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Synthesis and Biological Characterisation of Targeted Pro-Apoptotic Peptide.

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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https://www.hal.inserm.fr/inserm-00314521
Contributor : Amandine Hurbin <>
Submitted on : Wednesday, August 27, 2008 - 3:58:06 PM
Last modification on : Tuesday, November 17, 2020 - 8:42:05 AM

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Stéphanie Foillard, Zhao-Hui Jin, Elisabeth Garanger, Didier Boturyn, Marie-Christine Favrot, et al.. Synthesis and Biological Characterisation of Targeted Pro-Apoptotic Peptide.. ChemBioChem, Wiley-VCH Verlag, 2008, epub ahead of print. ⟨10.1002/cbic.200800327⟩. ⟨inserm-00314521⟩

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