Methyltransferase Screening

Now accepting orders and compounds for our March demethylase and methyltransferase screening and profiling promotion. Contact us today for a quote and receive a minimum 10% discount off standard prices and reference inhibitor is included free of charge on orders of all sizes. Pick and choose any or all demethylase / methyltransferase isozymes. Customers under existing contracts are not eligible. 

BPS Bioscience offers DNA and histone methyltransferase screening services. Trust us to provide you with high quality data with fast turnaround time. Our team of experts along with our broad services portfolio makes it easy to:

  • Screen for inhibitors/targets using our panel of over 30 assays
  • Select from IC50 determination and single point concentrations
  • Receive data within days of compound submission
  • Perform follow-up studies using the same proteins manufactured in-house
  • Get questions answered or project guidance in a time-efficient manner

DNA Methyltransferase Biochemical Assays:

DNMT1 DNMT3A/DNMT3L DNMT3B/DNMT3L


Histone Methyltransferase Biochemical Assays:

DOT1L G9a  PRMT9
EZH1 GLP SETDB1
EZH2 MLL1 Complex  SETD2
EZH2 (A677G) NSD1 SET7/9
EZH2-EED NSD2 SET8
EZH2 (Y641C) PRMT1 SMYD2
EZH2 (Y641F) PRMT3 SMYD3
EZH2 (Y641H) PRMT4 SUV39H1
EZH2 (Y641N) PRMT5 SUV39H2
EZH2 (Y641S) PRMT6  SUV4-20H1

 Biochemical Assay Format:

Our histone methyltransferase assays utilize highly specific antibodies that recognize methyl groups. First, SAM is incubated with a sample containing assay buffer and purified recombinant methyltransferase enzyme. Next, acceptor beads, a primary antibody, and then donor beads are added. The final step is to read the Alpha-counts. Note: Image not drawn to scale. 

Background:

Methyltransferases are enzymes that transfer a methyl group from S-adenosylmethionine (SAM) to their substrates. DNA methyltransferases modify DNA by adding a methyl group to cytosines. DNA methylation of CpG dinucleotides suppresses gene expression and is critical for transcriptional silencing during imprinting, X-inactivation and other developmental processes. DNA methylation also plays a crucial role in the development of nearly all types of cancer.

Methyltransferases can also modify proteins; histone methyltransferases methylate lysines and arginines on histone side chains (see figure above). Lysines may be mono-, di-, or trimethylated and arginines may be mono-, symmetrically or asymmetrically dimethylated. Each of these different ‘flavors’ of methylation can result in different chromatin conformations and gene expression levels.

Several histone methyltransferases have been linked to diseases, in particular cancer. The lysine methyltransferaseEZH2 is a prime example of this. EZH2 is a methyltransferase that is part of the Polycomb Repressive complex (PRC2). EZH2, along with EED, RbAP48, SUZ12 and AEBP2, form a 5-member complex that methylates Lysine 27 of Histone H3 (H3K27). Abnormal expression of EZH2 has been linked to breast, prostate, endometrial, and other human cancers. Several point mutations in EZH2 cause it to hypermethylate H3K27, and are strongly associated with non-Hodgkins lymphomas and leukemias. Not surprisingly, inhibition of EZH2 is a key target for anti-cancer drug discovery. To aid in discovery, BPS offers a number of EZH2 mutant enzymes.

Aside from purified enzymes, BPS offers assay kitsinhibitors/activators, and substrates. The substrates offered by BPS include purified full-length histone proteinstetramersoctamersnucleosomes, and a number of modified histones. This diverse portfolio provides researchers with optimal flexibility in their experiments.