Saturday, April 20, 2013 - Wednesday, April 24, 2013
Boston, MA
For the past four years, ASPET members attending the ASPET Annual Meeting at EB 2013 have spent a day volunteering in the local communities of the host city: In 2009, we built homes with Habitat for Humanity in the Upper 9th Ward in New Orleans; in 2010, 2011, and 2012 we prepared and served meals to homeless residents of Pasadena, Washington, DC, and San Diego, respectively. The Behavioral Pharmacology Division of ASPET is again sponsoring a volunteer opportunity at EB 2013 in Boston. We will spend Friday, April 19, 2013, helping Cradles to Crayons provide children living in homeless or low-income situations in Boston with the essential items they need to thrive. Special thanks to Iggy’s Bread of the World, Shaw's, Star Market, and Stop & Shop for their generous donations to help feed our volunteers! Further details will follow to those who express an interest in volunteering. If you plan to join us, please contact Charles P. France at france@uthscsa.edu, 210-567-6969 (voice), or 210-567-0104 (fax) at your earliest convenience.
Behavioral Pharmacology Society Meeting
Westin Boston Waterfront, Commonwealth Ballroom B/C
6:00 PM – 11:00 PM
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Behavioral Pharmacology Society Meeting
Westin Boston Waterfront, Grand Ballroom E
8:00 AM – 6:00 PM
2013 Teaching Institute: Training Models for Undergraduate Pharmacology: US/UK Perspectives
Boston Convention Center, Room 108
Noon – 2:30 PM
Chair: Nick J. Goulding, Barts and the London Sch. of Med. and Dentistry
Setting an agenda for undergraduate pharmacology
Nick J. Goulding, Barts and the London Sch. of Med. and Dentistry
Undergraduate degrees in the UK: Where are we going?
Susan Brain, King’s Col. London
Educating the next generation of in-vivo pharmacologists: Meeting the needs of industry and academia
David Lewis, Univ. of Leeds, Sch. of Biomed. Sci.
Pharmacology for undergraduates: The Duke model
Rochelle D. Schwartz-Bloom, Duke Univ. Med. Ctr.
Toward an integrated undergraduate pharmacology curriculum
Robert Watson, State Univ. of New York at Stony Brook
Panel Q & A: Future prospects for undergraduate education in pharmacology: An agenda for ASPET and BPS
Graduate Student Colloquium: Introducing the Individual Development Plan: A Key to Success
Boston Convention Center, Room 107C
2:00 PM – 5:00 PM
Chair: Lynn Wecker, University of South Florida
Break-out session group leaders: Marcus DeLatte, FDA, Silver Spring; Christine C. Carrico, ASPET; Ann Hanna-Mitchell, Univ. of Pittsburgh Sch. of Med.; Mary Jeanne Kallman, Covance Labs.; Harriet Kamendi, AstraZeneca; Susan Ingram, Oregon Hlth. & Sci. Univ.
As Yogi Berra once said, "You got to be careful if you don't know where you're going, because you might not get there.” Although Yogi was likely not thinking about a scientific career when he made that statement, the concept of the Individual Development Plan (IDP) as a tool to help individuals assess their skills, interests and values, has been used in the business and governmental sectors for some time, and has now permeated academia. Simply put, the IDP is typically used to identify professional goals and objectives, assess one's skill set relative to these goals, and develop a plan (both short-term and long-term) to acquire the skills required to achieve these goals. Most resources would agree that the IDP is currently recognized as the best practice in promoting professional development , and is recognized as an important, valuable and beneficial tool for professionals at all career stages with all types of goals. It also serves as a communications tool, enabling graduate students to communicate their long and short term goals with their mentors. Creating an IDP at the beginning of graduate school can lead to more effective time management and use of resources, and more focused efforts, targeted towards achieving career goals.
This colloquium will begin with a brief overview of ASPET’s new mentoring program and will quickly move into a synopsis of the steps used to create an IDP. You will learn how to map out your general career trajectory, match your skills and strengths with your career choices, and identify areas for development that build upon your current strengths. Once the process and steps are presented, attendees will begin to create their own IDP and should expect to have a solid first version by the time they complete the workshop, keeping in mind that the IDP is a 'living document' that continuously evolves throughout one's career.
Individual Development Plan: A Key to Success
Lynn Wecker, Univ. of South Florida
Introduction to ASPET mentoring program
Remy Brim, Bioethics Dept./NIH
Career Path Speakers:
Gunther Kern, AstraZeneca, Boston
Federico Bernal, NCI/NIH
Maja Köhn, European Molecular Biology Laboratory, Heidelberg
Stephani Sutherland, Freelance Science Writer, Scientific American MIND and Pain Research Forum
Myron Toews, Univ. of Nebraska Med. Ctr.
Mary Jeanne Kallman, Covance Labs.
Break-out session group leaders:
Myron Toews, Univ. of Nebraska Med. Ctr.
Christine K. Carrico, ASPET
Ann Hanna-Mitchell, Univ. of Pittsburgh Sch. of Med.
Mary Jeanne Kallman, Covance Labs.
Harriet Kamendi, AstraZeneca
Susan Ingram, Oregon Hlth. & Sci. Univ.
ASPET Business Meeting
Boston Convention Center, Room 107AB
6:00 PM – 7:30 PM
ASPET Opening and Awards Reception
Boston Convention Center, SW Lobby
7:30 PM – 9:30 PM
Sponsored by the National Board of Medical Examiners and Pharmacology Research & Perspectives
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Diversity Mentoring Breakfast
Westin Boston Waterfront, Revere
7:30 AM – 9:30 AM
Workshop: Art of Item Writing (NBME style) and Basics of Assessment
Westin Boston Waterfront, Grand Ballroom E
9:00 AM – 12:30 PM
ASPET gratefully acknowledges the educational grant from the National Board of Medical Examiners for supporting this workshop.
Sponsored by the Division for Pharmacology Education
Chair: Senthil
Kumar Rajasekaran, Oakland Univ. William Beaumont Sch. of Med.
Reflecting world-wide shifts
toward integrative curricula, this workshop focuses on writing MCQ
exams for basic science courses that assess the application of knowledge
to clinical situations and interpreting the data obtained from student
performance. Following an introduction to the topic, three 60 minute
sessions will be conducted to:
1) provide guidance and hands-on training in constructing and critiquing case-based assessment items;
2) help to understand the basics of exam item analysis and the ways one can interpret the results; and
3) discuss hot topics in medical education, including potential teaching and assessment methods for educational research.
Introduction to the workshop: Importance of correct item writing and current trends in recognizing educational research
Senthil Kumar Rajasekaran, Oakland Univ. William Beaumont Sch. of Med.
Developing high-quality multiple-choice test items for basic sciences
Mark Raymond, National Board of Medical Examiners
Setting pass/fail standards: Discussing item analysis
Mark Raymond, National Board of Medical Examiners
Hot topics in medical education research
Lynn Crespo, Univ. of South Carolina Sch. of Med., Greenville
Orthostatic intolerance: Insights into pharmacologic, physiologic and gender issues
Boston Convention Center, Room 106
9:30 AM – Noon
Sponsored by the Divisions for Cardiovascular Pharmacology & Integrative Systems, Translational and Clinical Pharmacology
Chairs: Julian Stewart, New York Med. Col. and Amy Arnold, Vanderbilt Univ. Sch. of Med.
Standing up from a supine or
seated position depends on rapid cardiovascular adaptations that are
driven by an interplay of autonomic, volume and hormonal mechanisms. The
inability of these mechanisms to adequately compensate for changes in
posture results in orthostatic intolerance. A growing number of
disorders have been associated with orthostatic intolerance and all are
more prevalent in women. This symposium will explore the underlying
physiologic mechanisms, gender difference and current pharmacologic
targets for both acute and chronic forms of orthostatic intolerance,
including syncope, fatigue, and postural orthostatic tachycardia
syndrome.
Vasovagal syncope: putative triggers and pharmacological and physiological approaches to management
Roger Hainsworth, Univ. of Leeds
Neural and non-neural control of orthostatic intolerance: implications for sex differences
Qi Fu, Texas Healthy Presbyterian Hosp. Dallas
Identifying sympathetic nervous system abnormalities in orthostatic intolerance
Elisabeth Lambert, Human Neurotransmitter Lab.
Ehlers Danlos Syndrome, joint hypermobility and orthostatic intolerance
Peter Rowe, Johns Hopkins Children's Ctr.
Hypo-osmolality pressor stimulus is linked to transient receptor potential vanilloid 4 (TRPV4) in the portal region
Junior Speaker: Tu Mai, Vanderbilt Univ.
Loss of muscle sympathetic nerve activity and blood pressure phase synchronization in postural vasovagal syncope
Junior Speaker: Christopher E. Schwartz, New York Med. Col.
