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This meeting took place in 2016



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Modern Phenotypic Drug Discovery: Defining the Path Forward (D1)


Organizer(s) Jonathan A. Lee, Ellen L. Berg and Eugene C. Butcher
April 2—6, 2016
Big Sky Resort • Big Sky, Montana USA
Discounted Abstract Deadline: Dec 2, 2015
Abstract Deadline: Jan 5, 2016
Scholarship Deadline: Dec 2, 2015
Discounted Registration Deadline: Feb 2, 2016

Sponsored by Abide Therapeutics Inc., Janssen R&D: Pharmaceutical Companies of Johnson & Johnson, Merck & Co., Inc., Pfizer Inc., Takeda Pharmaceutical Company Limited and Vertex Pharmaceuticals Incorporated

Summary of Meeting:
Innovation and productivity in pharmaceutical drug discovery have been below expectations. Surprisingly, more first-in-class small molecule drugs approved by the FDA (1999-2008) were identified by functional approaches reminiscent of pre-genomics pharmacology (phenotypic drug discovery) than by contemporary molecular targeted strategies. This observation, and the unexpected difficulties of target validation, have diminished the impact of the “genomics revolution” and are arguably associated with the decline in innovation and productivity of pharmaceutical research. As a result, pharmaceutical researchers have begun to reevaluate the “Molecular Mindset” which has dominated our collective drug-hunting culture, and explore modern approaches to phenotypic screening. However, there is currently no single scientific forum where scientists from pharma, biotech, academia and instrument/service providers can meet and discuss strategies/issues related to phenotypic drug discovery (PDD). In part, this is because PDD encompasses multiple therapeutic areas and involves diverse disciplines including drug discovery, chemistry, cell biology, stem cell biology, systems biology, genomics, bioengineering and informatics. This Keystone Symposia meeting uniquely provides this interdisciplinary environment and is a particularly attractive venue given the increasing role of academia in drug discovery research. The conference will be a forum for the global PDD research community in which scientists from diverse institutions and scientific disciplines can meet to share/discuss/debate topics related to advantages/disadvantages of PDD and how PDD can complement targeted approaches. Significantly, the conference will provide a much needed forum for the growing interest in PDD, and can conceivably become the cornerstone of the global scientific movement for the reintroduction of functional biology/physiology-driven pharmaceutical research.

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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


The meeting will begin on Saturday, April 2 with registration from 16:00 to 20:00 and a welcome mixer from 18:00 to 20:00. Conference events conclude on Wednesday, April 6 with a closing plenary session from 17:00 to 19:00, followed by a social hour and entertainment. We recommend return travel on Thursday, April 7 in order to fully experience the meeting.

SATURDAY, APRIL 2

16:00—20:00
Arrival and Registration

Lower Atrium
18:00—20:00
Welcome Mixer
No registration fees are used to fund alcohol served at this function.

Jefferson

SUNDAY, APRIL 3

07:00—08:00
Breakfast

Gallatin
08:00—08:30
Welcoming Remarks

Jefferson/Madison
* Jonathan A. Lee, Eli Lilly and Company, USA

* Ellen L. Berg, Bioseek Inc., USA

* Eugene C. Butcher, Stanford University, USA

08:30—09:30
Keynote Address
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
* Eugene C. Butcher, Stanford University, USA

David C. Swinney, iRND3, Institute for Rare and Neglected Diseases, USA
The Value of Phenotypic Assays to Drug Discovery: Historical Perspective

09:30—11:00
Why Revisit PDD?
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
* Eugene C. Butcher, Stanford University, USA

John Moffat, Genentech, Inc., USA
Phenotypic and Targeted Drug Discovery Are Complimentary Strategies

Bernard H. Munos, FasterCures, USA
Pharma Research Productivity: A New Perspective on Phenotypic vs. Target-Based Screening

09:30—09:50
Coffee Break

Lower Atrium
11:00—17:00
On Own for Lunch

11:00—13:00
Poster Setup

Gallatin
13:00—22:00
Poster Viewing

Gallatin
16:30—17:00
Coffee Available

Lower Atrium
17:00—19:00
PDD: Recent Clinical Successes
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
* Ellen L. Berg, Bioseek Inc., USA

Nicholas A. Meanwell, Bristol-Myers Squibb, USA
Phenotypic Screening for Antiviral Agents

Rebecca M. Pruss, Windhover Biomed, France
Maintenance of Motor Function in Spinal Muscular Atrophy by Olesoxime: A Recent Clinical Success for Phenotypic Drug Discovery

Jon Tinsley, Summit Therapeutics, UK
Modulators of Utrophin Production for the Treatment of Duchenne Muscular Dystrophy

Veronica Soloveva, USAMRIID, USA
Short Talk: Identification and Characterization of the Antiviral Activity of GS-5734 using Phenotypic Approaches

