Structure-function analyses of candidate small molecule RPN13 inhibitors with antitumor properties.

Structure-function analyses of candidate small molecule RPN13 inhibitors with antitumor properties.

We sought to design ubiquitin-proteasome system inhibitors active against solid cancers by targeting ubiquitin receptor RPN13 within the proteasome's 19S regulatory particle. The prototypic bis-benzylidine piperidone-based inhibitor RA190 is a michael acceptor that adducts Cysteine 88 of RPN13....

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Main Authors: Ravi K Anchoori, Marietta Tan, Ssu-Hsueh Tseng, Shiwen Peng, Ruey-Shyang Soong, Aliyah Algethami, Palmer Foran, Samarjit Das, Chenguang Wang, Tian-Li Wang, Hong Liang, Chien-Fu Hung, Richard B S Roden
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2020-01-01
Series:PLoS ONE
Online Access:https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0227727&type=printable

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