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Web Desc
Addressing the Challenges of Drug Discovery - Novel Targets, New Chemical Space and Emerging Approaches
Organizer(s): Stephen V. Frye, Michael Varney and James A. Wells
Date: March 19 - 23, 2012
Location: Granlibakken Tahoe, Tahoe City, CA, USA
Sponsored by Bayer USA Foundation, Bristol-Myers Squibb Company, Genentech, Inc. and Infinity Pharmaceuticals
Summary of Meeting:
The scientific and organizational landscape that underpins drug discovery is in a state of rapid evolution. The cellular signal transduction processes and biochemical pathways that enable life are increasingly understood at the molecular level and hypotheses for disease intervention can be proposed within this rational context. Technology to enable discovery of ligands to perturb the function of biological targets continues to advance and new methods to create small molecule tools to interrogate biological processes and potentially serve as drug leads are under development. However, while industry investment in R&D has grown exponentially, approval of new medicines has remained constant for several decades. Juxtaposition of this scientific opportunity, the continuing societal need for new drugs, and a failing model for translation of basic research into new medicines provides fertile soil for new ideas and approaches. This meeting will focus on addressing these challenges in drug discovery with an emphasis on novel biological targets, new chemical space and emerging organizational approaches to more effective translation. The goals of the meeting are: • To explore relatively uncharted protein target class families to define new druggable biological space • To survey promising new chemical approaches for ligand discovery • To highlight new organizational constructs for drug discovery with an emphasis on public/private partnerships The meeting aims to bring together medicinal chemists, disease biologists, chemical biologists, assay developers, and screeners from industry and academia, along with leaders of R&D organizations to create a dynamic exchange around the challenges facing drug discovery.
Scholarship Deadline: November 17 2011
Discounted Abstract Deadline: November 17 2011
Abstract Deadline: December 21 2011
Discounted Registration Deadline: January 19 2012
Keystone Symposia thanks our Sponsor(s) for generously supporting this meeting:
We gratefully acknowledge additional support for this conference from:
We gratefully acknowledge additional in-kind support for this conference from those foregoing speaker expense reimbursements:
Avila Therapeutics
Bristol-Myers Squibb Company
Carmot Therapeutics, Inc.
Epizyme, Inc.
Genentech, Inc.
GlaxoSmithKline
Hoffmann-La Roche, Inc.
Merck Research Laboratories
Optibrium Ltd.
We appreciate the organizations that provide Keystone Symposia with additional support, such as marketing and advertising:
Click here to view more of these organizations
Special thanks to the following for their support of Keystone Symposia initiatives to increase participation at this meeting by scientists from underrepresented backgrounds:
Click here to view more of these organizations
Program
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Monday, March 19
| 3:00PM - 7:30PM
Registration
Room: Pre Function
Monday, March 19
