Inhibitory effects of local anesthetics on the proteasome and their biological actions

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 tha...

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Detalles Bibliográficos
Autores principales: Bahrudin, Udin, Unno, Masaki, Nishio, Kazuya, Kita, Akiko, Li, Peili, Kato, Masaru, Inoue, Masashi, Tsujitani, Shunichi, Murakami, Takuto, Sugiyama, Rina, Saeki, Yasushi, Obara, Yuji, Tanaka, Keiji, Yamaguchi, Hiroshi, Sakane, Isao, Kawata, Yasushi, Itoh, Toshiyuki, Ninomiya, Haruaki, Hisatome, Ichiro, Morimoto, Yukio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5506043/
https://www.ncbi.nlm.nih.gov/pubmed/28698635
http://dx.doi.org/10.1038/s41598-017-04652-2

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