Combining epigenetic drugs with other therapies for solid tumours—past lessons and future promise

D Morel, D Jeffery, S Aspeslagh, G Almouzni… - Nature Reviews …, 2020 - nature.com
Epigenetic dysregulation has long been recognized as a key factor contributing to
tumorigenesis and tumour maintenance that can influence all of the recognized hallmarks of …

Molecular and therapeutic potential and toxicity of valproic acid

S Chateauvieux, F Morceau, M Dicato… - BioMed Research …, 2010 - Wiley Online Library
Valproic acid (VPA), a branched short‐chain fatty acid, is widely used as an antiepileptic
drug and a mood stabilizer. Antiepileptic properties have been attributed to inhibition of …

Valproic acid as epigenetic cancer drug: preclinical, clinical and transcriptional effects on solid tumors

A Duenas-Gonzalez, M Candelaria… - Cancer treatment …, 2008 - Elsevier
Among many anticancer drugs collectively named “targeted or molecular therapies”
epigenetic drugs are clearly promising. Differently from other agents targeting a single gene …

Epigenetic polypharmacology: A new frontier for epi‐drug discovery

D Tomaselli, A Lucidi, D Rotili… - Medicinal research …, 2020 - Wiley Online Library
Recently, despite the great success achieved by the so‐called “magic bullets” in the
treatment of different diseases through a marked and specific interaction with the target of …

[HTML][HTML] Drug repositioning for effective prostate cancer treatment

B Turanli, M Grøtli, J Boren, J Nielsen, M Uhlen… - Frontiers in …, 2018 - frontiersin.org
Drug repositioning has gained attention from both academia and pharmaceutical companies
as an auxiliary process to conventional drug discovery. Chemotherapeutic agents have …

Histone deacetylase inhibitors in cancer therapy

WK Rasheed, RW Johnstone… - Expert opinion on …, 2007 - Taylor & Francis
Histones are a family of nuclear proteins that interact with DNA, resulting in DNA being
wrapped around a core of histone octamer within the nucleosome. Acetylation/deacetylation …

[HTML][HTML] Downregulation of homologous recombination DNA repair genes by HDAC inhibition in prostate cancer is mediated through the E2F1 transcription factor

SK Kachhap, N Rosmus, SJ Collis, MSQ Kortenhorst… - PloS one, 2010 - journals.plos.org
Background Histone deacetylase inhibitors (HDACis) re-express silenced tumor suppressor
genes and are currently undergoing clinical trials. Although HDACis have been known to …

[PDF][PDF] Valproic acid, a molecular lead to multiple regulatory pathways

M Kostrouchova, Z Kostrouch… - FOLIA BIOLOGICA …, 2007 - orl.lf1.cuni.cz
Valproic acid (2-propyl pentanoic acid) is a drug used for the treatment of epilepsy and
bipolar disorder. Although very rare, side effects such as spina bifida and other defects of …

[HTML][HTML] Epigenetic regulation of interleukin 6 by histone acetylation in macrophages and its role in paraquat-induced pulmonary fibrosis

L Hu, Y Yu, H Huang, H Fan, L Hu, C Yin, K Li… - Frontiers in …, 2017 - frontiersin.org
Overexpression of interleukin 6 (IL-6) has been proposed to contribute to pulmonary fibrosis
and other fibrotic diseases. However, the regulatory mechanisms and the role of IL-6 in …

The epigenome as a therapeutic target in prostate cancer

AS Perry, RWG Watson, M Lawler… - Nature Reviews …, 2010 - nature.com
During cancer development and progression, tumor cells undergo abnormal epigenetic
modifications, including DNA methylation, histone deacetylation and nucleosome …