| 6:15PM - 7:15PM
Buffet Dinner
Room: Granhall
Monday, March 19
| 7:15PM - 8:30PM
Welcome and Keynote Address
Room: Mountain/Lake
Speaker 1 of 3
* Stephen V. Frye
, University of North Carolina, Chapel Hill, USA
Welcoming Remarks
Monday, March 19
| 7:15PM - 8:30PM
Welcome and Keynote Address
Room: Mountain/Lake
Speaker 2 of 3
*
James A. Wells
, University of California, San Francisco, USA
Introduction of Keynote Speaker
Monday, March 19
| 7:15PM - 8:30PM
Welcome and Keynote Address
Room: Mountain/Lake
Speaker 3 of 3
Peter S. Kim
, Stanford University, USA
Drug Discovery: A Perspective from Merck Research Laboratories
Tuesday, March 20
| 7:00AM - 8:00AM
Breakfast
Room: Granhall
Tuesday, March 20
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms I
Room: Mountain/Lake
Speaker 1 of 6
*
Peter J. Brown
, University of Toronto, Canada
Tuesday, March 20
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms I
Room: Mountain/Lake
Speaker 2 of 6
James E. Bradner
, Novartis Institutes for BioMedical Research, USA
Chemical Inhibition of Bromodomains
Tuesday, March 20
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms I
Room: Mountain/Lake
Speaker 3 of 6
Robert A. Copeland
, Accent Therapeutics, USA
Protein Methyltransferase Inhibitors as Personalized Cancer Therapeutics
Tuesday, March 20
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms I
Room: Mountain/Lake
Speaker 4 of 6
Lindsey Ingerman James
, University of North Carolina at Chapel Hill, USA
Short Talk: Inhibition of Methyl-Lysine Readers of the Histone Code by Small Molecule Chemical Probes
Tuesday, March 20
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms I
Room: Mountain/Lake
Speaker 5 of 6
Timothy M. Willson
, GlaxoSmithKline, USA
Circadian Rhythms and Drug Discovery
Tuesday, March 20
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms I
Room: Mountain/Lake
Speaker 6 of 6
R. Kip Guy
, St. Jude Children's Research Hospital, USA
The Dihydroisoquinolones (DHIQ’s) Orally Bioavailable Inhibitors of PfATP4 for the Treatment of Malaria
Tuesday, March 20
| 9:20AM - 9:40AM
Coffee Break
Room: Pre Function
Tuesday, March 20
| 11:00AM - 1:00PM
Poster Setup
Room: Bay
Tuesday, March 20
| 11:00AM - 11:00AM
On Own for Lunch and Recreation
Tuesday, March 20
| 1:00PM - 10:00PM
Poster Viewing
Room: Bay
Tuesday, March 20
| 4:30PM - 5:00PM
Coffee Available
Room: Pre Function
Tuesday, March 20
| 5:00PM - 7:00PM
Chemical Space I
Room: Mountain/Lake
Speaker 1 of 5
* Marcos E. Milla
, Synthorx, USA
Tuesday, March 20
| 5:00PM - 7:00PM
Chemical Space I
Room: Mountain/Lake
Speaker 2 of 5
Daniel A. Erlanson
, Carmot Therapeutics, Inc., USA
Fishing from Fragments into New Chemical Space
Tuesday, March 20
| 5:00PM - 7:00PM
Chemical Space I
Room: Mountain/Lake
Speaker 3 of 5
Brian K. Shoichet
, University of California, San Francisco, USA
The Chemical Basis of Pharmacology
Tuesday, March 20
| 5:00PM - 7:00PM
Chemical Space I
Room: Mountain/Lake
Speaker 4 of 5
James K. Chen
, Stanford University School of Medicine, USA
Small-Molecule Modulators of the Hedgehog Pathway
Tuesday, March 20
| 5:00PM - 7:00PM
Chemical Space I
Room: Mountain/Lake
Speaker 5 of 5
Samson Francis
, Indiana University, USA
Short Talk: Chemical Tools to Interrogate Two-Component System Signaling
Tuesday, March 20
| 7:00PM - 8:00PM
Dinner
Room: Granhall
Tuesday, March 20
