具有两个阳离子残基的肽基甲基锍盐作为激素原加工潜在抑制剂的合成及性质
The synthesis and properties of peptidylmethylsulphonium salts with two cationic residues as potential inhibitors of prohormone processing.
作者信息
Zumbrunn A, Stone S, Shaw E
机构信息
Friedrich Miescher-Institut, Basel, Switzerland.
出版信息
Biochem J. 1988 Dec 15;256(3):989-94. doi: 10.1042/bj2560989.
Abstract
Peptidylmethylsulphonium salts incorporating consecutive basic residues at the C-terminus of the peptidyl portion such as -Arg-Arg-, -Arg-Lys-, -Lys-Lys- and -Lys-Arg- were synthesized and examined as proteinase inhibitors. Serine proteinases with a specificity directed towards hydrolysis at cationic residues were found to be unaffected by these derivatives. On the other hand, cysteine proteinases, cathepsin B and, in particular, clostripain were readily inactivated by affinity labelling. The reagents thus are of promise for the study of prohormone processing promoted by cysteine proteinases.
摘要
合成了在肽基部分C末端含有连续碱性残基（如-Arg-Arg-、-Arg-Lys-、-Lys-Lys-和-Lys-Arg-）的肽基甲基磺酸盐，并将其作为蛋白酶抑制剂进行了研究。发现对阳离子残基水解具有特异性的丝氨酸蛋白酶不受这些衍生物的影响。另一方面，半胱氨酸蛋白酶、组织蛋白酶B，尤其是梭菌蛋白酶很容易通过亲和标记而失活。因此，这些试剂有望用于研究由半胱氨酸蛋白酶促进的激素原加工过程。
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