A structure-based designed small molecule depletes hRpn13Pru and a select group of KEN box proteins

A structure-based designed small molecule depletes hRpn13Pru and a select group of KEN box proteins

Abstract Proteasome subunit hRpn13 is partially proteolyzed in certain cancer cell types to generate hRpn13Pru by degradation of its UCHL5/Uch37-binding DEUBAD domain and retention of an intact proteasome- and ubiquitin-binding Pru domain. By using structure-guided virtual screening, we identify an...

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Main Authors: Xiuxiu Lu, Monika Chandravanshi, Venkata R. Sabbasani, Snehal Gaikwad, V. Keith Hughitt, Nana Gyabaah-Kessie, Bradley T. Scroggins, Sudipto Das, Wazo Myint, Michelle E. Clapp, Charles D. Schwieters, Marzena A. Dyba, Derek L. Bolhuis, Janusz W. Koscielniak, Thorkell Andresson, Michael J. Emanuele, Nicholas G. Brown, Hiroshi Matsuo, Raj Chari, Deborah E. Citrin, Beverly A. Mock, Rolf E. Swenson, Kylie J. Walters
Format: Article
Language:English
Published: Nature Portfolio 2024-03-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-024-46644-7
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