Design, Synthesis and Biological Evaluation of Ketoprofen Conjugated To RGD/NGR for Targeted Cancer Therapy
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Abstract:
It is well known that Arginine-Glycine-Aspartic acid (RGD) and Asparagine-Glycine-Arginine (NGR) peptides preferentially bind to integrin receptors and aminopeptidase Nrespectively and these two receptors play important roles in angiogenesis. Therefore ketoprofenas a non-selective cox Inhibitor was conjugated with linear RGD and NGR to take advantageof targeting capability of these two motifs and delivering ketoprofen to these cancer cellswith overexpression of integrin and aminopeptidase N. In order to investigate the impact ofpossible steric hindrance due to the attachment of the drug to the peptide, a linear six carbon(hexanoic acid) linker was also used as a spacer. Cytotoxic effect of the synthesized compoundswas evaluated against a group of cancer cell lines, including MCF-7, A2780 (αvβ3 positive),OVCAR3 (high αvβ3), HT-1-80 (high CD13) and SKOV-3 (CD13 positive). Both NGR andRGD conjugated forms of ketoprofen showed higher cytotoxic activity against OVCAR3 andHT-1-80 respectively.
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Journal title
volume 17 issue 4
pages 1297- 1305
publication date 2018-10-01
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