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依那普利拉对人血管紧张素I转换酶的多态性抑制作用

Polymorphic inhibition of human angiotensin I-converting enzyme by enalaprilat.

作者信息

Lee E J

机构信息

Department of Pharmacology, National University of Singapore, Kent Ridge.

出版信息

Eur J Clin Pharmacol. 1995;49(3):173-5. doi: 10.1007/BF00192376.

DOI:10.1007/BF00192376
PMID:8665992
Abstract

Many individuals possess an allele of the angiotensin I-converting enzyme (ACE) gene, which contains an extra 287-kb fragment in intron 16 (Rigat et al. 1992). Although the functionality of this fragment is at present unclear, the absence (deletion, D) or presence (insertion, I) of this fragment appears to be related to both the amount and activity of circulating ACE. This paper reports the possible polymorphic response of ACE to the ACE inhibitor enalaprilat in 54 normal Chinese subjects that is independent of the I/D polymorphism. The kinetics of ACE inhibition with enalaprilat was studied in serum from 54 normal Chinese subjects. Enalaprilat appKi ranged between 0.46 and 2.16 nM. An antimode was observed at 1.4 nM. Four subjects could be characterized as being poor responders to enalaprilat.

摘要

许多个体拥有血管紧张素I转换酶(ACE)基因的一个等位基因,该基因在第16内含子中含有一个额外的287 kb片段(Rigat等人,1992年)。尽管目前尚不清楚该片段的功能,但该片段的缺失(缺失型,D)或存在(插入型,I)似乎与循环ACE的量和活性都有关。本文报道了54名正常中国受试者中ACE对ACE抑制剂依那普利拉可能存在的多态性反应,且该反应与I/D多态性无关。在54名正常中国受试者的血清中研究了依那普利拉抑制ACE的动力学。依那普利拉的表观抑制常数(appKi)范围在0.46至2.16 nM之间。在1.4 nM处观察到一个反众数。四名受试者可被表征为对依那普利拉反应较差。

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本文引用的文献

1
Association analysis of a polymorphism of the angiotensin converting enzyme gene with essential hypertension in the Japanese population.日本人群中血管紧张素转换酶基因多态性与原发性高血压的关联分析。
Biochem Biophys Res Commun. 1993 Mar 15;191(2):399-404. doi: 10.1006/bbrc.1993.1231.
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Population genetics of the angiotensin-converting enzyme in Chinese.中国人血管紧张素转换酶的群体遗传学
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Independent, marked associations of alleles of the insulin receptor and dipeptidyl carboxypeptidase-I genes with essential hypertension.
胰岛素受体基因和二肽基羧肽酶-I基因的等位基因与原发性高血压存在独立、显著的关联。
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Quinapril--a preclinical review of the pharmacology, pharmacokinetics, and toxicology.喹那普利——药理学、药代动力学及毒理学的临床前综述。
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The two homologous domains of human angiotensin I-converting enzyme are both catalytically active.人血管紧张素I转换酶的两个同源结构域均具有催化活性。
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9
Structure of the angiotensin I-converting enzyme gene. Two alternate promoters correspond to evolutionary steps of a duplicated gene.血管紧张素I转换酶基因的结构。两个交替启动子对应于一个重复基因的进化步骤。
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10
Deletion polymorphism in the gene for angiotensin-converting enzyme is a potent risk factor for myocardial infarction.血管紧张素转换酶基因的缺失多态性是心肌梗死的一个重要危险因素。
Nature. 1992 Oct 15;359(6396):641-4. doi: 10.1038/359641a0.