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

Smit Kour, Sandeep Rana, Smitha Kizhake, Dragana Lagundžin, David Klinkebiel, Jayapal Reddy Mallareddy, Tom Huxford, Nicholas T. Woods, Amarnath Natarajan

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)32-36
Number of pages5
JournalRSC Chemical Biology
Volume3
Issue number1
DOIs
StatePublished - Jan 2022

ASJC Scopus subject areas

  • Chemistry (miscellaneous)
  • Biochemistry
  • Molecular Biology
  • Biochemistry, Genetics and Molecular Biology (miscellaneous)

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