Novel functions for cyclic nucleotide phosphodiesterases and their implications for pharmacological intervention
Boston Convention Center, Room 107AB
9:30 AM – Noon
Sponsored by the Divisions for
Molecular Pharmacology; Cardiovascular Pharmacology; Integrative
Systems, Translational and Clinical Pharmacology; and Neuropharmacology
Chair: Marco Conti, UCSF
Phosphodiesterases (PDEs),
the enzymes that degrade and inactivate cyclic nucleotides, are
considered critical components in cellular homeostasis, and the design
of PDE inhibitors occupies a prime role in pharmacology. The discovery
of several new genes and numerous variants has broadened the applications of PDE pharmacology. Genetic models and selective inhibitors have
uncovered a host of new functions that can be ascribed to a specific PDE
isoform. This session will focus on how the integration of specific PDE
variants into macromolecular complexes with receptors, channels and
kinases provides novel insights into the generation of signaling
microdomains and the specificity of cellular responses to external cues.
Domain structure and interactions in cyclic nucleotide phosphodiesterases: An atomic view of PDE regulation
Jayvardhan Pandit, Pfizer Global R&D, Groton Labs.
Novel insights into the mechanism of action of beta-adrenergic antagonists: Modulation of PDE4-beta-adrenergic receptor complexes
Wito Richter, UCSF
Phosphodiesterases and cyclic nucleotide compartments in the regulation of cardiac function
Rodolphe Fischmeister, Univ. de Paris-Sud XI, France
PDE inhibitors and the treatment of airway inflammation
Clive Page, King’s College, London
Post translation regulation of PDE10 and the implication in their physiological role in the CNS and in drug discovery
Nicholas Brandon, AstraZeneca, Cambridge
Correlating structure and function of drug metabolizing enzymes: An ongoing challenge
Boston Convention Center, Room 107C
9:30 AM – Noon
Sponsored by the Divisions for Drug Metabolism & Toxicology
Chairs: Emily Scott, Univ. of Kansas and Eric Johnson, Scripps Res. Inst.
The diversity and
flexibility of many of the active sites of human drug metabolizing
enzymes with different ligands makes correlations between structure and
function an ongoing challenge. The design of specific inhibitors of
certain cytochrome P450 enzymes requires knowledge of the enzyme
structure and the ability to integrate biophysical and computational
approaches to understand function. This symposium will explore the ways
that cytochrome P450 enzymes are being used as drug targets by exploring
the use of traditional (NMR) and newer (structure-based ADMET) methods
to predict metabolism.
Cytochrome P450 Structure: Common themes and variations on the theme
Eric Johnson, Scripps Res. Inst.
Investigations of human cytochrome P450 enzymes with solution NMR
Emily Scott, Univ. of Kansas
Predicting ligand interactions with metabolizing enzymes: An in silico structure-based approach
Maria Miteva, Univ. Paris Diderot
Novel pharmacoenhancer cobicistat: Discovery and development of a CYP3A inhibitor
Lianhong Xu, Gilead Sci., Inc.
Physical interactions among NADPH-cytochrome P450 reductase, CYP1A2, and CYP2B4 in the endoplasmic reticulum
Junior Speaker: John Connick, LSUHSC New Orleans
Cognitive enhancers for the treatment of neuropsychiatric disorders
Boston Convention Center, Room 108
9:30 AM – Noon
Sponsored by the Divisions for
Behavioral Pharmacology; Integrative Systems, Translational and
Clinical Pharmacology; and Neuropharmacology
Chairs: Kathleen M. Kantak, Boston Univ. and Roger D. Spealman, Harvard Med. Sch.
There is a current trend of
exploring cognitive-enhancing therapeutic drugs as treatments for a
number of neuropsychiatric disorders, including Alzheimer’s disease,
schizophrenia, anxiety and drug addiction. This session will review
novel preclinical research currently being done to discover new drug
targets across a spectrum of disorders. Findings show a striking
similarity in the drug targets that have been examined across multiple
neuropsychiatric disorders and it now seems likely that the discovery of
safe and effective cognitive-enhancing therapeutic drugs for one
disorder may translate to other disorders with neurocognitive deficits.
Targets for cognitive-enhancing pharmacotherapy
Joseph G. Wettstein, F. Hoffmann-La Roche Ltd.
Translational approaches to cognitive enhancing drugs for neuropsychiatric disorders
Trevor W. Robbins, Univ. of Cambridge
Novel cholinergic-based therapeutic strategies for Alzheimer’s disease and age-related memory decline
Alvin V. Terry, Georgia Hlth. Sci. Univ.
Therapeutic uses of cognitive enhancers in rat and monkey models of drug addiction
Bríd Á Nic Dhonnchadha, Boston Univ.
Neuroplasticity in rodent models of fear extinction and use of cognitive enhancers
Gary B. Kaplan, VA Boston Healthcare System
Summary and discussion
Kathleen M. Kantak, Boston Univ. and Roger D. Spealman, Harvard Med. Sch.
Emerging technologies for delivering neurotherapeutics across the blood-brain barrier
Boston Convention Center, Room 109A
9:30 AM – Noon
Sponsored by the Divisions for
Integrative Systems, Translational and Clinical Pharmacology;
Cardiovascular Pharmacology; Drug Discovery and Development; and
Neuropharmacology
Chairs: Nisha Nanaware-Kharade, Univ. of Arkansas for Med. Sci. and Eric C. Peterson, Univ. of Arkansas for Med. Sci.
The blood brain barrier is
vital for CNS homeostasis and the preservation of neuronal integrity. It
also plays a role in the pathology and progression of a broad spectrum
of CNS disorders, including Alzheimer’s disease, ALS, Parkinson’s
disease as well as presenting a challenging barrier to delivering drugs
into the CNS. This symposium will highlight some of the new technologies
developed for delivering drugs across the BBB, including neurosurgical
techniques, chemical-based strategies that modify the physicochemical
properties of the drug, and biotechnology-based strategies which “trick”
the endogenous BBB transporters.
Blood-brain barrier modeling for therapeutic screening purposes
Eric Shusta, Univ. of Wisconsin-Madison
Principles for targeting tight junction proteins and functions
Maria Balda, Univ. Col. London, Inst. of Ophthalmology
Intranasal drugs, biopharmaceuticals and stem cells bypass the blood-brain barrier to treat Alzheimer’s, Parkinson’s, stroke, brain tumors, PTSD, TBI and other CNS disorders
Willam H. Frey, Regions Hosp.
Gene delivery across the blood brain barrier for treating neurological disorders
Brian Kaspar, Nationwide Children's Hosp.
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JULIUS AXELROD AWARD LECTURE
Boston Convention Center, Room 107AB
2:00 PM – 2:50 PM
Gavril W. Pasternak, Memorial Sloan-Kettering Cancer Center
No pain, big gain: Truncated mu opioid receptor splice variants as drug targets
Introduction: Kim Neve, VA Med. Ctr.
JULIUS AXELROD SYMPOSIUM: Expanding the repertoire of G-protein coupled opioid receptor targets
Supported by the John V. Croker Fund
Boston Convention Center, Room 107AB
3:00 PM – 5:30 PM
Chair: Gavril W. Pasternak, Memorial Sloan-Kettering Cancer Center
Alternative pre-RNA splicing of the mu opioid receptor gene: Insight into complex mu opioid actions
Ying-Xian Pan, Memorial Sloan-Kettering Cancer Center
Opioid receptor heteromers: New pharmacology and new therapeutic possibilities
Lakshmi A. Devi, Mount Sinai Sch. of Med.
Biased agonism and trafficking: Discriminating opioid drug actions by receptor endocytosis
Mark Von Zastrow, UCSF
The genetics of opioid analgesia
Jeffrey Mogil, McGill Univ.
Translating pharmacology into career choices in the pharmaceutical and biotechnology industry
Boston Convention Center, Room 106
3:00 PM – 5:30 PM
Sponsored by the Divisions for
Pharmacology Education; Drug Discovery and Development; and Integrative
Systems, Translational and Clinical Pharmacology
Chairs: Janet Clark, Drexel Univ. Col. of Med. and other chair TBD
The integration of
pharmacology into the complex fabric of drug discovery and development
emphasizes just how critical the discipline is to evaluating a compound,
assessing its therapeutic potential, evaluating liabilities and then
integrating all of this into making a decision about progression into
humans. Leading pharmacologists in the various specialty areas of
expertise that contribute to the drug discovery and development process
will discuss how their pharmacological specialties contribute to the
process and share how they determined their career paths.
Educational initiatives in pharmacology for a career in the pharmaceutical or biotechnology industry
James Barrett, Drexel Univ. Col. of Med.
Pharmacology in target identification and validation
Peter Hutson, Shire Pharmaceut.
Pharmacogenetics in drug discovery and development
David Stone, Merck Res. Labs.
Pharmacoepidemiology: Studying drugs in populations
Sean Hennessy, Perelman Sch. of Med. at the Univ. of Pennsylvania
Clinical pharmacology and the development of drugs
Darrell Abernethy, FDA, Annapolis
Epigenetic control of drug metabolism and transport
Boston Convention Center, Room 107C
3:00 PM – 5:30 PM
Sponsored by the Divisions for
Drug Metabolism; Drug Discovery and Development; Integrative Systems,
Translational and Clinical Pharmacology; Molecular Pharmacology; and
Toxicology
Chairs: Aiming Yu, Univ. at Buffalo, SUNY and Yoichi Osawa, Univ. of Michigan
The importance of genetic
factors in the control of drug metabolism is well recognized; however
there is also increasing evidence that drug-metabolizing enzymes and
transporters are regulated by epigenetic factors such as DNA
methylation, histone modification, and noncoding RNA mechanisms. This
session will introduce new findings on epigenetic regulatory mechanisms
in drug metabolism and transport and the impact of epigenetic factors on
the pharmacological and toxicological effects of drugs and their
implications in therapy.
