Methyltransferases are a large group of enzymes methylating their substrates. The most common class of methyltransferases usually contains a Rossman fold for binding S-Adenosyl methionine (SAM), which is a classical methyl donor for methyltransferases and is converted to S-Adenosyl homocysteine (SAH) during methylation. Methyltransferases are known to be of relevance in epigenetic gene regulation by covalent modification of DNA and histones.

In particular, DNA methyltransferases (DNMTs) transfer a methyl group to DNA cytosines. DNA methylation suppresses gene expression, and is critical for transcriptional silencing during X-inactivation, imprinting and other developmental processes. Additionally, histone methyltransferases (HMTs) modify histone proteins by transferring methyl groups in SAM to lysine or arginine residues. HMTs also regulate or control DNA methylation by chromatin-dependent transcription repression or activation, which further affects gene expression levels. An ever-increasing body of evidence indicates that aberrant DNA methylation and histone methylation are implicated in genetic diseases, cancer, and metabolic diseases. Selective inhibition of DNMTs and HMTs may lead to demethylation and expression of the silenced tumor suppressor genes, and DNMTs as well as HMTs are among the first epigenetic targets to be addressed for drug development. Herein, DNMTs and HMT inhibitors are currently being developed as promising therapeutic drugs for the control of cancers and many other diseases.

Creative BioMart provides a menu of both DNA methyltransferase and histone methyltransferase screening assays to be applied in in vitro biochemical assessment of compound binding to a methyltransferase target and the measurement of inhibitor potency. The obtained results could act as a guide to optimize your compounds based on inhibitory activities and to make more informed decisions about the therapeutic potential of your lead compounds. All methyltransferases are produced in house and are also available for purchase. Aside from purified enzymes, the substrates in assay could also be found at Creative BioMart, including purified full-length histone proteins, tetramers, octamers, nucleosomes, and a number of modified histones. This diverse portfolio enables researchers to complete their experiments with optimal flexibility.

Methyltransferase Screening Services at Creative BioMart

DNA Methyltransferase Screening
DNA methylation catalyzed by DNMTs plays an important role in modulating epigenetic chromatin structure, and the changes in DNA methylation patterns are closely linked to diseases. Creative BioMart has developed a wide range of assay platforms for a series of DNMTs targets to assist your DNMTs-based drug discovery project with the most competitive price and highest data quality.

Histone Methyltransferase Screening
Histone methylation is involved in regulating genome compaction and gene expression. Several histone methyltransferases are associated with diseases, in particular cancer. HMT inhibitors have attracted growing attention in various therapeutic applications. Creative BioMart has confidence in accelerating your HMTs targeting therapy through a set of HMTs assays within fast turnaround time.

Highlights & Benefits of Methyltransferase Screening Service at Creative BioMart

1. A broad panel of assays for screening inhibitors or targets
2. Conducting both IC₅₀ (half maximal inhibitory concentration) determination and single dose profiling
3. Large scale high-throughput screening
4. Custom assay development to meet your needs
5. A wide range of HMTs targets available
6. Fast data feedback after days of sample submission
7. Broad applications in primary screening, lead optimization, structural activity relationship analysis

With screening and profiling services at Creative BioMart, your methyltransferase assays can be achieved in an inexpensive and time-saving manner. Our highly skilled and experienced experts are competent to present you high quality, reproducible data in a fraction of the time to meet all your project timelines and requirements. If you have any special requirements in methyltransferase screening profiling service, please feel free to contact us.

Reference
1. Tan, Siok-Lay; et al. Essential roles of the histone methyltransferase ESET in the epigenetic control of neural progenitor cells during development. Development. 2012, 139(20): 3806-3816.