Histone Methyltransferases Screening: Identifying Inhibitors against Epigenetic Modifiers, Slides of Biology

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HMT Inhibitor 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.

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.

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.

Thank you!

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