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

被引：26

作者：

Liu, Yi ^{[1
,2
]}

Wang, Guohao ^{[3
]}

Zhang, Huimin ^{[2
]}

Ma, Ying ^{[2
]}

Lang, Lixin ^{[2
]}

Jacobson, Orit ^{[2
]}

Kiesewetter, Dale O. ^{[2
]}

Zhu, Lei ^{[3
]}

Gao, Shi ^{[1
]}

Ma, Qingjie ^{[1
]}

Chen, Xiaoyuan ^{[2
]}

机构：

[1] Jilin Univ, China Japan Union Hosp, Changchun 130033, Jilin, Peoples R China

[2] NIBIB, LOMIN, NIH, Bethesda, MD 20892 USA

[3] Xiamen Univ, Sch Publ Hlth, Ctr Mol Imaging & Translat Med, State Key Lab Mol Vaccinol & Mol Diagnost, Xiamen 361102, Peoples R China

来源：

BIOCONJUGATE CHEMISTRY | 2016年 / 27卷 / 01期

基金：

美国国家科学基金会; 美国国家卫生研究院;

关键词：

ALBUMIN-BINDING; RECEPTOR; INSULIN; ANALOG; PHARMACOKINETICS; MALEIMIDES; MECHANISM; STRATEGY; AGONIST;

D O I：

10.1021/acs.bioconjchem.5b00625

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：54 / 58

页数：5

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