
Elucidating GPCR Functional Selectivity: Novel Opportunities for Drug Development
Tuesday, September 30, 2014
G protein-coupled receptors (GPCRs), the single largest class of druggable targets in therapeutic drug discovery, signal via canonical pathways involving heterotrimeric G proteins, and also via G protein–independent interactions with other signaling proteins, including β-arrestins, a process known as functional selectivity. Discovering ligands with the desired signaling bias at GPCRs will yield molecules with novel activities, and could lead to significantly improved therapeutics by enabling beneficial efficacy while reducing undesirable adverse effects. This symposium examines perspectives from academic and industrial scientists, highlighting basic and translational research. Researchers will discuss molecular and structural mechanisms underlying ligand bias and demonstrate how they quantify, design and develop functionally selective GPCR ligands for potential use in cardiovascular and central nervous system diseases.
*Reception to follow.
This event will also be broadcast as a webinar.
Please note: Transmission of presentations via the webinar is subject to individual consent by the speakers. Therefore, we cannot guarantee that every speaker's presentation will be broadcast in full via the webinar. To access all speakers' presentations in full, we invite you to attend the live event in New York City when possible.
Registration and Webinar Pricing
Member | $30 |
Member (Student / Postdoc / Resident / Fellow) | $15 |
Nonmember (Academia) | $65 |
Nonmember (Corporate) | $85 |
Nonmember (Non-profit) | $65 |
Nonmember (Student / Postdoc / Resident / Fellow) | $45 |
The Biochemical Pharmacology Discussion Group is proudly supported by
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Agenda
* Presentation titles and times are subject to change.
Tuesday September 30, 2014 | |
8:30 AM | Registration and Continental Breakfast |
9:00 AM | Welcome and Introduction |
9:10 AM | The Paradigm of GPCR Functional Selectivity and Implications for Drug Development |
9:30 AM | Beyond Signaling Bias |
10:10 AM | How Much Bias do we Need? Elucidating Ligand-Directed Signaling in vivo |
10:50 AM | Networking coffee break |
11:20 AM | Glycosylation of Proteas-activated Receptor-1 Regulates G Protein Signaling Pathway Bias |
12:00 PM | Extending the Bitopic Ligand Paradigm: A Novel Mechanism of Allostery in a G Protein-coupled Receptor Dimer |
12:40 PM | Networking lunch break |
1:40 PM | Keynote Presentation |
2:30 PM | Structural Features Responsible for GPCR Functional Selectivity |
3:10 PM | Networking coffee break |
3:40 PM | Implications for CPCR Functional Selectivity/Biased Signaling in the Actions of Dopamine |
4:20 PM | First Clinical Evidence That Biased Ligands Improve GPCR Therapeutic Pharmacology |
5:00 PM | Closing Remarks Networking reception |
6:00 PM | Close |
Speakers
Organizers
John A. Allen, PhD
Pfizer
John Allen earned a PhD in Physiology & Biophysics from the University of Illinois College of Medicine studying cell and molecular mechanisms regulating Gs/adenylyl cyclase/cAMP signaling followed by post-doctoral training at the University of North Carolina School of Medicine researching mechanisms of antipsychotic drug action and the neuropharmacology of serotonin and dopamine receptors. In 2011 John joined Pfizer Neuroscience where his research is aimed at identifying and advancing new therapeutic targets to treat neurological diseases including the profiling of GPCRs for preclinical drug development. His recent work has studied functional selectivity at the dopamine receptors and determined structural mechanisms enabling ligand bias. John is a member of the Society for Neuroscience and ASPET and has received research awards including a Young Investigator Award from the American College of Neuropsychopharmacology and a NARSAD Young Investigator Award.
Mercedes Beyna, MS
Pfizer
Mercedes Beyna is a scientist in the Neuroscience Research Unit at Pfizer. Her research focuses on target identification and assay development in the areas of psychiatric as well as neurodegenerative disorders. Captivated by neuroscience, she has worked in the field for over 10 years, in both academic and industrial laboratory settings. Before joining pharmaceutical R&D, Mercedes held lab manager and senior lab technician positions at New York University (NYU). Mercedes attended Binghamton University, earning her undergraduate degree in Biology, and subsequently received her Master's Degree in Biology from NYU. As the Pfizer lead in the Biochemical Pharmacology Discussion Group at the New York Academy of Sciences, she enjoys developing interesting and educational symposia.
