Methyltransferase PRMT5 assay in complex with MEP50 with surface plasmon resonance (SPR) format
PRMT5/MEP50 (RBC Cat# HMT-22-148)
PRMT5: Protein arginine N-methyltransferase 5
MEP50: Methylosome protein 50, WDR77
Binding kinetics of EPZ015666 on PRMT5:MEP50 with SAM and SAM analogs
Inhibitors of PRMT5 can be competitive, non-competitive, or uncompetitive with respect to SAM (or SAM-analogues) or substrate. To probe these distinct binding modes, the binding can be measured in the absence and presence of co-factors, such as SAM and SAM-analogues like SAH and MTA. Here, the binding of EPZ015666 to apo, MTA-bound, SAH-bound, and SAM-bound PRMT5:MEP50 is shown as an example of an inhibitor that binds preferentially to PRMT5 when the SAM-binding pocket is occupied. All data was collected using a Biacore 8K.