Overview of genetic and epigenetic mechanisms underlying variable drug metabolism and drug response
Magnus Ingelman-Sundberg, Karolinska Inst., Stockholm
Chromatin modification in control of drug metabolism during liver development
Xiaobo Zhong, Univ. of Connecticut Sch. of Med.
Role of epigenetic mechanisms in differential regulation of the dioxin-inducible CYP1A1 and CYP1B1 genes
Oliver Hankinson, UCLA David Geffen Sch. of Med.
Noncoding RNAs in post-transcriptional control of drug metabolism and transport
Aiming Yu, Univ. at Buffalo, SUNY
Long noncoding RNAs and transcription of cytochrome P450s in mouse liver during maturation
Junior Speaker: Lai Peng, Univ. of Connecticut
Innate immunity and cardiovascular disease: Unfolding the therapeutic potential of toll-like receptors
Boston Convention Center, Room 108
3:00 PM – 5:30 PM
Sponsored by the Divisions for Cardiovascular Pharmacology & Integrative Systems, Translational and Clinical Pharmacology
Chairs: R. Clinton Webb, Georgia Hlth. Sci. Univ. and Styliana Goulopoulou, Georgia Hlth. Sci. Univ.
Toll-like receptors (TLRs)
are pattern recognition receptors that activate the innate immune
response. In addition to exogenous infections ligands, TLRs sense
certain endogenous molecules that are released during host tissue
injury/death. Activation of TLRs leads to the activation of NF-kB and
the production of pro-inflammatory cytokines that may have both
beneficial (repair) and detrimental (Inflammation) effects on the host.
TLRs are expressed not only in immune cells but also in cardiac and
vascular tissue, suggesting that TLRs may be a link between innate
immunity, inflammation, and cardiovascular disease. This session will
address newly discovered TLR-associated molecular pathways that are
involved in the genesis of endothelial dysfunction and cardiovascular
remodeling characterizing various cardiovascular pathologies. The
therapeutic potential of TLR manipulation will be discussed.
Danger, tissue injury and immunity
Polly Matzinger, NIAID, NIH
Toll-like receptors in gestational hypertension
Brett Mitchell, Texas A&M Hlth. Sci. Ctr.
The impact of sex on innate and adaptive immunity in hypertension
Jennifer C. Sullivan, Georgia Regents University
Toll-like receptors: Therapeutic targets in cardiovascular disease?
Claudia Monaco, Imperial Col. London
The influence of methadone on toll-like receptor 4 and human mu opioid receptor expression
Junior Speaker: Summer Dodson, Oklahoma State Univ.
Chronic Toll-like receptor 9 activation mediates heightened vascular contractility via attenuated NOS activity in isolated aortic segments
Junior Speaker: Cameron McCarthy, Georgia Hlth. Scie. Univ.
Testosterone induces activation of the extrinsic apoptotic pathway in VSMC by mechanisms involving ROS generation
Junior Speaker: Rheure Lopes, Univ. of Sao Paulo
Therapeutic approaches for erectile dysfunction (ED) and benign prostatic hyperplasia (BPH): Present & future
Boston Convention Center, Room 109A
3:00 PM – 5:30 PM
Sponsored by the British Pharmacological Society; and the ASPET Divisions for Cardiovascular Pharmacology; Drug Discovery and Development; and Integrative Systems, Translational and Clinical Pharmacology
Chair: Selim Cellek, Cranfield Univ., Bedfordshire
Despite the successful pharmacological agents such as PDE5 inhibitors, alpha blockers and 5-alpha reductase inhibitors, erectile dysfunction and benign prostatic hyperplasia remain difficult-to-treat diseases. The aim of this symposium will be to provide an evidence-based overview of the novel pharmacological agents, stem cell, and gene therapy approaches that have recently been developed for the two diseases. In addition, the session will open a debate on the use of PDE5 inhibitors in both erectile dysfunction and benign prostatic hyperplasia as well as their use for other indications.
Pathophysiological link between ED and BPH
Selim Cellek, Cranfield Univ., Bedfordshire
Soluble guanylate cyclase activators for ED
Peter Sandner, Bayer HealthCare AG, Wuppertal
PDE5 inhibitors for treatment of BPH
Arthur Burnett, Johns Hopkins Hosp.
Novel therapeutic approaches to ED and BPH
Michael O’Leary, Harvard Med. Sch.
Use of PDE5 inhibitors in indications other than ED and BPH
Ian Eardley, Leeds Royal Infirmary
Student/Postdoc Best Abstract Competition
Westin Boston Waterfront, Grand Ballroom AB
6:30 PM – 8:30 PM
ASPET/BPS Student & Postdoc Mixer
Westin Boston Waterfront, Harbor Ballroom I
9:00 PM – 11:30 PM
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JOHN J. ABEL AWARD LECTURE
Boston Convention Center, Room 107C
8:30 AM – 9:20 AM
Arthur Christopoulos, Monash Univ.
Reciprocal relationships: The yin and yang of GPCR allostery
Introduction: Stephen Lanier, Med. Univ. of South Carolina
Advancing discoveries from the academic laboratory to the market
Boston Convention Center, Room 106
9:30 AM – Noon
Sponsored by the Divisions for Drug Discovery and Development & Pharmacology Education
Chair: Robert Leadley, Schoolcraft Col.
As pharmaceutical companies
continue to merge and downsize their basic research efforts in many
therapeutic areas, there is an increasing need and interest for academic
investigators to think entrepreneurially about their discoveries. This
symposium will help guide investigators through the various steps
leading to commercialization of their research by covering topics such
as intellectual property protection, private and public funding
opportunities, regulatory requirements, and the steps required to move a
discovery out of the lab and into the marketplace.
Intellectual property protection: What, when, and how to protect and share your discovery
Weston Gould
Regulatory hurdles from bench to bedside
Ronald L. Dundore, InfaCare Pharmaceut. Corp.
What to know when working with Technology Transfer Offices
Ronald J. Shebuski, Cardiovascular Research Consulting, LLC
Licensing: Do you have what they really want?
Chris Vlahos, Lilly Res. Labs.
Novel dynamics of cAMP: Towards new therapeutic interventions through compartmentalized signaling networks
Boston Convention Center, Room 107AB
9:30 AM – Noon
Sponsored by the British Pharmacological Society and the ASPET Division for Molecular Pharmacology
Chair: Martina Schmidt, Univ. of Groningen and Marc Peters-Golden, Univ. of Michigan Med. Sch.
The discovery of cAMP
transformed the understanding of cellular regulation by providing not
only the second messenger concept, but also the discovery of G proteins,
G protein-coupled receptors (GPCRs), and the conceptual roots of
compartmentalized signaling. Spatiotemporal dynamics in the subcellular
distribution of cAMP signaling networks likely determine the net
outcome of cAMP in chronic disorders. This session will explore the
spatiotemporal dynamics of compartmentalized cAMP signaling and the
roles of adenylyl cyclases, A-kinase anchoring proteins, G
protein-coupled receptors, and protein kinase A as possible drug
discovery targets.
Cyclic nucleotide signaling in subcellular compartments
Manuela Zaccolo, Univ. of Oxford, Balliol Col.
Adenylyl cyclase as orchestrators of cAMP microdomains
Dermot M.F. Cooper, Univ. of Cambridge
Cell signalling in space and time
John. D. Scott, Univ. of Washington
Higher order protein complexes and phospholipid interactions in GPCR signaling
John Tesmer, Univ. of Michigan
Dysregulation of cAMP networks in fibrotic lung disease
Marc Peters-Golden, Univ. of Michigan Med. Sch.
Developing Pharmacological Probes Targeting exchange protein directly activated by cAMP
Junior Speaker: Xiaodong Cheng, Univ. of Texas Medical Branch
Modulation of the cAMP pathway by Pseudomonas aeruginosa quorum sensing molecules
Junior Speaker: Leigh Stoddart, Univ. of Nottingham Med. Sch.
New kids on the block: Organic cation transporters and plasma membrane monoamine transporter in neurodegenerative, psychiatric and addictive disorders
Boston Convention Center, Room 107C
9:30 AM – Noon
Sponsored by the Divisions for Neuropharmacology; Drug Metabolism; Integrative Systems, Translational and Clinical Pharmacology; Molecular Pharmacology; and Toxicology
Chair: Lynnette C. Daws, Univ. of Texas Hlth. Sci. Ctr. at San Antonio
In addition to the traditional high affinity transporters for biogenic amines which are the targets for many CNS drugs, organic cation transporters and plasma membrane monoamine transporters have been recently discovered to transport biogenic amines in the brain as well. This symposium will address the significant role of these “newer” transporters in regulation of biogenic amine neurotransmission as it relates to their
1) distribution and cellular location in brain;
2) ability to transport biogenic amines, even in the presence of the high-affinity transporters for these neurotransmitters;
3) neuroprotective actions;
4) sensitivity to regulation by corticosterone and stress and implications for drug abuse and psychiatric disease; and
5) potential as targets for the development of improved therapeutics to treat psychiatric, addictive and neurodegenerative disorders.
