Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin
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Synthesis of paclitaxel–penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel–2′-pAntp[43–58]-NH23b and paclitaxel–2′-pAntp[52–58]-NH23c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug–peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.
Wang, S., et al. 2006. Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin. Bioorganic and Medicinal Chemistry Letters. 16(10): pp.2628-2631. Available from http://dx.doi.org/10.1016/j.bmcl.2006.02.035