Saturday, April 26 - Wednesday, April 30, 2014
San Diego, CA
Give a Day of Service to San Diego at EB 2014
Since 2009, some attendees at the EB meeting have given a day of volunteer service in the local communities (New Orleans, Pasadena, Washington DC, and San Diego). Volunteer activities have ranged from home construction, to painting, cleaning, stocking, food preparation, and service. The Behavioral Pharmacology Division of ASPET will again sponsor a volunteer opportunity at EB 2014 in San Diego. On Friday, April 25, 2014, we will, for the second time, spend the day at St. Vincent de Paul Village, doing whatever we can to help the dedicated people at Father Joe’s Villages provide assistance to San Diegans. 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 Dinner
Marriott Marquis & Marina, Presidio 1 & 2
6:00 PM – 10:00 PM
Invitation only - Separate pre-registration required
Behavioral Pharmacology Society Meeting
Marriott Marquis & Marina, San Diego Ballroom, Salon C
8:00 AM – 6:00 PM
Invitation only - Separate pre-registration required
2014 Teaching Institute: Practical technologies for effective teaching
San Diego Convention Center, Room 3
12:00 PM – 2:30 PM
Chairs: Renee L. Hayslett, Mercer Univ. and Catherine M. Davis, Johns Hopkins Univ. School of Med.
E-learning, m-learning: Where technology meets pedagogy
Rodney B. Murray, Univ. of the Sciences
Animated teaching: A simple way to make educational animations
Danton H. O’Day, Univ. of Toronto
“The games we play”: Incorporating gaming into pharmacology teaching
A. Laurel Gorman, Univ. of Central Florida Col. of Med.
Using camtasia (and related technologies) to create student-centered learning modules
Robert B. Stephenson, Michigan State Univ.
Q & A session
Graduate Student-Postdoctoral Colloquium: Success Skills for All Careers
San Diego Convention Center, Room 2
2:45 PM – 5:15 PM
Chair: Susan L. Ingram, Oregon Hlth. & Sci. Univ.
What got you here won't get you there: Upgrading your skills for career success
Philip Clifford, Univ. of Illinois at Chicago
Effective PowerPoint skills to get your point across
Lawrence Carter, Jazz Pharmaceuticals, Inc.
Big science on a modest budget: Using technology and networking to your advantage
Lakshmi Devi, Icahn Schl. of Med. at Mount Sinai Med. Ctr.
ASPET Business Meeting
San Diego Convention Center, Ballroom 20BC
6:00 PM – 7:30 PM
ASPET Opening and Awards Reception
San Diego Convention Center, Center Terrace
7:30 PM – 9:30 PM
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Diversity Mentoring Breakfast
Marriott Marquis & Marina, New York/Orlando
7:30 AM – 9:30 AM
Keynote Speaker: Victoria A. Love, Allergan
Keynote Address: Career paths for scientific writing
JULIUS AXELROD AWARD LECTURE
San Diego Convention Center, Room 2
8:30 AM – 9:20 AM
Lee E. Limbird, Fisk Univ.
Seasons of the lives of scientists: The journey from training to careers in discovery to service for society
JULIUS AXELROD SYMPOSIUM: Surprises at the synapse
Supported by the John V. Croker Fund
San Diego Convention Center, Room 2
9:30 AM – 12:00 PM
Chair: Lee E. Limbird, Fisk Univ.
Lessons from the life and scientific career of Julius Axelrod: The seasons of scientists lives
Lee E. Limbird, Fisk Univ.
A novel mechanism for methamphetamine regulation of the dopamine transporter intracellularly via the sigma-1 receptor
Habibeh Khoshbouei, Univ. of Florida
GPCR endocytosis and signaling in neurons
Mark Von Zastrow, Univ. of California San Francisco
Illuminating the alpha2-adrenergic receptor as a negative player in cognition
Qin Wang, Univ. of Alabama
Chronic loss of noradrenergic tone produces a Gi-to Gs switch in D2 receptor coupling and cocaine hypersensitivity via β-arrestin 2
David Weinshenker, Emory Univ.
