The two tripeptide sequences, arginine-glycine-aspartic acid (RGD) and asparagine-glycine-arginine (NGR) motifs have been identified based on phage display studies and they have been used widely in the field of targeted drug delivery. RGD is a well-known peptide sequence for targeting integrin receptors and can bind to avβ3 and avβ5 integrin receptors subunits, which are overexpressed in the angiogenesis process of cancer cells. Because av integrin is overexpressed on the surface of cancer cells, an integrin ligand can be used as a targeting system for cancer treatment. RGD peptide conjugated with cytotoxic agents (RGD-drug conjugates) is likely to exhibit a tumor-targeting and thus antiangiogenic synergetic effect. During the last few years, a number of RGD-cytotoxic drugs have been developed and showed promising activities in vitro and in vivo. Conjugation of camptothecin with RGD is an example for improving the therapeutic index of an antitumoral drug.[20c] Synthesis of dimeric RGD peptide-paclitaxel conjugate is another successful example of targeted drug delivery. Other motif that has been used for tumor targeting is NGR tripeptide. This sequence can bind to CD13 that is specially overexpressed in tumor blood vessels and is involved in angiogenesis, invasion, and metastasis. Because RGD is a peptide tag which targets the process of angiogenesis and NGR also targets tumor blood vessels, we decided to synthesize the conjugated forms of two famous NSAIDs, naproxen, and ibuprofen, with these two tripeptides. To investigate the impact of possible steric hindrance due to the attachment of the drug to the peptide, a linear six-carbon segment (hexanoic acid) was also used as a spacer.

The two tripeptide sequences, arginine-glycine-aspartic acid (RGD) and asparagine-glycine-arginine (NGR) motifs have been identified based on phage display studies and they have been used widely in the field of targeted drug delivery. RGD is a well-known peptide sequence for targeting integrin receptors and can bind to avβ3 and avβ5 integrin receptors subunits, which are overexpressed in the angiogenesis process of cancer cells. Because av integrin is overexpressed on the surface of cancer cells, an integrin ligand can be used as a targeting system for cancer treatment. RGD peptide conjugated with cytotoxic agents (RGD-drug conjugates) is likely to exhibit a tumor-targeting and thus antiangiogenic synergetic effect. During the last few years, a number of RGD-cytotoxic drugs have been developed and showed promising activities in vitro and in vivo. Conjugation of camptothecin with RGD is an example for improving the therapeutic index of an antitumoral drug.[20c] Synthesis of dimeric RGD peptide-paclitaxel conjugate is another successful example of targeted drug delivery. Other motif that has been used for tumor targeting is NGR tripeptide. This sequence can bind to CD13 that is specially overexpressed in tumor blood vessels and is involved in angiogenesis, invasion, and metastasis. Because RGD is a peptide tag which targets the process of angiogenesis and NGR also targets tumor blood vessels, we decided to synthesize the conjugated forms of two famous NSAIDs, naproxen, and ibuprofen, with these two tripeptides. To investigate the impact of possible steric hindrance due to the attachment of the drug to the peptide, a linear six-carbon segment (hexanoic acid) was also used as a spacer.

The two tripeptide sequences, arginine-glycine-aspartic acid (RGD) and asparagine-glycine-arginine (NGR) motifs have been identified based on phage display studies and they have been used widely in the field of targeted drug delivery. RGD is a well-known peptide sequence for targeting integrin receptors and can bind to avβ3 and avβ5 integrin receptors subunits, which are overexpressed in the angiogenesis process of cancer cells. Because av integrin is overexpressed on the surface of cancer cells, an integrin ligand can be used as a targeting system for cancer treatment. RGD peptide conjugated with cytotoxic agents (RGD-drug conjugates) is likely to exhibit a tumor-targeting and thus antiangiogenic synergetic effect. During the last few years, a number of RGD-cytotoxic drugs have been developed and showed promising activities in vitro and in vivo. Conjugation of camptothecin with RGD is an example for improving the therapeutic index of an antitumoral drug.[20c] Synthesis of dimeric RGD peptide-paclitaxel conjugate is another successful example of targeted drug delivery. Other motif that has been used for tumor targeting is NGR tripeptide. This sequence can bind to CD13 that is specially overexpressed in tumor blood vessels and is involved in angiogenesis, invasion, and metastasis. Because RGD is a peptide tag which targets the process of angiogenesis and NGR also targets tumor blood vessels, we decided to synthesize the conjugated forms of two famous NSAIDs, naproxen, and ibuprofen, with these two tripeptides. To investigate the impact of possible steric hindrance due to the attachment of the drug to the peptide, a linear six-carbon segment (hexanoic acid) was also used as a spacer.

The two tripeptide sequences, arginine-glycine-aspartic acid (RGD) and asparagine-glycine-arginine (NGR) motifs have been identified based on phage display studies and they have been used widely in the field of targeted drug delivery. RGD is a well-known peptide sequence for targeting integrin receptors and can bind to avβ3 and avβ5 integrin receptors subunits, which are overexpressed in the angiogenesis process of cancer cells. Because av integrin is overexpressed on the surface of cancer cells, an integrin ligand can be used as a targeting system for cancer treatment. RGD peptide conjugated with cytotoxic agents (RGD-drug conjugates) is likely to exhibit a tumor-targeting and thus antiangiogenic synergetic effect. During the last few years, a number of RGD-cytotoxic drugs have been developed and showed promising activities in vitro and in vivo. Conjugation of camptothecin with RGD is an example for improving the therapeutic index of an antitumoral drug.[20c] Synthesis of dimeric RGD peptide-paclitaxel conjugate is another successful example of targeted drug delivery. Other motif that has been used for tumor targeting is NGR tripeptide. This sequence can bind to CD13 that is specially overexpressed in tumor blood vessels and is involved in angiogenesis, invasion, and metastasis. Because RGD is a peptide tag which targets the process of angiogenesis and NGR also targets tumor blood vessels, we decided to synthesize the conjugated forms of two famous NSAIDs, naproxen, and ibuprofen, with these two tripeptides. To investigate the impact of possible steric hindrance due to the attachment of the drug to the peptide, a linear six-carbon segment (hexanoic acid) was also used as a spacer.