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  1. 教員研究業績
  2. 薬化学研究室
  1. 教員研究業績
  2. 薬化学研究室
  3. 原著論文

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/13450
ae6033da-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

WEKO 21754

Isono, Aoi

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Tsuji, Mieko

× Tsuji, Mieko

WEKO 21755

Tsuji, Mieko

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Sanada, Yu

× Sanada, Yu

WEKO 21756

Sanada, Yu

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Matsushita, Akari

× Matsushita, Akari

WEKO 21757

Matsushita, Akari

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Masunaga, Shinichiro

× Masunaga, Shinichiro

WEKO 21758

Masunaga, Shinichiro

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Hirayama, Tasuku

× Hirayama, Tasuku

WEKO 21759

Hirayama, Tasuku

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Nagasawa, Hideko

× Nagasawa, Hideko

WEKO 21760

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
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
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