(1107-D) The Development of a Novel Mobility Shift Analysis System for Kinase Small Molecule Drug Discovery using the SCIEX BioPhase 8800
Tuesday, February 6, 2024
2:00 PM – 3:00 PM EST
Location: Exhibit Halls AB
Abstract: The Mobility Shift Assay (MSA) for separation of substrate and product, in various forms of enzymatic reaction, has been popular with drug discovery for over 20 years. Caliper Lifesciences/Perkin Elmer (Revvity) successfully commercialized this methodology enabling many drug discovery companies to execute screens and medicinal chemistry support across many therapeutic areas and target classes. Carna Bioscience was one of the early adopters of the technology to support its own kinase drug discovery programs but also to provide support to its commercial kinase production service and to offer small molecule drug profiling across the kinome.
Perkin Elmer announced that the EZReaderII instrument and ecosystem (consumables and support etc.) were to be discontinued as of end of 2024, leaving many MSA-dedicated companies with no MSA options.
In this poster, we show how Carna Bioscience identified and operationalized the SCIEX BioPhase 8800 instrument to perform MSA for kinase drug discovery. This process started from scratch and touched on every aspect of the separation and analysis of kinase substrate and peptide products, including buffer conditions, separation variables, and even software peak recognition and measurement.
The resulting new system provides a way forward to maintain the benefits of MSA analysis for enzyme reactions in a medium-throughput method, as well as maintaining robust consistency with historical data.
Final optimization of the detection conditions and other variables are in progress, in order to further improve the throughput and automation of data analysis. The projected launch and full incorporation of the BioPhase 8800 into Carna’s work flow is Spring 2024.