Epigenetic regulation has been shown to be a contributing factor in a variety of diseases, and discovery of methyltransferase inhibitors is an area of intense activity. Methyltransferase enzymes methylate a variety of substrates using S-adenosylmethionine (SAM) as the methyl donor leaving S-adenosylhomocysteine (SAH) as a common product. Since the difference between SAH and SAM is merely one methyl group, developing assays that can selectively measure one over the other has been a technological hurdle. Scientists at BellBrook Labs have engineered a naturally occurring aptamer, or “riboswitch” with exquisite specificity for SAH. By directly detecting SAH in a homogeneous format with unparalleled sensitivity, it is possible to perform screening and enzymatic studies with virtually any methyltransferase. The new AptaFluor SAH Methyltransferase Assay will aid researchers in hit identification and characterization in the quest to develop methyltransferase inhibitors as treatments for debilitating disease.
In this webinar we discuss:
- Engineering a microbial riboswitch for direct detection of SAH in a homogeneous format with a positive TR-FRET readout
- Demonstrated assay robustness for use in hit identification and characterization studies including reagent stability, signal stability, and sensitivity
- Comparison of other assay methods with the new AptaFluor SAH Methyltransferase Assay
- Unparalleled assay sensitivity that can be harnessed for use with low turnover methyltransferase enzymes and SAM concentrations as low as 100 nM