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dc.contributor.author | Bahrudin, Udin | en |
dc.contributor.author | Unno, Masaki | en |
dc.contributor.author | Nishio, Kazuya | en |
dc.contributor.author | Kita, Akiko | en |
dc.contributor.author | Li, Peili | en |
dc.contributor.author | Kato, Masaru | en |
dc.contributor.author | Inoue, Masashi | en |
dc.contributor.author | Tsujitani, Shunichi | en |
dc.contributor.author | Murakami, Takuto | en |
dc.contributor.author | Sugiyama, Rina | en |
dc.contributor.author | Saeki, Yasushi | en |
dc.contributor.author | Obara, Yuji | en |
dc.contributor.author | Tanaka, Keiji | en |
dc.contributor.author | Yamaguchi, Hiroshi | en |
dc.contributor.author | Sakane, Isao | en |
dc.contributor.author | Kawata, Yasushi | en |
dc.contributor.author | Itoh, Toshiyuki | en |
dc.contributor.author | Ninomiya, Haruaki | en |
dc.contributor.author | Hisatome, Ichiro | en |
dc.contributor.author | Morimoto, Yukio | en |
dc.contributor.alternative | 西尾, 和也 | ja |
dc.contributor.alternative | 喜田, 昭子 | ja |
dc.contributor.alternative | 森本, 幸生 | ja |
dc.date.accessioned | 2017-11-14T05:52:34Z | - |
dc.date.available | 2017-11-14T05:52:34Z | - |
dc.date.issued | 2017-07-11 | - |
dc.identifier.issn | 2045-2322 | - |
dc.identifier.uri | http://hdl.handle.net/2433/227889 | - |
dc.description.abstract | Local anesthetics (LAs) inhibit endoplasmic reticulum-associated protein degradation, however the mechanisms remain elusive. Here, we show that the clinically used LAs pilsicainide and lidocaine bind directly to the 20S proteasome and inhibit its activity. Molecular dynamic calculation indicated that these LAs were bound to the β5 subunit of the 20S proteasome, and not to the other active subunits, β1 and β2. Consistently, pilsicainide inhibited only chymotrypsin-like activity, whereas it did not inhibit the caspase-like and trypsin-like activities. In addition, we confirmed that the aromatic ring of these LAs was critical for inhibiting the proteasome. These LAs stabilized p53 and suppressed proliferation of p53-positive but not of p53-negative cancer cells. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Springer Nature | en |
dc.rights | © The Author(s) 2017. | en |
dc.rights | This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. | en |
dc.subject | Drug development | en |
dc.subject | Molecular modelling | en |
dc.title | Inhibitory effects of local anesthetics on the proteasome and their biological actions | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.jtitle | Scientific Reports | en |
dc.identifier.volume | 7 | - |
dc.relation.doi | 10.1038/s41598-017-04652-2 | - |
dc.textversion | publisher | - |
dc.identifier.artnum | 5079 | - |
dc.identifier.pmid | 28698635 | - |
dcterms.accessRights | open access | - |
dc.identifier.eissn | 2045-2322 | - |
出現コレクション: | 学術雑誌掲載論文等 |
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