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

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...

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Detalles Bibliográficos
Autores principales: Kour, Smit, Rana, Sandeep, Kizhake, Smitha, Lagundžin, Dragana, Klinkebiel, David, Mallareddy, Jayapal Reddy, Huxford, Tom, Woods, Nicholas T., Natarajan, Amarnath
Formato: Online Artículo Texto
Lenguaje:English
Publicado: RSC 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8729175/
https://www.ncbi.nlm.nih.gov/pubmed/35128406
http://dx.doi.org/10.1039/d1cb00183c
Descripción
Sumario: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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