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This meeting took place in 2019
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Phenotypic Drug Discovery: Recent Advances and Insights from Chemical and Systems Biology (C1)
Organizer(s) Mark Mercola, Fabien Vincent, Monica Schenone and Arsenio Nueda
March 3—7, 2019
Beaver Run Resort • Breckenridge, CO USA
Discounted Abstract Deadline: Oct 30, 2018
Abstract Deadline: Dec 4, 2018
Scholarship Deadline: Oct 30, 2018
Discounted Registration Deadline: Jan 11, 2019
Sponsored by Merck & Co., Inc. and Pfizer Inc.
Summary of Meeting:
Unlike conventional target-centric drug discovery, Phenotypic Drug Discovery (PDD) places its focus on disease-relevant phenotypes and agnosticism with regard to molecular mechanism of action. Thus, it offers unique opportunities in terms of discovery of novel biology and first-in-class therapeutics but is matched with significant challenges, a number of which can be addressed by recent advances in chemical and systems biology. A key aspect of the conference will be to share information and processes on how best to employ phenotypic strategies to discover novel biology and effectively prosecute drug discovery programs. Specific topics will include: chemical biology advances and case studies in target identification; case studies of recently advanced clinical candidates and approved drugs; functional genomics and systems biology advances and case studies; project prosecution including lessons learned from lead optimization and pre-clinical development; complex cell-based models and new assay modalities. With few non-commercial meetings covering drug discovery as a discipline, this conference has the stature and breadth to bring together accomplished and influential scientists from industry and academia as demonstrated by the 2016 conference. Its scope will be broader than other PDD and Chemical Biology meetings since it will cover the entire range of activities and technologies from phenotypic assay systems, to target identification and FDA approval of novel therapeutics. Given that there is still an emphasis on target centric discovery in pharmaceutical companies, this conference can be instrumental in further promoting a shift in mindset and contributing to the consolidation of PDD as an integral part of the drug discovery paradigm. The vision for this conference would be to share success stories of newly approved drugs and late stage clinical candidates, along with key lessons and best practices, to inform future PDD projects.
View Scholarships/Awards
Unlike conventional target-centric drug discovery, Phenotypic Drug Discovery (PDD) places its focus on disease-relevant phenotypes and agnosticism with regard to molecular mechanism of action. Thus, it offers unique opportunities in terms of discovery of novel biology and first-in-class therapeutics but is matched with significant challenges, a number of which can be addressed by recent advances in chemical and systems biology. A key aspect of the conference will be to share information and processes on how best to employ phenotypic strategies to discover novel biology and effectively prosecute drug discovery programs. Specific topics will include: chemical biology advances and case studies in target identification; case studies of recently advanced clinical candidates and approved drugs; functional genomics and systems biology advances and case studies; project prosecution including lessons learned from lead optimization and pre-clinical development; complex cell-based models and new assay modalities. With few non-commercial meetings covering drug discovery as a discipline, this conference has the stature and breadth to bring together accomplished and influential scientists from industry and academia as demonstrated by the 2016 conference. Its scope will be broader than other PDD and Chemical Biology meetings since it will cover the entire range of activities and technologies from phenotypic assay systems, to target identification and FDA approval of novel therapeutics. Given that there is still an emphasis on target centric discovery in pharmaceutical companies, this conference can be instrumental in further promoting a shift in mindset and contributing to the consolidation of PDD as an integral part of the drug discovery paradigm. The vision for this conference would be to share success stories of newly approved drugs and late stage clinical candidates, along with key lessons and best practices, to inform future PDD projects.
View Scholarships/Awards
No registration fees are used to fund entertainment or alcohol at this conference
The meeting will begin on Sunday, March 3 with registration from 16:00 to 20:00 and a welcome mixer from 18:00 to 20:00. Conference events conclude on Thursday, March 7 with a closing plenary session from 17:00 to 19:00, followed by a social hour and entertainment. We recommend return travel on Friday, March 8 in order to fully experience the meeting.
