Water-Soluble closo-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy
| Autor: | Taiki Morita, Fumiko Nakagawa, Hiroyuki Nakamura, Hidehisa Kawashima |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Boron Compounds
closo-dodecaborate Cell chemistry.chemical_element Nanoconjugates 02 engineering and technology Endocytosis folate 01 natural sciences Article HeLa Folic Acid Neoplasms medicine Humans FRα Cytotoxicity Boron lcsh:QH301-705.5 biology 010405 organic chemistry Chemistry Folate Receptors GPI-Anchored water-soluble General Medicine 021001 nanoscience & nanotechnology biology.organism_classification 0104 chemical sciences Neutron capture medicine.anatomical_structure lcsh:Biology (General) A549 Cells Folate receptor boron neutron capture therapy Cancer research 0210 nano-technology HeLa Cells Protein Binding Conjugate |
| Zdroj: | Cells Volume 9 Issue 7 Cells, Vol 9, Iss 1615, p 1615 (2020) |
| ISSN: | 2073-4409 |
| DOI: | 10.3390/cells9071615 |
| Popis: | Water-soluble pteroyl-closo-dodecaborate conjugates (PBCs 1&ndash 4), were developed as folate receptor (FR&alpha ) targeting boron carriers for boron neutron capture therapy (BNCT). PBCs 1&ndash 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&ndash 3 showed significant cell uptake by FR&alpha positive cells, especially U87MG glioblastoma cells, although the accumulation of PBC 4 was low compared with PBCs 1&ndash 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&ndash 3 are primarily through FR&alpha receptor-mediated endocytosis. |
| Databáze: | OpenAIRE |
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