β-homo-amino acid scan of angiotensin IV

被引:57
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
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
收藏
页码:2291 / 2296
页数:6
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