Plasma membrane monoamine transporter: Structure, function, and therapeutic potential for mental illness
Joanne Wang, Univ. of Washington
Neurotoxicity in animal models of Parkinson’s disease is mediated by the organic cation transporter-3
Kim Tieu, Plymouth Univ., Peninsula Sch. of Med. and Dent.
Organic cation transporters and the plasma membrane monoamine transporter: Uncovering novel targets to treat depression
Lynette C. Daws, Univ. of Texas Hlth. Sci. Ctr. at San Antonio
Role of organic cation transporter-3 in stress effects on cocaine reinstatement
Paul J. Gasser, Marquette Univ.
Impaired monoamine and organic cation uptake in choroid plexus in mice with targeted disruption of the plasma membrane monoamine transporter (Slc29a4) gene
Junior Speaker: Haichuan Duan, Univ. of Washington
Role of the coagulation cascade in tissue injury and disease
Boston Convention Center, Room 108
9:30 AM – Noon
Sponsored by the Divisions for Toxicology & Integrative Systems, Translational and Clinical Pharmacology
Chair: James P. Luyendyk, Michigan State Univ.
The coagulation cascade comprises a highly regulated network of serine proteases terminating in the generation of the enzyme thrombin. Exposures spanning hepatotoxic drugs to inhaled particles have been shown to cause activation of the coagulation cascade, and coagulation cascade activation is now believed to not merely be the consequence of tissue injury, but a critical mechanism of disease progression and toxicological response. This session will explore various components of the coagulation cascade and the role they play in staph infection, ischemia/reperfusion kidney injury, nephrotoxicity, heart failure and liver disease.
Host prothrombin and fibrinogen are critical determinants of pathogen toxicity and host tissue damage following S. aureus infection
Matthew J. Flick, Cincinnati Children's Hosp.
Fibrinogen: A biomarker and therapeutic candidate in kidney damage
Vishal S. Vaidya, Harvard Med. Sch.
Contribution of coagulation proteases to the vascular inflammation in sickle cell disease
Rafal Pawlinski, UNC, Chapel Hill
Liver let die: Coagulation decides
James Luyendyk, Michigan State Univ.
Fatty acid activation of G protein-coupled receptors: Basic and clinical perspectives
Boston Convention Center, Room 109A
9:30 AM – Noon
ASPET gratefully acknowledges the educational grants from the Institut de Recherches Servier and Janssen Research & Development, LLC for supporting this symposium.
Sponsored by the ASPET Division for Molecular Pharmacology
Chairs: Graeme Milligan, Univ. of Glasgow and Celia Briscoe, Janssen
This session will review
what is known about the expression, function and regulation of members
of the G protein-coupled receptor family shown to be receptors for free
fatty acids. The speakers will also address the pharmacology and mode of
binding, both orthosteric and allosteric, of selected ligands, the
state of validation of each receptor as a potential therapeutic target
and the progress to date of translating the basic molecular knowledge of
these receptors into clinically useful drugs.
Overview of the free fatty acid receptor family and the enigma of GPR120
Celia Briscoe, Janssen
Developing novel ligands for free fatty acid receptors
Graeme Milligan, Univ. of Glasgow
GPR40 as a potential target for the treatment of type 2 diabetes
Vincent Poitout, Univ. of Montreal
GLPG0974, a selective FFA2 antagonist: a promising approach for treatment of neutrophil driven disorders?
Johan Beetens, Galapagos NV
Phosphorylation and internalization of short splicing variant of the omega 3 fatty acid sensor, GPR120
Junior Speaker: Omar Sanchez-Reyes, Universidad Nacional Autónoma de México
Canadian Society for Pharmacology & Therapeutics (CSPT) Trainee Oral Presentations
Boston Convention Center, Room 109B
9:30 AM – 12:00 PM
Chair: Fiona Parkinson, CSPT
Introduction
Fiona Parkinson, CSPT
Pharmacogenomics of vincristine-induced neurotoxicity in pediatric cancer patients
Ursula Amstutz, Univ.of British Columbia
Characterization of the vascular phenotype of the equilibrative nucleoside transporter 1 knockout mouse
K. Arielle Best, Western Univ.
Genetic and clinical determinants of CYP3A4 activity in patients using 4ß- hydroxycholesterol as an in vivo probe
Inna Ying Gong, Western Univ.
Tricyclic compounds inhibit the OATP1A2 transporter
Jennifer Lu, Univ. of Montreal
Therapeutic use of eNOS/Caveolin-1 antagonistic peptides for endothelial dysfunction and atherogenesis
Arpeeta Sharma, Univ. of British Columbia
Pharmacogenetics of warfarin safety and effectiveness in children
Kaitlyn Shaw, Univ. of British Columbia
Decreased nuclear receptor activity mediates downregulation of drug metabolizing enzymes in chronic kidney disease through epigenetic modulation
Thomas Velenosi, Western Univ.
Surgery-induced inflammation reduces morphine distribution into cerebrospinal fluid
Yan Wang, Dalhousie Univ.
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CANADIAN SOCIETY FOR PHARMACOLOGY AND THERAPEUTICS AWARD RECIPIENT LECTURES
Boston Convention Center, Room 109B
1:30 PM – 4:30 PM
Chair: Fiona Parkinson, CSPT
Senior Investigator Award Recipient
Rachel Tyndale, Univ. of Toronto, Toronto
Piafsky Young Investigator Award Recipient
Bernard Le Foll, Univ. of Toronto, Toronto
Distinguished Service and Education Award
Jean Gray, Halifax, Nova Scotia
2 "Isoherranen")
DRUG METABOLISM DIVISION EARLY CAREER ACHIEVEMENT AWARD LECTURE
Boston Convention Center, Room 108
2:00 PM – 2:50 PM
Nina Isoherranen, Univ. of Washington
The biochemistry and clinical significance of CYP26 enzymes in regulating retinoic acid homeostasis
Introduction: Ken Thummel, Univ. of Washington
Drug Metabolism Division James Gillette Award & Platform Session
Boston Convention Center, Room 108
3:00 PM – 5:30 PM
Impact of development and genetic variation on human hepatic CYP2B6 expression and activity
Andrea Gaedigk, Children's Mercy Hospital & Clinics
Differences in the catalytic properties of CYP2B6s between common marmoset and human
Shizuo Narimatsu, Okayama Univ
The effect of obesity and development on in vitro hepatic metabolism
Gina Danielson, Univ. of Minnesota
Transport by OATP1B1 and OATP1B3 enhances cytotoxicity of EGCG and certain substituted quercetins
Yuchen Zhang, Univ. of Kansas Med. Ctr.
Evidence for epigenetic regulation of UGT1A1 protein expression and activity in healthy human livers
Umit Yasar, Tufts Univ. Sch. of Med.
Active site gating controls substrate selectivity in cytosolic sulfotransferases A and spinophilin
Ian Cook, Albert Einstein Col. of Med.
James Gillette Best Paper Award:
The Role of FcRn in the disposition, metabolism and pharmacokinetics of soluble non-crosslinking immune complexes
Hamsell Alvarez, Merck Res. Labs.
James Gillette Best Paper Award:
Vitamin D receptor activation enhances Benzo[a]pyrene metabolism via CYP1A1 expression in macrophages
Presenting Author: Shigeyuki Uno Nihon Univ. Sch. of Med.
Neuropharmacology Division Postdoctoral Scientist Award Finalists
Boston Convention Center, Room 106
3:00 PM – 5:30 PM
Keynote Speaker: Lakshmi Devi, Mount Sinai Sch. of Med.
Cannabinoid 1 receptor as therapeutic target in preventing chronic epilepsy
Robert Di Maio, Univ. of Pittsburgh
Dimerization of G-protein coupled Receptors (GPCRs) in Appetite Regulation and Food Reward
Harriet Schellekens, Univ. Col. Cork Sch. of Pharmacy
GPR158 and GPR179: a subfamily of orphan GPCRs as a new class of G protein signaling modulators
Cesare Orlandi, Scripps Res. Inst.
Increased plasma ammonia concentration contributes to methamphetamine-induced blood-brain barrier damage
Nicole A. Northrop, Univ. of Toledo Col. of Med.
Amphetamine and methamphetamine differentially regulate biophysical properties of dopamine transporter
Kaustuv Saha, Univ. of Florida
Cross-talk between beta and alpha2 adrenergic receptors in sympathetic neurons relies on protein kinase A and spinophilin
Christopher M. Cottingham, Univ. of Alabama at Birmingham
Keynote Address: How to do big science on a modest budget: lessons from deorphanizing a G protein-coupled receptor
Lakshmi Devi, Mount Sinai Sch. of Med.
Molecular Pharmacology Division Postdoctoral Award Finalists
Boston Convention Center, Room 107AB
3:00 PM – 5:30 PM
Keynote Speaker: Brian Kobilka, Stanford Univ. Sch. of Med.
