Cambridge Healthtech Institute’s 3rd Annual
Ubiquitin-Induced Targeted Protein Degradation
Optimizing PROTACs and Small Molecule Degraders for Pursuing Undruggable Targets
April 14-15, 2020
The ubiquitin-proteasome system (UPS) is a well-controlled, selective mechanism for intracellular protein degradation and turnover, and acts as a key regulator in cancer, CNS, and other diseases. Over the past few years, a new generation of inhibitors and activators have been developed for disrupting protein-protein interactions and for hijacking the UPS for protein degradation. Proteolysis-targeting chimeric molecules (PROTACs), molecular glues, and other chemical entities are being developed for targeted protein degradation and have potential to seek out previously “undruggable” protein targets for drug discovery and therapeutic applications. However, some challenges do exist in terms of stability, biodistribution, and penetration of these molecules in vivo. The conference on Ubiquitin-Induced Targeted Protein Degradation will bring together experts who can discuss the potential, as well as the challenges underlying targeted protein degradation as a new approach for therapeutic intervention.
ASSAYS & MODELS FOR STUDYING DEGRADATION & TARGET SPECIFICITY
Use of Tip60 PROTACs in Cereblon-Knockin Mice
Wayne W. Hancock, MD, PhD, Professor, Pathology and Chief of Transplant Immunology, Children’s Hospital of Philadelphia and University of Pennsylvania
Chemical Tools to Evaluate E3: (Neo)Substrate Pairs
Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston
Engineered Ubiquitin Variants as Tools to Find Small Molecules Targeting Ubiquitin Enzymes
Jacky Chung, PhD, Scientist, Laboratory of Dr. Sachdev Sidhu, Donnelly Center, University of Toronto
Computational Exploration of Novel Drug Targets, Modalities and Design
Yuan Wang, PhD, Senior Principal Scientist, Head of TPD Data Science, UCB Pharma
DESIGN & OPTIMIZATION OF DEGRADERS AND INHIBITORS
ADME Properties of PROTACs and Oral Bioavailability Improvement Strategies
Upendra Dahal, PhD, Senior Scientist, Pharmacokinetics and Drug Metabolism, Amgen, Inc.
Target Engagement and Protein Degradation: Lessons Learned and Future Applications
Denise Field, PhD, Senior Scientist, I&I Chemistry and Chemical Biology, Pfizer Inc.
TARGETED PROTEIN DEGRADATION FOR ONCOLOGY
Targeted Degradation of Bromodomain-Containing Proteins for Cancer Therapy
Murali Ramachandra, PhD, CSO, Aurigene Discovery Technologies Limited
Ubiquitin-Mediated Small Molecule-Induced Target Elimination (uSMITE) for Cancer
Michael Plewe, PhD, Vice President, Medicinal Chemistry, Cullgen, Inc.
A Modular PROTAC Design for Target Destruction Using Single Amino Acid-Based Degradation Signal
Hai Rao, PhD, Professor, Molecular Medicine, University of Texas Health
TARGETED KINASE DEGRADATION STRATEGIES
Molecular Mechanisms of Small Molecule Mediated Ubiquitin Ligase Targeting
Eric Fischer, PhD, Assistant Professor, Cancer Biology/Biological Chemistry and Molecular Pharmacology, Dana-Farber Cancer Institute/Harvard Medical School
Targeting Focal Adhesion Kinase with PROTACs: From Tool to in Vivo
Joao Nunes, PhD, Investigator, Protein Degradation Group, Medicinal Science and Technology, GSK Medicine Research Centre
New Activities for Cereblon Modulators
Philip Chamberlain, DPhil, Executive Director, Structural and Chemical Biology, Celgene
* The program is subject to change without notice, due to unforeseen reason.