Publication

The timeline of epigenetic drug discovery: from reality to dreams

Ganesan, A., Arimondo, P. B., Rots, M. G., Jeronimo, C. & Berdasco, M., 2-Dec-2019, In : Clinical Epigenetics. 11, 1, 17 p., 174.

Research output: Contribution to journalReview articleAcademicpeer-review

The flexibility of the epigenome has generated an enticing argument to explore its reversion through pharmacological treatments as a strategy to ameliorate disease phenotypes. All three families of epigenetic proteins-readers, writers, and erasers-are druggable targets that can be addressed through small-molecule inhibitors. At present, a few drugs targeting epigenetic enzymes as well as analogues of epigenetic modifications have been introduced into the clinic use (e.g. to treat haematological malignancies), and a wide range of epigenetic-based drugs are undergoing clinical trials. Here, we describe the timeline of epigenetic drug discovery and development beginning with the early design based solely on phenotypic observations to the state-of-the-art rational epigenetic drug discovery using validated targets. Finally, we will highlight some of the major aspects that need further research and discuss the challenges that need to be overcome to implement epigenetic drug discovery into clinical management of human disorders. To turn into reality, researchers from various disciplines (chemists, biologists, clinicians) need to work together to optimise the drug engineering, read-out assays, and clinical trial design.

Original languageEnglish
Article number174
Number of pages17
JournalClinical Epigenetics
Volume11
Issue number1
Publication statusPublished - 2-Dec-2019

    Keywords

  • Epigenetics, DNA methylation, Histone modifications, Epidrugs, Therapy, HISTONE DEACETYLASE INHIBITOR, ACUTE MYELOID-LEUKEMIA, IN-VITRO, DEMETHYLATING AGENTS, CANCER EPIGENOME, POTENT INDUCERS, VALPROIC ACID, DIFFERENTIATION, THERAPY, MECHANISM

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