197151-79-4Relevant articles and documents
Water-soluble closo-docecaborate-containing pteroyl derivatives targeting folate receptor-positive tumors for boron neutron capture therapy
Nakagawa, Fumiko,Kawashima, Hidehisa,Morita, Taiki,Nakamura, Hiroyuki
, p. 1 - 9 (2020)
Water-soluble pteroyl-closo-dodecaborate conjugates (PBCs 1–4), were developed as folate receptor (FRα) targeting boron carriers for boron neutron capture therapy (BNCT). PBCs 1–4 had adequately low cytotoxicity with IC50 values in the range of 1~3 mM toward selected human cancer cells, low enough to use as BNCT boron agents. PBCs 1–3 showed significant cell uptake by FRα positive cells, especially U87MG glioblastoma cells, although the accumulation of PBC 4 was low compared with PBCs 1–3 and L-4-boronophenylalanine (L-BPA). The cellular uptake of PBC 1 and PBC 3 by HeLa cells was arrested by increasing the concentration of folate in the medium, indicating that the major uptake mechanisms of PBC 1–3 are primarily through FRα receptor-mediated endocytosis.
Folic acid conjugates of a bleomycin mimic for selective targeting of folate receptor positive cancer cells
Geersing, Arjan,de Vries, Reinder H.,Jansen, Gerrit,Rots, Marianne G.,Roelfes, Gerard
supporting information, p. 1922 - 1927 (2019/06/05)
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.
The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting
Guo, Hongjuan,Xie, Fang,Zhu, Meilin,Li, Yan,Yang, Zhi,Wang, Xuebin,Lu, Jie
, p. 2025 - 2029 (2011/05/02)
Aiming to develop a new 99mTc-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free α-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was
