Synthesis of analogues of pepstatin. Effect of structure in subsites P1', P2', and P2 on inhibition of porcine pepsin.
Synthesis of analogues of pepstatin. Effect of structure in subsites P1', P2', and P2 on inhibition of porcine pepsin.
复制标题
胃酶抑素类似物的合成。
DOI：
10.1021/jm00360a022
复制
发表时间：
1983
影响因子：
7.3
通讯作者：
Salituro,FG
中科院分区：
文献类型：
--
作者：
Rich,DH;Salituro,FG
合成了一系列在P2-、Pr和P2位置具有结构变化的胃蛋白酶抑制剂类似物，并测试了其对猪胃蛋白酶的抑制作用。本研究的标准肽为Iva-Val-Sta-Ala-Iaa。P2和Pr位置的结构变化对K的影响相对较小，然而，P2位置的小变化对K和时间依赖性抑制的影响更显着。还合成了一系列胃蛋白酶抑制剂片段，并测试了其对猪胃蛋白酶的抑制作用。
A series of pepstatin analogues having structural variations in the P2-, Pr, and P2 positions havebeen synthesized and tested for inhibition of porcine pepsin. The standard peptide for this study was Iva-Val-Sta-Ala-Iaa. Structural variations in the P2-and Pr positions have relatively little effect on K¿ however, small variations in the P2 position have a more dramatic effect on K-, and time-dependentinhibition. A series of pepstatin fragments were also synthesized and tested for inhibition of porcine pepsin.