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不稳定抑制剂对酶的不可逆抑制动力学

Kinetics of irreversible enzyme inhibition by an unstable inhibitor.

作者信息

Rakitzis E T

出版信息

Biochem J. 1974 Aug;141(2):601-3. doi: 10.1042/bj1410601.

DOI:10.1042/bj1410601
PMID:4616685
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1168119/
Abstract

A mathematical treatment for the general case of enzyme inactivation by an inhibitor that breaks down in solution in a first-order reaction is presented. Cathepsin D was inactivated by fluorescein isothiocyanate with a K(i) of 4.47mum. Kinetic constants were also determined for the inactivation of cathepsin D by 1,1-bis(diazoacetyl)-2-phenylethane, and the inactivation of pepsin C by diazoacetyl-dl-norleucine methyl ester.

摘要

本文给出了一种抑制剂在溶液中按一级反应分解时酶失活一般情况的数学处理方法。组织蛋白酶D被异硫氰酸荧光素失活，其抑制常数（K(i)）为4.47μM。还测定了1,1 - 双（重氮乙酰基）- 2 - 苯乙烷使组织蛋白酶D失活以及重氮乙酰 - dl - 正亮氨酸甲酯使胃蛋白酶C失活的动力学常数。

相似文献

1
Kinetics of irreversible enzyme inhibition by an unstable inhibitor.不稳定抑制剂对酶的不可逆抑制动力学
Biochem J. 1974 Aug;141(2):601-3. doi: 10.1042/bj1410601.
2
Inactivation of cathepsin D from human gastric mucosa and from stomach carcinoma by diazoacetyl-DL-norleucine methyl ester.重氮乙酰-DL-正亮氨酸甲酯对人胃黏膜和胃癌组织中组织蛋白酶D的失活作用
Biochem Pharmacol. 1978 Mar 1;27(5):827-9. doi: 10.1016/0006-2952(78)90537-3.
3
Acid proteases. I. Inactivation of Cladosporium acid protease by diazoacetyl-DL-norleucine methyl ester as an active-site-directed irreversible inhibitor.酸性蛋白酶。I. 重氮乙酰-DL-正亮氨酸甲酯作为活性位点导向的不可逆抑制剂对枝孢菌酸性蛋白酶的失活作用。
J Biochem. 1977 Jun;81(6):1739-44. doi: 10.1093/oxfordjournals.jbchem.a131634.
4
The structure and function of acid proteases. V. Comparative studies on the specific inhibition of acid proteases by diazoacetyl-DL-norleucine methyl ester, 1,2-epoxy-3-(p-nitrophenoxy) propane and pepstatin.酸性蛋白酶的结构与功能。V. 重氮乙酰-DL-正亮氨酸甲酯、1,2-环氧-3-(对硝基苯氧基)丙烷和胃蛋白酶抑制剂对酸性蛋白酶特异性抑制作用的比较研究。
J Biochem. 1976 Sep;80(3):497-506. doi: 10.1093/oxfordjournals.jbchem.a131304.
5
A radiochemical titrant for the determination of the operational molarity of solutions of acid proteinases.一种用于测定酸性蛋白酶溶液操作摩尔浓度的放射化学滴定剂。
Biochem J. 1979 Nov 1;183(2):389-94. doi: 10.1042/bj1830389.
6
The structure and function of acid proteases. Specific inactivation of an acid protease from Rhizopus chinensis by diazoacetyl-DL-norleucine methyl ester.酸性蛋白酶的结构与功能。重氮乙酰-DL-正亮氨酸甲酯对中华根霉酸性蛋白酶的特异性失活作用。
J Biochem. 1973 Jan;73(1):61-8.
7
Specific inhibition of acid proteases from brain, kidney, skeletal muscle, and insectivorous plants by diazoacetyl-DL-norleucine methyl ester and by pepstatin.重氮乙酰-DL-正亮氨酸甲酯和胃蛋白酶抑制剂对脑、肾、骨骼肌及食虫植物酸性蛋白酶的特异性抑制作用
J Biochem. 1974 Oct;76(4):897-9.
8
Bifunctional inhibitors of pepsin.胃蛋白酶双功能抑制剂
Proc Natl Acad Sci U S A. 1971 Nov;68(11):2765-8. doi: 10.1073/pnas.68.11.2765.
9
The effect of acid proteinase inhibitors on chicken pepsin.酸性蛋白酶抑制剂对鸡胃蛋白酶的作用。
Biochem J. 1975 Nov;151(2):319-26. doi: 10.1042/bj1510319.
10
The structure and function of acid proteases. IV. Inactivation of the acid protease from Mucor pusillus by acid protease-specific inhibitors.酸性蛋白酶的结构与功能。IV. 特异性酸性蛋白酶抑制剂对微小毛霉酸性蛋白酶的失活作用
J Biochem. 1976 Jul;80(1):61-7. doi: 10.1093/oxfordjournals.jbchem.a131258.