Animal models of polydrug abuse
San Diego Convention Center, Room 4
9:30 AM – 12:00 PM
SPONSORSHIP OPPORTUNITY AVAILABLE
Sponsored by the Divisions for Behavioral Pharmacology; Neuropharmacology; and Toxicology
Chairs: Paul W. Czoty, Wake Forest Univ. Sch. of Med. and Richard De La Garza, Baylor Col. of Med.
Although laboratory animal models have been extremely useful in characterizing the abuse liability of drugs, less success has been achieved in developing widely effective pharmacotherapies for addiction. Whereas the behavior of addicted individuals is largely characterized by the use of multiple licit and illicit drugs, subjects in preclinical animal and human studies are almost invariably exposed to a single substance. This symposium will highlight current efforts to develop animal models of polydrug exposure. The key presenters will describe their studies involving interactions of many abused drugs including cocaine, nicotine, alcohol, and constituents of marijuana.
Polysubstance abuse in humans necessitates appropriate animal models
Richard De La Garza, Baylor Col. of Med
Cocaine/nicotine mixtures: Reinforcing effects and medications discovery
Stephen J. Kohut, McLean Hosp./Harvard Med. Sch.
A nonhuman primate model of cocaine/alcohol co-abuse
Paul W. Czoty, Wake Forest Sch. of Med.
Cannabinoid system and nicotine addiction: Novel insights on their interactions
Bernard Le Foll, Centre for Addiction and Mental Health
Age differences in the reinforcing effects of nicotine-alcohol combinations
Francis M. Leslie, Univ. of California - Irvine
Career opportunities beyond the bench: Education as a viable path
San Diego Convention Center, Room 5A
9:30 AM – 12:00 PM
Sponsored by the Divisions for Pharmacology Education; Behavioral Pharmacology; Cardiovascular Pharmacology; Drug Discovery and Development; Drug Metabolism; Integrative Systems; Translational and Clinical Pharmacology; Molecular Pharmacology; Neuropharmacology; and Toxicology
Chairs: Jayne S. Reuben, Univ. of South Carolina Sch. of Med-Greenville and Karen Marcdante, Medical Col. of Wisconsin
Postdoc pharmacologists in various endeavors beyond bench research with a particular focus on education as a viable career path. There are more than 15 new medical schools that have been inaugurated within the last couple of years. In addition, there are many osteopathic, pharmacy, nursing and allied health schools that are being established as well. These new developments create an immediate need for content experts in the area of all basic sciences, including pharmacology, to teach the medical students. Participants will be exposed to the means by which they can identify, explore, and target these opportunities.
Opportunities for scientists in science and healthcare education
Jayne S. Reuben, Univ. of South Carolina Sch. of Med.-Greenville
How a teaching/research postdoc can prepare you for success in academia
Antonio T. Baines, North Carolina Central Univ.
Creating an educator portfolio
Dr. Karen Marcdante, Medical Col. of Wisconsin
Panel discussion and networking session
Drug discovery against protozoal pathogens
San Diego Convention Center, Room 5B
9:30 AM – 12:00 PM
Sponsored by the Divisions for Drug Discovery and Development & Molecular Pharmacology
Chair: Margaret A. Phillips, Univ. of Texas Southwestern Med. Ctr.
The protozoal parasites such as Plasmodium falciparum (malaria), Trypanosoma brucei (African sleeping sickness), Trypanosoma cruzi (Chagas' disease), and Leishmania cause significant morbidity and mortality throughout the world with the poorest and most vulnerable populations most at risk. Vaccines are not available to treat these diseases, and current drug therapy suffers from issues of resistance or toxicity. Significant effort is underway to identify new drugs against these diseases involving collaborations between academia, industry, and not-for-profit organizations. This symposium will focus on a number of new compounds for the treatment of these diseases that are entering the clinics or are in the drug discovery pipeline.
