Synthesis and activity of a folate peptide camptothecin prodrug |
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| Authors: | Henne Walter A Doorneweerd Derek D Hilgenbrink Andrew R Kularatne Sumith A Low Philip S |
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| Affiliation: | Department of Chemistry and Purdue Cancer Center, Purdue University, West Lafayette, IN 47907, USA. |
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| Abstract: | A folate receptor targeted camptothecin prodrug was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate linker. The conjugate was found to possess high affinity for folate receptor-expressing cells and inhibited cell proliferation in human KB cells with an IC(50) of 10nM. Activity of the prodrug was completely blocked by excess folic acid, demonstrating receptor-mediated uptake. |
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