Histone Methyltransferase (HMT)
Profiling & HTS

RBC Presents a Unique Assay Service:

HMT HotSpot^SM,together with an expanding line of active, human recombinant HMTs

Methyltransferase Enzymes:

Active human recombinant enzymes
Validated for drug discovery screening and profiling applications
HMT Products exclusive to RBC

The methylation of lysine and arginine in histones, especially in the N-terminal tails of histones H3 and H4, plays an essential role in the regulation of chromatin structure and the control of gene expression. For example, trimethylation of histone H3 lysine-4 (H3K4me3) in gene promoter regions is associated with transcriptional activation, while H3K27me3 in the gene body correlates with repression. Enzymes that catalyze modifications such as lysine/arginine methylation and lysine acetylation are often termed “epigenetic”, since they help create heritable states of gene activity without altering a cell’s genetics (DNA sequence). Disruptions in the regulation of epigenetic enzymes, such as overexpression of the H3K27 methyltransferase EZH2 or inappropriate localization of the H3K4 methyltransferaseMLL1, are linked to a variety of cancers. Such considerations have made HMTs the focus of increasing research and drug discovery efforts.

HMT HotSpot^SM

The only Gold Standard radioisotope based HMT assay service available for both profiling and low cost HTS;
The only assay technology that can use nucleosome, histone protein and peptide as substrates;
High quality, high sensitivity with flexible SAM concentration;
No need for substrate labeling;
No need for antibodies;
Minimum false positives and negatives;
No intermediate dilution;
No interference from fluorescent compounds;
Only nanoliters of compound needed.

HMT Services Available:

Larger scale HTS;
Large scale single dose, duplicate profiling;
IC50 profiling — 10 dose with curve fitting;
K_i determination;
Custom Assay development;
Research collaboration.

RBC’s new assays are the “Gold Standard” radioisotope based filtration assays that can be used for any enzyme reactions that use S-adenosyl-l-methionine (AdoMet or "SAM") as cofactor. For a free price quote or collaboration on special assay development, call 1-877-347-2368 or 1-610-722-0247 or email sales@reactionbiology.com.

Epigenetic factors and drug development:

Epigenetics involves the study of changes in the regulation of gene activity and expression independent on gene sequence. It has become an emerging frontier for drug discovery. Download the pdf on the background of HMT and epigenetic mechanisms.