Toll L, Almquist R G
Biochem Biophys Res Commun. 1986 Mar 28;135(3):770-7. doi: 10.1016/0006-291x(86)90995-2.
Ketomethylene containing peptide analogs, modeled after a snake venom pentapeptide, have been shown to be potent angiotensin converting enzyme inhibitors. Although the most potent compounds are up to five times more potent than captopril in inhibiting angiotensin converting enzyme activity, they are relatively weak inhibitors of [3H]captopril binding to membrane bound angiotensin converting enzyme. This indicates that inhibition of [3H]captopril binding and enzymatic activity is due to binding to distinct sites. These results suggest that the inhibitors bind to an additional site on the enzyme distinct from the captopril binding site.
以蛇毒五肽为模板的含酮亚甲基肽类似物已被证明是有效的血管紧张素转换酶抑制剂。尽管最有效的化合物在抑制血管紧张素转换酶活性方面比卡托普利强五倍，但它们对[3H]卡托普利与膜结合的血管紧张素转换酶结合的抑制作用相对较弱。这表明[3H]卡托普利结合的抑制和酶活性的抑制是由于与不同位点的结合。这些结果表明，抑制剂与酶上不同于卡托普利结合位点的另一个位点结合。
