JUNG, SUNG YOUB,郑圣烨,鄭聖燁,HWANG, SANG YOUN,黄祥渊,黃祥淵,CHOI, IN YOUNG,崔仁荣,崔仁榮,PARK, SUNG HEE,朴晟喜,朴晟喜,KWON, SE CHANG,权世昌,權世昌
申请号：
TW103100155
公开号：
TW201441253A
申请日:
2014.01.03
申请国别(地区):
TW
年份:
2014
代理人:
摘要：
The present invention relates to an insulinotropic peptide derivative with the modified N-terminal charge and a pharmaceutical composition including the same. Specifically, the insulinotropic peptide derivative is characterized in that the N-terminal positive charge of the insulinotropic peptide is modified to a neutral or negative charge at neutral pH. The insulinotropic peptide derivative according to the present invention is rapidly dissociated from the GLP-1 receptor owing to the above modification in the N-terminal charge, so as to maintain blood stability and to exhibit enhanced insulinotropic ability and blood glucose-lowering activity, compared to the native insulinotropic peptide. Accordingly, the insulinotropic peptide derivative is very useful for the treatment of type 2 diabetes.本發明關於具有經修飾之N端電荷之促胰島素肽衍生物以及包含該促胰島素衍生物之醫藥組成物。具體地,該促胰島素肽衍生物特徵在於該促胰島素肽之N端正電荷於中性pH經修飾為中性電荷或負電荷。根據本發明之促胰島素肽衍生物,相較於天然促胰島素肽,由於上述於N端電荷的修飾而快速地由GLP-1受體解離,以維持血液安定性及顯示增強的促胰島素能力與血液葡萄糖降低活性。因此,該促胰島素肽衍生物非常有用於治療第2型糖尿病。
