Multivalent RGD synthetic peptides as potent αVβ3 integrin ligands

被引:76
作者
Garanger, E
Boturyn, D
Coll, JL
Favrot, MC
Dumy, P
机构
[1] Univ Grenoble 1, CNRS, LEDSS, UMR 5616, F-38041 Grenoble 9, France
[2] Inst Albert Bonniot, INSERM, U578, Grp Rech Canc Poumon, F-38706 La Tronche, France
关键词
D O I
10.1039/b517706e
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We study herein the multivalency effect of a cluster of alpha(v)beta(3)-ligands held on a cyclodecapeptide template. An array of RAFT(c[-RGDfK-])(n) derivatives containing from one to sixteen clustered RGD motifs were synthesized and comparatively assayed in vitro on alpha(v)beta(3)-expressing cells. Efficient inhibition of the alpha(v)beta(3)-specific 23C6 monoclonal antibody fixation was observed with ligands displaying three and four copies of the cyclo[-RGDfK-] peptide.
引用
收藏
页码:1958 / 1965
页数:8
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