19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Gallatin
19:30—22:00
Poster Session 1

Gallatin

MONDAY, APRIL 4

07:00—08:00
Breakfast

Gallatin
08:00—11:00
Challenges to Modern PDD/Lessons Learned
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
* Jonathan A. Lee, Eli Lilly and Company, USA

Neil O. Carragher, University of Edinburgh, Scotland
Accelerating PDD through Integrating MOA Profiling with Agile Chemical Design: Shifting the Bottlenecks from Target Deconvolution to Disease Relevance

Ellen L. Berg, Bioseek Inc., USA
Phenotypic Chemical Biology for Predicting Efficacy and Safety

Fabien Vincent, Pfizer, USA
Lessons Learned in Phenotypic Screening

Michael Jackson, SBP Medical Discovery Institute, USA
Phenotypic Screening of Patient Derived Cells: Balancing Throughput with Relevance

Bridget Wagner, Broad Institute, USA
Short Talk: Small-Molecule Stimulation of Human Beta-Cell Proliferation

09:20—09:40
Coffee Break

Lower Atrium
11:00—12:00
Panel 1: PDD Trends and Roadblocks

Jefferson/Madison
* David C. Swinney, iRND3, Institute for Rare and Neglected Diseases, USA

Ellen L. Berg, Bioseek Inc., USA

Jonathan A. Lee, Eli Lilly and Company, USA

Bernard H. Munos, FasterCures, USA

Fabien Vincent, Pfizer, USA

Neil O. Carragher, University of Edinburgh, Scotland

Michael Jackson, SBP Medical Discovery Institute, USA

12:00—13:00
Poster Setup

Gallatin
13:00—22:00
Poster Viewing

Gallatin
12:00—14:30
On Own for Lunch

16:30—17:00
Coffee Available

Lower Atrium
17:00—19:00
New Biological Models
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
Eugen Dhimolea, Dana Farber Cancer Institute, Harvard Medical School, USA
Engineering 3-D in vitro Tumor Models of Antineoplastic Drug Resistance

Salman Khetani, University of Illinois at Chicago, USA
Microengineered Human Liver Models for Drug Screening and Disease Modeling

Sandy Hinckley, Sanford Burnham Prebys Medical Discovery Institute, USA
Short Talk: Phenotypic Screening of Neuronal Networks using High-throughput Multielectrode Arrays

Deborah Greene Nguyen, Organovo, USA
Short Talk: Bioprinted Three-dimensional (3D) Human Tissues for Toxicology and Disease Modeling

David Gerber, Galenea Corp., USA
Short Talk: Targeting Synaptic Function for CNS Drug Discovery

19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Gallatin
19:30—22:00
Poster Session 2

Gallatin

TUESDAY, APRIL 5

07:00—08:00
Breakfast

Gallatin
08:00—11:00
Translational PDD: Physiologically Relevant Models
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
* Fabien Vincent, Pfizer, USA

Andrew Reaume, Melior Discovery, Inc., USA
Case Studies and Overall Learnings from 10 Years of Phenotypic Screening with a Broad-Based Panel of In Vivo Models

Mark Mercola, Stanford University, USA
Functional and Chemical Genomics to Decipher Heart Failure Mechanisms

Tom Large, Sunovion Pharmaceuticals, USA
Discovery of Novel Psychiatric Drugs using a Target-agnostic, Systems Neurobiology Strategy

Jason Ptacek, BioSeek, a Division of DiscoveRx Corp, USA
Short Talk: Phenotypic Human Primary Cell Based Tumor Microenvironment Models for Evaluation of Drug Combinations for Immune Oncology

David A. Mann, Cellular Dynamics International Inc., USA
Short Talk: Relevant Phenotypic Drug Discovery: Innate, Induced and Engineered Human iPSC Models

Denise V. Barrault, University of Edinburgh, UK
Short Talk

09:20—09:40
Coffee Break

Lower Atrium
11:00—11:30
NIH Common Fund Program
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
Aaron Pawlyk, NIDDK, National Institutes of Health, USA
In Search of Phenotypes to Illuminate the Druggable Genome

11:30—13:00
Poster Setup

Gallatin
13:00—22:00
Poster Viewing

Gallatin
11:30—17:00
On Own for Lunch

16:30—17:00
Coffee Available

Lower Atrium
17:00—19:00
Biologically Relevant Chemical Diversity
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
* Paul Clemons, Broad Institute of Harvard and MIT, USA
Chemical Diversity Expressed through Small-Molecule Performance: Diverse Readouts, Phenotypes and Genetic Determinants

Herbert Waldmann, Max Planck Institute for Molecular Physiology, Germany
Natural Product Inspired Compound Collections: Evolutionary Principle, Chemical Synthesis, Phenotypic Screening and Target Identification

