Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

Bioorganic & Medicinal Chemistry Letters
Shudong WangPeter M Fischer

Abstract

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]-NH(2)3b and paclitaxel-2'-pAntp[52-58]-NH(2)3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8h under cell culture conditions. The drug-peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.

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Citations

May 25, 2013·International Journal of Pharmaceutics·Silvia ArpiccoLuigi Cattel
Sep 6, 2007·Journal of Peptide Science : an Official Publication of the European Peptide Society·Serafim PapasVassilios Tsikaris
Oct 19, 2013·Bioconjugate Chemistry·Simona MuraPatrick Couvreur
Aug 27, 2011·Bioorganic & Medicinal Chemistry·Shunzi LiKathlynn C Brown

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