β-Homo-amino Acid Scan of Angiotensin IV

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• 作者：Aneta Lukaszuk ; Heidi Demaegdt ; Erzsebet Szemenyei ; Gé ; za Tó ; th ; Dagmara Tymecka ; Aleksandra Misicka ; Philippe Karoyan ; Patrick Vanderheyden ; Georges Vauquelin ; Dirk Tourwé
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：April 10, 2008
• 年：2008
• 卷：51
• 期：7
• 页码：2291 - 2296
• 全文大小：123K
• 年卷期：v.51,no.7(April 10, 2008)
• ISSN：1520-4804

文摘

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 β²-homo amino acid- and β³-homo amino acid substitutions were used, allowed the identification of H-(R)β²hVal-Tyr-Ile-His-Pro-β³hPhe-OH as a potent and stable Ang IV analog with high selectivity for IRAP versus AP-N and the AT1 receptor.