Designing selective inhibitors for calcium-dependent protein kinases in apicomplexans
L. David Sibley, Washington Univ. in St. Louis
Hit-to-lead drug discovery around novel scaffolds for human African Trypanosomiasis
Michael H. Gelb, Univ. of Washington
Targeting malarial dihydroorotate dehydrogenase
Margaret A. Phillips, Univ. of Texas Southwestern Med. Ctr.
Discovery of plasmodium P14-kinase as a critical drug target
Case McNamara, Genomics Inst. of the Novartis Res. Fndn.
Junior Speaker: Epigenetic gene regulation as an antimalarial drug targeting opportunity
Nicholas A. Malmquist, Institut Pasteur
Junior Speaker: Discovering molecules to probe and treat malaria
Emily R. Derbyshire, Harvard Med. Sch.
Therapeutic potential of targeting oxidative stress pathways
San Diego Convention Center, Room 3
9:30 AM – 12:00 PM
Sponsored by the Divisions for Toxicology; Cardiovascular Pharmacology; Integrative Systems, Translational and Clinical Pharmacology; and Molecular Pharmacology
Chairs: Philip R. Mayeux, Univ. of Arkansas for Medical Sciences and Chunfu Wu, Shenyang Pharmaceutical Univ.
Oxidative stress is a major mechanism for various toxicities. The symposium will address mechanisms of oxidative stress important in toxicity, physiological responses to oxidative stress, and novel therapeutic approaches to alleviate oxidative stress.
Targeting mitochondrial oxidant generation in sepsis-induced renal injury
Philip R. Mayeux, Univ. of Arkansas for Medical Sciences
Function and therapeutic potential of the Keap1-Nrf2-ARE pathway
Curtis D. Klaassen, Univ. of Kansas Med. Ctr.
Biological activities and potential medical uses of resveratrol
Chunfu Wu, Shenyang Pharmaceutical Univ.
Design of metal-targeting and antioxidant small molecules for the use in neurodegenerative disorders
Kayla Green, Texas Christian Univ.
Junior Speaker: Targeting hepatic thioredoxin reductase by the acetaminophen metabolite N-acetyl-p-benzoquinone
Yi-Hua Jan, Rutgers Univ.
Junior Speaker: FeTTPs treatment reduces secondary injury associated in a mouse model of traumatic brain injury
Daniela Impellizzeri, Univ. of Messina
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ASPET/CNPHARS WELCOMING CEREMONY
San Diego Convention Center, Room 5A
2:00 PM – 2:10 PM
Richard R. Neubig, Michigan State Univ. and Guan-Hua Du, Inst. of Meteria Medica, Chinese Academy of Med. Sci. & Peking Union Med. Col.
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CNPHARS LECTURE
San Diego Convention Center, Room 5A
2:10 PM – 2:50 PM
Guan-Hua Du, Inst. of Meteria Medica, Chinese Academy of Med. Sciences & Peking Union Med. Col.
Target-net based drug discovery for Parkinson's disease treatment by HTS/HCS
Chair: John Glowa, NIH/NCCAM
Drug discovery in China and the United States
San Diego Convention Center, Room 5A
3:00 PM – 5:30 PM
Sponsored by the Chinese Pharmacological Society and the ASPET Division for Drug Discovery and Development
Chairs: John Glowa, NIH/NCCAM and Yongxiang Zhang, Beijing Inst. of Pharmacology & Toxicology
Because the 2014 meeting is a joint meeting with the Chinese Pharmacological Society, this session will be devoted to presentations on the state of drug discovery in China. Drugs will be discussed which are under development for the treatent of stroke, hypertension, and inflammation.
