A major challenge in the application of cytotoxic anti-cancer drugs is their general lack of selectivity, which often leads to systematic toxicity due to their inability to discriminate between malignant and healthy cells. A particularly promising target for selective targeting are the folate receptors (FR) that are often over-expressed on cancer cells. Here, we report on a conjugate of the pentadentate nitrogen ligand N4Py to folic acid, via a cleavable disulphide linker, which shows selective cytotoxicity against folate receptor expressing cancer cells.
Geersing, A., de Vries, R. H., Jansen, G., Rots, M. G., & Roelfes, G. (2019). Folic acid conjugates of a bleomycin mimic for selective targeting of folate receptor positive cancer cells. Bioorganic and Medicinal Chemistry Letters, 29(15), 1922-1927. https://doi.org/10.1016/j.bmcl.2019.05.047