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:
Bayer USA FoundationBristol-Myers Squibb CompanyGenentech, Inc.Infinity Pharmaceuticals
We gratefully acknowledge additional support for this conference from:
Avila TherapeuticsEpizyme, Inc.
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

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.