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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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
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author Kour, Smit
Rana, Sandeep
Kizhake, Smitha
Lagundžin, Dragana
Klinkebiel, David
Mallareddy, Jayapal Reddy
Huxford, Tom
Woods, Nicholas T.
Natarajan, Amarnath
author_facet Kour, Smit
Rana, Sandeep
Kizhake, Smitha
Lagundžin, Dragana
Klinkebiel, David
Mallareddy, Jayapal Reddy
Huxford, Tom
Woods, Nicholas T.
Natarajan, Amarnath
author_sort Kour, Smit
collection PubMed
description 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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spelling pubmed-87291752022-02-04 Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA Kour, Smit Rana, Sandeep Kizhake, Smitha Lagundžin, Dragana Klinkebiel, David Mallareddy, Jayapal Reddy Huxford, Tom Woods, Nicholas T. Natarajan, Amarnath RSC Chem Biol Chemistry 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. RSC 2021-10-28 /pmc/articles/PMC8729175/ /pubmed/35128406 http://dx.doi.org/10.1039/d1cb00183c Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/
spellingShingle Chemistry
Kour, Smit
Rana, Sandeep
Kizhake, Smitha
Lagundžin, Dragana
Klinkebiel, David
Mallareddy, Jayapal Reddy
Huxford, Tom
Woods, Nicholas T.
Natarajan, Amarnath
Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA
title Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA
title_full Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA
title_fullStr Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA
title_full_unstemmed Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA
title_short Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA
title_sort stapling proteins in the rela complex inhibits tnfα-induced nuclear translocation of rela
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8729175/
https://www.ncbi.nlm.nih.gov/pubmed/35128406
http://dx.doi.org/10.1039/d1cb00183c
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