The role of microRNA on serious cardiac diseases
Baofeng Yang, Harbin Medical Univ. China
Drugging undruggable molecular cancer targets
John Lazo, Univ. of Virginia
From the research on anti-inflammatory and immunopharmacology of a natural herbaceous peony to discovery of paeoniflorin-6'-O-benzene sulfonate
Wei Wei, Anhui Medical Univ. China
Heart failure: Next generation regenerative solutions
Andre Terzic, Mayo Clinic
Discovery of urea transporter as a novel diuretic drug target and potential diuretic compounds thienoquinolins
Baoxue Yang, Peking Univ. Hlth Sci. Ctr. China
GUCY2C as a novel drug target in obesity
Scott Waldman, Thomas Jefferson Univ.
Emerging technologies in neuropeptide research: Identification and validation of neuropeptide systems as therapeutic targets
San Diego Convention Center, Room 4
3:00 PM – 5:30 PM
Sponsored by the Divisions for Neuropharmacology; Drug Discovery and Development; Integrative Systems, Translational and Clinical Pharmacology; and Molecular Pharmacology
Chair: Stewart D. Clark, Univ. at Buffalo, SUNY
Neuropsychiatric and other neurological disorders have a devastating impact on individuals, families, and society, and present pharmacological treatments do not fully ameliorate or even treat the full spectrum of symptoms. One class of molecules that shows great promise in this regard is neuropeptides. Neuropeptides, only a fraction of which have been discovered, have powerful and long-lasting effects on brain function. In addition, neuropeptides’ target receptors are G protein-coupled receptors which have repeatedly been exploited as drug targets. The proposed symposium will highlight areas in which there have been methodological advances in the study of neuropeptides that will pave the way for the development of improved drugs for a spectrum of neurological disorders.
Neuropeptidomics: Approaches for the discovery of new neuropeptides and their functions
Jonathan V. Sweedler, Univ. of Illinois at Urbana-Champaign
The voltammetric detection and characterization of met-enkephalin fluctuations in live brain tissue
Leslie A. Sombers, North Carolina State Univ.
Fusions of diphtheria toxin and neuropeptides to selectively remove neurons
Stewart D. Clark, Univ. at Buffalo, SUNY
Optogenetic dissection of neural circuits and GPCR signaling in stress-induced behavior
Michael R. Bruchas, Washington Univ. Sch. of Med
Junior Speaker: Protease-activated peptide toxins for selective nanoparticle therapeutics
Andrew Jallouk, Washington Univ. in St. Louis
New insights derived from cell specific heterotrimeric G protein knockouts
San Diego Convention Center, Room 2
3:00 PM – 5:30 PM
Sponsored by the Divisions for Molecular Pharmacology; Cardiovascular Pharmacology; Drug Discovery and Development; and Integrative Systems, Translational and Clinical Pharmacology
Chairs: Fiona Murray, Univ. of California-San Diego and Paul Insel, Univ. of California-San Diego
Heterotrimeric G proteins transduce signals from G protein-coupled receptors (GPCRs) to effector proteins to modulate cellular function. G protein signaling constitutes a fundamental mechanism of intercellular communication used by all eukaryotes. Whole body knockouts of G proteins can be embryonic lethal and difficult to interpret, however much progress has been made of cell specific knockout of individual G-alpha proteins. This symposium aims to highlight the physiological role of heterotrimeric G-alpha proteins and recent advances in G protein function and signaling that have been made by cell-targeted knockout studies in mice.
The role of Gαs in immune cell function: Insight into allergy
Eyal Raz, Univ. of California-San Diego
Role of G Proteins in regulation of energy and glucose metabolism
Lee Weinstein, NIDDK, NIH
Gq-RGS signaling in diabetes and pancreatic cancer
Thomas Wilkie, UT Southwestern Med. Ctr.
Reciprocal functions of Gαi2 and Gαi3 in lymphocyte egress
Mei X. Wu, Harvard Med. Sch.
Junior Speaker: Intragenic suppressors of McCune-Albright Syndrome R201H mutations also suppress other constitutively active Gs alleles
Robin Rylaarsdam, Benedictine Univ.
