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
收藏
页码：54 / 58
页数：5
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