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Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
Published on: April 25, 2025
Synthesis and activity of a folate targeted monodisperse PEG camptothecin conjugate
Walter A Henne1, Sumith A Kularatne, John Hakenjos
1Division of Science, Governors State University, 1 University Parkway, University Park, IL 60484, USA.
Bioorganic & Medicinal Chemistry Letters
|September 26, 2013
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.
