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METHOD FOR PRODUCING ACTIVE FORM OF LONG-ACTING INSULIN ANALOGUE DERIVATIVE USING CLOSTRIPAIN

机译:使用梭司司满活性胰岛素类似物衍生物的活性形式的方法

摘要

The present invention relates to a method for producing an active form of a long-acting insulin analogue derivative, in which the amino acid at position 22 of the insulin B-chain is substituted from arginine (Arg) to lysine (Lys), so that the insulin analogue can be converted to an active form without cleavage of the B-chain even when it is reacted with clostripain. In a conventional method of converting pro-insulin to an active form by use of trypsin, an albumin binding domain is cleaved, making it difficult to convert the long-acting insulin analogue derivative to an active form. The production method according to the present invention overcomes this difficulty, and thus it can be effectively used for the production of a long-acting therapeutic agent for treatment of diabetes.
机译:本发明涉及一种用于制备长作用胰岛素类似物衍生物的活性形式的方法,其中胰岛素B链的位置22处的氨基酸由精氨酸(Arg)取代给赖氨酸(Lys),因此 胰岛素类似物可以转化为活性形式,即使当它与梭菌反应时,也可以转化为活性形式,而不会切割B链。 在通过使用胰蛋白酶将促胰岛素转化为活性形式的常规方法,裂解白蛋白结合结构域,使得难以将长效胰岛素类似物衍生物转化为活性形式。 根据本发明的制备方法克服了这种困难,因此可以有效地用于生产用于治疗糖尿病的长效治疗剂。

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