Pharmacological targeting of the cancer epigenome
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …
disease initiation, maintenance and therapy resistance. As a result, there have been …
A chemical probe toolbox for dissecting the cancer epigenome
J Shortt, CJ Ott, RW Johnstone, JE Bradner - Nature Reviews Cancer, 2017 - nature.com
Cancer cell hallmarks are underpinned by transcriptional programmes operating in the
context of a dynamic and complicit epigenomic environment. Somatic alterations of …
context of a dynamic and complicit epigenomic environment. Somatic alterations of …
Optimization of ligands using focused DNA-encoded libraries to develop a selective, cell-permeable CBX8 chromodomain inhibitor
Polycomb repressive complex 1 (PRC1) is critical for mediating gene expression during
development. Five chromobox (CBX) homolog proteins, CBX2, CBX4, CBX6, CBX7, and …
development. Five chromobox (CBX) homolog proteins, CBX2, CBX4, CBX6, CBX7, and …
A potent, selective CBX2 chromodomain ligand and its cellular activity during prostate cancer neuroendocrine differentiation
Polycomb group (PcG) proteins are epigenetic regulators that facilitate both embryonic
development and cancer progression. PcG proteins form Polycomb repressive complexes 1 …
development and cancer progression. PcG proteins form Polycomb repressive complexes 1 …
CBX6 Promotes HCC Metastasis Via Transcription Factors Snail/Zeb1-Mediated EMT Mechanism
J Wang, H He, Q Jiang, Y Wang, S Jia - OncoTargets and therapy, 2020 - Taylor & Francis
Purpose Hepatocellular carcinoma (HCC) is the most common malignant tumor worldwide
with high morbidity and mortality rates. We aimed to examine the expression of chromobox 6 …
with high morbidity and mortality rates. We aimed to examine the expression of chromobox 6 …
Chemical inhibitors targeting histone methylation readers
X Huang, Y Chen, Q Xiao, X Shang, Y Liu - Pharmacology & Therapeutics, 2024 - Elsevier
Histone methylation reader domains are protein modules that recognize specific histone
methylation marks, such as methylated or unmethylated lysine or arginine residues on …
methylation marks, such as methylated or unmethylated lysine or arginine residues on …
Robustness of in vitro selection assays of DNA-encoded peptidomimetic ligands to CBX7 and CBX8
KE Denton, S Wang, MC Gignac… - … the Science of Drug …, 2018 - journals.sagepub.com
The identification of protein ligands from a DNA-encoded library is commonly conducted by
an affinity selection assay. These assays are often not validated for robustness, raising …
an affinity selection assay. These assays are often not validated for robustness, raising …
Epigenetic small molecule modulators of histone and DNA methylation
Highlights•Histone and DNA methylation are associated with many diseases, esp.
cancer.•Inhibitors of DNA methyltransferases are approved leukemia drugs.•Inhibitors of …
cancer.•Inhibitors of DNA methyltransferases are approved leukemia drugs.•Inhibitors of …
Discovery of peptidomimetic ligands of EED as allosteric inhibitors of PRC2
KD Barnash, J The, JL Norris-Drouin… - ACS combinatorial …, 2017 - ACS Publications
The function of EED within polycomb repressive complex 2 (PRC2) is mediated by a
complex network of protein–protein interactions. Allosteric activation of PRC2 by binding of …
complex network of protein–protein interactions. Allosteric activation of PRC2 by binding of …
[HTML][HTML] CBX6 overexpression contributes to tumor progression and is predictive of a poor prognosis in hepatocellular carcinoma
H Zheng, W Jiang, T Tian, H Tan, Y Chen, G Qiao… - Oncotarget, 2017 - ncbi.nlm.nih.gov
Aberrant chromobox (CBX) family protein expression has been reported in a variety of
human malignancies. However, the role of CBX6 in hepatocellular carcinoma (HCC) …
human malignancies. However, the role of CBX6 in hepatocellular carcinoma (HCC) …