聚乙二醇-胃蛋白酶抑制剂缀合物的制备及初步表征
Preparation and preliminary characterization of poly(ethylene glycol)-pepstatin conjugate.
作者信息
Brygier J, Vincentelli J, Nijs M, Guermant C, Paul C, Baeyens-Volant D, Looze Y
机构信息
Protein Chemistry Unit, Faculty of Medicine, University of Brussels, Belgium.
出版信息
Appl Biochem Biotechnol. 1994 Apr;47(1):1-10. doi: 10.1007/BF02788670.
The carboxyl function of pepstatin has been coupled, through an amide bond, to methoxypoly(ethylene glycol) (5 kDa), to which an amino function had been previously grafted. The mPEG-pepstatin conjugate inhibits hog pepsin (aspartic proteinase) in vitro as pepstatin itself, however, with a 400 times higher apparent Ki. The conjugate apparently does not inhibit proteinases belonging to other proteinase families such as serine (trypsin, carboxypeptidase Y), cysteine (Papaya proteinase III), or metallo (collagenase) proteinases.
胃蛋白酶抑制剂的羧基功能已通过酰胺键与甲氧基聚乙二醇（5 kDa）偶联，该甲氧基聚乙二醇先前已接枝了氨基功能。甲氧基聚乙二醇 - 胃蛋白酶抑制剂缀合物在体外对猪胃蛋白酶（天冬氨酸蛋白酶）的抑制作用与胃蛋白酶抑制剂本身相同，然而，其表观抑制常数Ki高400倍。该缀合物显然不抑制属于其他蛋白酶家族的蛋白酶，如丝氨酸蛋白酶（胰蛋白酶、羧肽酶Y）、半胱氨酸蛋白酶（木瓜蛋白酶III）或金属蛋白酶（胶原酶）。
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