Weller H N, Rom M B
Squibb Institute for Medical Research, Princeton, New Jersey 08543-4000.
J Enzyme Inhib. 1988;2(3):183-98. doi: 10.3109/14756368809040725.
Conformationally constrained phenylbutyl(hydroxyphosphinyl)acyl dipeptides are potent inhibitors of angiotensin converting enzyme. The activity enhancement obtained by introducing conformational constraint into these molecules is greater than for related sulfhydryl and carboxyl analogs. The results are interpreted in terms of a binding model which optimally positions both zinc binding and hydrophobic groups for active site binding.
构象受限的苯基丁基（羟基亚膦酰基）酰基二肽是血管紧张素转换酶的有效抑制剂。通过将构象限制引入这些分子中所获得的活性增强大于相关的巯基和羧基类似物。根据一种结合模型对结果进行了解释，该模型将锌结合基团和疏水基团都最佳地定位在活性位点以进行结合。
