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  • Title: Enhanced potency dipeptide glycol renin inhibitors: studies in vitro and in the conscious rhesus.
    Author: Hanson GJ, Baran JS, Lowrie HS, Sarussi SJ, Yang PC, Babler M, Bittner SE, Papaioannou SE, Walsh GM.
    Journal: Biochem Biophys Res Commun; 1987 Aug 14; 146(3):959-63. PubMed ID: 3304296.
    Abstract:
    We prepared a series of novel dipeptide amides of the formula Boc-Phe-Leu-X, where X is a 3-amino-3-alkyl-1,2-propanediol with lower alkyl substitutions at C-1, in order to probe accessory binding sites in the enzyme renin. This approach was successful in generating potent inhibitors of human and hog renin in vitro. Moreover, these inhibitors were able to effect in vivo reduction of plasma renin activity (PRA) in the conscious salt-depleted rhesus monkey (i.v. route); this effect was related to the size of the C-1 alkyl group.
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