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底物类似物对γ-谷氨酰循环酶的选择性抑制作用。

Selective inhibition of gamma-glutamyl-cycle enzymes by substrate analogs.

作者信息

Griffith O W, Meister A

出版信息

Proc Natl Acad Sci U S A. 1977 Aug;74(8):3330-4. doi: 10.1073/pnas.74.8.3330.

Abstract

Substrate analogs have been obtained that selectively inhibit the reactions of the gamma-glutamyl cycle or that are susceptible to only limited metabolism by the cycle. Thus, glutathione synthesis may be inhibited and analogs of glutathione may be synthesized that do not participate in transpeptidation. Specific inhibitors of gamma-glutamylcyclotransferase and 5-oxoprolinase have been obtained. The findings offer new approaches to the in vivo study of the cycle and also to the design of more specifically directed analogs of inhibitors such as methionine sulfoximine and 6-diazo-5-oxonorleucine.

摘要

已经获得了能够选择性抑制γ-谷氨酰循环反应或仅易受该循环有限代谢影响的底物类似物。因此,可以抑制谷胱甘肽的合成,并合成不参与转肽作用的谷胱甘肽类似物。已经获得了γ-谷氨酰环转移酶和5-氧脯氨酸酶的特异性抑制剂。这些发现为该循环的体内研究以及设计更具特异性的抑制剂类似物(如蛋氨酸亚砜亚胺和6-重氮-5-氧代正亮氨酸)提供了新方法。

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