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Application of BRET Technology to Quantitatively Determine Kinase Inhibitor Potency in Live Cells

Matthew Robers is a Senior Research Scientist and Group Leader at Promega Corporation.  Matthew has authored 30 peer-reviewed publications and published patents on the application of novel assay chemistries to measure intracellular protein dynamics. Matthew's team currently focuses on the development of new technologies to assess target engagement, emphasizing techniques enabling quantitative analysis of compound affinity and residence time at selected targets within intact cells.

Kelvin Lam is the Senior Director of Business Development at Reaction Biology Corporation. He is also the Founder and President of Simplex Pharma Advisors, Inc., which offers consulting services to early drug discovery companies. Since 2003, he has been one of the Editors-in-Chief of Drug Discovery Today, Technologies (Elsevier). Previously he held leadership and scientist positions at Blue Sky Biosciences, Harvard Stem Cell Institute, Pfizer, Inc. and ScriptGen Pharmaceuticals. Kelvin holds a Ph.D. in Biochemistry from Boston University School of Medicine and a B.A. in Chemistry from University of Hawaii at Manoa. He completed his postdoctoral-training at Dana Farber Cancer Institute and Massachusetts General Hospital Cancer Center.

  • Matthew Robers and Kelvin Lam

  • Matt Robers - Promega Corporation
    Kelvin Lam - Reaction Biology

  • Original Webinar Date: Tuesday, November 6, 2018

Methods for measuring kinase inhibitor potency in live cells are limited. In this webinar, we describe how the NanoBRET™ Target Engagement technique is overcoming technical limitations of existing methods by broadly enabling quantitative determination of kinase inhibitor occupancy in live cells. We also discuss a collaboration between Promega and Reaction Biology Corporation that has enabled conversion of these assays into a service compatible with high-throughput cell-based profiling.

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Additional Webinar Information

While ready-to-use biochemical kinase assays exist that cover large portions of the kinome, there is a need for a similar broad set of cellular kinase assays that can interrogate compound potency in live cells.

In this webinar, we describe the NanoBRET™ Target Engagement (TE) technique—the first biophysical technique to broadly enable the quantitative determination of kinase inhibitor occupancy in live cells, without disruption of cellular membrane integrity. NanoBRET TE has enabled the development of live cell quantitative compound binding assays for >200 individual full-length protein kinases.

We will also discuss our collaboration with Reaction Biology Corporation (RBC) to enable services using NanoBRET TE kinase assays. In-cell potency determinations for various types of kinase inhibitors will be shown, including type I, II and allosteric compounds. Additionally, we will show a comparative analysis between NanoBRET TE cellular assays and biochemical kinase assays that reveals a surprising intracellular selectivity profile for an approved drug. These results demonstrate the value of assessing live-cell kinase target engagement, as the cellular environment may influence potency and selectivity profiles.