PerkinElmer, Inc. and EpiCypher are collaborating to offer AlphaLISA® assay kits which measure the binding of the BRD4 and P300 bromodomains to various acetylated histone H2A, H3, or H4 peptides. These kits are designed to help biopharmaceutical and academic researchers perform small molecule drug discovery analysis on epigenetic reader proteins.

Bromodomain and Extra-Terminal motif (BET) inhibitors are an emerging class of drugs (currently in development in the U.S. and Europe) with anti-cancer, immunosuppressive, and other effects. These molecules reversibly bind the Bromodomains of the BET family proteins (BRD2, BRD3, BRD4, and BRDT), and prevent interaction between BET proteins and acetylated histones and transcription factors.

Researchers at biopharmaceutical companies, CROs and academic screening centers aim to better understand the role of Bromodomain reader interactions with histone tails in cancer, inflammation, and developmental disorders. Better identification of more selective and specific BET inhibitors will enable advanced knowledge of disease mechanisms and discovery of selective drugs with minimized side-effects to treat cancer, inflammation, and developmental disorders.

The new AlphaLISA Bromodomain binding assays kits help researchers profile a wide range of compounds on different bromodomains and acetylated histone peptide tails used in pharmacologically relevant concentrations to generate more biologically relevant data.

PerkinElmer is the only provider of this unique combination of AlphaLISA technology, EpiCypher’s epigenetics reagents, and Bromodomains and histone tail peptide variants. Together they allow quantitation of protein-protein interactions under pharmacologically relevant conditions, enabling researchers to execute highly sensitive, reproducible assays for identifying selective drugs more efficiently.