Identification of substituted benzazepines as functionally selective ligands of the D1dopamine receptor
Jennie Conroy, NINDS/NIH
Development of a membrane anchored chemerin receptor agonist as a novel modulator of inflammation
Jamie Doyle, Tufts Medical Center
Non-Canonical Signaling by GPCR-Arrestin-Gβγ Ternary Complexes
Vanessa Wehbi, Univ. of Pittsburgh Sch. of Med.
Keynote Address: Probing G protein coupled receptors: a few of my favorite experiments
Brian Kobilka, Stanford Univ. Sch. of Med.
Drug Discovery and Development Symposium: Gliobiology: emerging concepts in neural-glia interactions in chronic disease
Boston Convention Center, Room 107C
3:00 PM – 5:30 PM
Chair: Michael F. Jarvis, AbbVie
Reciprocal interactions between motor neurons and surrounding astrocytes in ALS
John Weiss, Univ. of California, Irvine Sch. of Med.
Spinal cord neural-glia interactions in chronic pain
Ru-Rong Ji, Duke Univ. Med. Ctr.
Regulation of myelination by action potentials and an introduction to neuron-glia interactions
R. Douglas Fields, NICHD/NIH
Regeneration-related axon and Schwann cell interactions
Doug Zochodne, Univ. of Calgary
Local Ca2+ signals in the endothelium: Key regulators of vascular function and dysfunction
Boston Convention Center, Room 109A
3:00 PM – 5:30 PM
Sponsored by the Division for Cardiovascular Pharmacology
Chairs: Mark T. Nelson, Univ. of Vermont and Sean Marrelli, Baylor Col. of Med.
Endothelial cell Ca2+ is
broadly accepted as a key regulator of endothelial cell-dependent
dilation of small arteries. Recent studies using sophisticated Ca2+
imaging techniques have shown that endothelial cells experience local
changes in Ca2+ under physiological conditions, the frequency and
nature of which determine their effect on endothelial cell function.
This session will focus on localized endothelial cell Ca2+ signals
mediated by two pathways: Ca2+ influx through Transient Receptor
Potential (TRP) channels and inositol trisphosphate (IP3)-medicated Ca2+
release from intracellular stores. Understanding these Ca2+ signaling
mechanisms in the endothelium is a critical first step in identifying
the cause for endothelial cell dysfunction in vascular disorders such as
hypertension.
Conducted vasodilation in resistance arteries: Ca2+ signaling between endothelial cells
Steven S. Segal, Univ. of Missouri
TRPA1-induced endothelial calcium signals and vasodilation
Scott Early, Colorado State Univ.
Differential regulation of SK and IK channels during endothelium dependent hyperpolarization
Kim A. Dora, Univ. of Oxford
Elementary TRPV4 Ca2+ signals regulate endothelium dependent vasodilation
Swapnil K. Sonkusare, Univ. of Vermont
Endothelial Ca2+ wavelets and myoendothelial feedback
Donald G. Welsh, Univ. of Calgary
Alteration of endothelial CaMKII in AngII-induced hypertensive mice
Junior Speaker: Chimene Charbel, Montreal Heart Inst.
Behavioral Pharmacology and Neuropharmacology Divisions Joint Mixer
Westin Boston Waterfront, Grand Ballroom D
6:00 PM – 8:00 PM
Molecular Pharmacology Division Business Meeting and Mixer
Westin Boston Waterfront, Burroughs
7:00 PM – 9:00 PM
Pharmacology Education, Drug Discovery and
Development, & Integrative Systems, Translational and Clinical
Pharmacology Divisions Joint Mixer
Westin Boston Waterfront, Carlton
7:30 PM – 9:30 PM
Y.E.S. Young Experimental Scientist Mixer
Westin Boston Waterfront, Galleria
9:00 PM – 11:00 PM
*21 & older must have ID to receive drink tickets
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WiP into Shape Networking Walk
Westin Boston Waterfront Hotel, 7:00 AM – 9:00 AM
Meet at the concierge desk.
Pharmacology Education Division Program: The future of Ph.D. education in biomedicine: U.S. and European perspectives
Westin Boston Waterfront Hotel, Grand Ballroom E; 9:30 AM – Noon
Chair: Jane A. Mitchell, Imperial Col. London
PhD training in the USA: present and future
Joey V. Barnett, Vanderbilt Univ. Med. Ctr.
PhD education in the UK: why change?
Nick J. Goulding, Barts and the London Sch. of Med. and Dentistry
Standards of PhD education: the ORPHEUS perspective
Michael Mulvany, Aarhus Univ. Graduate Sch. of Hlth. Scie., Denmark
Research funder perspective: PhD graduate attributes – future needs
Alison Hall, NIGMS/NIH
Roundtable discussion
Acetaminophen induced hepatotoxicity: Lessons learned during the last four decades investigating mechanisms of toxicity
Boston Convention Center, Room 106
9:30 AM – Noon
Sponsored by the Divisions for Toxicology; Drug Discovery and Development; Drug Metabolism; and Pharmacology Education
Chairs: José E. Manautou, Univ. of Connecticut and Hartmut Jaeschke, Univ. of Kansas Med. Ctr.
2013 marks the 40th
anniversary of the publication of the pioneering work of Brodie and
co-workers in the Journal of Pharmacology and Experimental Therapeutics
demonstrating the role of drug metabolism and protein covalent binding
in acetaminophen-induced hepatotoxicity. While this work paved the way
for toxicological investigations aimed at elucidating the mechanism of
acetaminophen toxicity, the precise mechanism of liver toxicity has
eluded investigators. This session will highlight what is known 40 years
after the initial publication of Brodie’s paper, including the role of
biotransformation, the role of mitochondria and
oxidant stress, the hepatoprotective effects of Vanin-1, the use of
acetaminophen plasma protein adducts as diagnostic markers in
acetaminophen-induced hepatotoxicity.
Acetaminophen biotransformation and reactive intermediate toxicity: How did we get here?
Steven Cohen, Massachussetts Col. of Pharm. and Hlth. Sci.
Mitochondria – oxidant stress and other signaling events associated with acetaminophen hepatotoxicity in mice and humans
Hartmut Jaeschke, Univ. of Kansas Med. Ctr.
Role of Vanin-1 in acetaminophen hepatotoxicity: Regulation of thiol homeostasis and immune response to liver injury
José E. Manautou, Univ. of Connecticut
Acetaminophen plasma protein adducts: Diagnostic markers and disease mechanisms in mice and humans
Laura James, Univ. of Arkansas for Med. Sci.
Induction of neuronal nitric oxide synthase (nNOS) in livers of mice treated with toxic doses of acetaminophen
Junior Speaker: Rakhee Agarwal, Univ. of Arkansas for Med. Sci.
A "reductionist" approach to cardiovascular disease: Inorganic nitrate to nitrite to NO
Boston Convention Center, Room 107AB
9:30 AM – Noon
Sponsored by the British Pharmacological Society
Chairs: Amrita Ahluwalia, Queen Mary Univ. and David Lefer, Emory Univ. Sch. of Med.
While previously considered
inactive oxidative metabolites of endogenous nitric oxide (NO)
synthesis, inorganic nitrate and nitrite are now known to be reduced
back to NO to provide an alternative source of NO under certain
conditions. There is growing evidence that this pathway can act as a
rescue pathway in situations where the normal healthy endogenous
synthesis of NO has been compromised. This session will discuss the therapeutic potential of this pathway and the clinical studies
that have translated much of the basic science into therapeutics.
Inorganic nitrite-a metabolite with a mission!
Mark Gladwin, Vascular Medicine Inst.
Nitrite therapy in heart failure: Mechanisms and therapeutic potential
David Lefer, Emory Univ. Sch. of Med.
The red blood cell nitrite reductase: A therapeutic target in hypertension
Amrita Ahluwalia, Queen Mary Univ. of London
Dietary nitrate/nitrite and pulmonary hypertension
Reshma Baliga, Barts & The London Med. Sch., London
Purinergic transmission in visceral function and sensation
Boston Convention Center, Room 107C
9:30 AM – Noon
Sponsored by the Divisions for Integrative Systems, Translational and Clinical Pharmacology & Molecular Pharmacology
Chairs: James J. Galligan, Michigan State Univ., Hamid Akbarali, Virginia Commonwealth Univ.
Purines are primary neurotransmitters controlling GI motility, secretion and blood flow as well as contributing to control of bladder sensation and function. They also play an important role in visceral sensation and pain mechanisms. This session explores in detail the various aspects of purine function with a focus on the development of new therapeutic approaches to modulating purine mechanisms as a strategy to treat GI and bladder functional disorders.
Multiple purinergic neurotransmitters in the abdominal viscera
Violeta Mutafova-Yambolieva, Univ. of Nevada
Purinergic control of gastrointestinal secretion
Fivos Christofi, Ohio State Univ.
Purinergic synaptic transmission in the enteric nervous system and control of gut motility
James J. Galligan, Michigan State Univ.
