Eldorado Hotel & Spa Floorplan

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This meeting took place in 2018



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GPCR Structure and Function: Taking GPCR Drug Development and Discovery to the Next Level (B8)


Organizer(s) Roger K. Sunahara and Christian Felder
February 16—20, 2018
Eldorado Hotel & Spa • Santa Fe, New Mexico USA
Discounted Abstract Deadline: Oct 17, 2017
Abstract Deadline: Nov 15, 2017
Scholarship Deadline: Oct 17, 2017
Discounted Registration Deadline: Dec 18, 2017

Sponsored by Novo Nordisk A/S and Theravance Biopharma

Summary of Meeting:
G protein-coupled receptors (GPCRs) are a critical family of cell surface receptors that detect extracellular stimuli, facilitate intercellular communication and regulate cellular homeostasis. As such, GPCRs remain highly relevant drug discovery targets addressing key unmet medical needs. Recent advances in understanding GPCR signaling networks, coupled with the unraveling of structural details of GPCRs, their signaling partners and in some cases their signaling complexes, have enhanced our understanding of GPCR function. These advances have provided researchers the basic tools to interrogate critical but diverse aspects of GPCR signaling, such as receptor conformation, receptor-effector specificity and the role of receptor subcellular distribution, in signaling efficacy. All of these factors may influence ligand binding and therefore have impact on drug discovery. The availability of atomic-resolution structures of GPCRs alongside the introduction of functional coupling (e.g., biased signaling) is providing the potential for physiologically tailored and therefore disease-specific therapies. However, challenges remain as the design of small molecule tools and potential drugs is both labor-intensive and very costly, requiring large chemical library screening campaigns. In addition, improvements are still needed in GPCR ligand selectivity, signaling specificity and appropriate kinetics to achieve maximal efficacy and reasonable safety. Rational ligand design could significantly reduce both time and cost of drug discovery. Viable approaches are currently being explored through the combination of molecular dynamic simulations, GPCR crystallization and biophysical analysis. Drug efficacy and safety improvements are slow to emerge and can be addressed by the development of physiologically relevant GPCR ligands. Targeting allosteric sites, hetero- and homo-dimers and specific signaling pathways could provide such context- and disease-specific regulation. This conference will highlight the latest developments in GPCR structure/function, ligand discovery and design, intracellular signaling pathways and their impact on modern 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 24 hr (international) time


The meeting will begin on Friday, February 16 with registration from 16:00 to 20:00 and a welcome mixer from 18:00 to 20:00. Conference events conclude on Tuesday, February 20 with a closing plenary session from 17:00 to 19:15, followed by a social hour and entertainment. We recommend return travel on Wednesday, February 21 in order to fully experience the meeting.

FRIDAY, FEBRUARY 16

4:00—8:00 PM
Arrival and Registration

Eldorado Lounge
6:00—8:00 PM
Welcome Mixer
No registration fees are used to fund alcohol served at this function.

Eldorado Lounge

SATURDAY, FEBRUARY 17

7:00—8:00 AM
Breakfast

Anasazi Ballroom
8:00—9:00 AM
Welcome and Keynote Address
Meeting has ended...abstracts no longer viewable online.

Eldorado Grand Ballroom
* Roger K. Sunahara, University of California, San Diego, USA

Brian K. Kobilka, Stanford University School of Medicine, USA
The Structural Dynamics of GPCR Activation

9:00—11:15 AM
Structure and Function of GPCRs I
Meeting has ended...abstracts no longer viewable online.
Cutting edge research in GPCR structure and function using state of the art structural and biochemical approaches.

Eldorado Grand Ballroom
* Nicolas L. Villanueva, University of California, San Diego, USA

Robert Scott Prosser, University of Toronto, Canada
Molecular Underpinnings of GPCR Pharmacology and Mechanisms of GPCR Activation: Spectroscopic Studies of the Adenosine A2A Receptor

Coffee Break

Beili Wu, Shanghai Institute of Materia Medica, CAS, China
Structure of the Full-Length Glucagon Receptor

Scott C. Blanchard, Weill Cornell Medicine, USA
Single-Molecule Analysis of Ligand Efficacy in β2AR-G Protein Activation

Yonghoon Kwon, POSTECH, South Korea
Short Talk: Dimeric b2-Adrenergic Receptor Regulates the Basal Activity Subjected to Inverse Agonism

11:15 AM—5:00 PM
On Own for Lunch

11:15 AM—1:00 PM
Poster Setup

Anasazi Ballroom
1:00—10:00 PM
Poster Viewing

Anasazi Ballroom
4:30—5:00 PM
Coffee Available

Concourse
5:00—7:00 PM
Structure and Function of GPCRs II
Meeting has ended...abstracts no longer viewable online.
Structural aspects of arrestin-GPCR complexes and their implication to signaling bias.

