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马肝醇脱氢酶的设计抑制剂。活性位点金属离子取代的影响。

Designed inhibitors of horse liver alcohol dehydrogenase. Effect of active-site metal ion substitution.

作者信息

Freudenreich C, Pfangert U, Weis M, Zeppezauer M, Biellmann J F

出版信息

FEBS Lett. 1986 Feb 3;196(1):160-2. doi: 10.1016/0014-5793(86)80233-2.

DOI:10.1016/0014-5793(86)80233-2
PMID:3510908
Abstract

3-(p-Butoxyphenyl)propionamide, -thioamide and -hydrazide and the formamide of p-butoxybenzylamine were tested as inhibitors of cadmium(II) and cobalt(II) active-site substituted alcohol dehydrogenase. The results agree with a direct coordination of these inhibitors except for the hydrazide to the active-site metal ion, in the enzyme-NADH-inhibitor complex. The hydrazide might be situated at some distance from the metal ion without a direct coordination bond.

摘要

测试了3-(对丁氧基苯基)丙酰胺、3-(对丁氧基苯基)丙硫酰胺、3-(对丁氧基苯基)丙酰肼以及对丁氧基苄胺的甲酰胺作为镉(II)和钴(II)活性位点取代的乙醇脱氢酶抑制剂的效果。除了酰肼之外，在酶 - 烟酰胺腺嘌呤二核苷酸（NADH） - 抑制剂复合物中，这些抑制剂与活性位点金属离子直接配位的结果是一致的。酰肼可能位于距金属离子一定距离处，不存在直接的配位键。

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