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PHERAstar measures AlphaScreen assay to develop selective inhibitors for the human YEATS domain

320 PHERAstar measures AlphaScreen assay to develop selective inhibitors for the human YEATS domain
Thomas Christott, Cameron Coxon, James Bennett, Charline Giroud, Octovia Monteiro, Oleg Federov; Structural Genomics Consortium, University of Oxforg, UK

In epigenetics it is typical to classify the proteins involved in dynamic regulation of modifications of histones in chromatin as writers, which add modifications, erasers, which remove them and readers, which convert information contained in these modifications to phenotypic changes. Proteins containing the YEATS domain, named for it presence in the proteins; Yaf9, ENL, AF9, Taf14, and Sas5, are emerging as important readers of lysines that are acetylated or preferably crotonylated.

Described here is an assay based on AlphaScreen detection that is suitable for detecting inhibitors of the YEATS domain of ENL. ENL has been identified as drug target for its role in acute leukemia. Efforts are underway to develop similar probes for each member of the YEATS family.

The PHERAstar FSX provides the necessary detection capabilities to make such drug discovery campaigns possible.

Applicable Products

The following BMG Labtech microplate reader products are applicable.