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Design, Synthesis, and Evaluation of Lipopeptide Conjugates of Mercaptoundecahydrododecaborate for Boron Neutron Capture Therapy
https://gifu-pu.repo.nii.ac.jp/records/13450
https://gifu-pu.repo.nii.ac.jp/records/13450ae6033da-82ce-4179-a5cd-041fe5ed69f7
| Item type | 一般雑誌記事 / Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2019-03-04 | |||||
| タイトル | ||||||
| タイトル | Design, Synthesis, and Evaluation of Lipopeptide Conjugates of Mercaptoundecahydrododecaborate for Boron Neutron Capture Therapy | |||||
| 言語 | en | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Isono, Aoi
× Isono, Aoi× Tsuji, Mieko× Sanada, Yu× Matsushita, Akari× Masunaga, Shinichiro× Hirayama, Tasuku× Nagasawa, Hideko |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | We developed new 10B carriers for boron neutron capture therapy (BNCT) that can effectively transport and accumulate boron clusters into cells. These carriers consist of lipopeptide, mercaptoundecahydrododecaborate (BSH) and a disulfide linker. The carriers were conceived according to the structure of pepducine, a membrane‐penetrating lipopeptide targeting protease‐activated receptor 1 (PAR1). To improve the membrane permeability of BSH, the structure was optimised using various lipopeptides possessing different peptides and lipid moieties. These synthesised lipopeptides were conjugated with BSH and evaluated for intracellular uptake using T98G glioblastoma cells. Among them, the most effectively incorporated and accumulated in the cells was compound 5a, which has a peptide of 13 residues derived from the intracellular third loop of PAR1 and a palmitoyl group. For further improvement of 10B accumulation in cells, the introduction of an amine linker was investigated; an intracellular uptake comparable to 5a was found for compound 14, which has a piperazine linker. Compound 5a and compound 14 both showed a stronger radio‐sensitising effect than BSH on T98G cells under mixed‐neutron beam irradiation. The results demonstrate that lipopeptide conjugation is apparently effective for enhancing intracellular delivery and accumulation of BSH and improving the cytotoxic effect of BNCT. | |||||
| 書誌情報 |
en : ChemMedChem 発行日 2019 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 18607179 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1002/cmdc.201800793 | |||||
