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Enzymes that modify lysine and arginine residues on histone tails and other proteins, together with the enzymes that recognise these marks, play an important role in controlling gene expression, and, hence, protein transcription. Such epi-enzymes and epi-readers have received considerable attention from pharmaceutical companies due to their role in oncology and inflammatory disease areas. Consequently, there is a requirement for robust assay technologies suitable for screening these targets.
Almac have developed:
- FLEXYTE™ epi-enzyme assays for histone methyltransferases but configured in a similar manner for other classes such as histone acetyltransferases, histone deacetylases and peptidylarginine deiminases.
- FLEXYTE™ epi-reader assays targeted towards histone-bromodomain interactions, an area of increasing focus in oncology.
The FLEXYTE™ epigenetic assay platform uses fluorescence lifetime (FLT) as the reporting modality through the use of our proprietary long lifetime fluorophore, 9-aminoacridine (9AA).1 FLEXYTE™ FLT assays are homogeneous, antibody free, easily miniaturised and less prone to interference from auto-fluorescent species leading to fewer false positives and negatives during screening.