UCL Discovery
UCL home » Library Services » Electronic resources » UCL Discovery

Inhibition of AlkB Nucleic Acid Demethylases: Promising New Epigenetic Targets

Perry, GS; Das, M; Woon, ECY; (2021) Inhibition of AlkB Nucleic Acid Demethylases: Promising New Epigenetic Targets. Journal of Medicinal Chemistry 10.1021/acs.jmedchem.1c01694. (In press).

[thumbnail of 28. J Med Chem Perspective-EWoon-Open access.pdf] Text
28. J Med Chem Perspective-EWoon-Open access.pdf - Accepted version
Access restricted to UCL open access staff until 19 November 2022.

Download (26MB)

Abstract

The AlkB family of nucleic acid demethylases is currently of intense chemical, biological, and medical interest because of its critical roles in several key cellular processes, including epigenetic gene regulation, RNA metabolism, and DNA repair. Emerging evidence suggests that dysregulation of AlkB demethylases may underlie the pathogenesis of several human diseases, particularly obesity, diabetes, and cancer. Hence there is strong interest in developing selective inhibitors for these enzymes to facilitate their mechanistic and functional studies and to validate their therapeutic potential. Herein we review the remarkable advances made over the past 20 years in AlkB demethylase inhibition research. We discuss the rational design of reported inhibitors, their mode-of-binding, selectivity, cellular activity, and therapeutic opportunities. We further discuss unexplored structural elements of the AlkB subfamilies and propose potential strategies to enable subfamily selectivity. It is hoped that this perspective will inspire novel inhibitor design and advance drug discovery research in this field.

Type: Article
Title: Inhibition of AlkB Nucleic Acid Demethylases: Promising New Epigenetic Targets
DOI: 10.1021/acs.jmedchem.1c01694
Publisher version: https://doi.org/10.1021/acs.jmedchem.1c01694
Language: English
Additional information: This version is the author accepted manuscript. For information on re-use, please refer to the publisher's terms and conditions.
UCL classification: UCL
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/10138760
Downloads since deposit
0Downloads
Download activity - last month
Download activity - last 12 months
Downloads by country - last 12 months

Archive Staff Only

View Item View Item