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1. 发明授权

KR100864584B1 EXENDIN DERIVATIVE LINKED BIOTIN, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 有权
标题翻译：维生素衍生物链接生物素，其制备方法和包含其的药物组合物
公开(公告)号：KR100864584B1
公开(公告)日：2008-10-24
申请号：KR20080016833
申请日：2008-02-25
申请人： UNIV SUNGKYUNKWAN FOUND
发明人： LEE KANG CHOON , CHAE SU YOUNG , JIN CHENG HAO
IPC分类号： C07K14/575 , C07K14/46
CPC分类号： C07K14/57563
摘要： Biotin-linked exendin derivatives are provided to increase in vivo stability and in vivo retention time of exendin, and promote absorption of exendin through mucous membrane, so that they are useful for treating diseases caused by insulin oversecretion, blood glucose lowering, gastric or bowel movement inhibition, gastric or bowel empty inhibition, and digestion inhibition. A biotin-linked exendin derivatives have biotin in any one of a 12nd lysine residue and a 27th lysine residue of exendin 4 represented by SEQ ID NO:2. A method for preparing the biotin-linked exendin derivatives comprises the steps of: (i) adding exendin 4 of SEQ ID NO:2, biotin and reducing agent into buffer solution or organic solvent and reacting them; (ii) storing the reacting mixture at a certain temperature in a dark room; (iii) after reaction of step (ii), removing unreacted products; and (iv) separating and purifying the biotin-linked exendin. A method for treating diabetes such as type 2 diabetes comprises the biotin-linked exendin derivatives.
摘要翻译：提供生物素连接的毒蜥外泌激素衍生物以增加毒蜥外泌肽的体内稳定性和体内保留时间，并促进毒蜥外泌肽通过粘膜的吸收，使其可用于治疗由胰岛素过分泌，降血糖，胃或肠运动引起的疾病抑制，胃或肠空的抑制和消化抑制。生物素连接的毒蜥外泌肽衍生物在SEQ ID NO：2所示的第12赖氨酸残基和毒蜥外泌肽4的第27赖氨酸残基中的任一个中具有生物素。制备生物素连接的毒蜥外泌肽衍生物的方法包括以下步骤：（i）将SEQ ID NO：2的毒蜥外泌肽4，生物素和还原剂加入缓冲溶液或有机溶剂中并使其反应; （ii）将反应混合物在一定温度下储存在暗室中; （iii）步骤（ii）反应后，除去未反应的产物; 和（iv）分离和纯化生物素连接的毒蜥外泌肽。用于治疗糖尿病如2型糖尿病的方法包括生物素连接的毒蜥外泌肽衍生物。

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