PRMT5/MEP50 SPR Assay Service

Methyltransferase PRMT5 assay in complex with MEP50 with surface plasmon resonance (SPR) technique

Target Overview

Target

PRMT5 in complex with MEP50 in the absence and presence of co-factors

Synonyms

PRMT5: Protein arginine N-methyltransferase 5
MEP50: Methylosome protein 50, WDR77

Scientific information

Protein source

Reaction Biology Cat# HMT-22-148

Screening location

Malvern, PA, USA

Further information

More information can be found on our website SPR Assay Services for Drug Discovery

Binding kinetics of reference compound (EPZ015666) on PRMT5:MEP50 with SAM and SAM analogs

PRMT5/MEP50 binding kinetics

PRMT5 inhibitor

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.