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Literature DB >> 26641886

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

Yi Liu^1,2, Guohao Wang³, Huimin Zhang², Ying Ma², Lixin Lang², Orit Jacobson², Dale O Kiesewetter², Lei Zhu³, Shi Gao¹, Qingjie Ma¹, Xiaoyuan Chen².

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.

Entities: Chemical Disease Gene Species

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Year: 2015 PMID： 26641886 PMCID： PMC5219937 DOI： 10.1021/acs.bioconjchem.5b00625

Source DB: PubMed Journal: Bioconjug Chem ISSN： 1043-1802 Impact factor: 4.774

26 in total

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