Eldorado Grand Ballroom
* Vsevolod Katritch, University of Southern California, USA

Tracy M. Handel, University of California, San Diego, USA
Structure and Signaling Mechanisms of G Protein-Coupled and β-Arrestin-Biased Chemokine Receptors

H. Eric Xu, Van Andel Institute, USA
Molecular Assembly of Rhodopsin with GRK1 and Arrestin

Ka Young Chung, Sungkyunkwan University, South Korea
Conformational Mechanism of GPCR Signaling Analyzed by Hydrogen/Deuterium Exchange Mass Spectrometry

Anita K. Nivedha, City of Hope, USA
Short Talk: Identifying Functional Hotspot Residues for Biased Ligand Design in G-protein Coupled Receptors

7:00—8:00 PM
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Anasazi Ballroom
7:30—10:00 PM
Poster Session 1

Anasazi Ballroom

SUNDAY, FEBRUARY 18

7:00—8:00 AM
Breakfast

Anasazi Ballroom
8:00—11:15 AM
GPCRs: Naturally Great Drug Targets
Meeting has ended...abstracts no longer viewable online.
Use of cutting edge approaches in GPCR drug discovery and development.

Eldorado Grand Ballroom
* Irina Kufareva, University of California, San Diego, USA

Nagarajan Vaidehi, City of Hope National Medical Center, USA
Information Pipelines: Forward and Reverse Allostery in GPCRs

Fiona H. Marshall, Heptares Therapeutics Ltd., UK
Using X-Ray Structures of GPCRs to Guide Drug Discovery - Challenges for Allosteric Modulators

Coffee Break

Kathleen M. Caron, University of North Carolina at Chapel Hill, USA
RAMPS: The Natural Allosteric Modulators and their Role in Disease

Daniel Rosenbaum, University of Texas Southwestern Medical Center, USA
Structure-Function of the CB1 Cannabinoid Receptor

Kaushik Sarkar, UCB Celltech, UK
Short Talk: Discovery of Antibodies against PTH1R, A Class B GPCR: Characterisation of their Binding and Impact on PTH1R Function

Franziska Marie Heydenreich, University of Montreal, Canada
Short Talk: The Inner Workings of a GPCR: Molecular Basis for Signaling Bias and Functional Selectivity

11:15 AM—5:00 PM
On Own for Lunch

11:15 AM—1:00 PM
Poster Setup

Anasazi Ballroom
1:00—10:00 PM
Poster Viewing

Anasazi Ballroom
4:30—5:00 PM
Coffee Available

Concourse
5:00—7:00 PM
Novel Approaches to Drug Action and Discovery
Meeting has ended...abstracts no longer viewable online.
Use of novel approaches to study the mechanism of action of drugs and their future use in drug discovery.

Eldorado Grand Ballroom
* Dmitry Veprintsev, University of Nottingham, UK

Dirk Trauner, New York University, USA
How to Convert Any GPCR into a Photoreceptor

Bryan Roth, University of North Carolina at Chapel Hill, USA
New Technologies for Illuminating the Druggable GPCR-ome

Jeffrey Jeffrey Conn, Vanderbilt University, USA
Genetic Insights Lead to Discovery of Selective mGlu1 and mGlu3 Metabotropic Glutamate Receptor PAMs as Potential Treatments for Schizophrenia

Guan-Da Syu, Johns Hopkins Medicine, USA
Short Talk: Virion Display (VirD) Approach to Characterizing Non-Odorant GPCRs in Humans

7:00—8:00 PM
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Anasazi Ballroom
7:30—10:00 PM
Poster Session 2

Anasazi Ballroom

MONDAY, FEBRUARY 19

7:00—8:00 AM
Breakfast

Anasazi Ballroom
8:00—11:15 AM
Complexity of Cellular Signaling
Meeting has ended...abstracts no longer viewable online.
Complexity of GPCR-mediated signaling in cells where cellular context and sub-cellular distribution may play a role in specific signal transduction pathway activation.

Eldorado Grand Ballroom
* Jacob Mahoney, Stanford University, USA

Mark von Zastrow, University of California, San Francisco, USA
Subcellular Organization of GPCR Signaling

Madan Babu Mohan, MRC Laboratory of Molecular Biology, UK
Pharmacogenomics of G-Protein Coupled Receptor Drug Targets

Coffee Break

Ron O. Dror, Stanford University, USA
One Receptor, Many Partners: How Do GPCRs Stimulate Diverse Signaling Proteins?

