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  • Title: Renin inhibitors. I. Synthesis and structure-activity relationships of transition-state inhibitors containing homostatine analogues at the scissile bond.
    Author: Atsuumi S, Nakano M, Koike Y, Tanaka S, Matsuyama K, Nakano M, Morishima H.
    Journal: Chem Pharm Bull (Tokyo); 1992 Feb; 40(2):364-70. PubMed ID: 1606632.
    Abstract:
    The synthesis and structure-activity relationships of transition-state renin inhibitors containing the homostatine analogues at the scissile bond are described. These inhibitors incorporate the amino acid side chains corresponding to positions 7-12 (P4-P2') of angiotensinogen. Ethyl, 2-hydroxyethyl and 3-hydroxypropyl groups at position 2 of the homostatine analogues (P1') are more effective for increasing potency than the isopropyl group. A combination of residues at P1, P3 and P4 is important for potency and this result suggests that S1, S3 and S4 form a huge hydrophobic core together in renin.
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