Synthesis and activity of a folate targeted monodisperse PEG camptothecin conjugate
WA Henne, SA Kularatne, J Hakenjos… - Bioorganic & medicinal …, 2013 - Elsevier
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 IC 50 of 6 nM. Importantly, activity of
the prodrug was blocked by excess folate, demonstrating receptor-mediated celluar uptake
of the PEG conjugate.
using a monodisperse PEG spacer linked to folate via a releasable disulfide carbonate
linker. Cell cytotoxicity in human KB cells exhibited an IC 50 of 6 nM. Importantly, activity of
the prodrug was blocked by excess folate, demonstrating receptor-mediated celluar uptake
of the PEG conjugate.
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