What do DNMT inhibitors do?
DNMT inhibitors are modulators of gene expression and may increase the expression levels of many key genes, specifically the ones involved in the radiosensitizing processes. NF-κB is capable of activating a number of genes involved in stress response, inflammation, and apoptosis.
Which epigenetic drug is now approved to treat leukemia?
The FDA’s approval of tazemetostat, specifically for patients with advanced or metastatic epithelioid sarcoma who are not eligible for curative surgery, is the first approval of an epigenetic drug for a solid tumor. (Other epigenetic agents have been approved for blood cancers such as leukemia or multiple myeloma.)
How can you inhibit methylation?
The most well characterized and widely used drugs to inhibit DNA cytosine methylation and reactivate silenced genes are several nucleoside analogs, including 5-azacytidine (5-Aza-CR) and 5-aza-2′-deoxycytidine (5-Aza-CdR) (12,13), and several non-nucleoside drugs, including procainamide (14,15).
What is the concern with epigenetic therapy?
Researchers have found that flawed epigenetic patterns are common characteristics of many types of cancer cells. Changes in the epigenetic pattern can lead to tumor-suppressing genes being turned off or activating gene mutations, which can then cause tumor development.
Which is the best DNMT inhibitor for oncological disease?
The DNA methyltransferase (DNMT) inhibitors azacytidine and decitabine are the most successful epigenetic drugs to date and are still the most widely used as epigenetic modulators, even though their application for oncological diseases is restricted by their relative toxicity and poor chemical stability.
How are DNA methyltransferase inhibitors used in cancer therapy?
DNA methyltransferase inhibitors and their emerging role in epigenetic therapy of cancer
Where can I find DNA methyltransferase inhibitors in China?
1 Jiangsu Key Laboratory of Neuropsychiatric Diseases and Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Soochow University, 199 Ren-Ai Road, Suzhou, Jiangsu 215123, China.