PROGRAMS
Ubiquitin Drug Discovery and Diagnostics 2010
Date: August 23, 2010 — August 25, 2010
Location: Four Seasons Hotel, Philadelphia, PA
PROGRAMS DETAILS
Click to View Conference ProgramRegistration opens at 7:00am each day
Tuesday, August 24, 2010
7:00am Continental Breakfast (Ballroom Foyer)
8:00am Welcome by the Conference Chair
Dr. Joseph Bolen, CSO, Millennium: The Takeda Oncology Company
8:15am Welcome by the Hon. Michael A. Nutter, Mayor of Philadelphia
8:30am Keynote Address
The Ubiquitin-Proteasome Pathway and Drug Development:
Looking Backward and Looking Forward
Dr. Alfred L. Goldberg Professor of Cell Biology
Harvard Medical School, Boston MA
Harvard Medical School, Boston MA
Session 1 Understanding the Ubiquitome
Session Chair: Dr. Joseph Bolen, Millennium: The Takeda Oncology Company
9:15am Assembly and Structure of the Eukaryotic Proteasome
Dr. Mark Hochstrasser
Yale University
Yale University
9:40am Proteomic and informatic approaches in the study of the Ubiquitin Pathway
Dr. Wade Harper
Harvard Medical School
10:05am Coffee Break
10:40am Modulation of prion formation by the ubiquitin proteasome system
Harvard Medical School
10:05am Coffee Break
10:40am Modulation of prion formation by the ubiquitin proteasome system
and actin cytoskeleton
Dr. Keith D. Wilkinson, Emory University
Dr. Keith D. Wilkinson, Emory University
11:05am Postsynaptic mechanisms of ubiquitination and de-ubiquitination involved in
synapse structure and function
Dr. Gentry Patrick
University of California, San Diego
University of California, San Diego
11:30am Chemically ubiquitylated PCNA as a probe for eukaryotic translesion synthesis
Dr. Zhihao Zhuang
University of Delaware
University of Delaware
11:45am Modulating activity of a deubiquitinating enzyme OTUB1 via phosphorylatio
Dr. Mariola Edelmann
Mississippi State University
Dr. Mariola Edelmann
Mississippi State University
12:00pm Lunch in the Swann Restaurant
Session 2 Targeting Deubiquitylases for Therapy
Session Chair: Dr. Marco Gottardis, Bristol-Myers Squibb
1:30pm Enzyme regulatory mechanisms of USP7
Dr. James Ernst
Genentech, Inc.
1:55pm Ubiquitin Specific Proteases as novel drug targets – A case study
Dr. James Ernst
Genentech, Inc.
1:55pm Ubiquitin Specific Proteases as novel drug targets – A case study
Dr. Jonathan D. Wrigley
AstraZeneca
2:20pm Discovery of Ubiquitin Isopeptidase Inhibitors
Dr. Ben Nicholson
Progenra, Inc.
AstraZeneca
2:20pm Discovery of Ubiquitin Isopeptidase Inhibitors
Dr. Ben Nicholson
Progenra, Inc.
2:45pm The EXCRT-DUBs USP8 and AMSH Modulate ESCRT-0 to Control Receptor
Transit through the Sorting Endosome
Dr. Piers Nash
University of Chicago
Dr. Piers Nash
University of Chicago
3:00pm Coffee Break
3:20pm Deubiquitylases and exploration of chemical space
Dr. Christopher P. Austin
NIH Chemical Genomics Center
NIH Chemical Genomics Center
3:40pm Quantitative assays for classification of ubiquitin-proteasome drugs reveal a
selective inhibitor of p97 ATPase
Dr. Tsui-Fen Chou
Howard Hughes Medical Institute, California Institute of Technology
3:55pm Specificity of DUB inhibitors in cells profiled by
activity-based chemical proteomics
Dr. Benedikt M. Kessler
Oxford University
Oxford University
4:20pm Inhibition of proteasomal deubiquitinating enzyme Usp14
Dr. Dan Finley
Harvard University
Harvard University
4:45pm Dubya, an IAP-directed deubiquitylase controls Drosophila cell death
Dr. Michael J. Thomenius
Duke University Medical Center
Duke University Medical Center
5:00pm Business Roundtable Discussion Groups
(1) Biotech and Pharma Partnership: The new face of the industry
(1) Biotech and Pharma Partnership: The new face of the industry
Chair: Dr. Tom Argentieri, Sr. Director of Business Development, Progenra Inc.
Panel: Ms. Kate Shay, J.D., Corporate Law, Duane Morris, Philadelphia;
Panel: Ms. Kate Shay, J.D., Corporate Law, Duane Morris, Philadelphia;
Dr. Gad Soffer, Director, Business Development, Celgene Inc.
Many forces are at work to change the pharma industry. Lack of drug approvals to address for unmet needs, health care reform, and mergers of major pharmaceutical companies have created a new business climate. The drug discovery model is changing rapidly as pharma tries to reduce its cost and yet keep core R and D functions. What role will small biotech play in filling the pipeline of pharma development? Does the ubiquitome provide an opportunity for the discovery of novel drugs?
(2) Academia and Industry Partnership: Translational Research
Chair: Dr. David Counts, Sr. Director Business Development, Progenra Inc.
Panel: Robert C. Netter, Jr., Ph.D., J.D., Patent Attorney, Dann Dorfman Harrell Skillman, Philadelphia; Dr. Neil Wilkie, Programme Manger, ITI Life Science, Scotland
Panel: Robert C. Netter, Jr., Ph.D., J.D., Patent Attorney, Dann Dorfman Harrell Skillman, Philadelphia; Dr. Neil Wilkie, Programme Manger, ITI Life Science, Scotland
Unprecedented developments in “omics” driven science has created exciting opportunities for drug discovery in academia. NIH Road Map initiatives solicit “translational medicine” grant applications that are having a direct impact on drug discovery and diagnostics. At the same time, during economic stress and the resulting lack of jobs in the private sector, more academic researchers are competing for limited amounts of federal funds. There has never been the greater need to establish academic and industry partnerships to bring new technologies to the market. Academic colleagues are encouraged to offer their views on ways academic labs can develop joint programs with biotechs.
