How does the EZH2 inhibitor work?

EZH2 is upregulated in the injured pancreatic tissue. Increased expression of EZH2 represses the CDK inhibitor p16Ink4a, therefore, controls the proliferative potential of PDX1-positive progenitor cells that accumulate transiently in metaplastic lesions, which is required during pancreatic repair.

Is EZH2 a tumor suppressor?

EZH2 downregulates expression of tumor suppressor genes and upregulates oncogenes, promoting cancer cell survival, proliferation, epithelial to mesenchymal and invasion. In particular, EZH2 has been also reported to be associated with drug resistance to chemotherapy and targeted therapy.

What does the EZH2 gene do?

The EZH2 gene provides instructions for making a type of enzyme called a histone methyltransferase. Histone methyltransferases modify proteins called histones, which are structural proteins that attach (bind) to DNA and give chromosomes their shape.

Where is EZH2 found?

It is found in larger amounts than in healthy cells in a wide range of cancers including breast, prostate, bladder, uterine, and renal cancers, as well as melanoma and lymphoma. EZH2 is a gene suppressor, so when it becomes overexpressed, many tumor suppressor genes that are normally turned on, are turned off.

How is Tazemetostat administered?

Tazemetostat comes as a tablet to take by mouth. It is usually taken twice a day with or without food. Take tazemetostat at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.

Is Tazverik a chemotherapy drug?

TAZVERIK is not a chemotherapy treatment and does not kill cancer cells directly. A protein called EZH2 is found in many cells in the body. When there is increased activity, it can lead to tumor growth.

How do you test for EZH2 mutation?

How does it work? The doctor takes a small amount of cancerous tissue from the patient and sends it to a laboratory. In the laboratory, DNA is isolated from a patient’s tumor biopsy and mixed with chemical substances (reagents) to evaluate the presence or absence of the specific EZH2 mutations.

Why target EZH2 for cancer therapy?

Its important roles in the pathophysiology of cancer are now widely concerned. Therefore, targeting EZH2 for cancer therapy is a hot research topic now and different types of EZH2 inhibitors have been developed.

What is the function of the EZH2 gene?

EZH2 functions in various biological processes via 3 types of mechanism, including PRC2-dependent H3K27 methylation, PRC2-dependent non-histone protein methylation, and PRC2-independent gene transactivation. When mutation or abnormal expression happens, EZH2 is related to cancer initiation, metastasis, immunity, metabolism, and drug resistance

Is EZH2-mediated inactivation of IFN-γ-jak-stat1 signaling an effective therapeutic target in epithelial tumors?

EZH2-mediated inactivation of IFN-γ-JAK-STAT1 signaling is an effective therapeutic target in MYC-driven prostate cancer Although small-molecule targeting of EZH2 appears to be effective in lymphomas carrying EZH2 activating mutations, finding similar approaches to target EZH2-overexpressing epithelial tumors remains challenging.

What is the target of the Polycomb group protein EZH2?

The gene encoding the prostatic tumor suppressor PSP94 is a target for repression by the Polycomb group protein EZH2. Oncogene. 2007;26:4590–4595.