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The ubiquitin proteasome system (UPS) is an essential and highly regulated mechanism operating to tightly control intracellular protein degradation and turnover. Recently, researchers have found new ways to chemically modulate this cellular machinery, thereby altering protein homeostasis as a therapeutic strategy to achieve phenotypic novelty and providing new avenues for pharmacological development. In particular, specific components of the UPS, such as E3 ligases, deubiquitinases (DUBs) and ubiquitin-like protein (Ubl) activating enzymes are quickly emerging as promising targets as they provide specificity for targeting with the ability to alter cellular processes within a wide range of disease indications. As new strategies and tools emerge, novel UPS inhibitors are rapidly being developed and are collectively setting the foundation for a new generation of therapeutics.

Cambridge Healthtech Institute’s third 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

 


STRUCTURAL AND MECHANISTIC INSIGHTS INTO DEUBIQUITINASE ENzYMES

Diverse Mechanisms of Allosteric Activation in DUB Enzymes

Titia Sixma, Ph.D., Professor, Head of Division and Group Leader, Biochemistry, Netherlands Cancer Institute

Regulation of Mitochondrial Ubiquitination by USP30

Christian Cunningham, Ph.D., Scientist, Early Discovery Biochemistry Department, Genentech

 

DESIGN AND DEVELOPMENT OF NOVEL (DUB) INHIBITORS

Selective Ubiquitin Protease Inhibitors for Cancer Immunotherapy

Joseph Weinstock, Ph.D., Senior Director, Medicinal Chemistry, Progenra

Development of the Proteasome Deubiquitinase Inhibitor VLX1570 for Treatment of Multiple Myeloma

Padraig D’Arcy, Ph.D., Associate Professor, Cancer Pharmacology, Department of Oncology and Pathology, Karolinska Institute

Investigating Deubiquitination with Small Molecule and Ubiquitin-Based Probes

Zhihao Zhuang, Ph.D., Associate Professor, Department of Chemistry & Biochemistry, University of Delaware

Targeting DUBs for Oncology and CNS Disorders

Xavier Jacq, Ph.D., Head of Biology, MISSION Therapeutics

Development of Novel and Selective Inhibitors of USP7 with Cellular Activity

Gerald Gavory, Ph.D., Director, Head of Biology, Almac Discovery

Simultaneous Inhibition of Deubiquitinating Enzymes and Autophagy Synergistically Kills Breast Cancer Cells

Martina Bazzaro, Ph.D., Assistant Professor, Department of Obstetrics, Gynecology and Women’s Health and Masonic Cancer Center, University of Minnesota

 


DIVERSE STRATEGIES MODULATING THE UPS & PROTEIN DEGRADATION

New Strategies for the Identification of Chemical Inhibitors of E2 Enzymes: The Problem with Ubc9

John 'Jay' Schneekloth Jr., Ph.D., Investigator, Chemical Biology Laboratory; Head, Chemical Genetics Section, Center for Cancer Research, National Cancer Institute, NIH

In Situ Generated Activity-Based Probes for Ub/Ubl E1-E2-E3 Enzymes: Structure, Activity and Biological Sensing

Farid El Oualid, Ph.D., CSO & COO, R&D, UbiQ

Discovery and Development of Novel Proteasome Inhibitors

Jonathan Blank, Ph.D., Senior Scientist, Biochemistry, Takeda Oncology

 


TARGETING RING DOMAIN E3 LIGASES

Disrupting Protein-Protein Interactions of Cullin RING E3 Ubiquitin Ligases (CRLs)

Alessio Ciulli, Ph.D., Reader, Chemical & Structural Biology, College of Life Sciences, University of Dundee

Targeting Ubiquitination Activity of RING Domain in Cancer with Small Molecules

Tomasz Cierpicki, Ph.D., Assistant Professor, Pathology, University of Michigan

 


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
Sr. Business Development Manager
Cambridge Healthtech Institute
T: (+1) 781-972-5483
E: jstroup@healthtech.com 

 
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2014 Discovery on Target Brochure  

2014 BROCHURE 

PREMIER SPONSORS 

Cellecta 

Molecular Sensing 

Rosa Drug Development Advisors
 

VIEW ALL SPONSORS 

VIEW MEDIA PARTNERS 


SPONSORSHIPS & EXHIBITS 

The exhibit hall was sold out in 2014, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2015, contact:

Jon Stroup
Sr. Business Development Manager
781-972-5483
jstroup@healthtech.com 


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