Bryan L. Roth, MD, PhD
University of North Carolina School of Medicine
Bryan Roth MD, PhD, is the Michael Hooker Distinguished Professor of Pharmacology at UNC Chapel Hill Medical School. Dr. Roth received postdoctoral training in molecular pharmacology at NIH and his psychiatry training at Stanford. His research interests include chemical and synthetic biology particularly as they apply to G-protein coupled receptors. He has published nearly 400 papers and given 100's of invited talks. Dr. Roth serves on the boards of many pharmacology and chemistry journals and, in addition, is currently the Deputy Editor of the Journal of Clinical Investigation. Dr. Roth also directs the National Institute of Mental Health's small molecule screening program--now in its 16th year. Over the past 5 years, this program (NIMH-PDSP) has facilitated work on more than 500 projects and contributed to more than 500 publications and patents assisting investigators world-wide.
Jennifer Henry, PhD
The New York Academy of Sciences
Keynote Speaker
Robert J. Lefkowitz, MD
Duke University Medical Center
Robert J. Lefkowitz, MD is James B. Duke Professor of Medicine and Professor of Biochemistry at the Duke University Medical Center. He has been an Investigator of the Howard Hughes Medical Institute since 1976. He has received numerous awards and honors for his research, including the National Medal of Science, the Shaw Prize, the Albany Prize, and the 2012 Nobel Prize in Chemistry. He was elected to the USA National Academy of Sciences in 1988; the American Academy of Arts and Sciences in 1983, and the Institute of Medicine in 1994. He is best known for his studies of G protein coupled receptors, a field which he has pioneered for more than 45 years.
Speakers
John A. Allen, PhD
Pfizer
John Allen earned a PhD in Physiology & Biophysics from the University of Illinois College of Medicine studying cell and molecular mechanisms regulating Gs/adenylyl cyclase/cAMP signaling followed by post-doctoral training at the University of North Carolina School of Medicine researching mechanisms of antipsychotic drug action and the neuropharmacology of serotonin and dopamine receptors. In 2011 John joined Pfizer Neuroscience where his research is aimed at identifying and advancing new therapeutic targets to treat neurological diseases including the profiling of GPCRs for preclinical drug development. His recent work has studied functional selectivity at the dopamine receptors and determined structural mechanisms enabling ligand bias. John is a member of the Society for Neuroscience and ASPET and has received research awards including a Young Investigator Award from the American College of Neuropsychopharmacology and a NARSAD Young Investigator Award.
Laura Bohn, PhD
The Scripps Research Institute - Florida
Laura Bohn, PhD is a professor of Molecular Therapeutics and Neuroscience at The Scripps Research Institute. She is an internationally recognized researcher investigating the function of G protein-coupled receptors which are critical to how patients respond to various therapeutics, including the opioid analgesics and antipsychotic agents. Dr. Bohn earned Bachelors degrees in both Chemistry and Biochemistry from Virginia Tech and then went on to get her PhD in Biochemistry and Molecular Biology from St. Louis School of Medicine. She received post-doctoral training in the Howard Hughes Medical Institute at the Duke University Medical Center in the laboratory of Dr. Marc Caron. Dr. Bohn joined the faculty and achieved tenure at The Ohio State University College of Medicine in the Departments of Pharmacology and Psychiatry. She joined Scripps Florida in March, 2009, in the departments of Molecular Therapeutics and Neuroscience where she is pursuing new therapies for the treatment of pain. In recognition of her achievements, she has received the Women in Neuroscience/Society for Neuroscience Career Development Award, was awarded the 2009 Joseph Cochin Young Investigator Award presented by the College of Drug Dependence and received the John J. Abel Award in Pharmacology from the American Society for Pharmacological and Experimental Therapeutics and Pfizer. In the past 5 years, Dr. Bohn has served as a consultant to Trevena Inc., Purdue Pharma, LP, and Mencuro Therapeutics, Inc.; she currently collaborates with Eli Lilly & Company. Her research program at The Scripps Research Institute is funded by the National Institutes on Drug Abuse.
Marc G. Caron, PhD
Duke University Medical Center
Marc G. Caron holds a PhD from the University of Miami. He is a James B. Duke Professor of Cell Biology at Duke University Medical Center. His long-standing research interests have been in the mechanisms and regulation of G protein-coupled receptors and on the mechanisms of neurotransmission as controlled by neurotransmitter transporters. His recent efforts have been centered on using genetic approaches to develop animal models of abnormal neurobiological function including disorders associated with aberrant serotonergic, dopaminergic and reward mechanisms.