Junior Speaker: Elucidating the role of inhibitory G-protein, Gz, in β-cell preservation and regeneration
Allison Brill, Univ. of Wisconsin-Madison
New preclinical and clinical perspectives for smoking cessation
San Diego Convention Center, Room 3
3:00 PM – 5:30 PM
Sponsored by the Divisions for Behavioral Pharmacology; Cardiovascular Pharmacology; Integrative Systems, Translational and Clinical Pharmacology; Neuropharmacology; and Toxicology
Chairs: Rajeev I. Desai, McLean Hosp./Harvard Med. Sch. and Dorothy K. Hatsukami, Univ. of Minnesota
Tobacco smoking is the leading cause of preventable disease and premature death in the world (approximately 5 million annual deaths). Although behavioral and medication-based smoking cessation approaches are available, there is still a high degree of relapse among individuals who want to quit. This symposium will discuss current smoking cessation approaches and their limitations, and present new evidence from genetic (molecular), pharmacological, immunological, and behavioral studies across different species on novel potential smoking cessation treatments.
Small molecule alpha-conotoxin MII surrogates for the treatment of nicotine addiction
Linda P. Dwoskin, Univ. of Kentucky
Anti-nicotine vaccines and nicotinic partial agonists for smoking cessation
Rajeev I. Desai, McLean Hosp./Harvard Med. Sch.
Behavioral interventions for smoking cessation
Stephen T. Higgins, Univ. of Vermont
Targeting smoking cessation: Current approaches and their limitations and future perspectives
Dorothy K. Hatsukami, Univ. of Minnesota
Pharmacology Education Division Programming: Addressing prescribing errors through medical student education and assessment
San Diego Convention Center, Room 5B
3:00 PM – 5:30 PM
Supported by funding from Jazz Pharmaceuticals
Chairs: Senthil K. Rajasekaran, Eastern Virginia Med. Sch. and David W. Nierenberg, Dartmouth-Hitchcock Med. Ctr.
Medication errors are estimated to cost $37 billion and result in 7,000 annual deaths, with a majority of these errors due to improper dosing, wrong drug, or wrong duration. However, in most medical schools, pharmacology training is limited to the early basic science years. The ability to prescribe commonly used drugs safely and effectively should be a core competency of the newly qualified doctor. Given that prescribing is such a fundamental part of medical practice, it is important to develop appropriate and acceptable curricula and assessments to ensure that medical students are gaining these skills before they graduate and move on to their PGY I positions. This symposium will give the audience an opportunity to learn about such an assessment tool created in the UK and will provide tools to implement a curriculum to teach this competency to medical students.
Education in safe and effective prescribing practices
David W. Nierenberg, Dartmouth-Hitchcock Med. Ctr.
Assessing prescribing competence of senior medical students: A UK perspective
Simon Maxwell, Univ. of Edinburgh
A four-year longitudinal curricular model to teach prescribing skills to medical students
Senthil K. Rajasekaran, Eastern Virginia Med. Sch.
Global GI Club Science & Business Meeting
San Diego Convention Center, Room 14A
3:00 PM – 6:00 PM
Student/Postdoc Best Abstract Competition
Marriott Marquis & Marina, Marriott Hall 3/4
6:30 PM – 8:30 PM
ASPET Student & Postdoc Mixer
Marriott Marquis & Marina, Marriott Hall, Salon 2
9:00 PM – 11:30 PM
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JOHN J. ABEL AWARD LECTURE
San Diego Convention Center, Room 2
8:30 AM – 9:20 AM
Craig W. Lindsley, Vanderbilt Univ. Med. Ctr.
