GPCR-Based Drug Discovery  

 

ABOUT THIS CONFERENCE 

G protein-coupled receptors (GPCRs) are among the most common types of molecules that medicines work upon. These receptors continue to be a focus of new drug discovery not only due to their cell surface location which makes them accessible to ingested therapies, but also because of the role they play in so many cell types as the 'sensor or transmitter' of extra-cellular chemical signals into messages that result in cellular change.

Two back-to-back GPCR conferences will cover the challenges faced with the industry's current paradigm of target-driven discovery.

GPCR-Based Drug Discovery, the first day and a half conference of our back-to-back GPCR conferences, will cover screening and discovery strategies for compounds, including allosteric modulators, acting on GPCRs. A few talks will also be devoted to the findings and impact of the slew of recent crystal structures of medically relevant GPCRs that have been elucidated. New assays to uncover or methods to direct ligand-biased signaling will be another focus of the conference.

SUGGESTED EVENT PACKAGE:

September 23: Practical Aspects of Structure-Based Drug Discovery with GPCRs Short Course 2
September 23: Allosteric Modulators of GPCRs Short Course 4
September 24 - 25: GPCR-Based Drug Discovery Conference
September 25 - 26: GPCR-Targeted Therapies Conference 


Day 1 | Day 2 | Download Brochure 


Tuesday, September 24

7:00 am Registration and Morning Coffee


G PROTEIN-COUPLED RECEPTOR STRUCTURE

8:10 Chairperson’s Opening Remarks

8:15 Structural insights into Function and Pharmacology of GPCR Superfamily

Vsevolod (Seva) Katritch, Ph.D., Assistant Professor, The Scripps Research Institute

8:45 FEATURED PRESENTATION: Molecular Signatures of GPCRs

Christopher Tate, Ph.D., Professor, Laboratory of Molecular Biology, MRC, United Kingdom

9:15 GPCR Ligand Design via SAR-Guided Homology Models

Mark Bures, Ph.D., Research Advisor, Computational Chemistry, Eli Lilly

9:45 Grand Opening Coffee Break in the Exhibit Hall with Poster Viewing

ANTIBODIES AND GPCRs

10:45 Nanobodies for the Structural and Functional Characterization of GPCR Transmembrane Signaling: From Structure to Function to Drugs

Jan Steyaert, Ph.D., Head of Department, Structural Biology, Vrije University Brussels, Belgium

 Discover Rx logo11:15 Antibodies Against Difficult Targets: How to Tackle G-Protein Coupled ReceptorS 

Stefanie Urlinger, Ph.D., Director, Research & Development, MorphoSys AG

11:45 Monoclonal Antibodies against Endothelin A and B Human GPCR Subtypes

Frederic Ducancel, Ph.D., Head, Laboratory, Institute of Biology and Technology, Saclay, Atomic Energy Commission, France

12:15 pm Preclinical and Clinical Experience with PRO 140, a Humanized Anti-CCR5 Antibody for the Treatment and Prevention of HIV

Richard Trauger, Ph.D., CSO, CytoDyn

12:45 A Novel Regulatory Role of a Humanized Anti-CCR4 Antibody in Cancer Immunotherapy

DeKuan Chang, Ph.D., Research Fellow, Cancer Immunology & AIDS, Dana-Farber Cancer Institute

Morphosys logo1:15 LUNCHEON PRESENTATION: New Era of GPCR Drug Discovery: Multi-Pathway Screening Technologies

Elizabeth R. Quinn, Ph.D., Director, LeadHunter Discovery Services, DiscoveRx Corporation


LIGAND-BIASED SIGNALING

2:15 Chairperson’s Opening Remarks

2:20 FEATURED PRESENTATION: Allosteric Regulation of G Protein-Coupled Receptors: Implications to Functionally Selective Ligand Pharmacology

Roger K Sunahara, Ph.D., Associate Professor, Pharmacology, University of Michigan Medical School

2:50 Discovery of style='font-family:"Arial","sans-serif"'>β- Arrestin-Biased Agonists of Dopamine D2 Receptors

Kyle Butler, Ph.D., Post-Doctoral Fellow, Laboratory of Jian Jin, Division of Chemical Biology and Medicinal Chemistry,The University of North Carolina at Chapel Hill

3:20 Sponsored Presentation (Opportunity Available)

3:50 Refreshment Break in the Exhibit Hall with Poster Viewing

4:30 Directed Evolution of Conformationally-selective GPCR Antibodies and Applications to Discovering Biased Ligands

Aaron Ring, MD/PhD candidate, Laboratory of K. Christopher Garcia, Department of Structural Biology, Stanford University School of Medicine

5:00 GPCR-Biased Ligands as Improved Therapeutics: Promise and Progress

Jonathan Violin, Ph.D., Director, Biology, Trevena, Inc.

5:30 Interactive Breakout Discussion Groups

6:30 Welcome Reception in the Exhibit Hall with Poster Viewing

7:30 Close of Day

 

 

Day 1 | Day 2 | Download Brochure