| 8:00PM - 10:00PM
Poster Session 1
Room: Bay
Tuesday, March 20
| 8:00PM - 9:00PM
Social Hour
Room: Bay
Wednesday, March 21
| 7:00AM - 8:00AM
Breakfast
Room: Granhall
Wednesday, March 21
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms II
Room: Mountain/Lake
Speaker 1 of 6
* Rami Hannoush
, Genentech, USA
Wednesday, March 21
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms II
Room: Mountain/Lake
Speaker 2 of 6
Jeffery W. Kelly
, The Scripps Research Institute, USA
Current Insights into Transthyretin Aggregation-Associated Pathologies and Amelioration Thereof with the First in Class Drug Tafamidis
Wednesday, March 21
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms II
Room: Mountain/Lake
Speaker 3 of 6
Matthew R. Redinbo
, University of North Carolina at Chapel Hill, USA
Alleviating Cancer Drug Toxicity by Inhibiting a Bacterial Enzyme
Wednesday, March 21
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms II
Room: Mountain/Lake
Speaker 4 of 6
Jay A. Grobler
, Merck & Co., Inc., USA
Inhibiting the Strand Transfer activity of HIV-1 Integrase: A Novel Mechanism that Exploits Interactions with both the Enzyme and its DNA Substrate
Wednesday, March 21
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms II
Room: Mountain/Lake
Speaker 5 of 6
Vishva M. Dixit
, Genentech, Inc., USA
USP1 Inhibition: A Differentiation Strategy for Osteogenic Sarcoma
Wednesday, March 21
| 8:00AM - 11:00AM
Biological Space/Novel Targets and Mechanisms II
Room: Mountain/Lake
Speaker 6 of 6
T. Justin Rettenmaier
, Jnana Therapeutics, USA
Short Talk: Allosteric Modulation of Phosphoinositide-Dependent Kinase 1 (PDK1) in Cells
Wednesday, March 21
| 9:20AM - 9:40AM
Coffee Break
Room: Pre Function
Wednesday, March 21
| 11:00AM - 1:00PM
Poster Setup
Room: Bay
Wednesday, March 21
| 11:00AM - 11:00AM
On Own for Lunch and Recreation
Wednesday, March 21
| 1:00PM - 10:00PM
Poster Viewing
Room: Bay
Wednesday, March 21
| 4:30PM - 5:00PM
Coffee Available
Room: Pre Function
Wednesday, March 21
| 5:00PM - 7:15PM
Preclinical Approaches to Predicting Toxicity
Room: Mountain/Lake
Speaker 1 of 6
* Siegfried H. Reich
, Eli Lilly, USA
Wednesday, March 21
| 5:00PM - 7:15PM
Preclinical Approaches to Predicting Toxicity
Room: Mountain/Lake
Speaker 2 of 6
Kyle L. Kolaja
, Celgene, USA
Use of Stem Cell-Derived Tissues to Improve Cardiovascular Safety Assessment
Wednesday, March 21
| 5:00PM - 7:15PM
Preclinical Approaches to Predicting Toxicity
Room: Mountain/Lake
Speaker 3 of 6
Donald G. Robertson
, Bristol-Myers Squibb, USA
Metabolomics and Early Assessment of Drug Safety
Wednesday, March 21
| 5:00PM - 7:15PM
Preclinical Approaches to Predicting Toxicity
Room: Mountain/Lake
Speaker 4 of 6
James M. McKim, Jr.
, CeeTox, USA
Predictive in vitro Tox Models and Correlation to in vivo Toxicity
Wednesday, March 21
| 5:00PM - 7:15PM
Preclinical Approaches to Predicting Toxicity
Room: Mountain/Lake
Speaker 5 of 6
Amrita Basu
, Lockheed Martin, USA
Short Talk: Modeling Cellular Small-Molecule Sensitivity Profiles in Cancer Using Genetic and Gene-Expression Data
Wednesday, March 21
| 5:00PM - 7:15PM
Preclinical Approaches to Predicting Toxicity
Room: Mountain/Lake
Speaker 6 of 6
Mikko Taipale
, Whitehead Institute, USA
Short Talk: Profiling Kinase Inhibitor Specificities with A Quantitative Chaperone Interaction Assay