Purinergic signaling in visceral pain mechanisms
Christopher Keating, Univ. of Sheffield
Voltage-gated ion channel blockers as potential analgesic agents
Boston Convention Center, Room 108
9:30 AM – Noon
Sponsored by the Divisions for Drug Discovery and Development & Neuropharmacology
Chair: Michael F. Jarvis, AbbVie
Voltage-gated ion channels play an integral role in the regulation of membrane ion conductance, neurotransmitter release, and cellular excitability in neurons. Several nonselective sodium channel blocking drugs have reduced chronic pain in human trials. Recently discovered gain and loss of function mutations of one particular sodium channel isoform implicate this channel as a modulator of nociceptive sensitivity. Inhibition of low- voltage activated (T-type) and high-voltage active (N type) calcium channels leads to analgesia through modulation of neuronal membrane excitability and neurotransmitter release. These results will be discussed in the context of developing new small molecule channel modulators as potential analgesic agents lacking the addictive and analgesic tolerance potential of opioids.
Structure and function of voltage-gated sodium channels at atomic level
William A. Catterall, Univ. of Washington
Chasing men on fire: Sodium channels and pain
Steve Waxman, Yale Univ. Sch. of Med.
Novel means of targeting T-type calcium channels to treat pain
Gerald Zamponi, Univ. of Calgary
Antinociceptive pharmacology of small molecule sodium channel blockers
Michael F. Jarvis, Abbott Labs.
Discovery and early clinical development of potent and selective small molecule Cav2.2 calcium channel blockers
Simon Tate, Convergence Pharmaceut.
Transcription factors as therapeutic drug targets
Boston Convention Center, Room 109A
9:30 AM – Noon
Sponsored by the Divisions for Molecular Pharmacology; Drug Discovery and Development; and Toxicology
Chairs: Theresa M. Filtz, Oregon State Univ. Col. of Pharmacy and Mark Leid, Oregon State Univ. Col. of Pharmacy
Transcription factors are the proximal regulators of gene expression that control the nature of a cell — what type of cell it is, what it can become, how it responds — as well as the regulators of aberrant responses, growth and proliferation in diseases as varying as neoplastic transformation to cardiac hypertrophy to insulin resistance. Targeting transcription factors in disease should provide a highly selective means to manipulate cell response, function, growth and proliferation, but in general, transcription factors are considered to be difficult drug targets. The discovery that nuclear hormone receptors respond to endogenous small molecules has led to the realization that it might be possible to target transcription factors with small molecules. This session explores varying approaches in interrupting or mimicking the protein-protein and protein-DNA interactions that underlie the basic activity of transcription factor proteins.
Regulating the regulators: Transcription factor control by post-translational modification
Mark Leid, Oregon State Univ.
Activation of p53 tumor suppression by MDM2 antagonists
Lyubomir T. Vassilev, Hoffmann-La Roche, Inc.
Small molecule transcriptional modulators: Structure and mechanism
Anna Mapp, Univ. of Michigan
Synthetic strategies for targeting protein-protein interactions
Paramjit Arora, New York Univ.
Therapeutic applications of zinc finger nucleases
Edward Rebar, Sangamo BioSciences, Inc.
Canadian Society for Pharmacology & Therapeutics (CSPT): Practical Pharmacology
Boston Convention Center, Room 109B
9:30 AM – 11:30 AM
Chair: Richard B. Kim
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CSPT: Women and Pregnancy: Safety, Efficacy, Ethics and Research Needs in Pharmacology
Boston Convention Center, Room 109B
1:00 PM – 5:00 PM
Chair: David Knoppert, Children's Hlth. Res.Inst., London, Ont.
Opening remarks
David Knoppert, Children's Hlth. Res.Inst., London, Ont.
Pharmacokinetics and gender differences
Donald R. Mattison, Risk Sci. Intl.
Impact of Pregnancy on maternal pharmacokinetics of medications
Mary F. Hébert, Univ. of Washington
Pharmacokinetics and Bioequivalence – evaluating the risks
Gideon Koren, Univ. of Toronto
Gender barriers in policy and regulation
Martha Nolan, Society for Women’s Hlth. Res.
Removing risks to prescribing in pregnancy: next steps in research and regulation. Panel discussion
Moderated by Donald R. Mattison, Risk Sci. Intl.
Closing remarks
David Knoppert, Children's Hlth. Res.Inst., London, Ont.
Cardiovascular Pharmacology Division Trainee Showcase
Boston Convention Center, Room 107AB
2:30 PM – 4:30 PM
Sestrin2 is cardioprotective against ischemia/reperfusion injury by promoting LKB1-mediated AMPK activation
Alexander Morrison-Nozik, Univ. at Buffalo (SUNY)
Pregnane X receptor mediates dyslipidemia Induced by the HIV protease inhibitor amprenavir in mice
Robert Helsley, Univ. of Kentucky
Heterogeneity of ATP-sensitive K+ channels in cardiac myocytes: Enrichment at the intercalated disk
Miyoun Hong, New York Univ. Sch. of Med.
Genetic deletion of the TRPC3 channel blunts the development of angiotensin II-induced hypertension in mice
Asif Pathan, Univ. of Arkansas for Med. Sciences
Angiotensin II receptor blockade, but not ACE inhibition, reduces nocturnal hypertesion and natriuresis in autonomic failure patients with low renin activity
Amy Arnold, Vanderbilt Univ.
Aged eNOS-/- mice display increased APP expression, microglial activation, and impaired spatial memory
Susan Austin, Mayo Clinic
BENEDICT R. LUCCHESI DISTINGUISHED AWARD LECTURE IN CARDIAC PHARMACOLOGY
Boston Convention Center, Room 107AB
4:30 PM – 5:30 PM
Note: There has been a change in speakers.
Benedict R. Lucchesi, University of Michigan
Reperfusion injury: Can it be prevented?
Introduction: Nancy Rusch, Univ. of Arkansas for Med. Sci.
Negative symptoms of schizophrenia: Neuronal circuit, translation and future directions
Boston Convention Center, Room 106
3:00 PM – 5:30 PM
Sponsored by the Divisions for Drug Discovery and Development; Behavioral Pharmacology; and Neuropharmacology
Chairs: Ruggero Galici, Bristol-Myers Squibb and Leslie Jacobsen, Bristol-Myers Squibb
Negative symptoms are a primary cause of disability in schizophrenia, comprising restricted affect, lack of motivation and asociality. These diverse symptoms are not fully explained by the current understanding of the pathophysiology of schizophrenia. This session will bring together preclinical and clinical scientists to summarize the current knowledge on negative symptoms of schizophrenia and to discuss promising treatments and future directors for translational assays and model development.
Negative symptoms: Clinical features and prospects for treatment
Brian Kirkpatrick, Scott & White Healthcare
Emotion and motivation deficits in schizophrenia: The behavioral and neural substrates of negative symptom
Ann Kring, Univ. of California, Berkeley
Pharmacotherapies for negative symptoms of schizophrenia
Leslie Jacobsen, Bristol-Myers Squibb
Modeling negative symptoms of schizophrenia in animals
Athina Markou, UCSD
Integrative Systems, Translational and Clinical Pharmacology Division Hot Topics: A (r)evolution in drug discovery & therapy: From organs on a chip and 3D biomimetics to regenerative pharmacology
Boston Convention Center, Room 107C
3:00 PM – 5:30 PM
Chairs: George J. Christ, Wake Forest Sch. of Med. and Sitta Sittampalam, NIH Ctr. for Translational Therapeutics
Rapid fabrication of architecturally-correct human tissues in vitro by 3D bioprinting: Function follows form
Sharon Presnell, Organovo Inc.
Microscale engineering of tissues and organs
Linda Griffin, MIT
Human Organs-on-Chips
Anthony Bahinski, Harvard Univ.
Silk: A multifunctional biomaterial with applications for controlled
drug delivery, tissue repair and engineering 3D tissues
D. Kaplan, Tufts Univ.
Toxicology Division Symposium: The mitochondrion as a toxicological and pharmacological target
Boston Convention Center, Room 108
3:00 PM – 5:30 PM
Chair: Rick G. Schnellmann, Med. Univ. of South Carolina
New methods to identify changes in mitochondrial function
Craig C. Beeson, Med. Univ. of South Carolina
MitoQ and prevention of mitochondrial dysfunction
Victor Darley-Usmar, Univ. of Alabama, Birmingham
Mitochondrial etiology of Alzheimer’s and Parkinson’s disease
Douglas C. Wallace, Children’s Hosp. of Pennsylvania
Drugs that target mitochondrial biogenesis accelerate the recovery of cellular and organ function
Rick G. Schnellmann, Med. Univ. of South Carolina
Behavioral Pharmacology Division Symposium: The opioid-cannabinoid connection: A translational, behavioral perspective
Boston Convention Center, Room 109A
3:00 PM – 5:30 PM
Chairs: Margaret Haney, Columbia Univ. Col. of Physicians and Surgeons and Ziva D. Cooper, Columbia Univ. Col. of Physicians and Surgeons
The endogenous cannabinoid system: an emerging target to treat opioid and cannabinoid dependence
Aron H. Lichtman, Virginia Commonwealth Univ.