SUNDAY, MARCH 3
MONDAY, MARCH 4
TUESDAY, MARCH 5
WEDNESDAY, MARCH 6
THURSDAY, MARCH 7
FRIDAY, MARCH 8
Conference Program Print | View meeting in 12 hr (am/pm) time
The meeting will begin on Sunday, March 3 with registration from 16:00 to 20:00 and a welcome mixer from 18:00 to 20:00. Conference events conclude on Thursday, March 7 with a closing plenary session from 17:00 to 19:00, followed by a social hour and entertainment. We recommend return travel on Friday, March 8 in order to fully experience the meeting.
SUNDAY, MARCH 3
18:00—20:00
Welcome Mixer
No registration fees are used to fund alcohol served at this function.
08:00—09:15
Welcoming Remarks and Keynote Address
Big picture view of pharmaceutical development, challenges and new opportunities.
*
Mark Mercola,
Stanford University, USA
James E. Bradner,
Novartis Institutes for BioMedical Research, USA
Phenotype to Chemotype to Phenotype
Phenotype to Chemotype to Phenotype
09:15—11:15
Clinical Success Stories
Share success stories – newly approved drugs and late stage clinical candidates. Identify key lessons and best practices to inform future PDD projects.
*
Tom Large,
Blue Oak Pharmaceuticals, USA
Yoshihiro Watanabe,
Kanazawa University, Japan
Discovery of Trametinib as a MEK-Inhibitor Able to Alter Phosphorylation State of MEK
Discovery of Trametinib as a MEK-Inhibitor Able to Alter Phosphorylation State of MEK
Coffee Break
Fred Van Goor,
Vertex Pharmaceuticals Incorporated, USA
Combination Pharmacology to Treat the Underlying Cause of the Majority of People with Cystic Fibrosis
Combination Pharmacology to Treat the Underlying Cause of the Majority of People with Cystic Fibrosis
John Tallarico,
Novartis Institutes for BioMedical Research, USA
Novel Therapies from Phenotypic Screening
Novel Therapies from Phenotypic Screening
14:30—15:30
Workshop: Safety De-Risking
Gerhard Ecker,
University of Vienna, Austria
Semantically Integrated Life Science Data – The Power of Workflows for Analysis of Phenotypic Screening Data, Toxicological Read-Across, and Repurposing
Semantically Integrated Life Science Data – The Power of Workflows for Analysis of Phenotypic Screening Data, Toxicological Read-Across, and Repurposing
Ellen L. Berg,
Eurofins DiscoverX, USA
Phenotypic Profiling for Toxicity-Associated Signatures Applied to ToxCast Chemicals
Phenotypic Profiling for Toxicity-Associated Signatures Applied to ToxCast Chemicals
*
Fabien Vincent,
Pfizer Inc., USA
Safety De-Risking in Phenotypic Drug Discovery: Considerations and Strategies
Safety De-Risking in Phenotypic Drug Discovery: Considerations and Strategies
15:30—16:30
Panel Discussion
Ellen L. Berg,
Eurofins DiscoverX, USA
Neil O. Carragher,
University of Edinburgh, Scotland
Chun-wa Chung,
GlaxoSmithKline, UK
Tom Large,
Blue Oak Pharmaceuticals, USA
17:00—19:00
New Opportunities and Under-Represented Indications
Illustrate new opportunities for PDD among hard to study and treat diseases. Illustrate new disease modeling technology that can be a breakthrough in finding drug targets and drugs.
