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

Authors :: Liu Y
Wang G
Zhang H
Ma Y
Lang L
Jacobson O
Kiesewetter DO
Zhu L
Gao S
Ma Q
Chen X
Source :: Bioconjugate chemistry [Bioconjug Chem] 2016 Jan 20; Vol. 27 (1), pp. 54-8. Date of Electronic Publication: 2015 Dec 10.
Publication Year :: 2016
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.<br />Competing Interests: The authors declare no competing financial interest.