Pharmacological and neurobiological studies investigating opioid and endocannabinioid interactions in rodent models of stress-induced analgesia
David Finn, Natl. Univ. of Ireland, Galway
Pharmacological evidence for opioid modulation of the reinforcing effects of CB1 receptor agonists in non-human primates
Zuzana Justinova, NIDA, IRP, NIH
Naltrexone alters marijuana’s analgesic and intoxicating effects in daily marijuana smokers
Ziva D. Cooper, Columbia Univ. Col. of Physicians and Surgeons
The potential clinical efficacy of cannabinoid agonists in treating opioid-dependent patients
Adam Bisaga, NYS Psychiatric Inst.
Cardiovascular Pharmacology Division Mixer
Westin Boston Waterfront, Grand Ballroom D
6:00 PM – 8:00 PM
Drug Metabolism and Toxicology Divisions Joint Mixer
Westin Boston Waterfront, Commonwealth Ballroom A
7:00 PM – 9:00 PM
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NORMAN WEINER LECTURE
Boston Convention Center, Room 107C
8:30 AM – 9:20 AM
David E. Clapham, Boston Children’s Hospital, HHMI, Harvard Med. Sch.
Novel ion channels and their regulation
Introduction: Michael Wood, AstraZeneca Pharmaceuticals
Apolipoprotein E: A protein at the intersection of vascular and neurodegenerative disease biology
Boston Convention Center, Room 106
9:30 AM – Noon
Sponsored by the Divisions for Neuropharmacology & Cardiovascular Pharmacology
Chairs: Cheryl Wellington, Univ. of British Columbia and Michael Wood, AstraZeneca Pharmaceuticals
Apolipoprotein E (ApoE)
isoform variability has been identified as an important risk factor of
Alzheimer’s disease and as well as shown to influence the risk of
cardiovascular disease. ApoE is a multifunctional and polymorphic
protein synthesized and secreted by liver, brain, and tissue
macrophages. The molecular mechanisms underlying ApoE as a risk factor
for disease remain largely unknown. This program will examine evidence
for potential ApoE involvement in several disease settings, including
atherosclerosis, restenosis, Alzheimer’s disease, and traumatic brain
injury. A roundtable discussion will conclude the session by examining
how the current knowledge of ApoE disease biology can be exploited in
the search for new drugs to treat these disorders.
Molecular basis for differential effects of apolipoprotein E isoforms on lipoprotein metabolism
Michael C. Phillips, Univ. of Pennsylvania Sch. of Med.
Vascular contributions to the pathogenesis of Alzheimer’s disease
Richard Mayeux, Columbia Univ. Med. Ctr.
ApoE isoform-specific ApoE/Aß complex levels: potential mechanism(s) for AD risk, novel AD biomarker and therapeutic target
Mary Jo LaDu, Univ. of Illinois at Chicago
From concussion to dementia: A key role for apolipoprotein E in the central nervous system
Cheryl Wellington, Univ. of British Columbia
Roundtable Discussion
Michael Wood, AstraZeneca Pharmaceuticals
The 5-HT2C receptor: A new target for multiple therapeutics
Boston Convention Center, Room 109B
9:30 AM – Noon
Sponsored by the British Pharmacological Society and the ASPET Divisions for Molecular Pharmacology & Neuropharmacology
Chair: Lora Heisler, Univ. of Cambridge
The 5-HT2C receptor is
implicated in a wide variety of behaviors and physiological processes
via action in the CNS. 5-HT2C receptor activation provides a tonic
influence over the release of various neurotransmitters and
neuropeptides and has been implicated in depression, anxiety,
schizophrenia, reward, glucose homeostasis, and energy balance, to name a
few. With the advent of more advanced genetic technology and more
selective 5-HT2C receptor compounds, a greater understanding of the
functional role and potential therapeutic application of the 5-HT2C
receptor has begun to be realized. This session will look at insights
into the 6-HT2C receptor, that allow for a better understanding of
their potential for the treatment of a number of prevalent conditions,
including depression, obsessive-compulsive disorder, schizophrenia, drug
addiction, obesity and type 2 diabetes.
A bioinformatics approach to 5-HT2C receptor modulation of behavioral patterns
Laurence Tecott, UCSF
The effect of Htr2c post-transcriptional modifcation on 5-HT2C receptor regulated behaviour
Anthony Isles, Cardiff Univ. Sch. of Med.
A novel treatment for obesity: The 5-HT2C receptor agonist lorcaserin
Steven Smith, Sanford-Burnham Med. Res. Inst.
5-HT2C receptor agonists: A mechanistically new target for type 2 diabetes treatment
Lora Heisler, Univ. of Cambridge
5-HT2C Receptor agonist anorectic efficacy potentiated by 5-HT1B Receptor agonist co-application; an effect mediated via augmented pro-opiomelanocortin neuron activation
Junior Speaker: Barbara Doslikova, Univ. of Cambridge
New roles for signaling by G protein beta/gamma subunits
Boston Convention Center, Room 107C
9:30 AM – Noon
Sponsored by the Divisions for Molecular Pharmacology; Cardiovascular Pharmacology; and Neuropharmacology
Chair: Alan Smrcka, Univ. of Rochester Sch. of Med.
Heterotrimeric G protein beta/gamma subunits were discovered more than 30 years ago as essential components of the GPCR signal transduction machinery. More current studies have shown that instead of (in addition to) serving a scaffolding role, these components of the GPCR complex also play an important role in downstream signaling, implying a potential role as therapeutic targets. This session will explore their potential role in development, angiogenesis, parkinsonism, inflammation, heart failure, subcellular signaling, and neural circuitry.
Pharmacological targeting of Gbg subunits: Mechanisms and outcomes
Alan Smrcka, Univ. of Rochester Sch. of Med.
Translocation of Gbetagamma subunits to subcellular compartments
N. Gautam, Washington Univ. Sch. of Med.
Distinct roles for individual G bg isoforms in neurological signaling circuits
Janet Robishaw, Weis Ctr. for Res.
Scaffolding of Gbg by WD40 repeat proteins
Songhai Chen, Univ. of Iowa
G protein betagamma subunits in regulating trafficking and assembly of signaling complexes
Terry Hébert, McGill Univ.
Pharmacological enhancement of wakefulness
Boston Convention Center, Room 107B
9:30 AM – Noon
Sponsored by the Divisions for Behavioral Pharmacology; Integrative Systems, Translational and Clinical Pharmacology; and Neuropharmacology
Chair: Jeff Witkin, Eli Lilly and Co.
This symposium will investigate the clinical need for wake promoting agents for the treatment of sleep apnea, shift work and other conditions of fatigue. Both the pharmacological mechanisms that can impact wakefulness, cognitive augmentation, and their side effects, and new pharmacological mechanisms underlying wake-promoting neurobiology will be addressed.
Introduction to wake promotion
Dale M. Edgar, Eli Lilly and Co.
Physiological control systems for wakefulness
Luis De Lecea, Stanford Univ.
Modafanil (Provigil) as a wake-promoting agent
Jeff Vaught, Former CSO/Executive VP Cephalon
Histamine H3 Receptor Inverse Agonisim
Jean-Charles Schwartz, Bioprojet
Metabotropic glutamate receptors as targets for wake promotion
Keith A. Wafford, Eli Lilly and Co.
Signals activating pancreatic stem cells and beta cell regeneration
Boston Convention Center, Room 108
9:30 AM – Noon
Sponsored by the Divisions for Integrative Systems, Translational and Clinical Pharmacology & Molecular Pharmacology
Chair: Thomas M. Wilkie, UT Southwestern Med. Ctr. at Dallas
Complex physiology drives beta cell expansion in diabetes and pregnancy. Recent discoveries demonstrate the integration of metabolic cues, neural processing and efferent signaling involved in the stimulation of beta cell expansion in diabetes. This session will explore the use of pregnancy as a model for the hormonal stimulation of beta cell expansion, hypothalamic control of islet cell function, the role of RGS proteins in the pancreas as biomarkers of beta cell expansion, and the use of stem cells as human beta cell progenitors.
Integrated pathways for type 2 diabetes from mouse genetics and genomics
Alan Attie, Univ. of Wisconsin
Small molecule screens in beta cell lines for beta cell expansion
Bridget Wagner, Broad Inst. of Harvard & MIT
hESCs and iPSCs differentiation to pancreatic endocrine lineage
Shuibing Chen, Weill Cornell Med. Col.
GPCR signaling: RGS biomarkers for pancreas development, cancer and diabetes
Thomas M. Wilkie, UT Southwestern Med. Ctr. at Dallas
Pancreatic stem and progenitor cell niche: Pancreatic organogenesis throughout life
Lola M. Reid, UNC, Chapel Hill
The pharmacology of natural products
Boston Convention Center, Room 109A
9:30 AM – Noon
Sponsored by the Divisions for Behavioral Pharmacology; Drug Discovery and Development; Drug Metabolism; Integrative Systems, Translational and Clinical Pharmacology; and Toxicology
Chairs: Craig Hopp, NCCAM, NIH and John Williamson, NCCAM, NIH
The use of natural products by the public for the treatment of illness has steadily increased. Most of these products have not been proven to be clinically efficacious. Recent studies have highlighted pathways involved in the beneficial actions of natural products, involving inflammatory, immunomodulatory, cell proliferative, and antioxidant targets, as well as assorted pharmacokinetic mechanisms. This session will highlight scientifically based studies underlying the efficacy of cranberry juice for the treatment of urinary tract infections, anti-inflammatory mechanisms of omega-3-fatty acids, the pharmacological actions of cocoa extract, the pharmacology of phytoestrogens, and the potential for using tetra-hydro-palmatine to treat drug abuse.