*
Jonathan A. Lee,
PDD4Patients LLC, USA
Lucienne V. Ronco,
Fulcrum Therapeutics, USA
Identification of FTX-1821 a Molecule that Inhibits DUX4 Expression and Rescues FSHD Pathophysiology in FSHD Skeletal Muscle Myotubes
Identification of FTX-1821 a Molecule that Inhibits DUX4 Expression and Rescues FSHD Pathophysiology in FSHD Skeletal Muscle Myotubes
Clemens R. Scherzer,
Harvard Medical School, Brigham and Women's Hospital, USA
Turning Bits and Base Pairs into Precision Neurology
Turning Bits and Base Pairs into Precision Neurology
Scott S. Walker,
Merck & Co., Inc., USA
Large-Scale Antibacterial Phenotypic Screening and Systematic Hit Triage Reveal Novel Targets and Novel Inhibitors of Established Targets
Large-Scale Antibacterial Phenotypic Screening and Systematic Hit Triage Reveal Novel Targets and Novel Inhibitors of Established Targets
Eachan Oliver Johnson,
Broad Institute, USA
Short Talk: Large-Scale Chemical-Genetic Interaction Profiling Yields New Classes of Inhibitors of Mycobacterium tuberculosis
Short Talk: Large-Scale Chemical-Genetic Interaction Profiling Yields New Classes of Inhibitors of Mycobacterium tuberculosis
Patrick W. Faloon,
Biogen, USA
Short Talk: Identification of Small Molecules that Increase Productive Cellular Processing of Antisense Oligonucleotides (ASOs)
Short Talk: Identification of Small Molecules that Increase Productive Cellular Processing of Antisense Oligonucleotides (ASOs)
19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.
08:00—11:15
Chemical Biology and Novel Molecular Mechanisms of Action
Drugging targets considered traditionally undruggable. Small molecule probing of protein conformation/function.
*
Susanne Swalley,
Biogen, USA
Maurizio Pellecchia,
University of California, Riverside, USA
NMR-Based Fragment Screening for Oncology
NMR-Based Fragment Screening for Oncology
Coffee Break
Razvan L. Cornea,
University of Minnesota, USA
Targeting the Pathological Leak of a Calcium Channel for Heart Failure Therapeutics
Targeting the Pathological Leak of a Calcium Channel for Heart Failure Therapeutics
Monica Schenone,
Pfizer Inc., USA
Identification of p300/CBP as the Cellular Target of the Small Molecule “BRD16” Following a Phenotypic Screen
Identification of p300/CBP as the Cellular Target of the Small Molecule “BRD16” Following a Phenotypic Screen
Sannah Zoffmann,
F. Hoffmann-La Roche Ltd., Switzerland
Short Talk: Machine Learning-Powered Antibiotics Phenotypic Drug Discovery
Short Talk: Machine Learning-Powered Antibiotics Phenotypic Drug Discovery
Jean-Philippe Coppe,
University of California, San Francisco, USA
Short Talk: Mapping Phospho-Catalytic Dependencies of Therapy-Resistant Tumors Reveals New Actionable Vulnerabilities
Short Talk: Mapping Phospho-Catalytic Dependencies of Therapy-Resistant Tumors Reveals New Actionable Vulnerabilities
Julien Olivet,
Dana-Farber Cancer Institute, USA
Short Talk: Systematic Assessment of Druggable Cavities in a Histone Deacetylase Complex
Short Talk: Systematic Assessment of Druggable Cavities in a Histone Deacetylase Complex
11:15—12:15
Panel Discussion: Comparing/Contrasting the Practice of PDD
The discussion seeks to examine how PDD is viewed and practiced within various types of organizations (such as academia, industry, government, and start-ups). Rather than focusing on specific scientific projects, the discussion will seek to compare/contrast opinions, attitudes and experiences related to PDD from diverse environments. Discussion points will include, but are not limited to: perceived acceptance/importance of PDD, when/why PDD (vs TDD) is used, perceived strengths/weaknesses of PDD, experiences related to obtaining “buy-in” from managers/VC/funding agencies, therapeutic fit, what works in your organization, what needs to be improved.
