title: Epigenetic modulators as therapeutic targets in prostate cancer.
abstract: Prostate cancer is one of the most common non-cutaneous malignancies among men worldwide. Epigenetic aberrations, including changes in DNA methylation patterns and/or histone modifications, are key drivers of prostate carcinogenesis. These epigenetic defects might be due to deregulated function and/or expression of the epigenetic machinery, affecting the expression of several important genes. Remarkably, epigenetic modifications are reversible and numerous compounds that target the epigenetic enzymes and regulatory proteins were reported to be effective in cancer growth control. In fact, some of these drugs are already being tested in clinical trials. This review discusses the most important epigenetic alterations in prostate cancer, highlighting the role of epigenetic modulating compounds in pre-clinical and clinical trials as potential therapeutic agents for prostate cancer management.
authors.affiliation: Cancer Biology and Epigenetics Group-Research Center (CI-IPOP), Portuguese Oncology Institute of Porto (IPO-Porto), Research Center-LAB 3, F Bdg, 1st floor, Rua Dr. António Bernardino de Almeida, 4200-072 Porto, Portugal ; School of Allied Health Sciences (ESTSP), Polytechnic of Porto, Porto, Portugal.
authors.forename: Inês
authors.initials: I
authors.lastname: Graça
authors.affiliation: Cancer Biology and Epigenetics Group-Research Center (CI-IPOP), Portuguese Oncology Institute of Porto (IPO-Porto), Research Center-LAB 3, F Bdg, 1st floor, Rua Dr. António Bernardino de Almeida, 4200-072 Porto, Portugal.
authors.forename: Eva
authors.initials: E
authors.lastname: Pereira-Silva
authors.affiliation: Cancer Biology and Epigenetics Group-Research Center (CI-IPOP), Portuguese Oncology Institute of Porto (IPO-Porto), Research Center-LAB 3, F Bdg, 1st floor, Rua Dr. António Bernardino de Almeida, 4200-072 Porto, Portugal ; Department of Pathology, Portuguese Oncology Institute of Porto (IPO Porto), Rua Dr. António Bernardino de Almeida, 4200-072 Porto, Portugal ; Department of Pathology and Molecular Immunology, Institute of Biomedical Sciences Abel Salazar-University of Porto (ICBAS-UP), Porto, Portugal.
authors.forename: Rui
authors.initials: R
authors.lastname: Henrique
authors.affiliation: Cancer Research UK Centre, Cancer Sciences, The Somers Cancer Research Building, University of Southampton Faculty of Medicine, Southampton General Hospital, Southampton, S016 6YD UK.
authors.forename: Graham
authors.initials: G
authors.lastname: Packham
authors.affiliation: Cancer Research UK Centre, Cancer Sciences, The Somers Cancer Research Building, University of Southampton Faculty of Medicine, Southampton General Hospital, Southampton, S016 6YD UK.
authors.forename: Simon J
authors.initials: SJ
authors.lastname: Crabb
authors.affiliation: Cancer Biology and Epigenetics Group-Research Center (CI-IPOP), Portuguese Oncology Institute of Porto (IPO-Porto), Research Center-LAB 3, F Bdg, 1st floor, Rua Dr. António Bernardino de Almeida, 4200-072 Porto, Portugal ; Department of Pathology and Molecular Immunology, Institute of Biomedical Sciences Abel Salazar-University of Porto (ICBAS-UP), Porto, Portugal.
authors.forename: Carmen
authors.initials: C
authors.lastname: Jerónimo
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D004248:DNA (Cytosine-5-)-Methyltransferases / Q000037:antagonists & inhibitors*; D019175:DNA Methylation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D044127:Epigenesis, Genetic / Q000187:drug effects; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D056572:Histone Deacetylase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D006657:Histones / Q000037:antagonists & inhibitors / Q000378:metabolism*; D006801:Humans; D008297:Male; D051379:Mice; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism; D016019:Survival Analysis; D016896:Treatment Outcome
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006657:Histones; D004248:DNA (Cytosine-5-)-Methyltransferases
keywords: DNMTi; Histone modulators; Prostate cancer