Screening of a phage display library of exendin-4 mutants with the extracellular domain of rat GLP-1 receptor

被引:0
|
作者
Yin, Xiaopu [1 ]
Ma, Yushu [1 ]
Liu, Meiyun [1 ]
Gao, Weifeng [1 ]
Wei, Dongzhi [1 ]
机构
[1] E China Univ Sci & Technol, Inst Biochem, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China
来源
PROTEIN AND PEPTIDE LETTERS | 2007年 / 14卷 / 08期
关键词
exendin-4; GLP-1; receptor; phage display library;
D O I
暂无
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A phage display library of exendin-4 mutants was screened with the extracellular domain of rat glucagon-like peptide 1 receptor as the target. A novel variant of exendin-4 with higher affinity for the receptor fraction than that of the wild type was identified. The increased affinity was attributed to the substitution of Glu 16 by Val 16. Although the substitution probably caused an increased entropic cost to the helix region, the linker around Val 16 is more flexible resulting in the increase of affinity for the receptor.
引用
收藏
页码:816 / 821
页数:6
相关论文
共 50 条
  • [1] Distinct activation of GLP-1 receptor by exendin-4 and GLP-1
    Montrose-Rafizadeh, C
    Yang, H
    Pritchette, LA
    Eng, J
    DIABETES, 1998, 47 : A192 - A192
  • [2] Protection of the isolated rat heart by exendin-4, a GLP-1 receptor agonist
    Sonnel, David P.
    Engstrom, Thomas
    Treiman, Marek
    JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY, 2007, 42 : S182 - S182
  • [3] Differential structural properties of GLP-1 and exendin-4 determine their relative affinity for the GLP-1 receptor N-terminal extracellular domain
    Runge, Steffen
    Schimmer, Susann
    Oschmann, Jan
    Schiodt, Christine Bruun
    Knudsen, Sanne Moeller
    Jeppesen, Claus Bekker
    Madsen, Kjeld
    Lau, Jesper
    Thogersen, Henning
    Rudolph, Rainer
    BIOCHEMISTRY, 2007, 46 (19) : 5830 - 5840
  • [4] Exendin-4, a GLP-1 receptor agonist, stimulates rat pituitary-adrenocortical axis
    Malendowicz, LK
    Nowak, KW
    Nussdorfer, GG
    Zyterska, A
    Rebuffat, P
    Nowak, M
    BIOMEDICAL RESEARCH-TOKYO, 2001, 22 (06): : 273 - 276
  • [5] Expression and purification of exendin-4, a GLP-1 receptor agonist, in Escherichia coli
    Yin, XP
    Wei, DZ
    Yi, LN
    Tao, XY
    Ma, YS
    PROTEIN EXPRESSION AND PURIFICATION, 2005, 41 (02) : 259 - 265
  • [6] Exendin-4, a GLP-1 Receptor Agonist, Attenuates Prostate Cancer Growth
    Nomiyama, Takashi
    Kawanami, Takako
    Irie, Shinichiro
    Hamaguchi, Yuriko
    Terawaki, Yuichi
    Murase, Kunitaka
    Tsutsumi, Yoko
    Nagaishi, Ryoko
    Tanabe, Makito
    Morinaga, Hidetaka
    Tanaka, Tomoko
    Mizoguchi, Makio
    Nabeshima, Kazuki
    Tanaka, Masatoshi
    Yanase, Toshihiko
    DIABETES, 2014, 63 (11) : 3891 - 3905
  • [7] Cytoprotective effects of exendin-4, a GLP-1 receptor agonist, on the biliary epithelium
    Marzioni, M.
    Alpini, G.
    Saccomanno, S.
    Fava, G.
    Candelaresi, C.
    Rychlicki, C.
    Francis, H.
    Trozzi, L.
    Venter, J.
    Benedetti, A.
    JOURNAL OF HEPATOLOGY, 2008, 48 : S27 - S27
  • [8] Structure function analysis of exendin-4/GLP-1 analogs
    MontroseRafizadeh, C
    Yang, H
    Pritchette, LA
    Eng, J
    DIABETES, 1996, 45 : 553 - 553
  • [9] Vagal and Brain GLP-1 Receptor Populations Mediate the Hypophagic Effects of Peripheral GLP-1 Receptor Agonists, Liraglutide and Exendin-4
    Kanoski, Scott E.
    Fortin, Samantha
    Arnold, Myrtha
    Hayes, Matthew R.
    Grill, Harvey
    OBESITY, 2011, 19 : S48 - S48
  • [10] Brain activation following peripheral administration of the GLP-1 receptor agonist exendin-4
    Baraboi, Elena-Dana
    St-Pierre, David H.
    Shooner, Julie
    Timofeeva, Elena
    Richard, Denis
    AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY, 2011, 301 (04) : R1011 - R1024