*
Jonathan A. Lee,
PDD4Patients LLC, USA
Neil O. Carragher,
University of Edinburgh, Scotland
Bruce Posner,
University of Texas Southwestern Medical Center, USA
Veronica Soloveva,
Merck, USA
Bridget Wagner,
Broad Institute, USA
Guillermo Vela,
NeuScience, USA
Arsenio Nueda,
Almirall S.A., Spain
Christophe Antczak,
Novartis Institutes for BioMedical Research, USA
17:00—19:00
Project Prosecution and Pre-Clinical Advancement
Addressing roadblocks in advancing drugs from phenotypic assays through pre-clinical development. Strategies for selecting high probability leads.
*
Scott Wolkenberg,
Merck and Co., Inc., USA
Arsenio Nueda,
Almirall S.A., Spain
Harnessing the Power of Phenotypic Screening to Generate Novel Starting Points for Drug Discovery
Harnessing the Power of Phenotypic Screening to Generate Novel Starting Points for Drug Discovery
Chun-wa Chung,
GlaxoSmithKline, UK
Linking Differential Molecular Mode of Action to Distinct Pharmacology
Linking Differential Molecular Mode of Action to Distinct Pharmacology
Derek Lowe,
Novartis Institutes for BioMedical Research, USA
Advancement of Phenotypic Hits
Advancement of Phenotypic Hits
Hassan Javanbakht,
Gilead Sciences, USA
Short Talk: Phenotypic Screening in Antiviral Research
Short Talk: Phenotypic Screening in Antiviral Research
Hassan Al-Ali,
University of Miami, USA
Short Talk: Re-Thinking Drug Target Identification and Exploiting Polypharmacology
Short Talk: Re-Thinking Drug Target Identification and Exploiting Polypharmacology
19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.
08:00—11:00
Physiologically Complex and Realistic Disease Assays
Incorporating advances in stem cell disease modeling into drug discovery. Technological advances in complex and kinetic readouts. 3D organoids.
*
Tao P. Zhong,
East China Normal University, China
Randall T. Peterson,
University of Utah, USA
Zebrafish Behaviors as Phenotypes for Neuroactive Compound Discovery
Zebrafish Behaviors as Phenotypes for Neuroactive Compound Discovery
Mark Mercola,
Stanford University, USA
High-Throughput Kinetic Studies of iPSC-Derived Cardiomyocytes: Bringing the Patient to the Early Stages of Drug Discovery
High-Throughput Kinetic Studies of iPSC-Derived Cardiomyocytes: Bringing the Patient to the Early Stages of Drug Discovery
Coffee Break
Neil O. Carragher,
University of Edinburgh, Scotland
Advances in Phenotypic Screening: Accelerating the Discovery of New Chemical Entities and Drug Combinations towards in vivo Proof-of-Concept
Advances in Phenotypic Screening: Accelerating the Discovery of New Chemical Entities and Drug Combinations towards in vivo Proof-of-Concept
Christy Fryer,
Novartis Institutes for Biomedical Research, USA
Discovery of a ZIP7 Inhibitor from a Notch Pathway Screen
Discovery of a ZIP7 Inhibitor from a Notch Pathway Screen
Kristin Rockwell,
Pfizer, USA
Short Talk: Functional Genomics Screening in Primary Human T Cells to Identify Novel Targets for Autoimmune Diseases
Short Talk: Functional Genomics Screening in Primary Human T Cells to Identify Novel Targets for Autoimmune Diseases
14:30—15:30
Workshop: Clinical, Regulatory Case Studies with PDD Project Prosecution
*
Marco Prunotto,
F. Hoffmann-La Roche Ltd., Switzerland
Yevgeny Berdichevsky,
Lehigh University, USA
Screen in Organotypic Hippocampal Model of Drug-Resistant Epilepsy Reveals Novel Anticonvulsants
Screen in Organotypic Hippocampal Model of Drug-Resistant Epilepsy Reveals Novel Anticonvulsants
Herve Tiriac,
University of California, San Diego, USA
Organoid Profiling Identifies Common Responders to Chemotherapy in Pancreatic Cancer
Organoid Profiling Identifies Common Responders to Chemotherapy in Pancreatic Cancer
Kerry L. Spear,
Blue Oak Pharmaceuticals, USA
Next Generation of Drugs for Bipolar Depression: A Systems Biology Approach
Next Generation of Drugs for Bipolar Depression: A Systems Biology Approach
17:00—19:00
Functional Genomics and Systems Approaches
Functional genomics, machine learning and data mining.
