@article{oai:repo.qst.go.jp:00045479, author = {Foillard, Stephanie and Jin, Zhao-Hui and et.al and 金 朝暉}, issue = {14}, journal = {Chembiochem}, month = {Aug}, note = {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 V 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 V 3 integrin-containing tumour cells.}, pages = {2326--2332}, title = {Synthesis and Biological Characterisation of Targeted Pro-Apoptotic Peptide}, volume = {9}, year = {2008} }