Exploiting Allosteric Sites for Target Modulation
Collaborative role of pharmacology in education of healthcare professions
San Diego Convention Center, Room 5A
9:30 AM – 12:00 PM
Sponsored by the Divisions for Pharmacology Education; Behavioral Pharmacology; Cardiovascular Pharmacology; Drug Discovery and Development; Drug Metabolism; Integrative Systems, Translational and Clinical Pharmacology; Molecular Pharmacology; Neuropharmacology; and Toxicology
Chairs: Sandra Carlin Andrieu, LSUHSC New Orleans Sch of Dentistry and Robert J. Theobald, Jr., Kirksville Coll. of Osteopathic Med.
It is well known that interprofessional collaborative practice is key to the safe, high quality, accessible, patient-centered care desired by all. Achieving that vision for the future requires moving beyond profession-specific educational efforts to engage students of different professions in interactive learning with each other so that they enter the workforce ready to practice effective teamwork and team-based care. This symposium will address some of the core principles of integrative curricula and will provide participants with specific guidance on the role of pharmacology in both foundational sciences and organ system courses, including the interface with other professions and disciplines in healthcare and health science.
Introduction
Robert J. Theobald, Jr., Kirksville Coll. of Osteopathic Med.
Overview of interprofessional education: Where does pharmacology fit in this venue?
Sandra Carlin Andrieu, LSUHSC New Orleans Sch. of Dentistry
Nurses as the nation's largest health professions workforce — Responding to the clarion call for interprofessional collaborative practice and education
Jane Marie Kirschling, Univ. of Maryland Sch. of Nursing
Incorporating pharmacology in interprofessional education at the Medical University of South Carolina
Yiannis Koutalos, Med. Univ. of South Carolina
Creating successful interprofessional pharmacology education for healthcare students by avoiding the pitfalls
Lynn Wecker, Univ. South Florida Coll. of Med.
Panel discussion
Robert J. Theobald, Jr., Kirksville Coll. of Osteopathic Med.
Drug-induced idiosyncratic reactions and immunotoxicity
San Diego Convention Center, Room 5B
9:30 AM – 12:00 PM
Sponsored by the Divisions for Toxicology; Drug Discovery and Development; Drug Metabolism; Integrative Systems, Translational and Clinical Pharmacology; and Molecular Pharmacology
Chair: Jack Uetrecht, Univ. of Toronto
The immune system is the therapeutic target of many new drugs, but drugs can also cause immune-mediated adverse reactions, unrelated to the therapeutic effects of the drugs. Idiosyncratic drug reactions are a special problem for drug development because they are often not detected until the drug has been marketed. Biological drugs that target the immune system can cause paradoxical immunotoxicity as is the case with autoimmune hepatitis caused by immunosuppressants such as anti-TNFα antibodies. This symposium will discuss research that has provided important clues to the mechanisms underlying such idiosyncratic drug reactions.
Role of the adaptive immune system in idiosyncratic drug reactions
Jack Uetrecht, Univ. of Toronto
Idiosyncratic drug sensitivity reactions affecting blood cells
Richard Aster, Blood Center of Wisconsin
Unexpected and idiosyncratic effects of biotherapeutics on peripheral blood cells
Nancy Everds, Amgen, Inc.
Preclinical tools for risk assessing immune-mediated adverse drug reactions
Jessica Whritenour, Pfizer, Inc.
Fetal programming of adult cardiovascular disease
San Diego Convention Center, Room 4
9:30 AM – 12:00 PM
Sponsored by the Divisions for Integrative Systems, Translational and Clinical Pharmacology; Cardiovascular Pharmacology; and Toxicology
Chairs: Mark C. Chappell, Wake Forest Baptist Med. Ctr. and Allyson C. Marshall, Wake Forest Baptist Med. Ctr.
The fetal programming hypothesis is the concept that alterations in the fetal environment may result in developmental adaptations that predispose offspring to cardiovascular (hypertension) and metabolic (diabetes) diseases later in life. Potential effectors of fetal programming include nutrient and growth restriction, environmental stressors, and administration of drugs during pregnancy, as well as sex, fetal age, duration, and severity of exposure. While the original programming insults are diverse, studies reveal specific pathways that are particularly vulnerable to alteration from programming events, including the renin-angiotensin system (RAS), the sympathetic nervous system, and hypothalamic pituitary adrenal (HPA) axis. The focus of this symposium is to identify pathways vulnerable to insult by fetal programming and possible sites of pharmacological intervention to correct the programming effects.
