Targeting the Ubiquitin Proteasome System Header


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.

Preliminary Agenda


HARNESSING THE UPS SYSTEM FOR TARGETED PROTEIN DEGRADATION

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


STRUCTURAL AND MECHANISTIC INSIGHTS INTO
DEUBIQUITINASE ENZYMES

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


DESIGN AND DEVELOPMENT OF
NOVEL DEUBIQUITINASE (DUB) INHIBITORS

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


NOVEL STRATEGIES AND TOOLS MODULATING THE UPS

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)




For questions or suggestions about the meeting, please contact:
Kip Harry
Conference Director
Cambridge Healthtech Institute
T: (+1) 781-972-5454
E: kharry@healthtech.com

For sponsorship and exhibit sales information including sponsored podium presentations, contact:
Jon Stroup
Senior Manager, Business Development
Cambridge Healthtech Institute
T: (+1) 781-972-5483
E: jstroup@healthtech.com