Han Min Su, Oh Dong Ju, Kim Dong H
Department of Chemistry, Pohang University of Science and Technology, San 31Hyojadong, Pohang 790-784, South Korea.
Bioorg Med Chem Lett. 2004 Feb 9;14(3):701-5. doi: 10.1016/j.bmcl.2003.11.058.
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.
我们已经证明，诸如（S）-（1-苄基-2-硫代乙基）-氨基甲酸苄酯（3）之类的α-胰凝乳蛋白酶（α-CT）底物的含硫醇类似物在Zn（II）离子存在下可抑制α-CT（一种典型的丝氨酸蛋白酶）。它们构成了一类新型的α-CT小分子抑制剂，据信该抑制剂通过形成由α-CT、Zn（II）离子和抑制剂组成的三元复合物来抑制该酶。
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