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

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2006年 / 4卷 / 10期

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.

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页码：1958 / 1965

页数：8

相关论文

共 33 条

[21] Chemoselective pre-conjugate radiohalogenation of unprotected mono- and multimeric peptides via oxime formation [J].

Poethko, T ;

Schottelius, M ;

Thumshirn, G ;

Herz, M ;

Haubner, R ;

Henriksen, G ;

Kessler, H ;

Schwaiger, M ;

Wester, HJ .

RADIOCHIMICA ACTA, 2004, 92 (4-6) :317-327

[22] Chemoselectively template-assembled glycoconjugates as mimics for multivalent presentation of carbohydrates [J].

Renaudet, O ;

Dumy, P .

ORGANIC LETTERS, 2003, 5 (03) :243-246

[23]

Scheibler L, 1999, ANGEW CHEM INT EDIT, V38, P696, DOI 10.1002/(SICI)1521-3773(19990301)38:5<696::AID-ANIE696>3.0.CO

[24]

2-L

[25] Functionalisation of gold surfaces via topological templates [J].

Scheibler, L ;

Dumy, P ;

Stamou, D ;

Duschl, C ;

Vogel, H ;

Mutter, M .

TETRAHEDRON, 1998, 54 (15) :3725-3734

[26] Endothelial cells internalize and degrade RGD-modified proteins developed for tumor vasculature targeting [J].

Schraaa, AJ ;

Kok, RJ ;

Berendsen, AD ;

Moorlag, HE ;

Bos, EJ ;

Meijer, DKF ;

de Leij, LFMH ;

Molema, G .

JOURNAL OF CONTROLLED RELEASE, 2002, 83 (02) :241-251

[27] UNPROTECTED PEPTIDES AS BUILDING-BLOCKS FOR THE SYNTHESIS OF PEPTIDE DENDRIMERS WITH OXIME, HYDRAZONE, AND THIAZOLIDINE LINKAGES [J].

SHAO, J ;

TAM, JP .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1995, 117 (14) :3893-3899

[28] Preparation of a multitopic glycopeptide-oligonucleotide conjugate [J].

Singh, Y ;

Renaudet, O ;

Defrancq, E ;

Dumy, P .

ORGANIC LETTERS, 2005, 7 (07) :1359-1362

[29]

Smith Jeffrey W, 2003, Curr Opin Investig Drugs, V4, P741

[30] Multimeric cyclic RGD peptides as potential tools for tumor targeting: Solid-phase peptide synthesis and chemoselective oxime ligation [J].

Thumshirn, G ;

Hersel, U ;

Goodman, SL ;

Kessler, H .

CHEMISTRY-A EUROPEAN JOURNAL, 2003, 9 (12) :2717-2725

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