Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Substitution
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Amino Acids / chemistry*
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Aminopeptidases / antagonists & inhibitors
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Angiotensin II / analogs & derivatives*
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Angiotensin II / chemical synthesis
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Angiotensin II / chemistry
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Angiotensin II / pharmacology
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Animals
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Binding Sites
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CD13 Antigens / antagonists & inhibitors
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CHO Cells
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Cell Line
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Cell Membrane / drug effects
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Cricetinae
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Cricetulus
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Dose-Response Relationship, Drug
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Enzyme Activation / drug effects
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Humans
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Molecular Structure
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Receptor, Angiotensin, Type 1 / drug effects
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Structure-Activity Relationship
Substances
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Amino Acids
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Enzyme Inhibitors
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Receptor, Angiotensin, Type 1
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Angiotensin II
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angiotensin II, des-Asp(1)-des-Arg(2)-Ile(5)-
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Aminopeptidases
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CD13 Antigens