Granlibakken Tahoe Floorplan

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This meeting took place in 2012



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Addressing the Challenges of Drug Discovery – Novel Targets, New Chemical Space and Emerging Approaches (F1)


Organizer(s) Stephen V. Frye, Michael Varney and James A. Wells
March 19—23, 2012
Granlibakken Tahoe • Tahoe City, California USA
Abstract Deadline: Nov 17, 2011
Late Abstract Deadline: Dec 21, 2011
Scholarship Deadline: Nov 17, 2011
Early Registration Deadline: Jan 19, 2012

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.

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No registration fees are used to fund entertainment or alcohol at this conference

Conference Program    Print  |   View meeting in 12 hr (am/pm) time


MONDAY, MARCH 19

15:00—19:30
Registration

Pre Function
18:15—19:15
Buffet Dinner

Granhall
19:15—20:30
Welcome and Keynote Address
Meeting has ended...abstracts no longer viewable online.

Mountain/Lake
* Stephen V. Frye, University of North Carolina, Chapel Hill, USA
Welcoming Remarks

* James A. Wells, University of California, San Francisco, USA
Introduction of Keynote Speaker

Peter S. Kim, Stanford University, USA
Drug Discovery: A Perspective from Merck Research Laboratories


TUESDAY, MARCH 20

07:00—08:00
Breakfast

Granhall
08:00—11:00
Biological Space/Novel Targets and Mechanisms I
Meeting has ended...abstracts no longer viewable online.

Mountain/Lake
* Peter J. Brown, University of Toronto, Canada

James E. Bradner, Novartis Institutes for BioMedical Research, USA
Chemical Inhibition of Bromodomains

Robert A. Copeland, Accent Therapeutics, USA
Protein Methyltransferase Inhibitors as Personalized Cancer Therapeutics

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

Timothy M. Willson, GlaxoSmithKline, USA
Circadian Rhythms and Drug Discovery

R. Kip Guy, St. Jude Children's Research Hospital, USA
The Dihydroisoquinolones (DHIQ’s) Orally Bioavailable Inhibitors of PfATP4 for the Treatment of Malaria

09:20—09:40
Coffee Break

Pre Function
11:00—13:00
Poster Setup

Bay
11:00
On Own for Lunch and Recreation

13:00—22:00
Poster Viewing

Bay
16:30—17:00
Coffee Available

Pre Function
17:00—19:00
Chemical Space I
Meeting has ended...abstracts no longer viewable online.

Mountain/Lake
* Marcos E. Milla, Synthorx, USA

Daniel A. Erlanson, Carmot Therapeutics, Inc., USA
Fishing from Fragments into New Chemical Space

Brian K. Shoichet, University of California, San Francisco, USA
The Chemical Basis of Pharmacology

James K. Chen, Stanford University School of Medicine, USA
Small-Molecule Modulators of the Hedgehog Pathway

Samson Francis, Indiana University, USA
Short Talk: Chemical Tools to Interrogate Two-Component System Signaling

19:00—20:00
Dinner

Granhall
20:00—22:00
Poster Session 1

Bay
20:00—21:00
Social Hour

Bay

WEDNESDAY, MARCH 21

07:00—08:00
Breakfast

Granhall
08:00—11:00
Biological Space/Novel Targets and Mechanisms II
Meeting has ended...abstracts no longer viewable online.

Mountain/Lake
* Rami Hannoush, Genentech, USA

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

Matthew R. Redinbo, University of North Carolina at Chapel Hill, USA
Alleviating Cancer Drug Toxicity by Inhibiting a Bacterial Enzyme

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

Vishva M. Dixit, Genentech, Inc., USA
USP1 Inhibition: A Differentiation Strategy for Osteogenic Sarcoma

T. Justin Rettenmaier, University of California San Francisco, USA
Short Talk: Allosteric Modulation of Phosphoinositide-Dependent Kinase 1 (PDK1) in Cells

09:20—09:40
Coffee Break

Pre Function
11:00—13:00
Poster Setup

Bay
11:00
On Own for Lunch and Recreation

13:00—22:00
Poster Viewing

Bay
16:30—17:00
Coffee Available

Pre Function
17:00—19:15
Preclinical Approaches to Predicting Toxicity
Meeting has ended...abstracts no longer viewable online.

