• 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

基于二肽基和三肽基α-酮醛（乙二醛）的蛋白酶体胰凝乳蛋白酶样活性抑制剂。

Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl alpha-keto aldehydes (glyoxals).

作者信息

Lynas J F, Harriott P, Healy A, McKervey M A, Walker B

机构信息

Centre for Peptide and Protein Engineering, School of Biology and Biochemistry, Queen's University Belfast, Northern Ireland, U.K.

出版信息

Bioorg Med Chem Lett. 1998 Feb 17;8(4):373-8. doi: 10.1016/s0960-894x(98)00030-4.

DOI:10.1016/s0960-894x(98)00030-4
PMID:9871688
Abstract

A series of peptidyl alpha-keto aldehydes (glyoxals) have been synthesised as putative inhibitors of the chymotryptic-like activity of proteasome. The most potent peptides, Cbz-Leu-Leu-Tyr-COCHO and Bz-Leu-Leu-Leu-COCHO, function as slow-binding reversible inhibitors, exhibiting final Ki values of approximately 3.0 nM. These are among the lowest values so far reported for (tri)peptide-based aldehyde-related inhibitors.

摘要

一系列肽基α-酮醛（乙二醛）已被合成，作为蛋白酶体类胰凝乳蛋白酶活性的假定抑制剂。最有效的肽，Cbz-Leu-Leu-Tyr-COCHO和Bz-Leu-Leu-Leu-COCHO，作为慢结合可逆抑制剂发挥作用，最终Ki值约为3.0 nM。这些是迄今为止基于（三）肽的醛相关抑制剂报道的最低值之一。

相似文献

1
Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl alpha-keto aldehydes (glyoxals).基于二肽基和三肽基α-酮醛（乙二醛）的蛋白酶体胰凝乳蛋白酶样活性抑制剂。
Bioorg Med Chem Lett. 1998 Feb 17;8(4):373-8. doi: 10.1016/s0960-894x(98)00030-4.
2
Selective inhibition of the chymotrypsin-like activity of the 20S proteasome by 5-methoxy-1-indanone dipeptide benzamides.
Bioorg Med Chem Lett. 1998 Feb 3;8(3):209-14. doi: 10.1016/s0960-894x(98)00015-8.
3
Inhibition of the chymotrypsin-like activity of the pituitary multicatalytic proteinase complex.垂体多催化蛋白酶复合体胰凝乳蛋白酶样活性的抑制作用。
Biochemistry. 1992 Oct 6;31(39):9421-8. doi: 10.1021/bi00154a014.
4
Peptide glyoxals: a novel class of inhibitor for serine and cysteine proteinases.肽乙二醛：一类新型的丝氨酸和半胱氨酸蛋白酶抑制剂。
Biochem J. 1993 Jul 15;293 ( Pt 2)(Pt 2):321-3. doi: 10.1042/bj2930321.
5
Characterization of peptidyl boronic acid inhibitors of mammalian 20 S and 26 S proteasomes and their inhibition of proteasomes in cultured cells.哺乳动物20S和26S蛋白酶体的肽基硼酸抑制剂的表征及其对培养细胞中蛋白酶体的抑制作用。
Biochem J. 2000 Mar 1;346 Pt 2(Pt 2):447-54.
6
Specific inhibition of the chymotrypsin-like activity of the proteasome induces a bipolar morphology in neuroblastoma cells.蛋白酶体胰凝乳蛋白酶样活性的特异性抑制可诱导神经母细胞瘤细胞形成双极形态。
Chem Biol. 1996 Nov;3(11):905-12. doi: 10.1016/s1074-5521(96)90179-9.
7
Alzheimer's disease: correlation of the suppression of beta-amyloid peptide secretion from cultured cells with inhibition of the chymotrypsin-like activity of the proteasome.阿尔茨海默病：培养细胞中β-淀粉样肽分泌的抑制与蛋白酶体胰凝乳蛋白酶样活性的抑制之间的相关性。
J Neurochem. 1999 Jul;73(1):195-204. doi: 10.1046/j.1471-4159.1999.0730195.x.
8
Effects of the combination of a proteasome inhibitor (PSI) and an inhibitor of ubiquitin-ligases (Leu-Ala) on the ultrastructure of human leukemic U937 cells.
Folia Histochem Cytobiol. 2002;40(2):135-6.
9
Kinetic studies of the branched chain amino acid preferring peptidase activity of the 20S proteasome: development of a continuous assay and inhibition by tripeptide aldehydes and clasto-lactacystin beta-lactone.20S蛋白酶体对支链氨基酸偏好性肽酶活性的动力学研究：连续测定法的开发以及三肽醛和裂环乳杆菌素β-内酯的抑制作用
Biochemistry. 1998 May 26;37(21):7792-800. doi: 10.1021/bi980097q.
10
P'-extended alpha-ketoamide inhibitors of proteasome.
Bioorg Med Chem Lett. 1999 Sep 6;9(17):2603-6. doi: 10.1016/s0960-894x(99)00443-6.

引用本文的文献

1
Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors.天然产物骨架作为设计和合成20S人蛋白酶体抑制剂的灵感来源。
RSC Chem Biol. 2020 Dec 1;1(5):305-332. doi: 10.1039/d0cb00111b. Epub 2020 Sep 16.
2
Proteasome inhibitors: an expanding army attacking a unique target.蛋白酶体抑制剂：一支不断壮大的攻击独特靶点的队伍。
Chem Biol. 2012 Jan 27;19(1):99-115. doi: 10.1016/j.chembiol.2012.01.003.
3
Metals in anticancer therapy: copper(II) complexes as inhibitors of the 20S proteasome.金属在抗癌治疗中的作用：铜（II）配合物作为 20S 蛋白酶体的抑制剂。
Eur J Med Chem. 2009 Nov;44(11):4353-61. doi: 10.1016/j.ejmech.2009.05.019. Epub 2009 May 24.
4
Proteasome-mediated effects on amyloid precursor protein processing at the gamma-secretase site.蛋白酶体对γ-分泌酶位点淀粉样前体蛋白加工的影响。
Biochem J. 2005 Jan 15;385(Pt 2):545-50. doi: 10.1042/BJ20041145.
5
A 13C-NMR study of the inhibition of papain by a dipeptide-glyoxal inhibitor.二肽 - 乙二醛抑制剂对木瓜蛋白酶抑制作用的¹³C - 核磁共振研究。
Biochem J. 2002 Sep 15;366(Pt 3):983-7. doi: 10.1042/BJ20020499.
6
Antitrypanosomal activities of proteasome inhibitors.蛋白酶体抑制剂的抗锥虫活性。
Antimicrob Agents Chemother. 2002 Jun;46(6):2038-40. doi: 10.1128/AAC.46.6.2038-2040.2002.
7
13C-NMR study of the inhibition of delta-chymotrypsin by a tripeptide-glyoxal inhibitor.三肽-乙二醛抑制剂对δ-胰凝乳蛋白酶抑制作用的13C核磁共振研究
Biochem J. 2002 Mar 1;362(Pt 2):339-47. doi: 10.1042/0264-6021:3620339.
8
The ubiquitin-proteasome pathway and proteasome inhibitors.泛素-蛋白酶体途径与蛋白酶体抑制剂
Med Res Rev. 2001 Jul;21(4):245-73. doi: 10.1002/med.1009.
9
Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity.环氧莫司汀是一种强效且具选择性的蛋白酶体抑制剂，具有体内抗炎活性。
Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8. doi: 10.1073/pnas.96.18.10403.