Jonathan A. Javitch, MD, PhD
Columbia University and New York State Psychiatric Institute
Jonathan A. Javitch obtained his BS and MS in Biological Sciences at Stanford University. He completed the joint MD-PhD program at the Johns Hopkins University School of Medicine where as a graduate student with Solomon Snyder he demonstrated that a key step in the neurotoxicity of MPTP is the uptake of its metabolite MPP+ by the dopamine transporter. Dr. Javitch completed a medical internship and psychiatric residency at the Columbia Presbyterian Hospital and the New York State Psychiatric Institute. He did postdoctoral work on the structure of dopamine receptors with Dr. Arthur Karlin at Columbia University. Dr. Javitch is currently the Lieber Professor of Experimental Therapeutics in Psychiatry and Professor of Pharmacology in the Center for Molecular Recognition and in Physiology and Cellular Biophysics at the Columbia University College of Physicians and Surgeons, Director of the Lieber Center for Schizophrenia Research and Treatment, and Chief of the Division of Molecular Therapeutics at the New York State Psychiatric Institute. His research focuses on the structure, function and regulation of G protein-coupled receptors and neurotransmitter transporters.
Terry Kenakin, PhD
University of North Carolina School of Medicine
Beginning his career as a synthetic chemist, Terry Kenakin received a PhD in Pharmacology at the University of Alberta, Edmonton Canada. After a post-doctoral Fellowship at University College London, U.K., he joined Burroughs-Wellcome as an associate Scientist. From there he continued working in drug discovery at Glaxo Inc., GlaxoWellcome and finally GlaxoSmithKline. Leaving his position as a Director at GlaxoSmithKline Research and Development laboratories at Research Triangle Park, N.C. USA, Dr. Kenakin is now a professor in the Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill. Currently he is engaged in studies aimed at the optimal design of drug activity assays systems, the discovery and testing of allosteric molecules for therapeutic application and the quantitative modeling of drug effects. In addition, he is Director of the Pharmacology curriculum at the UNC School of Medicine. He is a member of numerous editorial boards as well as editor in Chief of the Journal of Receptors and Signal Transduction and Co-editor in Chief of Current Opinion in Pharmacology. He has authored numerous articles and has written 10 books on Pharmacology.
Bryan L. Roth, MD, PhD
University of North Carolina School of Medicine
Bryan Roth MD, PhD, is the Michael Hooker Distinguished Professor of Pharmacology at UNC Chapel Hill Medical School. Dr. Roth received postdoctoral training in molecular pharmacology at NIH and his psychiatry training at Stanford. His research interests include chemical and synthetic biology particularly as they apply to G-protein coupled receptors. He has published nearly 400 papers and given 100's of invited talks. Dr. Roth serves on the boards of many pharmacology and chemistry journals and, in addition, is currently the Deputy Editor of the Journal of Clinical Investigation. Dr. Roth also directs the National Institute of Mental Health's small molecule screening program--now in its 16th year. Over the past 5 years, this program (NIMH-PDSP) has facilitated work on more than 500 projects and contributed to more than 500 publications and patents assisting investigators world-wide.
JoAnn Trejo, PhD
University of California, San Diego
Dr. JoAnn Trejo (BS, UC Davis and PhD, UC San Diego) is a Professor in the School of Medicine at the University of California, San Diego. Dr. Trejo conducts research, published in > 60 papers, focused on defining the pathways that regulate vascular inflammation and breast cancer progression. She has received numerous grants from the National Institutes of Health (NIH), Komen Foundation, UC Tobacco-related Disease Research Program and the American Heart Association (AHA) including the prestigious AHA Established Investigator Award. Dr. Trejo is a leader in the scientific community. She was elected to serve on Council of the American Society for Cell Biology (ASCB), as Chair of Gordon Research Conferences and a member of several NIH Study Sections. Dr. Trejo is committed to increasing the diversity of science and gives frequent lectures on this topic. She is a Life member of Society for the Advancement of Chicanos and Native Americans in Science (SACNAS), a member of the ASCB Women in Cell Biology Committee, ASCB Minority Affairs Committee and Keystone Symposia Diversity Advisory Committee. Dr. Trejo is the recipient of the 2015 American Society for Biochemistry and Molecular Biology Ruth Kirchstein Diversity in Science Award. She is currently the Director of the San Diego Institutional Research and Academic Career Development Award (IRACDA), an NIH sponsored postdoctoral training program that aims to develop a diverse group of highly trained biomedical scientists and is the Vice Chair of Education in the Department of Pharmacology at UC San Diego.
