Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA.
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ABSTRACT:
SUBMITTER: Kour S
PROVIDER: S-EPMC8729175 | biostudies-literature | 2022 Jan
REPOSITORIES: biostudies-literature
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Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA.
Kour Smit S Rana Sandeep S Kizhake Smitha S Lagundžin Dragana D Klinkebiel David D Mallareddy Jayapal Reddy JR Huxford Tom T Woods Nicholas T NT Natarajan Amarnath A
RSC chemical biology 20211028 1
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. ...[more]
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