Inhibition of renin by substrate analogue inhibitors containing the olefinic amino acid 5(S)-amino-7-methyl-3(E)-octenoic acid.
The olefinic dipeptide 5(S)-amino-7-methyl-3(E)-octenoic acid (1) was synthesized and used to make the olefinic peptides Leu psi [E-CH = CH]Gly-Val-Phe-OCH3 (2) and His-Leu psi [E-CH = CH]Gly-Val-Phe-OCH3 (3). These olefinic peptides were found to exhibit renin inhibitory activity against both hog kidney renin and human amniotic renin that was comparable to the substrate analogue inhibitors Leu-Leu-Val-Phe-OCH3 and His-Leu-Leu-Val-Phe-OCH3.
D000596:Amino Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D021542:Amino Acids, Neutral; D000653:Amniotic Fluid / Q000201:enzymology; D000818:Animals; D005260:Female; D006801:Humans; D007202:Indicators and Reagents; D007668:Kidney / Q000201:enzymology; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D009904:Optical Rotation; D011247:Pregnancy; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D013552:Swine; D000092502:Renin Inhibitors
D000596:Amino Acids; D021542:Amino Acids, Neutral; D007202:Indicators and Reagents; D000092502:Renin Inhibitors; C042927:5-amino-7-methyl-3-octenoic acid