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Molecular Pharmacology

Gordon Research Conference

How Form, Function, Content and Context Shape GPCR Signaling

February 10 - 15, 2019

Chairs

and

Vice Chairs

and

Ventura Beach Marriott

2055 Harbor Boulevard

Ventura, California, United States

Venue and Travel Information

Conference Description

The 2019 Gordon Research Conference on Molecular Pharmacology will highlight the latest advances in understanding G protein-coupled receptors (GPCRs) and how they mediate regulation of physiological processes. GPCRs are well established effective therapeutic targets and presentations will focus on how we can further improve therapeutic development across diverse disease states, including cancer, metabolic disorders, cardiovascular disease, and pain.

The program will focus on:

How ligands and modulators interact with receptors
How receptors respond to these interactions
How context, both spatial and temporal, effects the signaling output; and importantly
How we can harness these events to treat disease

Related Meeting

This GRC will be held in conjunction with the "Molecular Pharmacology" Gordon Research Seminar (GRS). Those interested in attending both meetings must submit an application for the GRS in addition to an application for the GRC. Refer to the associated GRS program page for more information.

Conference Program

Sunday
4:00 pm - 8:00 pm	Arrival and Check-in
6:00 pm - 7:00 pm	Dinner
7:30 pm - 7:40 pm	Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm	Keynote Session: Pharmacology of GPCR Function in Neurological Disorders From genetic models to ligands beyond opioids. Discussion Leader:
7:40 pm - 8:15 pm	"Structural and Spatiotemporal Basis of GPCR Pluridimensional Functional Selectivity"
8:15 pm - 8:25 pm	Discussion
8:25 pm - 8:45 pm	"Reducing Abuse and Aiding Analgesia: Targeting the Dopamine D3 Receptor to Address the Opioid Crisis"
8:45 pm - 8:50 pm	Discussion
8:50 pm - 9:10 pm	"Viral GPCRs Rewire Signaling and Accelerate Glioblastoma Growth"
9:10 pm - 9:15 pm	Discussion
9:15 pm - 9:25 pm	Selected from Poster Abstracts: "Structure of a Membrane Adenylyl Cyclase Bound to a G Protein α-Subunit"
9:25 pm - 9:30 pm	Discussion
Monday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	The Importance of Subcellular Location to Drug Targeting and Signaling Whether in real estate or in drug targeting, subcellular location is still critical to targeting and signaling. Discussion Leader:
9:00 am - 9:25 am	"Novel Allosteric Modulators"
9:25 am - 9:30 am	Discussion
9:30 am - 9:55 am	"Ubiquitin Drives GPCR Inflammatory Signaling"
9:55 am - 10:00 am	Discussion
10:00 am - 10:25 am	"Disease-Associated Mutation in PTH Unveils Ca²⁺ Allostery and the Role of Gq in PTH-Receptor Signaling via cAMP"
10:25 am - 10:30 am	Discussion
10:30 am - 10:55 am	Coffee Break
10:55 am - 11:05 am	"The Role of Spatial Signaling in GPCR Function"
11:05 am - 11:10 am	Discussion
11:10 am - 11:35 am	"Compartmentalized Signaling of GPCRs"
11:35 am - 11:40 am	Discussion
11:40 am - 12:00 pm	"Structural Basis for Rapid Desensitization of GPCR Signaling"
12:00 pm - 12:05 pm	Discussion
12:05 pm - 12:25 pm	"GPCR Signaling in Time and Space"
12:25 pm - 12:30 pm	Discussion
12:30 pm - 1:30 pm	Lunch
1:30 pm - 4:00 pm	Free Time
3:00 pm - 4:00 pm	The GRC Power Hour™ The GRC Power Hour™ is designed to address challenges women face in science and issues of diversity and inclusion. The program supports the professional growth of all members of our communities by providing an open forum for discussion and mentoring. Organizers: and
