Angiotensin IV displays only low affinity for native insulin-regulated aminopeptidase (IRAP)

被引：9

作者：

Demaegdt, Heidi ^{[1
]}

De Backer, Jean-Paul ^{[1
]}

Lukaszuk, Aneta ^{[2
]}

Toth, Geza ^{[3
]}

Szemenyei, Erzsebet ^{[3
]}

Tourwe, Dirk ^{[2
]}

Vauquelin, Georges ^{[1
]}

机构：

[1] Vrije Univ Brussel, Res Grp Expt Pharmacol, Dept Mol & Biochem Pharmacol, B-1050 Brussels, Belgium

[2] Vrije Univ Brussel, Dept Organ Chem, B-1050 Brussels, Belgium

[3] Hungarian Acad Sci, Inst Biochem, Biol Res Ctr, H-6726 Szeged, Hungary

来源：

FUNDAMENTAL & CLINICAL PHARMACOLOGY | 2012年 / 26卷 / 02期

关键词：

affinity; angiotensin II; chelators; 3H]AL-11; native IRAP; AT(4) RECEPTOR-LIGAND; CYSTINYL AMINOPEPTIDASE; BINDING; CELLS; POTENT; RAT;

D O I：

10.1111/j.1472-8206.2011.00948.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Radioligand binding studies revealed that Ang IV binds to insulin-regulated aminopeptidase (IRAP)/AT4 receptors with high affinity. Yet, as these experiments were routinely carried out in the presence of chelators, only the catalytic zinc-depleted apo-form of IRAP was labelled. While the chelators remove the catalytic zinc from IRAP and protect Ang IV from proteolytic degradation, the aminopeptidase N selective inhibitor 7B only exerts the latter effect. By using 7B along with the new stable Ang IV-analog [3H]AL-11, we here show that the native enzyme is only a low-affinity target for Ang IV.

引用

页码：194 / 197

页数：4

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