Cranberry: Role in prevention of bacterial adhesion
Amy Howell, Rutgers, the State Univ. of New Jersey
Novel pro-resolving mechanisms and omega-3 fatty acids
Charles Serhan, Brigham and Women’s Hosp. and Harvard Med. Sch.
Natural product's potential for drug abuse treatment
David Y.W. Lee, Harvard Med. Sch.
Pharmacological effects of cacao flavanols: From receptors to clinical endpoints
Francisco Villarreal, UCSD Sch. of Med.
Prevention of estrogen carcinogenesis by botanical dietary supplements for women's health
Judy L. Bolton, Univ. of Illinois at Chicago
Panel Discussion (Questions for Speakers and NCCAM)
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Peripheral mechanisms of opioid analgesia
Boston Convention Center, Room 106
3:00 PM – 5:30 PM
Sponsored by the Divisions for Neuropharmacology; Behavioral Pharmacology; and Molecular Pharmacology
Chair: Kelly A. Berg, Univ. of Texas Hlth. Sci. Ctr.
While opioids are a key drug
class for the treatment of pain, their CNS effects with the attendant
legal and social issues cause significant drawbacks. One approach to
eliminate these drawbacks is to target opioid receptors located on
primary sensory neurons that mediate pain neurotransmission in the
periphery. This symposium will discuss the roles of peripheral delta
opioid receptors (DOR) and kappa opioid receptors (KOR) in the molecular
mechanisms involved in pain regulation. The potential role of DOR-KOR
heteromizeration and interactions with arrestin in the mechanisms
underlying peripherally restricted opioid analgesia will be discussed.
Results from in vitro experimental strategies and
molecular/computational modeling will be integrated with ex vivo and in
vivo findings in peripheral sensory neurons to generate insight in the
significance of opioid receptors in peripheral mechanisms of opioid
analgesia.
Current status of pain therapeutics
Ken Hargreaves, Univ. of Texas Hlth. Sci. Ctr. San Antonio
Molecular determinants and thermodynamics of opioid receptor signaling
Marta Filizola, Mount Sinai Sch. of Med.
6'GNTI is a G protein-biased kappa opioid receptor agonist that inhibits arrestin recruitment
Marie-Laure Rives, Columbia Univ. Med. Ctr.
DOR-KOR heteromer-mediated signaling and antinociception in primary sensory neurons
William P. Clarke, Univ. of Texas Hlth. Sci. Ctr. San Antonio
Sleep apnea: A sleeping giant in disease pathologies
Boston Convention Center, Room 107B
3:00 PM – 5:30 PM
Sponsored by the Divisions for Integrative Systems, Translational and Clinical Pharmacology; Behavioral Pharmacology; Cardiovascular Pharmacology; and Neuropharmacology
Chairs: Issy Laher, Univ. of British Columbia and Najib Ayas, Univ. of British Columbia
Sleep apnea is a common disease that is characterized by repetitive episodes of asphyxia and is recognized as an independent risk factor for cardiovascular morbidity and mortality. This symposium will summarize the currently available information on the cardiovascular, metabolic and other consequences of sleep apnea, pharmacological and non-pharmacological management strategies for sleep apnea, and the use of different animal models to study sleep apnea.
Sleep apnea for non-experts
Najib Ayas, Univ. of British Columbia
Animal models of sleep apnea
Vsevolod Polotsky, Johns Hopkins Univ.
Sleep apnea as a risk factor for cardiovascular diseases
T. Douglas Bradley, Univ. of Toronto/Mount Sinai Hosp.
Sleep apnea and type 2 diabetes
Esra Tasali, Univ. of Chicago Med. Ctr.
Biomarkers in sleep apnea
Atul Malhotra, Brigham and Women's Hosp. and Harvard Med. Sch.
Stem cells: Pharmacology and therapeutics
Boston Convention Center, Room 108
3:00 PM – 5:30 PM
Sponsored by the British
Pharmacological Society-Young Scientists and the ASPET Divisions for
Integrative Systems, Translational and Clinical Pharmacology &
Behavioral Pharmacology
Chairs: Daniel Reed, Imperial Col. London and Jane A. Mitchell, Imperial Col. London
The application of stem
cells in pharmacology is quickly gathering momentum and pharmacology is
of great importance for the optimal use of stem cells in regenerative
medicine. This session, organized by the Young Scientists Group of the
British Pharmacological Society, will address how and why pharmacology
is important in stem cell research and vice versa. Speakers will address
how stem cells can be used in cardiovascular pharmacology and the
treatment of cardiovascular disease, the pharmacologic mobilization and
activation of endogenous stem cells and stem cell progenitors, the role
of stem cells in neuroprotection, and the use of stem cell derived cells
as model systems for screening.
Introduction to stem cells in pharmacology
Daniel Reed, Imperial Col. London
Stem cells as a platform for biotherapeutic drug safety screening
Jane A. Mitchell, Imperial Col. London
Stem cells: the future of therapy for pulmonary hypertension
Duncan J. Stewart, Ottawa Hosp. Res. Inst.
Cell based solutions for cardiovascular disease
Doris A. Taylor, Texas Heart Inst.
Microfluidic and materials approaches to determining cell fate
Armon Sharei and Janeta Zoldan, MIT
Bioinformatic analysis of microglia-neural stem cell interactions: a role for wnt5a
Junior Speaker: Maya Woodbury, Boston Univ. Sch. of Med.
Systems biology answering pharmacological questions
Boston Convention Center, Room 109A
3:00 PM – 5:30 PM
Sponsored by the Divisions for Toxicology & Integrative Systems, Translational and Clinical Pharmacology
Chairs: Rick Neubig, Univ. of Michigan and John Lazo, Univ. of Virginia Sch. of Med.
While the paradigm of one-drug-one-target has lead to important advances in therapeutics, it is becoming clear that the complex interplay of biological systems can greatly influence the response of a drug. Moreover, drugs often exploit multiple targets within an organism. A more complete understanding of all of the interacting elements of a signaling pathway, transcriptional network, or neural circuit may be necessary to accurately predict the response to a given drug. Complex biological interactions such as redundancy and feedback have important implications for both acute responses and the development of resistance. The availability of large data sets of protein structure and interactions, genomic variations, and compound actions permit a more thorough analysis of such questions. Leading researchers in this new and rapidly developing area will discuss how the use of complex systems approaches can be used to explore mechanisms of drug resistance, design novel therapeutic agents, and predict efficacy.
Systems medicine, innovation technologies and proactive P4 medicine: Transforming healthcare
Leroy Hood, Inst. for Systems Biol.
Network models in cancer pharmacology
Dana Pe’er, Columbia Univ.
Practical applications of systems biology in the pharmaceutical industry
Bruce Gomes, Novartis Inst. for BioMedical Res., Inc.
Metabolic network analysis to predict therapeutic responses
Jason Papin, Univ. of Virginia
SIR JAMES BLACK LECTURE
Boston Convention Center, Room 157ABC
2:00 PM – 2:50 PM
Robert J. Lefkowitz, Duke Univ. Med. Ctr.
Molecular mechanisms of biased agonism at 7 transmembrane receptors
Introduction: Humphrey Rang, British Pharmacological Society
Note: This lecture and session are part of a colloquium on G-Protein Coupled Receptors
which continues Wednesday evening and Thursday. While this lecture and
session are open to any EB registrant, attendance at the poster session,
dinner, and remainder of the colloquium Wednesday evening and Thursday
requires separate registration.
Colloquium Symposium:
Bridging the efficacy divide: Novel molecular insights driving biased ligand drug discovery
Boston Convention Center, Room 157ABC
3:00 PM – 5:30 PM
Chairs: Arthur Christopoulos, Monash Univ., Victoria and Robert J. Lefkowitz, Duke Univ. Med. Ctr.
Biased ligands: Developing better drugs through selective signaling at GPCRs
Jonathan Violin, Tevana Inc.
Ligand-biased signaling under the light of BRET
Michel Bouvier, Univ. of Montréal
Allosteric modulation of endogenous metabolites: Implications for on- and off-target drug action and bias
Patrick M. Sexton, Monash Univ., Victoria
Moving from biased signaling to functional (physiological) bias
Andrew Tobin, Univ of Leicester
The atypical antipsychotic clozapine induces 5-HT2AR-mediated signaling and behavioral events in a beta-arrestin2-independent but Akt-dependent manner
Junior Speaker: Cullen Schmid, The Scripps Res. Inst.
For the remainder of the G-Protein Coupled Receptors Program, click here.
ASPET Closing Reception
Boston Convention Center, Ballroom Foyer
6:00 PM – 8:00 PM
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