Journal
BIOCONJUGATE CHEMISTRY
Volume 27, Issue 1, Pages 54-58Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.5b00625
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Funding
- National Science Foundation of China [81571708, 81501506]
- Research Fund of Science and Technology Department of Jilin Province [20150520154JH]
- Hygiene Specific Subjects of Jilin Province [SCZSY201508]
- National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health
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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.
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