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:30 pm - 9:30 pm	Biased Signaling Biased receptors/biased agonism - going in vivo to address functional selectivity, context or just selectivity. Discussion Leader:
7:30 pm - 7:55 pm	"Single Molecule Analysis of GPCR Coupling in Living Cells"
7:55 pm - 8:00 pm	Discussion
8:00 pm - 8:20 pm	"Biased GPCR Signaling: Progress, Prospects and a Fresh Perspective"
8:20 pm - 8:25 pm	Discussion
8:25 pm - 8:45 pm	"In Vivo Metabolic Roles of Distinct G Protein- and β-Arrestin-Dependent Signaling Pathways"
8:45 pm - 8:50 pm	Discussion
8:50 pm - 9:10 pm	"GPCRs: Opening the Gateway to Pathways that Prevent Neurodegeneration"
9:10 pm - 9:15 pm	Discussion
9:15 pm - 9:25 pm	"Screening Complex Mega and Giga Compound Libraries by Docking"
9:25 pm - 9:30 pm	Discussion
Tuesday
7:30 am - 8:30 am	Breakfast
8:30 am - 9:00 am	Group Photo
9:00 am - 12:30 pm	Opiate and Non-Opiate Analgesics Identifying the issues with classical opiate and non-analgesics and discussing mechanisms and novel therapeutics. Discussion Leader:
9:00 am - 9:25 am	"Neutral Antagonists at MOR and Opportunities for Treating Neonatal Abstinence Withdrawal Syndromes"
9:25 am - 9:30 am	Discussion
9:30 am - 9:55 am	"Molecular Pharmacology of CGRP Receptors: Migraine and Beyond"
9:55 am - 10:00 am	Discussion
10:00 am - 10:20 am	"Tone-Specific Pharmacology: GPCR Allosteric Modulators for Targeting Pain"
10:20 am - 10:25 am	Discussion
10:25 am - 11:00 am	Coffee Break
11:00 am - 11:25 am	"Mechanisms of CB2 Receptor-Induced Analgesia"
11:25 am - 11:30 am	Discussion
11:30 am - 11:50 am	"NOP/MOP Bifunctional Non-Addicting Analgesics for Opioid Crisis"
11:50 am - 11:55 am	Discussion
11:55 am - 12:05 pm	"Structural Bases of μ-Opioid Receptor (MOPr) Activation and Coupling"
12:05 pm - 12:10 pm	Discussion
12:10 pm - 12:30 pm	General Discussion
12:30 pm - 1:30 pm	Lunch
1:30 pm - 4:00 pm	Free Time
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:30 pm - 9:30 pm	New Tools for GPCRs as Therapeutic Targets for Neurological Disorders Novel strategies and progress in drug development for neurological disorders. Discussion Leader:
7:30 pm - 7:55 pm	"Optical Probing of Neuromodulatory GPCRs"
7:55 pm - 8:00 pm	Discussion
8:00 pm - 8:25 pm	"Activation and Allosteric Modulation of Neuroreceptors"
8:25 pm - 8:30 pm	Discussion
8:30 pm - 8:55 pm	"Photopharmacology of G Protein-Coupled Receptor Signaling"
8:55 pm - 9:00 pm	Discussion
9:00 pm - 9:10 pm	"Insights into the Selectivity of Adenosine Receptors"
9:10 pm - 9:15 pm	Discussion
9:15 pm - 9:30 pm	General Discussion
Wednesday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	Atypical GPCRs: Adhesion and Deorphanized GPCR Superfamily Members Recent developments in figuring out what some of the GPRx family members do. Discussion Leader:
9:00 am - 9:25 am	"Chemogenetic Approaches to Validate Poorly Characterized GPCRs"
9:25 am - 9:30 am	Discussion
9:30 am - 9:55 am	"New Players in Neurological Functions: GPR88"
9:55 am - 10:00 am	Discussion
10:00 am - 10:20 am	"Finding Receptors for Bioactive Molecules"
10:20 am - 10:25 am	Discussion
10:25 am - 10:50 am	Coffee Break
10:50 am - 11:10 am	"Force-Dependent Allostery in Cell-Cell Adhesion"
11:10 am - 11:15 am	Discussion
11:15 am - 11:35 am	"Structural and Functional Studies of Adhesion GPCRs and Their Ligands"
11:35 am - 11:40 am	Discussion
11:40 am - 12:00 pm	"Adhesion GPCR-Mediated Cell-Matrix Interaction in Neural Development"
12:00 pm - 12:05 pm	Discussion
12:05 pm - 12:25 pm	"Collagen Regulation of a New GPR56-Directed Signaling Process"
