Drug discovery for epigenetics targets

Autor: Catherine Bardelle, James M. Smith, Nidhal Selmi, Alice Lanne, Robert J. Sheppard, Daniel Hillebrand O'donovan, Jon Read, Geoffrey A. Holdgate
Rok vydání: 2021
Předmět:
Zdroj: Drug discovery today. 27(4)
ISSN: 1878-5832
Popis: Dysregulation of the epigenome is associated with the onset and progression of several diseases, including cancer, autoimmune, cardiovascular, and neurological disorders. Members from the three families of epigenetic proteins (readers, writers, and erasers) have been shown to be druggable using small-molecule inhibitors. Increasing knowledge of the role of epigenetics in disease and the reversibility of these modifications explain why pharmacological intervention is an attractive strategy for tackling epigenetic-based disease. In this review, we provide an overview of epigenetics drug targets, focus on approaches used for initial hit identification, and describe the subsequent role of structure-guided chemistry optimisation of initial hits to clinical candidates. We also highlight current challenges and future potential for epigenetics-based therapies.
Databáze: OpenAIRE