Martin J. Lohse, Max Delbrück Center for Molecular Medicine, Germany
The Kinetics of Biased Signaling in GPCRs

Nevin A. Lambert, Medical College of Georgia, USA
Short Talk: Cellular Assays Based on Mini G Proteins

Ieva Sutkeviciute, University of Pittsburgh, USA
Short Talk: Structural Determinants and Physiological Implications of PTH Receptor Endosomal Signaling

11:15 AM—5:00 PM
On Own for Lunch

11:15 AM—1:00 PM
Poster Setup

Anasazi Ballroom
1:00—10:00 PM
Poster Viewing

Anasazi Ballroom
4:30—5:00 PM
Coffee Available

Concourse
5:00—7:00 PM
The GPCR Superfamily: Broad Mechanisms of Action
Meeting has ended...abstracts no longer viewable online.
Broad mechanisms of activation of various members of the GPCR superfamily and their implications in disease.

Eldorado Grand Ballroom
* Graeme Milligan, University of Glasgow, UK

Gregory Tall, University of Michigan Medical School, USA
Adhesion GPCRs: A One and Done Family of Receptors and their Implications in Disease

Susan G. Amara, NIMH, National Institutes of Health, USA
GPCR Signaling in Dopamine Neurons: An Intracellular Trace-Amine Receptor, TAAR1, Mediates the Actions of Amphetamines

Patrick M. Sexton, Monash University, Australia
Structure and Function of Class B GPCRs

Benjamin R. Myers, University of Utah School of Medicine, USA
Short Talk: Dissecting the Regulation of the 7TM Oncoprotein Smoothened Using a New Set of in vitro and Cell-Based Tools

7:00—8:00 PM
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Anasazi Ballroom
7:30—10:00 PM
Poster Session 3

Anasazi Ballroom

TUESDAY, FEBRUARY 20

7:00—8:00 AM
Breakfast

Anasazi Ballroom
8:00—11:15 AM
GPCRs in vivo: Implications in Disease
Meeting has ended...abstracts no longer viewable online.
GPCR signaling in disease using various animal models to predict and/or simulate human disease.

Eldorado Grand Ballroom
* Debbie L. Hay, University of Auckland, New Zealand

Arthur Christopoulos, Monash University, Australia
GPCR Allosteric Modulators: Discovery and Relevance to Disease Context

Michael R. Bruchas, Washington University School of Medicine, USA
Optical Approaches for Dissecting GPCR Signaling in Motivated Behavior

Coffee Break

J. Silvio Gutkind, University of California, San Diego, USA
GPCR and G Protein Mutations in Cancer

Andrew B. Tobin, University of Glasgow, Scotland
From Cognition to Seizures: Novel Molecular Mechanism Underlying Key Muscarinic Receptor Action

Li Yang, East Carolina University, USA
Short Talk: Proton-Sensing GPCRs in Inflammation and Cancer

Nicola J. Smith, Victor Chang Cardiac Research Institute, Australia
Short Talk: Orphan Receptor GPR37L1 Contributes to the Sexual Dimorphism of Central Cardiovascular Control

11:15 AM—5:00 PM
On Own for Lunch

4:30—5:00 PM
Coffee Available

Concourse
5:00—7:00 PM
Drug Discovery and the Realistic Process
Meeting has ended...abstracts no longer viewable online.
Drug discovery and development from the industrial perspective. The discussion will focus on how target validation, PK/PD, medicinal chemistry, clinical trials and time influence successful drug development.

Eldorado Grand Ballroom
* Sophie J. Bradley, University of Glasgow, UK

Kurt Rasmussen, Eli Lilly and Company, USA
Development of Novel Treatments for Opiate Addiction

Stephen Hitchcock, Takeda Pharmaceuticals, USA
The Journey from Expression Profiling to Clinical Development: Identification of Cell Type Selective Orphan GPCRs and the Discovery of Surrogate Ligands to Probe their Therapeutic Potential

Kevin M. Biglan, Eli Lilly and Company, USA
Preclinical Profile of a Dopamine D1 Potentiator Suggests Therapeutic Utility in Neuropsychiatric Disorders

Joshua Allen, Oncoceutics, Inc., USA
Short Talk: Differentiated Receptor Pharmacology of Imipridone ONC201: The First DRD2 Antagonist in Clinical Development for Oncology

7:00—7:15 PM
Meeting Wrap-Up: Outcomes and Future Directions (Organizers)
Meeting has ended...abstracts no longer viewable online.

Eldorado Grand Ballroom
7:15—8:15 PM
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Anasazi Ballroom
8:00—11:00 PM
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.

Anasazi Ballroom

WEDNESDAY, FEBRUARY 21

 
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:

Novo Nordisk A/S Theravance Biopharma

We gratefully acknowledge additional support from these exhibitors at this conference:

Thermo Fisher Scientific
Please stop by to meet these exhibitors during the conference.


We gratefully acknowledge additional support for this conference from:

Eurofins Pharma Discovery Services Journal of General Physiology

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



Heptares Therapeutics Ltd


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, 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