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...

Full description

Saved in:
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:EN
Published: Nature Portfolio 2017
Subjects:
R
Q
Online Access:https://doaj.org/article/f5cdc61bc8ea4f0a8fc5652c9651c68c
Tags: Add Tag
No Tags, Be the first to tag this record!