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
相关论文
共 50 条
  • [31] Effect of glucagon-like peptide-1 analogue; Exendin-4, on cognitive functions in type 2 diabetes mellitus; possible modulation of brain derived neurotrophic factor and brain Visfatin
    Abdelwahed, O. M.
    Tork, O. M.
    el Din, M. M. Gamal
    Rashed, L.
    Zickri, M.
    BRAIN RESEARCH BULLETIN, 2018, 139 : 67 - 80
  • [32] Effect of exendin-4 on bone remodelling in normal and type 2 diabetic rats
    Sancho, V.
    Nuche-Berenguer, B.
    Arnes, L.
    Esbrit, P.
    Villanueva-Penacarrillo, M. L.
    DIABETOLOGIA, 2007, 50 : S243 - S243
  • [33] Synthesis of multilayered alginate microcapsules for release of exendin-4 to treat type 1 diabetes mellitus
    Park, Sol Ji
    Shin, Soojeong
    Koo, Ok Jae
    Choi, Jiye
    Moon, Jun Ho
    Yoo, Young Je
    Jang, Goo
    Ahn, Curie
    Lee, Byeong Chun
    XENOTRANSPLANTATION, 2011, 18 (05) : 312 - 312
  • [34] Biological activity of AC3174, a peptide analog of exendin-4
    Hargrove, Diane M.
    Kendall, Eric S.
    Reynolds, James M.
    Lwin, Aung N.
    Herich, John P.
    Smith, Pamela A.
    Gedulin, Bronislava R.
    Flanagan, Shawn D.
    Jodka, Carolyn M.
    Hoyt, Julie A.
    McCowen, Kevin M.
    Parkes, David G.
    Anderson, Christen M.
    REGULATORY PEPTIDES, 2007, 141 (1-3) : 113 - 119
  • [35] Exenatide (synthetic exendin-4) continuously improves glucose control over three months in patients with type 2 diabetes
    Taylor, K
    Nielsen, L
    Cole, L
    Han, CJ
    Varns, A
    Kim, D
    Baron, A
    Fineman, M
    Kolterman, O
    DIABETES, 2003, 52 : A130 - A131
  • [36] Biological activity of AC3174, a peptide analog of exendin-4
    Hargrove, D
    Kendall, E
    Reynolds, J
    Jodka, C
    Mack, C
    Parkes, D
    Prickett, K
    Srivastava, V
    Herich, J
    Hoyt, J
    Roan, J
    Wilson, J
    OBESITY RESEARCH, 2004, 12 : A117 - A117
  • [37] Effects of five-day dosing of synthetic exendin-4 (AC2993) in people with type 2 diabetes
    Buse, J
    Fineman, M
    Gottlieb, A
    Gaines, E
    Kolterman, O
    DIABETES, 2000, 49 : A100 - +
  • [38] Anti-inflammatory effects of exendin-4, a glucagon-like peptide-1 analog, on human peripheral lymphocytes in patients with type 2 diabetes
    He, Lan
    Wong, Chun Kwok
    Cheung, Kitty K. T.
    Yau, Ho Chung
    Fu, Anthony
    Zhao, Hai-lu
    Leung, Karen M. L.
    Kong, Alice P. S.
    Wong, Gary W. K.
    Chan, Paul K. S.
    Xu, Gang
    Chan, Juliana C. N.
    JOURNAL OF DIABETES INVESTIGATION, 2013, 4 (04) : 382 - 392
  • [39] Action of exendin-4 treatment upon glucose transport in liver and muscle, in normal and type 2 diabetic state
    Arnes, L.
    Sancho, V.
    Valverde, I.
    Villanueva, M. L.
    DIABETOLOGIA, 2008, 51 : S361 - S361
  • [40] The effects of Exendin-4 on bone marrow-derived mesenchymal cells
    Luciani, Paola
    Fibbi, Benedetta
    Mazzanti, Benedetta
    Deledda, Cristiana
    Ballerini, Lara
    Aldinucci, Alessandra
    Benvenuti, Susanna
    Saccardi, Riccardo
    Peri, Alessandro
    ENDOCRINE, 2018, 60 (03) : 423 - 434
12345