PHD Screening


Plant homeodomain (PHD)-finger containing proteins are important epigenetic regulators and are of interest as potential drug targets. PHD-fingers are C4HC3 type zinc-finger binding domains present in many chromatin-modifying proteins. These small 50-100 residue domains bind to histones, enabling the enzyme to localize to specific targets and promote the recruitment of transcription factors or chromatin-associated protein complexes. It is well known that some PHD-fingers recognize specific histone modifications, including unmethylated and methylated H3K4, acetylated H3K14, H3K9me3, and methylated arginine residues primarily at H3R2. Mutations, deletions or chromosomal translocations of PHD-finger encoding genes are associated with a range of diseases, including cancer, immunodeficiency, and neurological disorders.

With the state-of-the-art AlphaScreen technology platform and expertise, Creative BioMart is currently able to offer the PHD-finger inhibitor screening service, and PHD-finger inhibitors will be useful in exploring biological functions and therapeutic potential of PHD-fingers.

PHD Screening Assay at Creative BioMart

AlphaScreen is a homogenous bead-based assay for studying protein-protein interactions. We use a streptavidin-conjugated donor and a nickel-conjugated acceptor bead pair to detect the interaction of the His-tagged PHD fusion protein and the C-terminally biotinylated histone peptide, and then measure the AlphaScreen signal changes as inhibitor concentrations increased to quantify the level of binding and determine IC50 values (half maximal inhibitory concentration).

Schematic Diagram of AlphaScreen Assay

Figure 1. Schematic Diagram of AlphaScreen Assay

Advantages of Choosing Creative BioMart

  1. Skillful technical team: supported by a knowledgeable team with years of drug research experience, Creative BioMart provides state-of-the-art inhibitor screening service of PHD-finger containing proteins to deliver high-quality leading compounds to your development program of epigenetic therapy.
  2. Highly customized service: we will take full advantage of the drug discovery platform to further explore the workflow and tools tailored to your research focus.
  3. Reliable data quality: our experienced team of experts performs quality control after each procedure to ensure credible results. Optimized assay conditions will be determined to ensure the interactions could be detected in the linear range of the assay, with a good signal-to-background ratio.

Workflow of Our Service at Creative BioMart

Figure 2. Workflow of Our Service at Creative BioMart

If you are interested in drug discovery associated with PHD-finger containing proteins, please contact us for more information and a detailed quote.

Reference
1. Bhushan B.; et al. Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases. Bioorganic & Medicinal Chemistry. 2018.

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