Is EZH2 a histone methyltransferase?

Is EZH2 a histone methyltransferase?

Enhancer of zeste homolog 2 (EZH2) is a histone-lysine N-methyltransferase enzyme that catalyzes the addition of methyl groups to histone H3 at lysine 27, leading to gene silencing. Mutation or over-expression of EZH2 has been linked to many cancers including renal carcinoma.

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.

What does a histone methyltransferase do?

Histone methyltransferases (HMT) are histone-modifying enzymes (e.g., histone-lysine N-methyltransferases and histone-arginine N-methyltransferases), that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins.

How do EZH2 inhibitors work?

EZH2 expression in cancer cells inhibits T-cell activation by suppressing the MHC-I antigen presentation pathway and upregulating PD-L1 expression. Besides cancer cells, EZH2 expression in Treg cells is crucial for maintaining their regulatory phenotype and function, which also results in reduced T-cell activation.

Is EZH2 a gene?

EZH2 (Enhancer Of Zeste 2 Polycomb Repressive Complex 2 Subunit) is a Protein Coding gene. Diseases associated with EZH2 include Weaver Syndrome and Lymphoma.

What is EZH2 mutation?

EZH2 mutations have been observed in myelodysplastic syndromes, lymphoma, colorectal cancer, and endometrial cancer. In MDS, these mutations often involve deletions or translocations which are believed to be associated with loss of function.

Why does histone acetylation activate gene expression?

Acetylation of histones alters accessibility of chromatin and allows DNA binding proteins to interact with exposed sites to activate gene transcription and downstream cellular functions.

How does histone methylation affect transcription?

Methylation and demethylation of histones turns the genes in DNA “off” and “on,” respectively, either by loosening their tails, thereby allowing transcription factors and other proteins to access the DNA, or by encompassing their tails around the DNA, thereby restricting access to the DNA.