Inhibition of alpha-chymotrypsin with thiol-bearing substrate analogues in the presence of zinc ion.
We have demonstrated that thiol-bearing analogues of alpha-chymotrysin (alpha-CT) substrates such as (S)-(1-benzyl-2-thiolethyl)-carbamic acid, benzyl ester (3) inhibits alpha-CT, a prototypical serine protease, in the presence of Zn(II) ion. They constitute a novel class of small molecule inhibitors for alpha-CT believed to inhibit the enzyme by forming a ternary complex consisting of alpha-CT, Zn(II) ion, and the inhibitor.
Han
Min Su
MS
Department of Chemistry, Pohang University of Science and Technology, San 31Hyojadong, Pohang 790-784, South Korea.
Oh
Dong Ju
DJ
Kim
Dong H
DH
D002918:Chymotrypsin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D007700:Kinetics; D011480:Protease Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D013438:Sulfhydryl Compounds / Q000737:chemistry*; D015032:Zinc / Q000378:metabolism / Q000494:pharmacology*
D011480:Protease Inhibitors; D013438:Sulfhydryl Compounds; D002918:Chymotrypsin; C117608:alpha-chymotrypsin; D015032:Zinc