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

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

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 indi...

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Bibliographic Details
Main Authors: Udin Bahrudin, Masaki Unno, Kazuya Nishio, Akiko Kita, Peili Li, Masaru Kato, Masashi Inoue, Shunichi Tsujitani, Takuto Murakami, Rina Sugiyama, Yasushi Saeki, Yuji Obara, Keiji Tanaka, Hiroshi Yamaguchi, Isao Sakane, Yasushi Kawata, Toshiyuki Itoh, Haruaki Ninomiya, Ichiro Hisatome, Yukio Morimoto
Format: Article
Language:English
Published: Nature Portfolio 2017-07-01
Series:Scientific Reports
Online Access:https://doi.org/10.1038/s41598-017-04652-2

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