Water-Soluble <i>closo</i>-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy
Water-soluble pteroyl-<i>closo</i>-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 IC<sub>50</sub> values in the range of 1~3 mM toward...
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MDPI AG
2020-07-01
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| Series: | Cells |
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| Online Access: | https://www.mdpi.com/2073-4409/9/7/1615 |
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| author | Fumiko Nakagawa Hidehisa Kawashima Taiki Morita Hiroyuki Nakamura |
| author_facet | Fumiko Nakagawa Hidehisa Kawashima Taiki Morita Hiroyuki Nakamura |
| author_sort | Fumiko Nakagawa |
| collection | DOAJ |
| description | Water-soluble pteroyl-<i>closo</i>-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 IC<sub>50</sub> 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. |
| first_indexed | 2024-03-10T18:42:01Z |
| format | Article |
| id | doaj.art-e9114f2dce384c908e468000f8d4bddc |
| institution | Directory Open Access Journal |
| issn | 2073-4409 |
| language | English |
| last_indexed | 2024-03-10T18:42:01Z |
| publishDate | 2020-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Cells |
| spelling | doaj.art-e9114f2dce384c908e468000f8d4bddc2023-11-20T05:46:52ZengMDPI AGCells2073-44092020-07-0197161510.3390/cells9071615Water-Soluble <i>closo</i>-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture TherapyFumiko Nakagawa0Hidehisa Kawashima1Taiki Morita2Hiroyuki Nakamura3School of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, JapanLaboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, JapanLaboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, JapanSchool of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, JapanWater-soluble pteroyl-<i>closo</i>-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 IC<sub>50</sub> 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.https://www.mdpi.com/2073-4409/9/7/1615boron neutron capture therapyfolateFRα<i>closo</i>-dodecaboratewater-soluble |
| spellingShingle | Fumiko Nakagawa Hidehisa Kawashima Taiki Morita Hiroyuki Nakamura Water-Soluble <i>closo</i>-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy Cells boron neutron capture therapy folate FRα <i>closo</i>-dodecaborate water-soluble |
| title | Water-Soluble <i>closo</i>-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy |
| title_full | Water-Soluble <i>closo</i>-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy |
| title_fullStr | Water-Soluble <i>closo</i>-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy |
| title_full_unstemmed | Water-Soluble <i>closo</i>-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy |
| title_short | Water-Soluble <i>closo</i>-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy |
| title_sort | water soluble i closo i docecaborate containing pteroyl derivatives targeting folate receptor positive tumors for boron neutron capture therapy |
| topic | boron neutron capture therapy folate FRα <i>closo</i>-dodecaborate water-soluble |
| url | https://www.mdpi.com/2073-4409/9/7/1615 |
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