The ubiquitin proteasome system (UPS) is an essential and highly regulated mechanism operating to tightly control intracellular protein degradation and turnover. While the concept of targeting specific components of the UPS to modulate protein degradation has been around for some time now, recent advances in our understanding of the role and molecular mechanisms of UPS components in disease – mainly DUBs and E3 ligases, the development of high-quality chemical tools and novel inhibitors, as well as preclinical studies demonstrating chemical tractability and therapeutic potential – have dramatically taken the Ubiquitin Proteasome System from an improbable target class, to one of the most robust and exciting arenas for the discovery of novel drugs. Indeed, over the past year, we have seen the generation of several DUB inhibitors poised for clinical development, novel approaches and inhibitors disrupting the protein-protein interactions of E3 ligases and PROTACs-derived degradation of target proteins.
Cambridge Healthtech Institute’s fourth annual Targeting the Ubiquitin Proteasome System will once again gather an interdisciplinary collection of leaders working to advance the rapidly expanding field of UPS drug discovery.
Small-Molecule PROTACs for Protein Degradation
Alessio Ciulli, Ph.D., Associate Professor, Chemical & Structural Biology, School of Life Sciences, University of Dundee
A New Paradigm in Drug Action: Differentiated Gain of Function among IMiD Structural Analogues Binding the E3 Ubiquitin Ligase, CRL4CRBN
Brian Cathers, Ph.D., Executive Director, Co-Leader & Head, Drug Discovery, Protein Homeostasis Thematic Center of Excellence, Celgene
Mechanism and Specificity of Deubiquitinating Enzyme USP14
Daniel Finley, Ph.D., Professor, Cell Biology, Harvard Medical School
Talk Title to be Announced
Ingrid E. Wertz, M.D., Ph.D., Senior Scientist, Molecular Oncology and Early Discovery Biochemistry, Genentech, Inc.
Chemical Proteomics in the Ubiquitin System – DUBs Take Center Stage
Benedikt Kessler, Ph.D., Professor, Biochemistry and Life Science Mass Spectrometry, Target Discovery Institute, Nuffield Department of Medicine, University of Oxford
Selective De-Ubiquitylase Inhibitors for Cancer Immunotherapy
Tauseef R. Butt, Ph.D., President and CEO, Progenra, Inc.
Development and Exploitation of Ubi-Plex™, an Innovative Purpose-Built Drug Discovery Platform for Deubiquitinating Enzymes (DUBs)
Gerald Gavory, Ph.D., Director, Head of Biology, Almac Discovery
Discovery of Highly Selective Macrocyclic Inhibitors of DUBs: USP9x as a Case Study
Deborah Dodge, Senior Scientist, Ensemble Therapeutics
Discovery of Novel Protein Homeostasis Inhibitors Utilizing FORMA’s Drug Discovery Engine
Stephanos Ioannidis, Ph.D., Director, Medicinal Chemistry, FORMA Therapeutics
Targeting Ubiquitin-Like Proteins
Lawrence R. Dick, Ph.D., Scientific Fellow, Takeda Oncology
Inhibition of E2/E3 Protein-Protein Interaction as Novel Strategy to Interfere with E3 Ligase Activity
Kamyar Hadian, Ph.D., Head, Assay Development and Screening Platform, Institute of Molecular Toxicology and Pharmacology, German Research Center for Environmental Health (GmbH)
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Cambridge Healthtech Institute
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