Brief introduction
Mark C. Chappell, Wake Forest Baptist Med. Center and Allyson C. Marshall, Wake Forest Baptist Med. Ctr.
Prenatal programming of hypertension: Renal mechanisms and interventions
Michel Baum, Univ of Texas Southwestern Med. Ctr.
Hyperglycemia and sex specific cardiovascular programming
Jeffrey Segar, Univ. of Iowa Carver Coll. of Med.
Betamethasone induced programming of the brain renin-angiotensin system
Junior Speaker: Hossam A. Shaltout, Wake Forest Univ. Sch. of Med.
Fetal programming of the hypothalamic-pituitary-adrenal axis
Stephen G. Matthews, Univ. of Toronto
Nuclear receptors as therapeutic targets
San Diego Convention Center, Room 2
9:30 AM – 12:00 PM
Sponsored by the Divisions for Molecular Pharmacology; Drug Metabolism; Integrative Systems, Translational and Clinical Pharmacology; and Toxicology
Chairs: Donald P. McDonnell, Duke Univ. Med. Ctr. and David Mangelsdorf, Univ. of Texas Southwestern Med. Ctr.
The nuclear receptor (NR) superfamily of ligand-regulated transcription factors has been exploited in the development of a large number of drugs that target a wide range of endocrinopathies and cancers. Whereas most of the currently available therapeutics were developed empirically, it is clear that there may be more useful ways to manipulate NR function in various diseases. The assembled group of speakers are leaders in this field and will provide an exciting update of emerging strategies that target this superfamily of transcriptional regulators.
Orphan nuclear receptors Nr4a1 as targets in acute myeloid leukemia
Orla Conneely, Baylor Col. of Med.
LXRs as a link between inflammation and metabolism
Peter Tontonoz, Univ. of California-Los Angeles
Regulation of metabolism by nuclear receptor-FGF signaling pathways
Steven A. Kliewer, Univ. of Texas Southwestern Med. Ctr.
Targeting the androgen signaling axis in cancer
Donald P. McDonnell, Duke Univ. Med. Ctr.
Junior Speaker: Sumo-modification of pxr alters protein cofactor interactions
Sarah K. Woody, Univ. of Kansas
Sleep disruptions associated with neuropsychiatric and degenerative disorders: Implications, preclinical models and development of novel pharmacotherapies
San Diego Convention Center, Room 3
9:30 AM – 12:00 PM
Supported by funding from Data Sciences International (DSI)
Sponsored by the Divisions for Behavioral Pharmacology; Integrative Systems, Translational and Clinical Pharmacology; Neuropharmacology; and Toxicology
Chairs: Robert W. Gould, Vanderbilt Univ. Med. Sch. and Carrie K. Jones, Vanderbilt Univ. Med. Sch.
Current drug treatments for neuropsychiatric and degenerative disorders aim to alleviate primary clinical symptoms without sufficiently treating sleep disturbances such as restlessness, insomnia, sleep apnea, reduced rapid eye movement (REM) sleep, and excessive daytime sleepiness. Insomnia is now recognized not as a consequence of, but a predictor for and often mainstay throughout many neuropsychiatric conditions. Further, sleep disturbances are linked to cognitive deficits, another untreated symptom associated with many neuropsychiatric and degenerative conditions. This symposium will describe sleep disturbances across a range of clinical conditions, effects of current treatments on sleep, and translational preclinical models employed to understand causes and develop novel treatments for sleep disturbances.
Sleep disturbances associated with neuropsychiatric disorders: A brief overview
Carrie K. Jones, Vanderbilt Univ. Med. Sch.
