Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA
Literature Information
Publication Date
2021-10-28
DOI
10.1039/D1CB00183C
Impact Factor
0
Authors
Smit Kour, Sandeep Rana, Smitha Kizhake, David Klinkebiel, Jayapal Reddy Mallareddy, Tom Huxford
View Original
Abstract
Tumor necrosis factor (TNF) α-induced nuclear translocation of the NF-κB subunit RELA has been implicated in several pathological conditions. Here we report the discovery of a spirocyclic dimer (SpiD7) that covalently modifies RELA to inhibit TNFα-induced nuclear translocation. This is a previously unexplored strategy to inhibit TNFα-induced NF-κB activation.
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