MBT Domain Inhibitor Screening, Slides of Biology

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MBT Domain Inhibitor

Screening

Epigenetic posttranslational modifications (PTMs) of histone are critical for the regulation of eukaryotic transcription. Enzymes establishing and maintaining the epigenetic code are called “writer” and “eraser” by creating or removing posttranslational marks, respectively. Readers are specific binding proteins that recognize histone PTMs and mediate epigenetic signaling. The structure of reader domains provides a typical cavity or surface groove that can accommodate a specific epigenetic mark. Interactions between reader domain and the flanking sequence of the modified amino acid allow the protein containing reader domain to distinguish similar epigenetic marks, such as histone lysine mono-, di- and trimethylation.

Given the physiological importance of epigenetic reader domains in gene transcription, pharmacological manipulation of these proteins may represent a promising new area for drug discovery against a broad array of disease states. The discovery of selective inhibitors targeting epigenetic readers has tremendously promoted the understanding of the epigenetic regulatory mechanisms as well as the molecular and structural determinants of binding specificity and druggability of these reader domains. To help make reader domain research possible, Creative BioMart offers a broad panel of reader domain assays. A versatile assay platform is utilized for the screening of small-molecule inhibitors and the detailed characterization of inhibitors. Our collection of reader domain assays can be used for screening, lead optimization or selectivity profiling to identify reader domain inhibitors. Our proficient experts will participate in every step of the process to provide high-quality solutions to make discovery possible. Along with this procedure, novel inhibitors of epigenetic reader domains

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