| 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.
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