Sekizaki Haruo, Itoh Kunihiko, Toyota Eiko, Tanizawa Kazutaka
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Japan.
J Pept Sci. 2002 Sep;8(9):521-8. doi: 10.1002/psc.406.
A procedure has been developed for the synthesis of oligopeptide amide using inverse substrates as acyl donors with amino acid amide instead of p-nitroanilide as acyl acceptor and trypsins of different origin (bovine, Streptomyces griseus and chum salmon trypsins) as the catalyst. The effectiveness of this procedure was demonstrated by the synthesis of a pentapeptide, Boc-[Leu5]-enkephalin amide, as a model compound. The method was the first enzymatic method shown to be successful at each successive coupling step for the synthesis of the oligopeptide. Bovine and chum salmon trypsins were superior to Streptomyces griseus trypsin as the catalyst.
已经开发出一种合成寡肽酰胺的方法，该方法使用反向底物作为酰基供体，以氨基酸酰胺代替对硝基苯胺作为酰基受体，并使用不同来源的胰蛋白酶（牛胰蛋白酶、灰色链霉菌胰蛋白酶和大麻哈鱼胰蛋白酶）作为催化剂。通过合成五肽Boc-[Leu5]-脑啡肽酰胺作为模型化合物，证明了该方法的有效性。该方法是第一种在寡肽合成的每个连续偶联步骤中都成功的酶促方法。牛胰蛋白酶和大麻哈鱼胰蛋白酶作为催化剂优于灰色链霉菌胰蛋白酶。
