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Development of Keap1-interactive small molecules that regulate Nrf2 transcriptional activity

Georgakopoulos, ND; Gatliff, J; Wells, G; (2016) Development of Keap1-interactive small molecules that regulate Nrf2 transcriptional activity. Current Opinion in Toxicology , 1 pp. 1-8. 10.1016/j.cotox.2016.08.002. Green open access

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Abstract

There has been considerable progress recently in the discovery and development of Keap1-interactive compounds that enhance Nrf2 transcriptional activity. The compounds fall into two broad classes: electrophilic cysteine-reactive compounds and non-electrophilic Keap1-Nrf2 protein–protein interaction inhibitors. This short review highlights structures from both classes and discusses their development, biological properties, and the future prospects for developing therapeutic agents. Molecules of both types have potential applications in areas including inflammatory conditions, chronic neurodegenerative diseases and possibly cancer chemoprevention.

Type: Article
Title: Development of Keap1-interactive small molecules that regulate Nrf2 transcriptional activity
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.cotox.2016.08.002
Publisher version: http://dx.doi.org/10.1016/j.cotox.2016.08.002
Language: English
Additional information: Copyright © 2016 Elsevier B.V. All rights reserved. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
Keywords: Keap1; Nrf2; Protein–protein interactions; Ubiquitination; Parkinson's disease; Alzheimer's disease; Cancer chemoprevention
UCL classification: UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > SoP Pharmaceutical and Bio Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/1523781
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