Histone Methyltransferase Screening


Histone methyltransferases (HMTs) perform covalent methylation of lysine or arginine residues of histones, and constitute one of the major classes of epigenetic modifiers with importance in transcriptional control and chromatin remodeling. The enzymatic methylation of H3 and H4 is achieved by lysine methyltransferases (KMTs) and arginine methyltransferases (PRMTs), with S-adenosyl-L-methionine (SAM) as the methyl donor, which could transfer up to three methyl groups, thus generating mono-, di-, or trimethylated lysine, and in mono- or di- (asymmetric or symmetric) methylated arginine, respectively. Aberrant HMT methylation is known to be of relevance with cancers, inflammatory diseases, and neurodegenerative disorders, which has sparked interests in HMTs of epigenetic modifications as promising drug targets. The inhibition of HMTs may lead to the expression of the silenced genes and HMT inhibitors are currently developed for various therapeutic applications.

 Proposed general chemical mechanism of SAM-dependent HMTs.

Figure 1. Proposed general chemical mechanism of SAM-dependent HMTs. (Smith, B. C.; et al. 2009)

Creative BioMart has become the premier provider of HMT assay services, including both lysine methyltransferases screening and arginine methyltransferases screening, available for both profiling and low cost high throughput screening. A wide range of HMT enzyme targets, including DOT1, EZH1, EZH2, G9a, NSD1, NSD2, PRMT1, and so on, are accessible in our chemiluminescent assays. Our talented scientists are committed to serving our clients with years of experience and skills to facilitate your HMTs based drug discovery with high quality data and fast turnaround time. To aid your drug discovery projects, Creative BioMart produces exclusive epigenetics related proteins and substrates for sale. Small molecule inhibitor library has also been established at Creative BioMart.

Procedure of Histone Methyltransferases Screening at Creative BioMart

HMTs assays at Creative BioMart involve highly specific antibodies that can recognize methyl groups. SAM is incubated with a sample containing assay buffer and purified recombinant HMT. Acceptor beads, a primary antibody, and then donor beads are then added to the mixture. Finally, the Alpha-counts is read.

General procedure of HMT screening assay

Figure 2. General procedure of HMT screening assay

Benefits of Our Histone Methyltransferase Screening Service

  1. A panel of assays to screen inhibitors or targets
  2. Offering a wide range of HMTs targets
  3. IC50 determination and single point concentrations
  4. Fast turnaround time
  5. Receive quality data results
  6. Get project guidance in a time-efficient manner

Histone Methyltransferase Biochemical Assays

Histone Lysine Methyltransferase Screening
EZH2 (Y641S) EZH1 EZH2 EZH2 (A677G)
EZH2 (A738T) EZH2-EED EZH2 (P132S) EZH2 (Y641C)
EZH2 (Y641F) EZH2 (Y641H) EZH2 (Y641N) SETDB1
SETD2 SET7/9 SET8 SMYD2
PRDM9 SUV39H1 SUV39H2 SUV4-20H1
DOT1L G9a GLP MLL1 Complex
NSD1 NSD2  
Histone Arginine Methyltransferases Screening
PRMT1 PRMT3 PRMT4 PRMT5
PRMT6 PRMT8 PRMT9

Researchers from Creative BioMart are dedicating to assisting you to identify inhibitors against HMTs with the greatest probability to success at the most competitive price. Creative BioMart is looking forward to working close with your team and make your projects advance from hit identification to clinical investigation. Our services are tailored to meet your specific needs. contact us for more information about our HMT screening services.

Reference
1. Smith, B. C.; et al. Chemical mechanisms of histone lysine and arginine modifications. Biochim Biophys Acta. 2009, 1789(1): 45–57.

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