引用本文的文献

1
Experimental approach to the kinetic study of unstable site-directed irreversible inhibitors: kinetic origin of the apparent positive co-operativity arising from inactivation of trypsin by p-amidinophenylmethanesulphonyl fluoride.不稳定的定点不可逆抑制剂动力学研究的实验方法：对氨基苯甲脒基甲磺酰氟使胰蛋白酶失活产生的表观正协同性的动力学起源
Biochem J. 1994 Apr 1;299 ( Pt 1)(Pt 1):29-35. doi: 10.1042/bj2990029.
2
Kinetics of irreversible enzyme inhibition by an unstable inhibitor.不稳定抑制剂对酶的不可逆抑制动力学
Biochem J. 1981 Nov 1;199(2):462-3. doi: 10.1042/bj1990462.
3
Kinetics of protein modification reactions.蛋白质修饰反应的动力学
Biochem J. 1984 Jan 15;217(2):341-51. doi: 10.1042/bj2170341.
4
Chemical modification of enzymes: reaction with an unstable inhibitor.酶的化学修饰：与不稳定抑制剂的反应
Biochem J. 1985 May 1;227(3):1025-7. doi: 10.1042/bj2271025.
5
Computer simulations of the kinetics of irreversible enzyme inhibition by an unstable inhibitor.不稳定抑制剂对酶不可逆抑制动力学的计算机模拟
Biochem J. 1986 Dec 15;240(3):817-20. doi: 10.1042/bj2400817.
6
Alternative methods for the determination of rate constants describing enzyme inactivation by an unstable inhibitor.测定不稳定抑制剂使酶失活的速率常数的替代方法。
Biochem J. 1987 Sep 15;246(3):804-6. doi: 10.1042/bj2460804.
7
Kinetics of protein modification, and/or enzyme inactivation, reactions by an unstable modifying agent.不稳定修饰剂引发的蛋白质修饰和/或酶失活反应的动力学
Biochem J. 1987 Sep 15;246(3):803-5. doi: 10.1042/bj2460803.
8
Inactivation of cathepsin D by dithiophosgene and by 2,2-dichloro-1,3-dithiacyclobutanone.二硫代光气和2,2-二氯-1,3-二硫杂环丁烷对组织蛋白酶D的失活作用
Biochem J. 1976 Mar 1;153(3):737-9. doi: 10.1042/bj1530737.
9
Kinetic analysis of the inhibition of sulfate transport in human red blood cells by isothiocyanates.异硫氰酸盐对人红细胞中硫酸盐转运抑制作用的动力学分析。
J Membr Biol. 1978 Jun 28;41(2):101-15. doi: 10.1007/BF01972628.
10
Activation of cathepsin D by glycine ethyl ester.甘氨酸乙酯对组织蛋白酶D的激活作用。
Biochem J. 1979 Jan 1;177(1):355-6. doi: 10.1042/bj1770355.

本文引用的文献

1
Some properties of specific cholinesterase with particular reference to the mechanism of inhibition by diethyl p-nitrophenyl thiophosphate (E 605) and analogues.特异性胆碱酯酶的某些特性，特别涉及对硫代磷酸O,O-二乙基对硝基苯酯（E605）及其类似物的抑制机制。
Biochem J. 1950 Apr;46(4):451-60. doi: 10.1042/bj0460451.
2
Antibiotic principle from Moringa pterygosperma. IX. Inhibition of transaminase by isothiocyanates.翅荚决明的抗生素原理。IX. 异硫氰酸酯对转氨酶的抑制作用。
Indian J Med Res. 1958 Jan;46(1):75-7.
3
Biosynthesis of the purines. XV. The effect of aza-L-serine and 6-diazo-5-oxo-L-norleucine on inosinic acid biosynthesis de novo.嘌呤的生物合成。十五。氮杂-L-丝氨酸和6-重氮-5-氧代-L-正亮氨酸对从头合成肌苷酸的影响。
J Biol Chem. 1957 Mar;225(1):163-76.
4
Enzyme inhibitors. XVII. Kinetic studies on the irreversible inhibition of adenosine deaminase.酶抑制剂。十七。腺苷脱氨酶不可逆抑制的动力学研究。
J Med Chem. 1967 Jul;10(4):686-9. doi: 10.1021/jm00316a036.
5
The kinetics of the reaction of N,N-dimethyl-2-phenylaziridinium ion with bovine erythrocyte acetylcholinesterase.N,N-二甲基-2-苯基氮杂环丙烷离子与牛红细胞乙酰胆碱酯酶反应的动力学
Can J Biochem. 1970 Mar;48(3):244-50. doi: 10.1139/o70-044.
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An active site peptide from pepsin C.胃蛋白酶C的活性位点肽段。
Biochem J. 1971 Jun;123(1):75-82. doi: 10.1042/bj1230075.
7
Bifunctional inhibitors of pepsin.胃蛋白酶双功能抑制剂
Proc Natl Acad Sci U S A. 1971 Nov;68(11):2765-8. doi: 10.1073/pnas.68.11.2765.
8
Experimental evidence for a hydrophobic active center of glutamic-aspartic transaminase. Specific interaction of holoenzyme and apoenzyme with two fluorescein derivatives.谷氨酸-天冬氨酸转氨酶疏水活性中心的实验证据。全酶和脱辅酶与两种荧光素衍生物的特异性相互作用。
Eur J Biochem. 1973 Oct 18;38(3):537-52. doi: 10.1111/j.1432-1033.1973.tb03089.x.
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Preparation and properties of lysozyme modified by fluorescein-isothiocyanate.异硫氰酸荧光素修饰溶菌酶的制备及性质
J Biochem. 1973 May;73(5):971-8. doi: 10.1093/oxfordjournals.jbchem.a130181.
10
The inhibition of cholinesterase by diethyl phosphorochloridate.二乙基氯磷酸酯对胆碱酯酶的抑制作用。
Biochim Biophys Acta. 1972 Oct 12;284(2):427-34. doi: 10.1016/0005-2744(72)90139-8.