β-homo-amino acid scan of angiotensin IV

被引：58

作者：

Lukaszuk, Aneta ^{[1
]}

Demaegdt, Heidi ^{[2
]}

Szemenyei, Erzsebet ^{[3
]}

Toth, Geza ^{[3
]}

Tymecka, Dagmara ^{[4
]}

Misicka, Aleksandra ^{[4
,5
]}

Karoyan, Philippe ^{[6
]}

Vanderheyden, Patrick ^{[2
]}

Vauquelin, Georges ^{[2
]}

Tourwe, Dirk ^{[1
]}

机构：

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

[2] Vrije Univ Brussels, Dept Mol & Biochem Pharmacol, B-1050 Brussels, Belgium

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

[4] Warsaw Univ, Fac Chem, PL-02093 Warsaw, Poland

[5] Polish Acad Sci, Med Res Ctr, PL-02106 Warsaw, Poland

[6] Univ Paris 06, CNRS, UMR 7613, Paris, France

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 07期

关键词：

D O I：

10.1021/jm701490g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Angiotensin IV, a metabolite of angiotensin II, inhibits the enzyme insulin regulated aminopeptidase or IRAP and also, although with lower potency, aminopeptidase-N (AP-N). When both beta(2)-homo amino acid- and beta(3)-homo amino acid substitutions were used, allowed the identification of H-(R) beta(2)hVal-Tyr-Ile-His-Pro-beta(3) hPhe-OH as a potent and stable Ang IV analog with high selectivity for IRAP versus AP-N and the AT1 receptor.

引用

页码：2291 / 2296

页数：6

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