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 …

HDACs and HDAC inhibitors in cancer development and therapy

Y Li, E Seto - Cold Spring Harbor perspectives in …, 2016 - perspectivesinmedicine.cshlp.org
Over the last several decades, it has become clear that epigenetic abnormalities may be one
of the hallmarks of cancer. Posttranslational modifications of histones, for example, may play …

Histone deacetylases (HDACs): evolution, specificity, role in transcriptional complexes, and pharmacological actionability

G Milazzo, D Mercatelli, G Di Muzio, L Triboli… - Genes, 2020 - mdpi.com
Histone deacetylases (HDACs) are evolutionary conserved enzymes which operate by
removing acetyl groups from histones and other protein regulatory factors, with functional …

A first-generation pediatric cancer dependency map

NV Dharia, G Kugener, LM Guenther, CF Malone… - Nature …, 2021 - nature.com
Exciting therapeutic targets are emerging from CRISPR-based screens of high mutational-
burden adult cancers. A key question, however, is whether functional genomic approaches …

Selective gene dependencies in MYCN-amplified neuroblastoma include the core transcriptional regulatory circuitry

AD Durbin, MW Zimmerman, NV Dharia, BJ Abraham… - Nature …, 2018 - nature.com
Childhood high-risk neuroblastomas with MYCN gene amplification are difficult to treat
effectively. This has focused attention on tumor-specific gene dependencies that underlie …

[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology

CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …

Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment

X Peng, Z Sun, P Kuang, J Chen - European Journal of Medicinal Chemistry, 2020 - Elsevier
Histone deacetylases (HDACs) are a class of enzymes that remove acetyl from the ε-N-
acetyl lysine of histones, allowing histones to wrap DNA more tightly. HDACs play an …

Therapeutic strategies to inhibit MYC

MR McKeown, JE Bradner - Cold Spring …, 2014 - perspectivesinmedicine.cshlp.org
MYC is a master regulator of stem cell state, embryogenesis, tissue homeostasis, and aging.
As in health, in disease MYC figures prominently. Decades of biological research have …

Optimization of class I histone deacetylase PROTACs reveals that HDAC1/2 degradation is critical to induce apoptosis and cell arrest in cancer cells

JP Smalley, IM Baker, WA Pytel, LY Lin… - Journal of medicinal …, 2022 - ACS Publications
Class I histone deacetylase (HDAC) enzymes 1, 2, and 3 organize chromatin as the catalytic
subunits within seven distinct multiprotein corepressor complexes and are established drug …

CRISPR-Cas9 screen reveals a MYCN-amplified neuroblastoma dependency on EZH2

L Chen, G Alexe, NV Dharia, L Ross… - The Journal of …, 2018 - Am Soc Clin Investig
Pharmacologically difficult targets, such as MYC transcription factors, represent a major
challenge in cancer therapy. For the childhood cancer neuroblastoma, amplification of the …