(3) Role of the NIH in Drug Discovery
Chair: Dr. David Newman, Chief, NPB, DTP, NCI-FCRDC
Panel: Dr. Christopher Austin, Director, Chemical Genomics Center, NIH;
Dr. Ben Nicholson, Director, Biology, Progenra Inc.
Panel: Dr. Christopher Austin, Director, Chemical Genomics Center, NIH;
Dr. Ben Nicholson, Director, Biology, Progenra Inc.
Historically the NIH has played a key role in development of drugs, many of which are currently in use. Recent bold actions taken by the NIH have created new programs that have the potential to change the face of drug discovery. Natural products have been the source of many marketed drugs, and the NIH has made its extensive collection of natural products extracts available to countless drug discovery (screening) campaigns. In addition, the National Center for Chemical Genomics at NIH is spearheading programs to identify small molecule probes that will act as key tools for validating drug targets and as important drug leads. Although these NIH programs are not well publicized, scientists in academia and industry are encouraged to benefit from the opportunities that they provide.
6:00pm Poster Viewing & Cocktail Hour
7:30pm Dinner in the Ballroom Rounds
7:30pm Dinner in the Ballroom Rounds
Wednesday, August 25, 2010
7:00am Continental Breakfast in the Ballroom Foyer
Session 3 Targeting E3 ligases for therapy
Session Chair: Dr. Arthur Haas, Louisiana State University
8:30am Novel Mechanism-based E1 Inhibitors in Drug Discovery
Dr. Jesse Chen
Millennium: The Takeda Oncology Company
8:55am Structural Insights and Functional Complexity of E2 - RING Finger E3 Interactions
Millennium: The Takeda Oncology Company
8:55am Structural Insights and Functional Complexity of E2 - RING Finger E3 Interactions
Dr. Allan Weissman
National Cancer Institute at Frederick (MD)
National Cancer Institute at Frederick (MD)
9:20am Regualation of the cell cycle by the SCFCyclin F ubiquitin ligase complex
Dr. Michele Pagano
Howard Hughes Medical Institute, New York University School of Medicine
Howard Hughes Medical Institute, New York University School of Medicine
9:45am Mechanism for recognition of polyubiquitin chains: Balancing affinity through
interplay between multivalent binding and dynamics
Dr. Leo Spyracopoulos
University of Alberta
University of Alberta
10:00am Coffee Break
10:40am Identification of E3 Ligase Inhibitors Using a Novel Assay
Dr. Michael Eddins
Progenra, Inc.
Progenra, Inc.
11:05am Modulation of Parkin E3 Ligase Activity with Small Molecules
Dr. Jennifer Johnston
Elan Pharmaceuticals, Inc.
Dr. Jennifer Johnston
Elan Pharmaceuticals, Inc.
11:30am HectH9 inhibitors as potential anti-cancer therapeutics
Dr. Stefanie Peter
University of Würzburg
Dr. Stefanie Peter
University of Würzburg
11:45am KF-1 ubiquitin ligase: anxiety suppressor model
Dr. Tamotsu Hashimoto-Gotoh
Kyoto Prefectural University of Medicine
Kyoto Prefectural University of Medicine
12:00pm Lunch in Swann Restaurant
Session 4 Ubiquitin Pathway Inhibitors in the Clinic
Session 4 Ubiquitin Pathway Inhibitors in the Clinic
Session Chair: Dr. Keith Wilkinson, Emory University
1:30pm ONX0912: an in vitro and in vivo evaluation of an orally bioavailable proteasome
inhibitor
Dr. Shirin Kapur
Onyx Pharmaceuticals
Onyx Pharmaceuticals
1:55pm Proteomics of mitotic ubiquitome of Xenopus laevis embryo
Dr. Jacek Kubiak
University of Montreal
Dr. Jacek Kubiak
University of Montreal
2:05pm A Proteomics Approach to Profile Human Ubiquitome
Dr. Yi Shi
Baylor College of Medicine
Baylor College of Medicine
2:20pm Targeting Protein Degradatation as a Therapeutic Strategy in Myeloma
Dr. Kenneth Anderson
Dana-Farber Cancer Institute
2:45pm Preventing the UPS-dependent degradation of frataxin, the protein defective in
Dr. Kenneth Anderson
Dana-Farber Cancer Institute
2:45pm Preventing the UPS-dependent degradation of frataxin, the protein defective in
Friedreich’s Ataxia
Dr. Silvia Fortuni
University of Rome
3:00pm Coffee Break
Dr. Silvia Fortuni
University of Rome
3:00pm Coffee Break
3:30pm Role of proteasome inhibition in organ transplantation
Dr. E. Steve Woodle
University of Cincinnati
Dr. E. Steve Woodle
University of Cincinnati
3:55pm Inhibition of NEDD8-activating enzyme for cancer treatment: Preclinical
validation to clinical application of MLN4924
Dr. Peter G. Smith
Millennium: The Takeda Oncology Company
Millennium: The Takeda Oncology Company
4:20pm Effective Proteasome Inhibitors for Inflammation and Septic Shock
Dr. Nilofer Qureshi
University of Missouri, Kansas City
University of Missouri, Kansas City
4:35pm Autophagy inhibition for myeloma therapy
Dr. Dan Vogl
University of Pennsylvania
Dr. Dan Vogl
University of Pennsylvania
5:00pm Conference Concludes














