Short chain peptide inhibitors containing 1-Naphthyl-alanine demonstrate high potency and specificity for human renin in vitro.
May inform renin inhibitor design; leaves open clinical translation pending in vivo validation.
The phenylalanine residue in the C-terminal sequence of angiotensin II was found to be important for the design of renin inhibitors. 1-Naphthyl-alanine(Nal(1))-containing tripeptide analogues such as benzyloxycarbonyl-Nal (1)-His-Leucinal (ES-188) and benzyloxycarbonyl-Nal(1)-His-(3S,4S)-4-amino-3-hydroxy-6-methylheptanoic acid (Statine) 2(S)-methylbuthylamid (ES-254) showed high potency and specificity to human renin.
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Matsueda et al. (1985) studied this question.
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