*
Aravind Subramanian,
Broad Institute, USA
Anna Greka,
Harvard Medical School, USA
Toward Targeted, Mechanism-Based Therapies for Kidney Diseases
Toward Targeted, Mechanism-Based Therapies for Kidney Diseases
Alexandre R. Colas,
Sanford-Burnham Medical Research Institute, USA
Novel Single Cell and High-Throughput Phenotypical Platform to Study Atrial Rhythm in hPSCs
Novel Single Cell and High-Throughput Phenotypical Platform to Study Atrial Rhythm in hPSCs
19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.
08:00—09:00
Keynote Address
*
Monica Schenone,
Pfizer Inc., USA
Benjamin F. Cravatt III,
The Scripps Research Institute, USA
Activity-Based Proteomics – Protein and Ligand Discovery on a Global Scale
Activity-Based Proteomics – Protein and Ligand Discovery on a Global Scale
09:00—11:30
Compound Profiling and Repositioning
*
John Moffat,
Genentech, Inc., USA
Christopher A. Lipinski,
Chrstopher A. Lipinski PhD LLC, USA
High-Throughput in vivo Phenotypic Screening for Drug Repurposing: Discovery of MLR-1023, a Novel Insulin Sensitizer and Novel Lyn Kinase Activator with Clinical Proof-of-Concept
High-Throughput in vivo Phenotypic Screening for Drug Repurposing: Discovery of MLR-1023, a Novel Insulin Sensitizer and Novel Lyn Kinase Activator with Clinical Proof-of-Concept
Coffee Break
Marco Prunotto,
F. Hoffmann-La Roche Ltd., Switzerland
Molecular Information Phenotype-Based Drug Discovery: A 5 Year Journey
Molecular Information Phenotype-Based Drug Discovery: A 5 Year Journey
Bruce Posner,
University of Texas Southwestern Medical Center, USA
Identifying Subtype-Selective Vulnerabilities and Biomarkers in Non-Small Cell Lung Cancer
Identifying Subtype-Selective Vulnerabilities and Biomarkers in Non-Small Cell Lung Cancer
Mo Mandegar,
Tenaya Therapeutics, USA
Short Talk: Artificial Intelligence Accelerates Early-Stage Target and Drug Discovery
Short Talk: Artificial Intelligence Accelerates Early-Stage Target and Drug Discovery
Christian T. Meyer,
Vanderbilt University, USA
Short Talk: A Consensus Framework for Calculating Drug Synergy
Short Talk: A Consensus Framework for Calculating Drug Synergy
17:00—18:45
Target Identification / Deconvolution
*
Ellen L. Berg,
Eurofins DiscoverX, USA
Dyann F. Wirth,
Harvard School of Public Health, USA
Target ID for Malaria
Target ID for Malaria
Bridget Wagner,
Broad Institute, USA
The Importance of Phenotypic Screening in Identifying New Targets for Disease Therapeutics
The Importance of Phenotypic Screening in Identifying New Targets for Disease Therapeutics
Herbert Waldmann,
Max Planck Institute for Molecular Physiology, Germany
Chemotype – Phenotype - Target
Chemotype – Phenotype - Target
Heidi Greulich,
Broad Institute of MIT and Harvard, USA
Short Talk: PDE3A Modulation for the Treatment of Cancer
Short Talk: PDE3A Modulation for the Treatment of Cancer
19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.
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.
*Session Chair †Invited, not yet responded.
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