Jonathan D. Violin, PhD
Trevena Inc.
Dr. Violin helped to launch Trevena in 2008 from its scientific foundations at Duke University, and leads Trevena’s investor relations program. Prior to this, he led Trevena’s biology group, focused on cardiovascular and CNS diseases, and was responsible for high throughput screening, cellular and molecular pharmacology, and in vivo pharmacology teams. He helped Trevena identify and progress three novel molecules to clinical development, including TRV027, now in a Phase 2b study for acute heart failure, and TRV130, now in Phase 2 studies for treating post-operative pain. Prior to joining Trevena, he was a post-doctoral fellow in the laboratory of Dr. Robert Lefkowitz at Duke University Medical Center, where he studied biased ligands and beta-arrestin functions for a variety of GPCRs. His research helped establish how biased ligands elicit unique cellular pharmacology with potential to translate into differentiated therapeutics. Dr. Violin holds a Ph.D. from the Department of Pharmacology at the University of California, San Diego, where he developed biosensors to study the spatial and temporal dynamics of kinase signaling. He also received an M.B.A. with a concentration in Health Sector Management from the Fuqua School of Business and a B.S. in Chemical Pharmacology from Duke University.
Sponsors
For sponsorship opportunities please contact Perri Wisotsky at pwisotsky@nyas.org or 212.298.8642.
Academy Friend
Grant Support
This activity is supported by an education grant from Lilly. For further information concerning Lilly grant funding visit www.lillygrantoffice.com.
This program is supported in part by a grant from Merck and Co., Inc.
This program is supported in part by a grant from Otsuka America Pharmaceutical, Inc.
Promotional Partners
The American Society for Pharmacology and Experimental Therapeutics (ASPET)
Society of Biological Psychiatry
The Biochemical Pharmacology Discussion Group is proudly supported by
Mission Partner support for the Frontiers of Science program provided by 
Abstracts
The Paradigm of GPCR Functional Selectivity and Implications for Drug Development
John A. Allen, PhD, Pfizer, Inc.
Beyond Signaling Bias
Terry Kenakin, PhD, University of North Carolina at Chapel Hill School of Medicine
How Much Bias do we Need? Elucidating Ligand-Directed Signaling in vivo
Laura Bohn, PhD, The Scripps Research Institute
Glycosylation of Protease-activated Receptor-1 Regulates G Protein Signaling Pathway Bias
JoAnn Trejo, PhD, University of California, San Diego
Extending the Bitopic Ligand Paradigm: A Novel Mechanism of Allostery in a G Protein-coupled Receptor Dimer
Jonathan A Javitch, MD, PhD2,3
Coauthor: J Robert Lane, PhD1, Prashant Donthamsetti, MSc2,3, Jeremy Shonberg, PhD4, Chris J Draper-Joyce, BSc1,Samuel Dentry, BSc1, Mayako Michino, PhD5, Lei Shi, PhD5,6, Laura López, PhD1, Peter J Scammels, PhD4,Benvenuto Capuano, PhD4, Patrick M Sexton, PhD1, Arthur Christopoulos, PhD1
1Drug Discovery Biology, Department of Pharmacology, Monash Institute of Pharmaceutical Sciences, Monash University
2Departments of Psychiatry, and Pharmacology, College of Physicians and Surgeons, Columbia University
3Division of Molecular Therapeutics, New York State Psychiatric Institute
4Department of Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University
5Department of Physiology and Biophysics, Weill Medical College of Cornell University
6Institute for Computational Biomedicine, Weill Medical College of Cornell University
Keynote Presentation: A Brief History of β-arrestins: From Birth to Bias
Robert J. Lefkowitz, MD, Duke University Medical Center
Structural features responsible for GPCR functional selectivity
Bryan Roth, MD, PhD, University of North Carolina at Chapel Hill School of Medicine
Implications for GPCR Functional Selectivity/Biased Signaling in the Actions of Dopamine
Marc G. Caron, PhD, Duke University Medical Center
First Clinical Evidence That Biased Ligands Improve GPCR Therapeutic Pharmacology
Jonathan Violin, PhD, Trevena, Inc
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