结构和立体化学产物类似物对胃蛋白酶催化反应的抑制作用。
The inhibition of pepsin-catalysed reactions by structural and stereochemical product analogues.
作者信息
Kitson T M, Knowles J R
出版信息
Biochem J. 1971 Apr;122(2):241-7. doi: 10.1042/bj1220241.
Abstract
- The inhibition of pepsin-catalysed hydrolysis of N-acetyl-l-phenylalanyl-l-phenylalanylglycine by products and product analogues was studied. 2. Inhibitors of the l-configuration give rise to linear non-competitive inhibition, whereas those of the d-configuration show linear competitive behaviour. 3. Non-competitive inhibition by the product N-acetyl-l-phenylalanine indicates an ordered release of products, which supports a common mechanism (involving an ;amino-enzyme') for pepsin-catalysed transpeptidation and hydrolysis reactions. 4. The differences in the types of inhibition caused by product analogues of the l- and d-series emphasize the stereospecificity of the binding of these inhibitors to free enzyme and to the putative amino-enzyme intermediate. 5. The results suggest that it is the anion of the acyl product that is released first in the hydrolytic reaction (see Kitson & Knowles, 1971).
摘要
- 研究了产物及产物类似物对胃蛋白酶催化的N-乙酰-L-苯丙氨酰-L-苯丙氨酰甘氨酸水解反应的抑制作用。2. L-构型的抑制剂会引起线性非竞争性抑制，而D-构型的抑制剂则表现出线性竞争性行为。3. 产物N-乙酰-L-苯丙氨酸的非竞争性抑制表明产物是按顺序释放的，这支持了胃蛋白酶催化的转肽反应和水解反应的共同机制（涉及“氨基酶”）。4. L-和D-系列产物类似物所引起的抑制类型差异强调了这些抑制剂与游离酶及假定的氨基酶中间体结合的立体特异性。5. 结果表明，在水解反应中首先释放的是酰基产物的阴离子（见Kitson和Knowles，1971）。
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The inhibition of pepsin-catalysed reactions by structural and stereochemical product analogues.结构和立体化学产物类似物对胃蛋白酶催化反应的抑制作用。
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本文引用的文献
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2
THE CHYMOTRYPSIN-CATALYZED HYDROLYSIS AND SYNTHESIS OF N-ACETYL-L-TYROSINE HYDROXAMIC ACID.胰凝乳蛋白酶催化的N-乙酰-L-酪氨酸异羟肟酸的水解与合成
J Biol Chem. 1964 May;239:1640-52.
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Biochem J. 1971 Apr;122(2):249-56. doi: 10.1042/bj1220249.
7
The rate-determining step in pepsin-catalysed reactions, and evidence against an acyl-enzyme intermediate.胃蛋白酶催化反应中的速率决定步骤，以及反对酰基酶中间体的证据。
Biochem J. 1969 Jun;113(2):369-75. doi: 10.1042/bj1130369.
8
The inhibition of pepsin-catalysed reactions by products and product analogues. Kinetic evidence for ordered release of products.产物及产物类似物对胃蛋白酶催化反应的抑制作用。产物有序释放的动力学证据。
Biochem J. 1969 Jun;113(2):363-8. doi: 10.1042/bj1130363.
9
The pH-dependence of pepsin-catalysed reactions.胃蛋白酶催化反应的pH依赖性。
Biochem J. 1969 Jun;113(2):353-62. doi: 10.1042/bj1130353.
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