Mountain/Lake
* Siegfried H. Reich, Eli Lilly, USA

Kyle L. Kolaja, Celgene, USA
Use of Stem Cell-Derived Tissues to Improve Cardiovascular Safety Assessment

Donald G. Robertson, Bristol-Myers Squibb, USA
Metabolomics and Early Assessment of Drug Safety

James M. McKim, Jr., CeeTox, USA
Predictive in vitro Tox Models and Correlation to in vivo Toxicity

Amrita Basu, Lockheed Martin, USA
Short Talk: Modeling Cellular Small-Molecule Sensitivity Profiles in Cancer Using Genetic and Gene-Expression Data

Mikko Taipale, Whitehead Institute, USA
Short Talk: Profiling Kinase Inhibitor Specificities with A Quantitative Chaperone Interaction Assay

19:15—20:00
Dinner

Granhall
20:00—22:00
Poster Session 2

Bay
20:00—21:00
Social Hour

Bay

THURSDAY, MARCH 22

07:00—08:00
Breakfast

Granhall
08:00—11:15
Chemical Space II
Meeting has ended...abstracts no longer viewable online.

Mountain/Lake
* Lawrence G. Hamann, Novartis Institutes for BioMedical Research, USA

Ruben Abagyan, University of California, San Diego, USA
Docking to a Comprehensive Multi-Conformational Pocketome to Predict Bioactivity

Chris Abell, University of Cambridge, UK
Exploring and Extending Fragment-Based Approaches

Russell C. Petter, Arrakis Therapeutics, USA
The Resurgence of Covalent Inhibitors

Jack Taunton, University of California, San Francisco, USA
Tuning the Secreted Proteome with Sec61 Modulators

Katarzyna Kaczanowska, The Scripps Research Institute, USA
Short Talk: Development of GABAB Receptor Positive Modulators for Nicotine Dependence

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

09:20—09:40
Coffee Break

Pre Function
11:15
On Own for Lunch and Recreation

16:30—17:00
Coffee Available

Pre Function
17:00—19:00
New and Novel Approaches to Drug Discovery
Meeting has ended...abstracts no longer viewable online.

Mountain/Lake
* Michael Varney, Genentech, Inc., USA

Matthew Segall, Optibrium Ltd., UK
Overcoming Psychological Barriers to Good Decision Making in Drug Discovery

Christopher P. Austin, National Institutes of Health, USA
Translational Therapeutics Development at NIH

Melissa Fitzgerald, Pfizer,

Melissa Fitzgerald, Pfizer,

19:00—19:15
Concluding Remarks
Meeting has ended...abstracts no longer viewable online.

Mountain/Lake
* Michael Varney, Genentech, Inc., USA

19:15—20:15
Dinner

Granhall
19:15—20:15
Social Hour

Granhall
20:00—23:00
Entertainment

Granhall

FRIDAY, MARCH 23

 
Departure


*Session Chair †Invited, not yet responded.



We gratefully acknowledge support for this conference from:


Directors' Fund


These generous unrestricted gifts allow our Directors to schedule meetings in a wide variety of important areas, many of which are in the early stages of research.

Click here to view all of the donors who support the Directors' Fund.



Keystone Symposia thanks our Sponsors for generously supporting this meeting:

Bayer USA Foundation Bristol-Myers Squibb Company
Genentech, Inc. Infinity Pharmaceuticals

We gratefully acknowledge additional support for this conference from:

Epizyme, Inc.
Avila Therapeutics


We gratefully acknowledge additional in-kind support for this conference from those foregoing speaker expense reimbursements:



Bristol-Myers Squibb Company


Carmot Therapeutics, Inc.


Epizyme, Inc.


Genentech, Inc.


GlaxoSmithKline


Hoffmann-La Roche, Inc.


Merck Research Laboratories


Optibrium Ltd.


Avila Therapeutics


We appreciate the organizations that provide Keystone Symposia with additional support, such as marketing and advertising:


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Special thanks to the following for their support of Keystone Symposia initiatives to increase participation at this meeting by scientists from underrepresented backgrounds:


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If your organization is interested in joining these entities in support of Keystone Symposia, please contact: Sarah Lavicka, Director of Development, Email: sarahl@keystonesymposia.org,
Phone:+1 970-262-2690

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Phone:+1 970-262-2676