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Crystallographic and SAR analyses reveal the high requirements needed to selectively and potently inhibit SIRT2 deacetylase and decanoylase.晶体学和构效关系分析揭示了选择性且强效抑制SIRT2去乙酰化酶和癸酰化酶所需的高要求。
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2
X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells.X 射线晶体结构指导发现新型选择性、底物模拟的 SIRT2 抑制剂，对非小细胞肺癌细胞具有活性。
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Identification of a novel small molecule that inhibits deacetylase but not defatty-acylase reaction catalysed by SIRT2.鉴定一种新型小分子，该小分子抑制去乙酰化酶，但不抑制 SIRT2 催化的脱脂酰基酶反应。
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Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.具有苯甲酰胺骨架的新型沉默调节蛋白2（SIRT2）抑制剂的设计、合成及构效关系研究
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Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors.新型人源 SIRT2 选择性抑制剂的设计、合成及生物活性研究。
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Mechanism-based inhibitors of SIRT2: structure-activity relationship, X-ray structures, target engagement, regulation of α-tubulin acetylation and inhibition of breast cancer cell migration.基于机制的SIRT2抑制剂：构效关系、X射线晶体结构、靶点结合、α-微管蛋白乙酰化调控及对乳腺癌细胞迁移的抑制作用
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本文引用的文献

1
X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells.X 射线晶体结构指导发现新型选择性、底物模拟的 SIRT2 抑制剂，对非小细胞肺癌细胞具有活性。
Eur J Med Chem. 2018 Jul 15;155:806-823. doi: 10.1016/j.ejmech.2018.06.041. Epub 2018 Jun 19.
2
Identification of a novel small molecule that inhibits deacetylase but not defatty-acylase reaction catalysed by SIRT2.鉴定一种新型小分子，该小分子抑制去乙酰化酶，但不抑制 SIRT2 催化的脱脂酰基酶反应。
Philos Trans R Soc Lond B Biol Sci. 2018 Jun 5;373(1748). doi: 10.1098/rstb.2017.0070.
3
Potent mechanism-based sirtuin-2-selective inhibition by an -generated occupant of the substrate-binding site, "selectivity pocket" and NAD-binding site.基于机制的强效沉默调节蛋白2选择性抑制作用，由底物结合位点、“选择性口袋”和烟酰胺腺嘌呤二核苷酸结合位点的生成占据者介导。
Chem Sci. 2017 Sep 1;8(9):6400-6408. doi: 10.1039/c7sc02738a. Epub 2017 Jul 21.
4
Structure-based discovery of new selective small-molecule sirtuin 5 inhibitors.基于结构的新型选择性小分子 SIRT5 抑制剂的发现。
Chem Biol Drug Des. 2018 Jan;91(1):257-268. doi: 10.1111/cbdd.13077. Epub 2017 Aug 18.
5
SIRT2 and glycolytic enzyme acetylation in pluripotent stem cells.多能干细胞中的 SIRT2 和糖酵解酶乙酰化。
Nat Cell Biol. 2017 Apr 27;19(5):412-414. doi: 10.1038/ncb3522.
6
Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as new potent and selective human sirtuin 2 inhibitors.发现 2-((4,6-二甲基嘧啶-2-基)硫代)-N-苯基乙酰胺衍生物作为新型强效和选择性的人 SIRT2 抑制剂。
Eur J Med Chem. 2017 Jul 7;134:230-241. doi: 10.1016/j.ejmech.2017.04.010. Epub 2017 Apr 12.
7
The mechanism of sirtuin 2-mediated exacerbation of alpha-synuclein toxicity in models of Parkinson disease.在帕金森病模型中，沉默调节蛋白2介导α-突触核蛋白毒性加剧的机制。
PLoS Biol. 2017 Mar 3;15(3):e2000374. doi: 10.1371/journal.pbio.2000374. eCollection 2017 Mar.
8
Development of 1,2,4-Oxadiazoles as Potent and Selective Inhibitors of the Human Deacetylase Sirtuin 2: Structure-Activity Relationship, X-ray Crystal Structure, and Anticancer Activity.1,2,4-恶二唑类化合物作为人去乙酰化酶Sirtuin 2的强效选择性抑制剂的研发：构效关系、X射线晶体结构及抗癌活性
J Med Chem. 2017 Mar 23;60(6):2344-2360. doi: 10.1021/acs.jmedchem.6b01609. Epub 2017 Mar 14.
9
Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket.基于噻吩并嘧啶酮的Sirtuin-2（SIRT2）选择性抑制剂结合于配体诱导的选择性口袋中。
J Med Chem. 2017 Mar 9;60(5):1928-1945. doi: 10.1021/acs.jmedchem.6b01690. Epub 2017 Feb 15.
10
Sirtuin 5: a review of structure, known inhibitors and clues for developing new inhibitors.Sirtuin 5：结构综述、已知抑制剂及开发新型抑制剂的线索。
Sci China Life Sci. 2017 Mar;60(3):249-256. doi: 10.1007/s11427-016-0060-7. Epub 2016 Nov 17.

晶体学和构效关系分析揭示了选择性且强效抑制SIRT2去乙酰化酶和癸酰化酶所需的高要求。

Crystallographic and SAR analyses reveal the high requirements needed to selectively and potently inhibit SIRT2 deacetylase and decanoylase.

作者信息

Yang Ling-Ling, Xu Wei, Yan Jie, Su Hui-Lin, Yuan Chen, Li Chao, Zhang Xing, Yu Zhu-Jun, Yan Yu-Hang, Yu Yamei, Chen Qiang, Wang Zhouyu, Li Lin, Qian Shan, Li Guo-Bo

机构信息

College of Food and Bioengineering , Xihua University , Sichuan 610039 , China . Email:

Key Laboratory of Drug Targeting and Drug Delivery System of Ministry of Education , Department of Medicinal Chemistry , West China School of Pharmacy , Sichuan University , Chengdu 610041 , China . Email:

出版信息

Medchemcomm. 2018 Dec 7;10(1):164-168. doi: 10.1039/c8md00462e. eCollection 2019 Jan 1.

DOI:10.1039/c8md00462e
PMID:30774863
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6350764/
Abstract

A high-quality X-ray crystal structure reveals the mechanism of compound inhibiting SIRT2 deacetylase and decanoylase. Structure-activity relationship (SAR) analysis of the synthesized derivatives of reveals the high requirements needed for selective inhibitors to bind with the induced hydrophobic pocket and potently inhibit sirtuin 2 deacetylase.

摘要

高质量的X射线晶体结构揭示了化合物抑制SIRT2脱乙酰酶和癸酰化酶的机制。对该化合物合成衍生物的构效关系（SAR）分析表明，选择性抑制剂与诱导产生的疏水口袋结合并有效抑制沉默调节蛋白2脱乙酰酶需要满足很高的条件。