title: Stable Evans Blue Derived Exendin-4 Peptide for Type 2 Diabetes Treatment.
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.
authors.affiliation: China-Japan Union Hospital of Jilin University , Changchun, Jilin 130033, China.|Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineer-ing (NIBIB), National Institutes of Health (NIH) , Bethesda, Maryland 20892, United States.
authors.forename: Yi
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University , Xiamen, 361102, China.
authors.forename: Guohao
authors.initials: G
authors.lastname: Wang
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineer-ing (NIBIB), National Institutes of Health (NIH) , Bethesda, Maryland 20892, United States.
authors.forename: Huimin
authors.initials: H
authors.lastname: Zhang
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineer-ing (NIBIB), National Institutes of Health (NIH) , Bethesda, Maryland 20892, United States.
authors.forename: Ying
authors.initials: Y
authors.lastname: Ma
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineer-ing (NIBIB), National Institutes of Health (NIH) , Bethesda, Maryland 20892, United States.
authors.forename: Lixin
authors.initials: L
authors.lastname: Lang
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineer-ing (NIBIB), National Institutes of Health (NIH) , Bethesda, Maryland 20892, United States.
authors.forename: Orit
authors.initials: O
authors.lastname: Jacobson
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineer-ing (NIBIB), National Institutes of Health (NIH) , Bethesda, Maryland 20892, United States.
authors.forename: Dale O
authors.initials: DO
authors.lastname: Kiesewetter
authors.affiliation: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University , Xiamen, 361102, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Zhu
authors.affiliation: China-Japan Union Hospital of Jilin University , Changchun, Jilin 130033, China.
authors.forename: Shi
authors.initials: S
authors.lastname: Gao
authors.affiliation: China-Japan Union Hospital of Jilin University , Changchun, Jilin 130033, China.
authors.forename: Qingjie
authors.initials: Q
authors.lastname: Ma
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineer-ing (NIBIB), National Institutes of Health (NIH) , Bethesda, Maryland 20892, United States.
authors.forename: Xiaoyuan
authors.initials: X
authors.lastname: Chen
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004355:Drug Stability; D005070:Evans Blue / Q000737:chemistry*; D000077270:Exenatide; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D008301:Maleimides / Q000737:chemistry; D008810:Mice, Inbred C57BL; D009282:Naphthalenesulfonates / Q000737:chemistry / Q000494:pharmacology*; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D012709:Serum Albumin / Q000737:chemistry; D014688:Venoms / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C000624441:Abextide II; D007004:Hypoglycemic Agents; D008301:Maleimides; D009282:Naphthalenesulfonates; D010455:Peptides; D012709:Serum Albumin; D014688:Venoms; C043592:maleimide; D005070:Evans Blue; D000077270:Exenatide