Renin inhibitors containing psi[CH2O] pseudopeptide inserts.
Renin inhibitors 2-4 with the D-Lys renin inhibitory peptide (RIP) sequence, but containing Leu psi[CH2O]Ala (2), Leu psi[CH2O]Val (3), and Leu psi[CH2O]Leu (4) at the P1-P1' site, were of a comparable potency to RIP. N-Terminal Boc-protected inhibitors containing Pro psi[CH2O]Phe in positions P4-P3 were potent inhibitors of renin, with Boc-Phe-Pro psi[CH2O]Phe-His-Leu psi[CH(OH)CH2]Val-Ile-(2-aminomethyl) pyridine (17) having an IC50 of 1.6 X 10(-9) M.
TenBrink
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Cardiovascular Diseases Research, Upjohn Company, Kalamazoo, Michigan 49001.
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Harris
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Johnson
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D000595:Amino Acid Sequence; D000808:Angiotensinogen / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006801:Humans; D008969:Molecular Sequence Data; D013329:Structure-Activity Relationship; D000092502:Renin Inhibitors
D000808:Angiotensinogen; D000092502:Renin Inhibitors