Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA.

Smit KourSandeep RanaSmitha KizhakeDragana LagundžinDavid KlinkebielJayapal Reddy MallareddyTom HuxfordNicholas T WoodsAmarnath Natarajan

Published in: RSC chemical biology (2021)

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.

Keyphrases

rheumatoid arthritis
high glucose
diabetic rats
signaling pathway
oxidative stress
drug induced
endothelial cells
immune response