PMID- 30767728 OWN - NLM STAT- MEDLINE DCOM- 20200406 LR - 20200408 IS - 1557-8100 (Electronic) IS - 1536-2310 (Linking) VI - 23 IP - 2 DP - 2019 Feb TI - Epigenomics-Guided Drug Development: Recent Advances in Solving the Cancer Treatment "jigsaw puzzle". PG - 70-85 LID - 10.1089/omi.2018.0206 [doi] AB - The human epigenome plays a key role in determining cellular identity and eventually function. Drug discovery undertakings have focused mainly on the role of genomics in carcinogenesis, with the focus turning to the epigenome recently. Drugs targeting DNA and histone modifications are under development with some such as 5-azacytidine, decitabine, vorinostat, and panobinostat already approved by the Food and Drug Administration (FDA) and the European Medicines Agency (EMA). This expert review offers a critical analysis of the epigenomics-guided drug discovery and development and the opportunities and challenges for the next decade. Importantly, the coupling of epigenetic editing techniques, such as clustered regularly interspersed short palindromic repeat (CRISPR)-CRISPR-associated protein-9 (Cas9) and APOBEC-coupled epigenetic sequencing (ACE-seq) with epigenetic drug screens, will allow the identification of small-molecule inhibitors or drugs able to reverse epigenetic changes responsible for many diseases. In addition, concrete and sustainable innovation in cancer treatment ought to integrate epigenome targeting drugs with classic therapies such as chemotherapy and immunotherapy. FAU - Dzobo, Kevin AU - Dzobo K AD - 1 International Centre for Genetic Engineering and Biotechnology (ICGEB), Cape Town Component, Cape Town, South Africa. AD - 2 Division of Medical Biochemistry and Institute of Infectious Disease and Molecular Medicine, Department of Integrative Biomedical Sciences, Faculty of Health Sciences, University of Cape Town, Cape Town, South Africa. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - United States TA - OMICS JT - Omics : a journal of integrative biology JID - 101131135 SB - IM MH - Clustered Regularly Interspaced Short Palindromic Repeats/genetics MH - DNA Methylation/genetics MH - Epigenesis, Genetic/*genetics MH - Epigenomics/*methods MH - Humans OTO - NOTNLM OT - CRISPR OT - clinical trials OT - drug development OT - drug discovery OT - drugs OT - epigenetics OT - epigenomics OT - functional genomics EDAT- 2019/02/16 06:00 MHDA- 2020/04/09 06:00 CRDT- 2019/02/16 06:00 PHST- 2019/02/16 06:00 [entrez] PHST- 2019/02/16 06:00 [pubmed] PHST- 2020/04/09 06:00 [medline] AID - 10.1089/omi.2018.0206 [doi] PST - ppublish SO - OMICS. 2019 Feb;23(2):70-85. doi: 10.1089/omi.2018.0206.