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23/06/2021
Understanding how a small molecule compound interacts with its target protein is essential for developing successful drugs. In vitro measurements of ligand affinity and duration of drug-target interactions (e.g., residence time) often do not translate in vivo. Using the NanoBRET™ Target Engagement (TE) method, we will show the impact of oncogenic KRAS (G12C) on engagement potency for downstream effectors, including BRAF. We have also developed a pan-KRAS NanoBRET™ TE assay and will demonstrate detection of a variety of orthosteric and allosteric engagement mechanisms at this challenging target.
You will learn about:
•NanoBRET TE assays broadly enable the quantitative determination of compound affinity/potency for specific targets inside
•Protein-protein interactions and target protein activation stats have a strong influence on drug compound pharmacology using the RAS-MAPK as an example
•NanoBRET TE assays can be used to connect structural features of inhibitors to their biochemical properties in a cellular system
Registration link : https://bit.ly/3hLF7bb Free Registration
