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.
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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 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 > Pharma and Bio Chemistry |
| URI: | https://discovery.ucl.ac.uk/id/eprint/1523781 |
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