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Targeted protein degradation and proximity pharmacology

December 14, 2020, 10:00 am EDT / 4:00 pm CEST

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Program

Host and moderator: Ingo Hartung (Merck Healthcare KGaA)

15 min
Satpal Virdee (University of Dundee
E3 Discovery with Protein-based Probes
15 min
Dirk Trauner (New York University)
Optical Control of Protein Degradation
15 min
Fleur Ferguson (UC San Diego)
An Experimental Map of the Degradable Kinome as a Resource for Expedited Degrader Development
15 min
Nicolas Thomae (Friedrich Miescher Institute for Biomedical Research)
What makes two proteins stick: dissecting molecular glue action
15 min
Chris De Savi (Kymera Therapeutics)
Discovery of potent and selective IRAK4 and STAT3 targeted protein degraders for inflammation and oncology indications
15 min
Lindsey James (University of North Carolina at Chapel Hill)
Regulation of Histone Methylation with Methyl-lysine Reader Targeted Degraders

BIO SKETCHES

Headshot of Ingo Hartung

Ingo Hartung (Merck Healthcare KGaA)

Ingo Hartung is heading Medicinal Chemistry GER at Merck Healthcare KGaA since 2019. He is an experienced medicinal chemist with a demonstrated history of successfully driving projects into clinical development in cardiology and oncology and steering project portfolios. He is especially interested in innovative NCE modalities, such as protein degraders and modulators of RNA function, and lead finding technologies for difficult-to-drug targets.

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Satpal Virdee (University of Dundee)

Satpal Virdee is a program leader in protein ubiquitylation at the MRC Protein Phosphorylation and Ubiquitylation Unit at the University of Dundee. He is interested in studying E3 ligases at the biochemical, structural and cellular level. His lab recently developed probe technologies that enable parallel profiling of the activity state of potentially hundreds of E3 ligases (activity-based protein profiling). This technology allows one to not only address which E3 ligases are switched on and off during fundamental cellular processes, but to identify those that belong to undiscovered classes with medical importance. 

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Dirk Trauner (New York University)

Dirk Trauner is the Janice Cutler Chair in Chemistry at New York University. The broad objective of his research is to demonstrate the power of chemical synthesis with challenging target molecules and to use it toward the establishment of synthetic biological pathways. Photopharmacology is a special focus of his research group.

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Fleur Ferguson (UC San Diego)

Fleur Furguson received her M.Sc in chemistry from Imperial College London, and her Ph.D in chemistry from the University of Cambridge. She performed her postdoctoral research in the laboratory of Professor Nathanael S. Gray at Harvard Medical School and Dana-Farber Cancer Institute.

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Nicolas Thomae (Friedrich Miescher Institute for Biomedical Research

The Thomä laboratory is interested in chromatin-bound machines and their regulation by the ubiquitin proteasome system. Guided by structural biology, we use a range of genetic, chemical and complex biochemical reconstitution approaches to study protein function in genome maintenance and transcription. A particular focus is on dissecting how chromatin and the ubiquitin transferase system interplay.

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Chris De Savi (Kymera Therapeutics)

Chris De Savi is Vice President and Head of Drug Discovery at Kymera Therapeutics. Kymera Therapeutics is a biopharmaceutical company developing novel protein degrader therapeutics to selectively degrade disease causing proteins with the goal of completely removing them from the body. Chris’ team contributes to all drug discovery phases at

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Lindsey James (University of North Carolina at Chapel Hill)

Lindsey James is an Assistant Professor in the Division of Chemical Biology and Medicinal Chemistry in the Eshelman School of Pharmacy at the University of North Carolina. Her laboratory integrates expertise in medicinal chemistry, chemical biology, and chromatin biology in order to discover novel epigenetic inhibitors and protein degraders in order to better define the role of epigenetic proteins in disease and as potential therapeutics.

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