HDAC inhibitors work by blocking Histone De-ACetylase enzyme, which removes acetyl groups from the proteins that encase DNA, that is histones. They are triggered by CpG sequences on DNA promoters; HDACs put chromatin in a configuration that favors LACK of transcription. So, blocking HDACs favors transcription – see prior post. Continue reading
Category Archives: Epigenetic Regulation
Epigenetic signature in blood for breast cancer risk
As reported in Genomic Medicine on June 27, an epigenetic signature in patients with BRCA1 and BRCA2 mutations was found by examining DNA methylation (DNAme) patterns on whole blood samples. Importantly, this signature predicted for a high risk of developing breast cancer even in those patients who did NOT have BRCA1 and BRCA2 mutations. 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
IDH1 and IDH2 inhibitors
IDH1 and IDH2 are enzymes in the Krebs Cycle of glucose metabolism – IDH1 (AG-120) is active in the cyotplasm and IDH2 (AG-221) is active in the mitochondria. Phase 1 clinical studies of these compounds are underway. Continue reading