Thirty years of HDAC inhibitors: 2020 insight and hindsight

TCS Ho, AHY Chan, A Ganesan - Journal of medicinal chemistry, 2020 - ACS Publications
It is now 30 years since the first report of a potent zinc-dependent histone deacetylase
(HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory …

[HTML][HTML] An update of epigenetic drugs for the treatment of cancers and brain diseases: a comprehensive review

Z Sahafnejad, S Ramazi, A Allahverdi - Genes, 2023 - mdpi.com
Epigenetics has long been recognized as a significant field in biology and is defined as the
investigation of any alteration in gene expression patterns that is not attributed to changes in …

[HTML][HTML] A next generation connectivity map: L1000 platform and the first 1,000,000 profiles

A Subramanian, R Narayan, SM Corsello, DD Peck… - Cell, 2017 - cell.com
We previously piloted the concept of a Connectivity Map (CMap), whereby genes, drugs,
and disease states are connected by virtue of common gene-expression signatures. Here …

[HTML][HTML] Ketone body signaling mediates intestinal stem cell homeostasis and adaptation to diet

CW Cheng, M Biton, AL Haber, N Gunduz, G Eng… - Cell, 2019 - cell.com
Little is known about how metabolites couple tissue-specific stem cell function with
physiology. Here we show that, in the mammalian small intestine, the expression of Hmgcs2 …

HDAC inhibition upregulates PD-1 ligands in melanoma and augments immunotherapy with PD-1 blockade

DM Woods, AL Sodré, A Villagra, A Sarnaik… - Cancer immunology …, 2015 - AACR
Expression of PD-1 ligands by tumors and interaction with PD-1–expressing T cells in the
tumor microenvironment can result in tolerance. Therapies targeting this coinhibitory axis …

p53 as a target for the treatment of cancer

MJ Duffy, NC Synnott, PM McGowan, J Crown… - Cancer treatment …, 2014 - Elsevier
Abstract TP53 (p53) is the most frequently mutated gene in cancer, being altered in
approximately 50% of human malignancies. In most, if not all, cancers lacking mutation, wild …

Regulation of bronchial epithelial barrier integrity by type 2 cytokines and histone deacetylases in asthmatic patients

P Wawrzyniak, M Wawrzyniak, K Wanke… - Journal of Allergy and …, 2017 - Elsevier
Background Tight junctions (TJs) form a barrier on the apical side of neighboring epithelial
cells in the bronchial mucosa. Changes in their integrity might play a role in asthma …

Histone deacetylase (HDAC) inhibitors in recent clinical trials for cancer therapy

K Keller, M Jung - Epigenetic Therapy of Cancer: Preclinical Models and …, 2013 - Springer
Histone deacetylases are key enzymes of epigenetic regulation and are therefore involved
in crucial cellular events like transcription, differentiation, apoptosis and cell division. The …

Translating p53 into the clinic

CF Cheok, CS Verma, J Baselga… - Nature reviews Clinical …, 2011 - nature.com
Mutations in the TP53 gene are a feature of 50% of all reported cancer cases. In the other
50% of cases, the TP53 gene itself is not mutated but the p53 pathway is often partially …

[HTML][HTML] Augmenting antitumor immune responses with epigenetic modifying agents

E Héninger, TEG Krueger, JM Lang - Frontiers in immunology, 2015 - frontiersin.org
Epigenetic silencing of immune-related genes is a striking feature of the cancer genome that
occurs in the process of tumorigenesis. This phenomena impacts antigen processing and …