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  • Title: Synthesis and activity of a folate targeted monodisperse PEG camptothecin conjugate.
    Author: Henne WA, Kularatne SA, Hakenjos J, Carron JD, Henne KL.
    Journal: Bioorg Med Chem Lett; 2013 Nov 01; 23(21):5810-3. PubMed ID: 24064501.
    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 6nM. Importantly, activity of the prodrug was blocked by excess folate, demonstrating receptor-mediated celluar uptake of the PEG conjugate.
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