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Biochem J. 1993 Jul 15;293 ( Pt 2)(Pt 2):321-3. doi: 10.1042/bj2930321.
2
Peptides containing acylated C-terminal gem diamines: novel irreversible inactivators of the cysteine and serine proteinases.
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Synthesis of peptidyl ene diones: selective inactivators of the cysteine proteinases.肽基烯二酮的合成：半胱氨酸蛋白酶的选择性失活剂。
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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
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Synthesis and properties of Cbz-Phe-Arg-CHN2 (benzyloxycarbonylphenylalanylarginyldiazomethane) as a proteinase inhibitor.作为蛋白酶抑制剂的苄氧羰基苯丙氨酰精氨酰重氮甲烷（Cbz-Phe-Arg-CHN2）的合成与性质
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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。
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The synthesis of peptidylfluoromethanes and their properties as inhibitors of serine proteinases and cysteine proteinases.肽基氟甲烷的合成及其作为丝氨酸蛋白酶和半胱氨酸蛋白酶抑制剂的性质。
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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。
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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
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Peptidyl inverse esters of p-methoxybenzoic acid: a novel class of potent inactivator of the serine proteases.对甲氧基苯甲酸的肽基反式酯：一类新型的丝氨酸蛋白酶强效失活剂。
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Cathepsin B, Cathepsin H, and cathepsin L.组织蛋白酶B、组织蛋白酶H和组织蛋白酶L。
Methods Enzymol. 1981;80 Pt C:535-61. doi: 10.1016/s0076-6879(81)80043-2.
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On the size of the active site in proteases. I. Papain.关于蛋白酶活性位点的大小。I. 木瓜蛋白酶。
Biochem Biophys Res Commun. 1967 Apr 20;27(2):157-62. doi: 10.1016/s0006-291x(67)80055-x.
3
Determination of the operational molarity of solutions of bovine alpha-chymotrypsin, trypsin, thrombin and factor Xa by spectrofluorimetric titration.通过荧光光谱滴定法测定牛α-糜蛋白酶、胰蛋白酶、凝血酶和Xa因子溶液的操作摩尔浓度。
Biochem J. 1973 Jan;131(1):107-17. doi: 10.1042/bj1310107.
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Use of peptide aldehydes to generate transition-state analogs of elastase.使用肽醛来生成弹性蛋白酶的过渡态类似物。
Biochemistry. 1973 Jan 2;12(1):47-51. doi: 10.1021/bi00725a009.
5
Aldehydes as inhibitors of papain.醛类作为木瓜蛋白酶的抑制剂。
J Biol Chem. 1972 Dec 25;247(24):8195-7.
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Human cathepsin B1. Purification and some properties of the enzyme.人组织蛋白酶B1。该酶的纯化及某些特性。
Biochem J. 1973 Apr;131(4):809-22. doi: 10.1042/bj1310809.
7
The 1.8 A structure of the complex between chymostatin and Streptomyces griseus protease A. A model for serine protease catalytic tetrahedral intermediates.抑肽酶与灰色链霉菌蛋白酶A复合物的1.8埃结构。丝氨酸蛋白酶催化四面体中间体的模型。
J Mol Biol. 1985 May 5;183(1):89-103. doi: 10.1016/0022-2836(85)90283-9.
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Mechanism of slow-binding inhibition of human leukocyte elastase by trifluoromethyl ketones.
Biochemistry. 1987 May 19;26(10):2682-9. doi: 10.1021/bi00384a005.
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Inhibition of serine proteases by peptidyl fluoromethyl ketones.肽基氟甲基酮对丝氨酸蛋白酶的抑制作用。
Biochemistry. 1986 Jul 1;25(13):3760-7. doi: 10.1021/bi00361a005.
10
The inhibition of human neutrophil elastase and cathepsin G by peptidyl 1,2-dicarbonyl derivatives.肽基1,2 - 二羰基衍生物对人中性粒细胞弹性蛋白酶和组织蛋白酶G的抑制作用
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肽乙二醛：一类新型的丝氨酸和半胱氨酸蛋白酶抑制剂。

Peptide glyoxals: a novel class of inhibitor for serine and cysteine proteinases.

作者信息

Walker B, McCarthy N, Healy A, Ye T, McKervey M A

机构信息

Division of Biochemistry, School of Biology and Biochemistry, Queen's University of Belfast, U.K.

出版信息

Biochem J. 1993 Jul 15;293 ( Pt 2)(Pt 2):321-3. doi: 10.1042/bj2930321.

DOI:10.1042/bj2930321
PMID:8343111
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1134361/
Abstract

A series of novel synthetic dipeptides, containing a C-terminal glyoxal grouping (-COCHO), have been tested as inhibitors against typical members of the serine- and cysteine-proteinase families. For example, the sequences benzyloxycarbonyl (Cbz)-Pro-Phe-CHO (I) and Cbz-Phe-Ala-CHO (II), which fulfil the known primary and secondary specificity requirements of chymotrypsin and cathepsin B respectively, have been found to be potent reversible inhibitors of their respective target proteinase. Thus I was found to inhibit chymotrypsin with a Ki of approximately 0.8 microM, whereas II exhibits a Ki of approximately 80 nm against cathepsin B. These Ki values are some 10-fold and 3-fold lower than those reported for the corresponding peptide-aldehyde inhibitors of chymotrypsin and cathepsin B upon which the peptidyl-glyoxals were fashioned. Unexpectedly, the sequence Cbz-Pro-Ala-CHO, which was designed to inhibit elastase-like proteinases, exhibited no inhibitory activity towards porcine pancreatic elastase, even when used at concentrations as high as 200 microM.

摘要

一系列含有C端乙二醛基团（-COCHO）的新型合成二肽已作为丝氨酸蛋白酶家族和半胱氨酸蛋白酶家族典型成员的抑制剂进行了测试。例如，分别满足胰凝乳蛋白酶和组织蛋白酶B已知一级和二级特异性要求的序列苄氧羰基（Cbz）-Pro-Phe-CHO（I）和Cbz-Phe-Ala-CHO（II），已被发现是其各自靶蛋白酶的有效可逆抑制剂。因此，发现I抑制胰凝乳蛋白酶的Ki约为0.8微摩尔，而II对组织蛋白酶B的Ki约为80纳米。这些Ki值分别比基于其设计的相应胰凝乳蛋白酶和组织蛋白酶B的肽醛抑制剂报道的值低约10倍和3倍。出乎意料的是，设计用于抑制类弹性蛋白酶的序列Cbz-Pro-Ala-CHO，即使在高达200微摩尔的浓度下使用，对猪胰弹性蛋白酶也没有抑制活性。