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[氨基酸的有机磷类似物对牛肾血管紧张素转换酶的抑制作用]

[Inhibition of the angiotensin-converting enzyme from bovine kidney by organophosphorus analogs of amino acids].

作者信息

Shumiantseva V V, Gandurina I A, Osipova T I, Kugaevskaia E V

出版信息

Vopr Med Khim. 1990 Jul-Aug;36(4):74-6.

PMID:2238538
Abstract

Reactions of amino acid phosphoorganic derivatives with angiotensin-converting enzyme (dipeptidyl carboxypeptidase) were studied. Substitution of the amino acid carboxyl group by HS- or P(O) (OH)2-groups did not cause the enzyme considerable inhibition. The enzymatic activity was inhibited by 20-50% in presence of 1 X 10(-3) M Asp, Met and Cys phosphoorganic derivatives. These amino acid derivatives may be used as potential antihypertensive drugs because of their metabolic stability and inhibitory action on the enzyme.

摘要

研究了氨基酸磷酸有机衍生物与血管紧张素转换酶(二肽基羧肽酶)的反应。用HS-或P(O)(OH)₂基团取代氨基酸羧基不会对该酶产生显著抑制作用。在1×10⁻³M的天冬氨酸、蛋氨酸和半胱氨酸磷酸有机衍生物存在下,酶活性被抑制了20% - 50%。由于这些氨基酸衍生物具有代谢稳定性以及对该酶的抑制作用,它们可用作潜在的抗高血压药物。

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