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Updated: Jul 2, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
Published on: June 30, 2013
Synthesis and biological characterisation of targeted pro-apoptotic peptide
Stéphanie Foillard1, Zhao-hui Jin, Elisabeth Garanger
1Département de Chimie Moléculaire, UMR CNRS-UJF 5250, ICMG FR 2607, 301, rue de la chimie, BP 53, FR 38041 Grenoble Cedex 9, France.
Abstract:
We report herein the synthesis and in vitro assay of new, multimeric RGD-peptide conjugates for cell-targeted drug delivery. We generated a peptide scaffold comprising two functional domains, one a tumour blood vessel "homing" motif and the other a programmed cell-death-inducing peptide sequence. RGD peptides were selected to direct the molecular conjugate to alpha(V)beta(3) integrin-containing tumour cells. The pro-apoptotic (Lys-Leu-Ala-Lys-Leu-Ala-Lys)(2) peptide was found to be nontoxic outside cells, but toxic when internalized into targeted cells as it disrupted the mitochondrial membrane. The synthesis of these targeted pro-apoptotic conjugates was carried out by assembling three different units (that is, scaffold, RGD units and pro-apoptotic peptide) through chemoselective ligations. We show that one compound displays significant biological effect in alpha(V)beta(3) integrin-containing tumour cells.
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