12:25 pm - 12:30 pm	Discussion
12:30 pm - 1:30 pm	Lunch
1:30 pm - 4:00 pm	Free Time
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:00 pm - 7:30 pm	Business Meeting Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
7:30 pm - 9:30 pm	Systems and Proteomics Recent development in data mining, the implications of drug development, and their influence on complex signaling pathways. Discussion Leader:
7:30 pm - 7:50 pm	"An Approach for Spatiotemporally Resolving GPCR Protein Interaction Networks Regulating Receptor Signaling"
7:50 pm - 7:55 pm	Discussion
7:55 pm - 8:15 pm	"Genome-Wide Discovery of New Microbial Molecular Probes from Chemical Genetic Interactions"
8:15 pm - 8:20 pm	Discussion
8:20 pm - 8:40 pm	"Illuminating the Dark Corridors of the GPCR-ome"
8:40 pm - 8:45 pm	Discussion
8:45 pm - 9:05 pm	"Regulation of Exocytosis by Inhibitory GPCRs and Gβγ Subunits"
9:05 pm - 9:10 pm	Discussion
9:10 pm - 9:25 pm	"Alternative Splicing of GPCR Signalling Components as a Source of Tissue-Specific Receptor Pharmacology"
9:25 pm - 9:30 pm	Discussion
Thursday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	How Form and Function Are Tightly Linked in GPCRs How structures continue to provide mechanistic insight; high resolution structure determination by x-ray diffraction and cryoEM; how structures finally help drug design; GPCRs as moving pictures: more than telling a thousand words. Discussion Leader:
9:00 am - 9:25 am	"Multiple Conformations of Photoactivated Rhodopsin: Role in Signal Transduction"
9:25 am - 9:30 am	Discussion
9:30 am - 9:55 am	"The Role of GPCR Dynamic in Signaling"
9:55 am - 10:00 am	Discussion
10:00 am - 10:25 am	"The Molecular Basis for High-Affinity Agonist Binding at the β1-Adrenoceptor"
10:25 am - 10:30 am	Discussion
10:30 am - 10:40 am	"Probing Conformational Dynamics by Solution NMR"
10:40 am - 10:45 am	Discussion
10:45 am - 11:10 am	Coffee Break
11:10 am - 11:35 am	"Structural Basis for CXCR Signaling Illuminated by Experimental and Computational Approaches"
11:35 am - 11:40 am	Discussion
11:40 am - 12:00 pm	"Structural and Functional Diversity in Receptor-Arrestin Complexes"
12:00 pm - 12:05 pm	Discussion
12:05 pm - 12:25 pm	"Structural Insights into Class B GPR Signalling and Allostery"
12:25 pm - 12:30 pm	Discussion
12:30 pm - 1:30 pm	Lunch
1:30 pm - 4:00 pm	Free Time
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:30 pm - 9:30 pm	Keynote Session: Innovative Drug Screening and Design Approaches Computational and novel methodologies and good old fashioned medicinal chemistry - repurposing GPCR drugs for disease: new life as anti-cancer therapeutics. Discussion Leader:
7:30 pm - 7:50 pm	"DNA-Encoded Libraries for Drug Discovery"
7:50 pm - 7:55 pm	Discussion
7:55 pm - 8:15 pm	"Structure-Based Virtual Ligand Screening and Design for New GPCR Probes"
8:15 pm - 8:20 pm	Discussion
8:20 pm - 8:40 pm	"Structure-Guided Strategies: How to Find Useful GPCR Ligands"
8:40 pm - 8:45 pm	Discussion
8:45 pm - 9:10 pm	"From Binding to Biophysics: My 50 Years (and Counting) of GPCR Research"
9:10 pm - 9:15 pm	Discussion
9:15 pm - 9:25 pm	"Molecular Mechanisms of Biased Agonism at the Angiotensin Receptor"
9:25 pm - 9:30 pm	Discussion
Friday
7:30 am - 8:30 am	Breakfast
9:00 am	Departure

Contributors

Research reported in this publication was supported by the National Institute On Drug Abuse of the National Institutes of Health under Award Number R13DA047877. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.

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