Epigenetic modulation and understanding of HDAC inhibitors in cancer therapy

MJ Ramaiah, AD Tangutur, RR Manyam - Life sciences, 2021 - Elsevier
The role of genetic and epigenetic factors in tumor initiation and progression is well
documented. Histone deacetylases (HDACs), histone methyl transferases (HMTs), and DNA …

Epigenetic protein families: a new frontier for drug discovery

CH Arrowsmith, C Bountra, PV Fish, K Lee… - Nature reviews Drug …, 2012 - nature.com
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …

Rational approaches, design strategies, structure activity relationship and mechanistic insights for anticancer hybrids

K Nepali, S Sharma, M Sharma, PMS Bedi… - European journal of …, 2014 - Elsevier
A Hybrid drug which comprises the incorporation of two drug pharmacophores in one single
molecule are basically designed to interact with multiple targets or to amplify its effect …

[HTML][HTML] Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells

M Göttlicher, S Minucci, P Zhu, OH Krämer… - The EMBO …, 2001 - embopress.org
Histone deacetylases (HDACs) play important roles in transcriptional regulation and
pathogenesis of cancer. Thus, HDAC inhibitors are candidate drugs for differentiation …

[HTML][HTML] Negative control of p53 by Sir2α promotes cell survival under stress

J Luo, AY Nikolaev, S Imai, D Chen, F Su, A Shiloh… - Cell, 2001 - cell.com
The NAD-dependent histone deacetylation of Sir2 connects cellular metabolism with gene
silencing as well as aging in yeast. Here, we show that mammalian Sir2α physically interacts …

Histone deacetylase inhibitors: molecular mechanisms of action

WS Xu, RB Parmigiani, PA Marks - Oncogene, 2007 - nature.com
This review focuses on the mechanisms of action of histone deacetylase (HDAC) inhibitors
(HDACi), a group of recently discovered 'targeted'anticancer agents. There are 18 HDACs …

Histone deacetylases and cancer: causes and therapies

PA Marks, RA Rifkind, VM Richon, R Breslow… - Nature Reviews …, 2001 - nature.com
Together, histone acetyltransferases and histone deacetylases (HDACs) determine the
acetylation status of histones. This acetylation affects the regulation of gene expression, and …

Histone-deacetylase inhibitors: novel drugs for the treatment of cancer

RW Johnstone - Nature reviews Drug discovery, 2002 - nature.com
The opposing actions of histone acetyltransferases (HATs) and histone deacetylases
(HDACs) allow gene expression to be exquisitely regulated through chromatin remodelling …

Dimethyl sulfoxide to vorinostat: development of this histone deacetylase inhibitor as an anticancer drug

PA Marks, R Breslow - Nature biotechnology, 2007 - nature.com
In our quest to understand why dimethyl sulfoxide (DMSO) can cause growth arrest and
terminal differentiation of transformed cells, we followed a path that led us to discover …

A selective HDAC8 inhibitor potentiates antitumor immunity and efficacy of immune checkpoint blockade in hepatocellular carcinoma

W Yang, Y Feng, J Zhou, OKW Cheung, J Cao… - Science translational …, 2021 - science.org
Insufficient T cell infiltration into noninflamed tumors, such as hepatocellular carcinoma
(HCC), restricts the effectiveness of immune-checkpoint blockade (ICB) for a subset of …