Beyond Degradation: Cell-based and Biophysical PROTAC Characterization using BRD4 as a Target

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During PROTAC development various assays are required to inform and progress the design-make-test cycle. PROTAC’s have been developed to BRD4 – a member of the BET (bromodomain and extra-terminal) family. 

At Charnwood Discovery we have used cell-based and biophysical techniques to investigate the BRD4-targeting PROTAC ‘dBET6’ to elucidate a binding mechanism, confirm proteasomal degradation and monitor its impact on cellular behavior. 

In the Webinar we demonstrate a set of orthogonal techniques used to probe BRD4 PROTAC activity that we might typically implement in a PROTAC development cascade to build confidence in target depletion and associated biological validation.

About the Presenter

Dr Gary Allenby

Dr Gary Allenby

Director of Bioscience

Gary brings together innovative technology from R&D partners with client projects to create synergies and novel readouts, improving assay quality and reducing client project SAR cycle times. He leverages over 30 years of pre-clinical drug discovery experience and a number of scientific papers in leading journals to aid the discovery of new chemical entities.

Dr James Chamberlain

Dr James Chamberlain

Senior Research Scientist

James obtained his undergraduate degree in Biochemistry from the University of York. He then moved to the University of Nottingham for his Masters and PhD. James is our in-house expert on using our IncuCyte SX5 for live-cell imaging and works closely with the rest of our bioscience team to deliverer robust, reliable assays.

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