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Beta-homo-amino acid scan of angiotensin IV

Aneta Lukaszuk1, Heidi Demaegdt, Erzsebet Szemenyei

  • 1Department of Organic Chemistry, Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium. alukaszu@vub.ac.be

Journal of Medicinal Chemistry
|April 5, 2008
PubMed

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.

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