胃蛋白酶抑制剂类似物的合成。P1'、P2'和P2亚位点结构对猪胃蛋白酶抑制作用的影响。
Synthesis of analogues of pepstatin. Effect of structure in subsites P1', P2', and P2 on inhibition of porcine pepsin.
作者信息
Rich D H, Salituro F G
出版信息
J Med Chem. 1983 Jun;26(6):904-10. doi: 10.1021/jm00360a022.
A series of pepstatin analogues having structural variations in the P2', P1', and P2 positions have been synthesized and tested for inhibition of porcine pepsin. The standard peptide for this study was Iva-Sta-Val-Ala-Iaa. Structural variations in the P2' and P1' positions have relatively little effect on Ki; however, small variations in the P2 position have a more dramatic effect on Ki and time-dependent inhibition. A series of pepstatin fragments were also synthesized and tested for inhibition of porcine pepsin.
已经合成了一系列在P2'、P1'和P2位置具有结构变化的胃蛋白酶抑制剂类似物，并测试了它们对猪胃蛋白酶的抑制作用。本研究的标准肽是Iva-Sta-Val-Ala-Iaa。P2'和P1'位置的结构变化对Ki的影响相对较小；然而，P2位置的微小变化对Ki和时间依赖性抑制有更显著的影响。还合成了一系列胃蛋白酶抑制剂片段，并测试了它们对猪胃蛋白酶的抑制作用。
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