Category Archives: Epigenetic Regulation

Etinostat blocks Treg activity via FOXP3 suppression

Histone deacetylase (HDAC) inhibitors block the removal of acetyl groups from histone proteins. Since acetylation of histones puts chromatin in a more favorable condition for transcription, HDAC inhibitors maintain this favorable state. HDAC inhibitors have been approved for use in cutaneous T-cell lymphoma. They act by sustaining transcription of tumor suppressor genes, which leads to cell cycle arrest and apoptosis. Continue reading

Hypomethylating agents are effective in myelodysplastic syndrome

Results of studies in patients with low- and intermediate-risk myelodysplastic syndrome (MDS) treated with hypomethylating agents (low dose azacytidine or decitabine) followed for a median of 18 months were presented at the Society of Hematologic Oncology meeting in Houston on September 9, 2016. Continue reading

Intra-tumor heterogeneity leads to sampling bias and biomarker failure – Conor McAuliffe, Contributor

A growing understanding of genetic variation both between histologically similar tumors from different patients and within individual tumors themselves is shedding light on the difficulties in treating cancer and developing biomarkers to diagnose it. It has long been known that a single tumor displays differences in morphology, nuclear shape, proliferation, and proportions of constituent cell types. However, these differences may be only be the “tip of the iceberg” as vast genetic and epigenetic variations that underlie them have been discovered between and within tumors. Continue reading

The Roles of P53, BRCA1, and PTEN in Hereditary Cancers – Lauren Fitzgerald, Contributor

Cancer results from accumulated mutations in the cancer cell’s genome. These mutations can occur spontaneously in any cell throughout an individual’s lifetime, often increasing with age or exposure to carcinogenic or mutagenic compounds. These are called somatic mutations that do not exist in every cell, and cannot be passed along from one generation to the next. However, in approximately 5 to 10% of all cancer cases, mutations are passed along through the germ line and can predispose an individual to various types of cancers. Continue reading

BET Bromodomain Inhibition in Prostate Cancer Treatment

BET bromodomain inhibitors are epigenetic regulators that act by repressing expression of oncogenes, including MYC and BCL-2, that are aberrantly highly expressed in many cancer cells, resulting in inhibited cell proliferation and induction of apoptotic cell death. Continue reading

Biomarkers for Wnt activation Predict For HER-2(-) Breast Cancer and NSCLC Response to Vantictumab

OncoMed is developing several compounds that target Wnt and Notch pathways, which are important in cancer and cancer stem cell maintenance, survival, and proliferation. Biomarkers for response of Her-2-negative breast cancer and non-small cell lung cancer (NSCLC) following treatment with Vantictumab, anti-Wnt monoclonal antibody, have been developed. Continue reading

Tazemetostat Histone Methyltransferase Inhibitor for Hematologic and Solid Tumors

Tazemetostat is a small molecule inhibitor of EZH2 being developed by Epizyme, Inc for the treatment of patients with Non-Hodgkin Lymphoma, including germinal center and non-germinal center diffuse large B-cell lymphoma and follicular lymphoma, as well as genetically-defined solid tumors. In many human cancers, misregulated EZH2 enzyme activity results in misregulation of genes that control cell proliferation—without these control mechanisms, cancer cells are free to grow rapidly.  Continue reading

Prostate Cancer Genetic Map Unveiled

Researchers have identified a handful of mutations in patients with advanced prostate cancer for which therapeutics are already available, or in development. The genomes of 150 patients with metastatic (Stage 4) hormone-resistant disease were analyzed in order to develop a precision medicine framework for the treatment of advanced prostate cancer. Continue reading

Entinostat Doesn’t Just Restore Sensitivity to Aromatase Inhibitors

Entinostat is currently in a Phase III trial in combination with Aromasin (exemestane – aromatase inhibitor that blocks the synthesis of estrogen) in patients with metastatic breast cancer who have recurred following treatment with an aromatase inhibitor. Continue reading

Super Enhancer Switches for Gene Regulation – Syros

Biotech company Syros Pharmaceuticals just raised $53.1 MM in a Series B financing after raising a $30 MM Series A financing in 2013. This is big money for a small company – and, the money comes from some very savvy biotech investment funds. Continue reading