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 …
documented. Histone deacetylases (HDACs), histone methyl transferases (HMTs), and DNA …
HDACs and HDAC inhibitors in cancer development and therapy
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 …
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 …
removing acetyl groups from histones and other protein regulatory factors, with functional …
A first-generation pediatric cancer dependency map
Exciting therapeutic targets are emerging from CRISPR-based screens of high mutational-
burden adult cancers. A key question, however, is whether functional genomic approaches …
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
Childhood high-risk neuroblastomas with MYCN gene amplification are difficult to treat
effectively. This has focused attention on tumor-specific gene dependencies that underlie …
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 …
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 …
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 …
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 …
subunits within seven distinct multiprotein corepressor complexes and are established drug …
CRISPR-Cas9 screen reveals a MYCN-amplified neuroblastoma dependency on EZH2
Pharmacologically difficult targets, such as MYC transcription factors, represent a major
challenge in cancer therapy. For the childhood cancer neuroblastoma, amplification of the …
challenge in cancer therapy. For the childhood cancer neuroblastoma, amplification of the …