Tag Archives: HDAC

Decoy double strand breaks lead to mitotic catastrophe independent of BRCA1/2 mutations status

BRCA1/2 are DNA repair enzymes that are the essential components of homologous repair (HR), which is invoked when DNA doubles strand breaks are encountered. HR works via consultation of sister chromatids during late S to early G2 of the cell cycle – without repair of double strand breaks, mitotic catastrophe ensues: Continue reading

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

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

Epigenetic-modulation in myelodysplastic syndrome – DNA methylation and histone acetylation

Epigenetic regulation is critical for gene expression.  Epigenetic pathways are frequently dysregulated in cancer, which can lead to suppression of tumor suppressor genes and expression of oncogenes. Continue reading