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Synthesis and activity of a folate targeted monodisperse PEG camptothecin conjugate |
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| Authors: | Walter A. Henne Sumith A. Kularatne John Hakenjos Joshua D. Carron Kristene L. Henne |
| Affiliation: | 1. Division of Science, Governors State University, 1 University Parkway, University Park, IL 60484, USA;2. On Target Laboratories, 1281 Win Hentschel Blvd., West Lafayette, IN 47906, USA;3. Argonne National Laboratories, 9700 South Cass Ave, Lemont, IL 60439, USA |
| Abstract: | A folate targeted camptothecin small molecule drug conjugate (SMDC) was synthesized using a monodisperse PEG spacer linked to folate via a releasable disulfide carbonate linker. Cell cytotoxicity in human KB cells exhibited an IC50 of 6 nM. Importantly, activity of the prodrug was blocked by excess folate, demonstrating receptor-mediated celluar uptake of the PEG conjugate. |
| Keywords: | Monodisperse PEG PEG Folate conjugate Small molecule drug conjugate SMDC Camptothecin |
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