Selection of peptide ligands binding to fibroblast growth factor receptor 1

被引:18
作者
Fan, HK
Duan, YF
Zhou, H [1 ]
Li, W
Li, F
Guo, LL
Roeske, RW
机构
[1] Jilin Univ, Coll Life Sci, Changchun 130023, Peoples R China
[2] Jilin Univ, Minist Educ, Key Lab Supramol Struct & Spect, Changchun 130023, Peoples R China
[3] Indiana Univ, Sch Med, Dept Biochem & Mol Biol, Indianapolis, IN 46202 USA
关键词
FGFR1; ligands; phage display library; synthetic peptide;
D O I
10.1080/15216540214308
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
Inappropriate expression of fibroblast growth factors (FGFs) or activation of FGF receptors (FGFRs) could contribute to several human angiogenic pathologies. In an attempt to design antagonists of FGF, we developed a screening procedure for identifying peptide ligands binding to FGFR1. To retain the natural conformation of FGFR1 during screening, we expressed recombinant FGFR1 on the surface of Sf9 insect cells. A 6-mer phage display peptide library was then screened on the cell surface and a group of hydrophobic peptide sequences were identified. Further experiments demonstrated that the phages displaying these sequences can specifically bind to FGFR1. The docking analysis suggests that the peptide ValTyrMetSerProPhe can specifically bind to the hydrophobic surface of FGFR1. The synthetic peptide Ac-ValTyrMetSerProPheNH(2) can inhibit mitogenic activity of aFGF and has the potential to become a therapeutic agent as an aFGF antagonist.
引用
收藏
页码:67 / 72
页数:6
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