Inhibition of acrosin by benzamidines.
Acrosin proved to be very susceptible to inhibition by benzamidine derivatives. Most of the inhibitors were at least 10-fold more potent against acrosin than against trypsin. The most potent inhibitors of acrosin of this series were amidinophenyl compounds with a keto group or a carbon amide moiety in the side chain. Comparison of the structure-activity relationships for the inhibition of acrosin and trypsin showed differences in the binding sites of both enzymes.
D000176:Acrosin / Q000037:antagonists & inhibitors*; D000578:Amidines / Q000494:pharmacology*; D001550:Benzamidines / Q000494:pharmacology*; D055598:Chemical Phenomena; D002621:Chemistry; D011480:Protease Inhibitors; D013329:Structure-Activity Relationship; D014361:Trypsin Inhibitors / Q000494:pharmacology
D000578:Amidines; D001550:Benzamidines; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; D000176:Acrosin