021/acschembio.5b00237. Epub 2015 Apr 29.

引用本文的文献

1
Activity of combinations of bactericidal and bacteriostatic compounds in -infected mice: an overview.感染小鼠中杀菌和抑菌化合物组合的活性:综述。
Front Microbiol. 2025 Aug 1;16:1616149. doi: 10.3389/fmicb.2025.1616149. eCollection 2025.
2
Pyrazolopyridine pyrimidone hybrids as potential DprE1 inhibitors, design, synthesis and biological evaluation as antitubercular agents.吡唑并吡啶嘧啶酮杂化物作为潜在的DprE1抑制剂:作为抗结核药物的设计、合成及生物学评价
Sci Rep. 2025 Aug 12;15(1):29586. doi: 10.1038/s41598-025-14734-1.
3
A Computational Approach to Repurposing Natural Products for DprE1 Inhibition.

本文引用的文献

1
Detection of Mycobacteria by Culture and DNA-Based Methods in Animal-Derived Food Products Purchased at Spanish Supermarkets.在西班牙超市购买的动物源性食品中通过培养法和基于DNA的方法检测分枝杆菌
Front Microbiol. 2017 Jun 9;8:1030. doi: 10.3389/fmicb.2017.01030. eCollection 2017.
2
Loss of WDFY3 ameliorates severity of serum transfer-induced arthritis independently of autophagy.WDFY3的缺失可改善血清转移诱导性关节炎的严重程度,且与自噬无关。
Cell Immunol. 2017 Jun;316:61-69. doi: 10.1016/j.cellimm.2017.04.001. Epub 2017 Apr 22.
3
Tuberculosis - drugs in the 2016 development pipeline.
一种将天然产物重新用于抑制DprE1的计算方法。
Scientifica (Cairo). 2025 Jul 9;2025:2105236. doi: 10.1155/sci5/2105236. eCollection 2025.
4
Revolutionizing tuberculosis treatment: Breakthroughs, challenges, and hope on the horizon.变革性的结核病治疗:突破、挑战与未来的希望。
Acta Pharm Sin B. 2025 Mar;15(3):1311-1332. doi: 10.1016/j.apsb.2025.01.023. Epub 2025 Jan 31.
5
Computational approaches: atom-based 3D-QSAR, molecular docking, ADME-Tox, MD simulation and DFT to find novel multi-targeted anti-tubercular agents.计算方法:基于原子的3D-QSAR、分子对接、ADME-Tox、分子动力学模拟和密度泛函理论,以寻找新型多靶点抗结核药物。
BMC Chem. 2025 Feb 13;19(1):39. doi: 10.1186/s13065-024-01357-2.
6
Targeting decaprenylphosphoryl-β-D-ribose 2'-epimerase for Innovative Drug Development Against Mycobacterium Tuberculosis Drug-Resistant Strains.靶向癸异戊烯基磷酸化-β-D-核糖2'-表异构酶用于开发抗结核分枝杆菌耐药菌株的创新药物
Bioinform Biol Insights. 2024 May 28;18:11779322241257039. doi: 10.1177/11779322241257039. eCollection 2024.
7
Synthesis, Activity, Toxicity, and In Silico Studies of New Antimycobacterial -Alkyl Nitrobenzamides.新型抗分枝杆菌α-烷基硝基苯甲酰胺的合成、活性、毒性及计算机模拟研究
Pharmaceuticals (Basel). 2024 May 9;17(5):608. doi: 10.3390/ph17050608.
8
Mycobacterial Targets for Thiourea Derivatives: Opportunities for Virtual Screening in Tuberculosis Drug Discovery.硫脲衍生物的分枝杆菌靶标:结核病药物发现中的虚拟筛选机会。
Curr Med Chem. 2024;31(29):4703-4724. doi: 10.2174/0109298673276076231124104513.
9
Discovery and characterization of antimycobacterial nitro-containing compounds with distinct mechanisms of action and efficacy.发现并鉴定具有不同作用机制和疗效的抗分枝杆菌含硝基化合物。
Antimicrob Agents Chemother. 2023 Sep 19;67(9):e0047423. doi: 10.1128/aac.00474-23. Epub 2023 Aug 23.
10
Mycobacterium tuberculosis DprE1 Inhibitor OPC-167832 Is Active against Mycobacterium abscessus .结核分枝杆菌 DprE1 抑制剂 OPC-167832 对脓肿分枝杆菌有效。
Antimicrob Agents Chemother. 2022 Dec 20;66(12):e0123722. doi: 10.1128/aac.01237-22. Epub 2022 Nov 9.
结核病——2016年处于研发阶段的药物
Nat Rev Dis Primers. 2017 Mar 9;3:17015. doi: 10.1038/nrdp.2017.15.
4
Structural studies of Mycobacterium tuberculosis DprE1 interacting with its inhibitors.结核分枝杆菌DprE1与其抑制剂相互作用的结构研究。
Drug Discov Today. 2017 Mar;22(3):526-533. doi: 10.1016/j.drudis.2016.09.014. Epub 2016 Sep 22.
5
Virtual Screening and X-ray Crystallography Identify Non-Substrate Analog Inhibitors of Flavin-Dependent Thymidylate Synthase.虚拟筛选和X射线晶体学鉴定黄素依赖性胸苷酸合酶的非底物类似物抑制剂。
J Med Chem. 2016 Oct 13;59(19):9269-9275. doi: 10.1021/acs.jmedchem.6b00977. Epub 2016 Sep 29.
6
Therapeutic Potential of the Mycobacterium tuberculosis Mycolic Acid Transporter, MmpL3.结核分枝杆菌分枝菌酸转运蛋白MmpL3的治疗潜力
Antimicrob Agents Chemother. 2016 Aug 22;60(9):5198-207. doi: 10.1128/AAC.00826-16. Print 2016 Sep.
7
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.受BTZ043启发的1,3-苯并噻嗪酮叠氮化物及点击化学产物的设计、合成与抗结核活性
ACS Med Chem Lett. 2016 Jan 4;7(3):266-70. doi: 10.1021/acsmedchemlett.5b00424. eCollection 2016 Mar 10.
8
Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases.某些新型5,6,7,8-四氢吡啶并[4',3':4,5]噻吩并[2,3-d]嘧啶-4(3H)-酮席夫碱的合成、体外抗分枝杆菌评估及对接研究
Bioorg Med Chem Lett. 2016 Feb 1;26(3):836-840. doi: 10.1016/j.bmcl.2015.12.083. Epub 2015 Dec 24.
9
Nitroarenes as Antitubercular Agents: Stereoelectronic Modulation to Mitigate Mutagenicity.作为抗结核药物的硝基芳烃:立体电子调制以减轻致突变性
ChemMedChem. 2016 Feb 4;11(3):331-9. doi: 10.1002/cmdc.201500462. Epub 2016 Jan 11.
10
Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-β-D-ribose 2'-oxidase.作为抗分枝杆菌剂的苯并噻唑的发现:合成、构效关系以及与结核分枝杆菌癸异戊烯基磷酸化-β-D-核糖2'-氧化酶的结合研究
Bioorg Med Chem. 2015 Dec 15;23(24):7694-710. doi: 10.1016/j.bmc.2015.11.017. Epub 2015 Nov 18.