多价RGD合成肽作为有效的αVβ3整合素配体。
Multivalent RGD synthetic peptides as potent alphaVbeta3 integrin ligands.
作者信息
Garanger Elisabeth, Boturyn Didier, Coll Jean-Luc, Favrot Marie-Christine, Dumy Pascal
机构信息
Ingénierie Moléculaire et Chimie Bioorganique, LEDSS, CNRS UMR 5616, ICMG FR 2607, Université Joseph Fourier, BP 53, 38041 Grenoble Cedex 9, France.
出版信息
Org Biomol Chem. 2006 May 21;4(10):1958-65. doi: 10.1039/b517706e. Epub 2006 Apr 3.
We study herein the multivalency effect of a cluster of alphaVbeta3-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 alphaVbeta3-expressing cells. Efficient inhibition of the alphaVbeta3-specific 23C6 monoclonal antibody fixation was observed with ligands displaying three and four copies of the cyclo[-RGDfK-] peptide.
我们在此研究了固定在环十肽模板上的一组αVβ3配体的多价效应。合成了一系列含有1至16个成簇RGD基序的RAFT(c[-RGDfK-])n衍生物，并在表达αVβ3的细胞上进行了体外比较测定。观察到展示三个和四个环[-RGDfK-]肽拷贝的配体对αVβ3特异性23C6单克隆抗体固定有有效抑制作用。
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