Abstract
Combination of RGD cell adhesion peptide with GHK cell modulator peptide synergistically improves targeting of tumor cells. Amphiphilic peptides can be effectively displayed on liposomal surface for peptide screening and drug delivery applications.
Highlights
Modification of both plain and formulated drugs with targeting ligands is an attractive approach to enhance delivery into cancer cells/tissues, reduce therapeutic doses/side effects and improve treatment of multi-drug resistant (MDR) tumors.[4,5] Oligopeptides are one of the most powerful molecular tools for tumor targeting by virtue of their natural specificity and potential safety in addition to higher availability and stability compared to full-length proteins such as antibodies
The amphiphilic peptides C12-GGRGD-NH2 and C12-GGGHK-NH2 (Fig. 1) synthesized by the Fmoc solid-phase peptide synthesis (SPPS) method consisted of RGD and GHK bioactive motifs, a diglycyl spacer and a lauric acid (C12) residue
RGD/GHK mixed micelles induced ca. 3-fold higher fluorescence of the probe than the singlepeptide systems attributed to additional electrostatic interactions of the peptide moieties, which does not significantly promote the unimer–micelle transition compared with RGD alone (Fig. S1, Electronic supplementary information (ESI)†)
Summary
Modification of both plain and formulated drugs with targeting ligands is an attractive approach to enhance delivery into cancer cells/tissues, reduce therapeutic doses/side effects and improve treatment of MDR tumors.[4,5] Oligopeptides are one of the most powerful molecular tools for tumor targeting by virtue of their natural specificity and potential safety in addition to higher availability and stability compared to full-length proteins such as antibodies. Molecular biology and in silico techniques can be used to identify cancer-specific peptide sequences,[6] whereas solid-phase peptide synthesis (SPPS) methods provide effective production as well as on-resin derivatization of the sequence of interest for drug development purposes.[7]. The state of the art in cancer-specific oligopeptides and their applications is considered in recent reviews.[6,8,9] Distinct tumor targeting can be provided by the simplest peptide sequences from extracellular matrix (ECM) components carrying different cell-adhesive peptide motifs.
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