Motivating the research toward targeting malignant brain tumor (MBT) domains is their role in oncogenesis. The MBT domain, named after the l (3) mbt family of tumor suppressor genes, is a motif of approximately 100 amino acids found in tandem repeats in proteins that bind to the lower methylation states of lysine residues present in histone tail peptides. MBT domains are known to localize to chromatin and repress transcription. They are unique within the methyllysine reader family because of their highly predictable druggability and domain-repeat structures.

Creative BioMart utilizes the affinity of AlphaScreen beads to detect the binding of various histone tail peptides with lower methylation states to MBT proteins for the discovery of MBT domain antagonists.

MBT Domain Screening Assay at Creative BioMart

The HTS assay based on amplified luminescence proximity homogeneous assay (AlphaScreen) technology is ideal for use as a screening assay in the discovery of inhibitors of binding partners that interact with Kd values in the micromolar range.

When excited at 680 nm, the donor beads convert ambient oxygen to singlet oxygen. If the beads are within 200 nm of each other, then the singlet oxygen initiates a chemiluminescent reaction in the acceptor bead that emits light in the range of 520-620 nm. The donor beads can produce thousands of singlet oxygen molecules per second, resulting in the amplification of the binding signal.

Figure 1. Examples of AlphaScreen Assay for Discovery of MBT Antagonists. (Wigle, Tim J.; et al. 2010).

Advantages of Choosing Creative BioMart

1. Flexible & One-stop service: we can provide you with comprehensive support from the design of the experimental program to the execution of the experiment to the analysis of the experimental data, and we can also offer free consulting services.
2. State-of-the-art technology platform: we have a mature first-class platform based on AlphaScreen technology, including AlphaScreen assay and subsequent series of validation, dedicated to the discovery of epigenetic drugs.
3. High-quality data & Professional data analysis: with years of experience in drug discovery, our technicians are capable of ensuring data repeatability and reliability. In addition, our professional data analysis helps you mine information that promotes the development of research from large amounts of data.

Figure 2. Workflow of Our Service at Creative BioMart

If you have any questions or specific requirement about our services, please feel free to contact us for more information.

Reference
1. Wigle, Tim J.; et al. Screening for inhibitors of low-affinity epigenetic peptide-protein interactions: an AlphaScreen™-based assay for antagonists of methyl-lysine binding proteins. Journal of Biomolecular Screening. 2010, 15(1): 62-71.