Nicole E. Bodycombe, Pfizer, USA
Compound Subsets in Phenotypic Screening

Andrea Galmozzi, The Scripps Research Institute, USA
Short Talk: Phenotypic Screening of Fully Functionalized Fragment-Based Chemical Probes Reveals PGRMC2 As A New Regulator of Adipocyte Physiology of Therapeutic Potential for Obesity-Linked Diabetes

19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Gallatin
19:30—22:00
Poster Session 3

Gallatin

WEDNESDAY, APRIL 6

07:00—08:00
Breakfast

Gallatin
08:00—09:00
Keynote Address
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
* John Moffat, Genentech, Inc., USA

Enrique Saez, The Scripps Research Institute, USA
Chemical Proteomic Strategies to Advance Phenotypic Screening

09:00—11:30
Target/MOA Identification/Deconvolution
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
* John Moffat, Genentech, Inc., USA

Monica Schenone, Broad Institute of MIT and Harvard, USA
Target Identification and Mechanism of Action in Drug Discovery

Jeremy Jenkins, Novartis Institutes for BioMedical Research, USA
Systems Approaches to Elucidating Compound-Effect Pathways

Andreas Bender, University of Cambridge, UK
Towards Understanding Phenotypic Readouts - Utilizing Multiple Types of Chemical and Biological Data to Rationalize Compound Action

Vladimir Chupakhin, Janssen Pharmaceuticals, Belgium
Short Talk: The New Approaches for a Computational Target Deconvolution of the Phenotypic Hits

Susanne Swalley, Novartis Institutes for Biomedical Research, USA
Short Talk: Phenotypic Drug Discovery in SMA: Parallel Efforts in Preclinical Development and Target Identification

09:40—10:00
Coffee Break

Lower Atrium
11:30—12:30
Panel 2: Identification of Molecular Targets and Biological "Mechanisms of Action": How Much is Enough?

Jefferson/Madison
* Eugene C. Butcher, Stanford University, USA

Susanne Swalley, Novartis Institutes for Biomedical Research, USA

Tom Large, Sunovion Pharmaceuticals, USA

Marco Prunotto, F. Hoffmann-La Roche Ltd., Switzerland

Nicholas A. Meanwell, Bristol-Myers Squibb, USA

Rebecca M. Pruss, Windhover Biomed, France

12:30—17:00
On Own for Lunch

16:30—17:00
Coffee Available

Lower Atrium
17:00—19:00
Network Biology: New Technologies and Informatics
Meeting has ended...abstracts no longer viewable online.

Jefferson/Madison
Andrea Califano, Columbia University, USA
Systematic Elucidation of Druggable Dependencies in Human Malignancies: A New Take on Precision Medicine

Sean Bendall, Stanford University, USA
Revealing Hidden Behavior One Cell at a Time

Anne E. Carpenter, Broad Institute of Harvard and MIT, USA
Increasing the Content of High-Content Phenotypic Assays: Targeting Diseases and Characterizing Compounds via Cell Painting and Image-Based Profiling

* Marco Prunotto, F. Hoffmann-La Roche Ltd., Switzerland
Short Talk: Application of Molecular Phenotype to Phenotypic Drug Discovery: Results of a PoC Study

19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Gallatin
20:00—23:00
Entertainment
Entertainment is not subsidized by conference registration fees nor any U.S. federal government grants. Funding for this expense is provided by other revenue sources.

Gallatin

THURSDAY, APRIL 7

 
Departure


*Session Chair †Invited, not yet responded.



Keystone Symposia thanks our Sponsors for generously supporting this meeting:

Abide Therapeutics Inc. Janssen R&D: Pharmaceutical Companies of Johnson & Johnson
Merck & Co., Inc. Pfizer Inc.
Takeda Pharmaceutical Company Limited Vertex Pharmaceuticals Incorporated

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.



We gratefully acknowledge additional support for this conference from:

Evercyte GmbH

We gratefully acknowledge the generous grant for this conference provided by:


National Institutes of Health
National Center for Advancing Translational Sciences (NCATS)

Grant No. 1R13TR001586-01

Funding for this conference was made possible (in part) by (1R13 TR001586-01) from the National Center for Advancing Translational Sciences. The views expressed in written conference materials or publications and by speakers and moderators do not necessarily reflect the official policies of the Department of Health and Human Services; nor does mention by trade names, commercial practices, or organizations imply endorsement by the U.S. Government.


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



Emulate, Inc.


Novartis Institutes for BioMedical Research


Pfizer Inc.


Summit Therapeutics Inc


Sunovion Pharmaceuticals Inc.


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


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

Click here for more information on Industry Support and Recognition Opportunities.

If you are interested in becoming an advertising/marketing in-kind partner, please contact:
Yvonne Psaila, Director, Marketing and Communications, Email: yvonnep@keystonesymposia.org,
Phone:+1 970-262-2676