EZH2 encodes a SET domain-containing lysine methyltransferase that is the catalytic subunit of the polycomb repressive complex 2 (PRC2). EZH2 alone has no detectable histone-methylating activity; other members of the PRC2 complex, including EED, SUZ12, RbAp48, and AEBP2, are required for full activity. The PRC2 represses gene expression via trimethylation of histone H3 at lysine 27 (H3K27). Point mutations in EZH2 such as Tyr641*, Ala677, and Ala687 cause EZH2 to hypermethylate H3K27, and have been identified in patients with leukemia and non-Hodgkin B-cell lymphomas. Overexpression and hyperactivity of EZH2 have also been implicated in the pathogenesis of human myeloma, as well as prostate, breast, and endometrial carcinomas, making inhibition of the EZH2 oncoprotein a key strategy for drug discovery.
Some mutations in EZH2 have been identified as the source of Weaver Syndrome, a disorder characterized by skeletal abnormalities, developmental delay, and susceptibility to many cancers. Identification of specific EZH2 DNA mutations has permitted the development of diagnostic tests to definitively distinguish Weaver Syndrome from disorders with similar phenotypes, such as Sotos Syndrome, caused by mutations in the NSD1 gene. In contrast to the enhanced trimethylation activity of H3K27 found in Point mutations in EZH2 such as Tyr641*, Ala677, and Ala687, the Weaver Syndrome EZH2 mutations (including Tyr153del, His689, and Pro132) lead to reduced methylation activity, suggesting Weaver Syndrome is caused by loss-of-function mutations in EZH2.
In addition to the mutants above, BPS also introduces the inactive Phe667 mutant version, as well as the recently published Arg679 and Glu740 mutations, along with assay kits specific for two different Tyr641 mutations.
BPS was the first company to offer EZH1 and EZH2 enzymes, assay kits and screening services to life science researchers worldwide. BPS offers full 5-member PRC2 complex, as well as a number of smaller PRC2 complexes for protein binding studies. BPS also provieds screening services to identify inhibitors of EZH1 (WT), EZH2 (WT), EZH2 (Y641C), EZH2 (Y641F), EZH2 (Y641H), EZH2 (Y641N), and EZH2 (Y641S).
BPS continues to actively develop innovative EHZ-related products and services, and additional products will be available in the coming months to further assist scientists in identifying and validating novel EZH2 inhibitors for drug discovery.
To learn more about BPS Bioscience’s EZH2 products, visit our website at http://bpsbioscience.com/
* corresponding to GenBank Accession #NM_001203247
About BPS Bioscience, Inc.
Headquartered in San Diego, California, BPS Bioscience, Inc. is a leading manufacturer of Histone Methyltransferases and other epigenetic enzymes, including Acetyltransferases, Bromodomains, HDACs, Histone Demethylases, Methyl-lysine Readers, Poly ADP Ribose Polymerases (PARPs), and Ubiquitin Enzymes. BPS offers one of the largest selections of recombinant enzymes and assay kits for drug discovery and continues to expand its portfolio of innovative drug discovery products. BPS also provides custom protein expression, biochemical and cell based assays, and compound screening and profiling services. BPS has provided products and services to pharmaceutical companies and academic institutes in over 45 countries worldwide. By being at the forefront of technology development, BPS focuses on providing quality life science products and services in a timely manner that will help our customers to accelerate drug discovery and development for treatment of human diseases. Visit BPS’s website for more information:
BPS Bioscience, Inc.
BPS Bioscience, Inc.