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

doi:10.1039/d1cb00183c

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 journal › Article › peer-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 language	English (US)
Pages (from-to)	32-36
Number of pages	5
Journal	RSC Chemical Biology
Volume	3
Issue number	1
DOIs	https://doi.org/10.1039/d1cb00183c
State	Published - Jan 2022

ASJC Scopus subject areas

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

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10.1039/d1cb00183c

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title = "Stapling proteins in the RELA complex inhibits TNFα-induced nuclear translocation of RELA",

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.",

author = "Smit Kour and Sandeep Rana and Smitha Kizhake and Dragana Lagund{\v z}in and David Klinkebiel and Mallareddy, {Jayapal Reddy} and Tom Huxford and Woods, {Nicholas T.} and Amarnath Natarajan",

note = "Publisher Copyright: {\textcopyright} The Royal Society of Chemistry.",

year = "2022",

month = jan,

doi = "10.1039/d1cb00183c",

language = "English (US)",

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AU - Kour, Smit

AU - Rana, Sandeep

AU - Kizhake, Smitha

AU - Lagundžin, Dragana

AU - Klinkebiel, David

AU - Mallareddy, Jayapal Reddy

AU - Huxford, Tom

AU - Woods, Nicholas T.

AU - Natarajan, Amarnath

PY - 2022/1

Y1 - 2022/1

N2 - 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.

AB - 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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EP - 36

JO - RSC Chemical Biology

JF - RSC Chemical Biology

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ER -

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

Abstract

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