Wednesday, March 21
| 7:15PM - 8:00PM
Dinner
Room: Granhall
Wednesday, March 21
| 8:00PM - 10:00PM
Poster Session 2
Room: Bay
Wednesday, March 21
| 8:00PM - 9:00PM
Social Hour
Room: Bay
Thursday, March 22
| 7:00AM - 8:00AM
Breakfast
Room: Granhall
Thursday, March 22
| 8:00AM - 11:15AM
Chemical Space II
Room: Mountain/Lake
Speaker 1 of 7
* Lawrence G. Hamann
, Novartis Institutes for BioMedical Research, USA
Thursday, March 22
| 8:00AM - 11:15AM
Chemical Space II
Room: Mountain/Lake
Speaker 2 of 7
Ruben Abagyan
, University of California, San Diego, USA
Docking to a Comprehensive Multi-Conformational Pocketome to Predict Bioactivity
Thursday, March 22
| 8:00AM - 11:15AM
Chemical Space II
Room: Mountain/Lake
Speaker 3 of 7
Chris Abell
, University of Cambridge, UK
Exploring and Extending Fragment-Based Approaches
Thursday, March 22
| 8:00AM - 11:15AM
Chemical Space II
Room: Mountain/Lake
Speaker 4 of 7
Jennifer C. Petter
, Arrakis Therapeutics, USA
The Resurgence of Covalent Inhibitors
Thursday, March 22
| 8:00AM - 11:15AM
Chemical Space II
Room: Mountain/Lake
Speaker 5 of 7
Jack Taunton
, University of California, San Francisco, USA
Tuning the Secreted Proteome with Sec61 Modulators
Thursday, March 22
| 8:00AM - 11:15AM
Chemical Space II
Room: Mountain/Lake
Speaker 6 of 7
Katarzyna Kaczanowska
, The Scripps Research Institute, USA
Short Talk: Development of GABAB Receptor Positive Modulators for Nicotine Dependence
Thursday, March 22
| 8:00AM - 11:15AM
Chemical Space II
Room: Mountain/Lake
Speaker 7 of 7
Hazem Abdelkarim
, University of Illinois, Chicago, USA
Short Talk: The Development and Implementation of Nanorulers as a Novel Drug Discovery Tool to Characterize HDAC3/NCoR2 Interface
Thursday, March 22
| 9:20AM - 9:40AM
Coffee Break
Room: Pre Function
Thursday, March 22
| 11:15AM - 11:15AM
On Own for Lunch and Recreation
Thursday, March 22
| 4:30PM - 5:00PM
Coffee Available
Room: Pre Function
Thursday, March 22
| 5:00PM - 7:00PM
New and Novel Approaches to Drug Discovery
Room: Mountain/Lake
Speaker 1 of 5
* Michael Varney
, Genentech, Inc., USA
Thursday, March 22
| 5:00PM - 7:00PM
New and Novel Approaches to Drug Discovery
Room: Mountain/Lake
Speaker 2 of 5
Matthew Segall
, Optibrium Ltd., UK
Overcoming Psychological Barriers to Good Decision Making in Drug Discovery
Thursday, March 22
| 5:00PM - 7:00PM
New and Novel Approaches to Drug Discovery
Room: Mountain/Lake
Speaker 3 of 5
Christopher P. Austin
, National Institutes of Health, USA
Translational Therapeutics Development at NIH
Thursday, March 22
| 5:00PM - 7:00PM
New and Novel Approaches to Drug Discovery
Room: Mountain/Lake
Speaker 4 of 5
Melissa Fitzgerald
, Pfizer, USA
Thursday, March 22
| 5:00PM - 7:00PM
New and Novel Approaches to Drug Discovery
Room: Mountain/Lake
Speaker 5 of 5
Melissa Fitzgerald
, Pfizer, USA
Thursday, March 22
| 7:00PM - 7:15PM
Concluding Remarks
Room: Mountain/Lake
Speaker 1 of 1
* Michael Varney
, Genentech, Inc., USA
Thursday, March 22
| 7:15PM - 8:15PM
Dinner
Room: Granhall
Thursday, March 22
| 7:15PM - 8:15PM
Social Hour
Room: Granhall
Thursday, March 22
| 8:00PM - 11:00PM
Entertainment
Room: Granhall
Thursday, March 22
| 8:15PM - 11:00PM
Cash Bar
Room: Granhall
Friday, March 23
| 10:25AM - 10:25AM
Departure
*Session Chair.
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