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Stable Evans Blue Derived Exendin-4 Peptide for Type 2 Diabetes Treatment.


ABSTRACT: In the treatment of type 2 diabetes mellitus, it is very important to develop therapeutics with prolonged circulation half-life. Exendin-4 is a glucagon like peptide-1 receptor (GLP-1R) agonist that has been modified in different ways for imaging insulinoma and for treating type-2 diabetes. In this work, we synthesized a maleimide derivative of truncated Evans blue dye (MEB-C3-Mal) to conjugate with (Cys(40))exendin-4 to obtain a highly stable MEB-C3-(Cys(40))exendin-4 (denoted as Abextide II). Through in situ binding with endogenous albumin, Abextide II lowers blood glucose level and prolongs the hypoglycemic effect in a type 2 diabetes mouse model more than the FDA approved Albiglutide.

SUBMITTER: Liu Y 

PROVIDER: S-EPMC5219937 | biostudies-literature | 2016 Jan

REPOSITORIES: biostudies-literature

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Stable Evans Blue Derived Exendin-4 Peptide for Type 2 Diabetes Treatment.

Liu Yi Y   Wang Guohao G   Zhang Huimin H   Ma Ying Y   Lang Lixin L   Jacobson Orit O   Kiesewetter Dale O DO   Zhu Lei L   Gao Shi S   Ma Qingjie Q   Chen Xiaoyuan X  

Bioconjugate chemistry 20151210 1


In the treatment of type 2 diabetes mellitus, it is very important to develop therapeutics with prolonged circulation half-life. Exendin-4 is a glucagon like peptide-1 receptor (GLP-1R) agonist that has been modified in different ways for imaging insulinoma and for treating type-2 diabetes. In this work, we synthesized a maleimide derivative of truncated Evans blue dye (MEB-C3-Mal) to conjugate with (Cys(40))exendin-4 to obtain a highly stable MEB-C3-(Cys(40))exendin-4 (denoted as Abextide II).  ...[more]

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