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- Title
Water-Soluble closo-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy.
- Authors
Nakagawa, Fumiko; Kawashima, Hidehisa; Morita, Taiki; Nakamura, Hiroyuki
- Abstract
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.
- Subjects
BORON-neutron capture therapy; FOLIC acid; ENDOCYTOSIS; HELA cells
- Publication
Cells (2073-4409), 2020, Vol 9, Issue 7, p1615
- ISSN
2073-4409
- Publication type
Article
- DOI
10.3390/cells9071615