In utero exposure to valproic acid changes sleep patterns in juvenile rats: A potential preclinical model for studying sleep disturbances in autism spectrum disorders
Jessica Mong, Univ. of Maryland Sch. of Med.
Hypothalamic-pituitary-adrenal axis dysfunctions associated with sleep disturbances in post-traumatic stress disorder
Eric Vermetten, Leiden Univ. Med. Ctr. and Univ. Med. Ctr. Utrecht
Subtype-selective muscarinic acetylcholine receptor modulation of sleep/wake architecture for the treatment of psychiatric disorders
Robert W. Gould, Vanderbilt Univ. Med. Sch.
Modulation of sleep disruptions in neuropsychiatric disorders by medication or transcranial direct current stimulation
Robert Goeder, Univ. Hosp. Schleswig-Holstein
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B.B. BRODIE AWARD LECTURE IN DRUG METABOLISM
San Diego Convention Center, Room 5A
2:00 PM – 2:50 PM
Bruce D. Hammock, Univ. of California-Davis
Epoxide Hydrolases in Drug Metabolism and as Drug Targets
P.B. DEWS AWARD LECTURE IN BEHAVIORAL PHARMACOLOGY
San Diego Convention Center, Room 4
2:00 PM – 2:50 PM
James H. Woods, Univ. of Michigan Sch. of Med.
The Stimulus Functions of Drugs
Behavioral Pharmacology Division Symposium: Making the right choice: Translational use of choice procedures in understanding the neurobiology and development of pharmacotherapies for drug addiction
San Diego Convention Center, Room 4
3:00 PM – 5:30 PM
Chairs: Matthew L. Banks, Virginia Commonwealth Univ. and Michael A. Nader, Wake Forest Univ.
Choice procedures are perhaps the most homologous model in which to study behavior. Although choice procedures are almost exclusively used in human laboratory studies of substance abuse, there is a small but growing body of literature in both rodent and nonhuman primate models of substance abuse that are employing choice porcedures. This symposium will discuss the utility of choice procedures to provide insight into novel biological targets and potential pharmacological strategies for substance abuse. The discussions will involve theoretical considerations, experimental design issues for studies involving humans and animals, and how this baseline can inform researchers about the neurobiology and pharmacology of drug abuse.
Gender difference in drug vs. food choice behaviors
Tod Kippin, Univ. of California-Santa Barbara
The use of choice procedures to understand drug mixtures
Junior Speaker: Kevin Freeman, Univ. of Mississippi Med. Ctr.
Utility of choice procedures for medication development for drug dependence in preclinical studies
Matthew L. Banks, Virginia Commonwealth Univ.
Utility of choice procedures in human drug abuse laboratory studies
William W. Stoops, Univ of Kentucky Coll. of Med.
Junior Speaker: Psychophysiological prediction of drug choice
Scott J. Moeller, Icahn Sch. of Med. at Mount Sinai
Mitochondrial fragments: A novel mediator between inflammation and cardiovascular disease
San Diego Convention Center, Room 3
3:00 PM – 5:30 PM
Sponsored by the Divisions for Cardiovascular Pharmacology; Integrative Systems, Translational and Clinical Pharmacology; and Toxicology
Chairs: R. Clinton Webb, Georgia Regents Univ. and Camilla Ferreira Wenceslau, Georgia Regents Univ.
This symposium will deal with emerging data providing insight in the role of mitochondrial constituents and mitochondrial dysfunction in the genesis of cardiovascular diseases. The pro-inflammatory actions of fragmented mitochondria in the extracellular space comprise a newly discovered area of investigation, first described in 2010. This interaction between mitochondrial constituents and the immune system has been recently associated with cardiovascular diseases (e.g., heart failure, preeclampsia, and diabetes). Further, signaling mechanisms associated with mitochondrial biogenesis and bioenergetics have been found in conditions such as hypertension and the metabolic syndrome. Potential therapeutic targets related to mitophagy, mitochondrial biogenesis, and energetics will be addressed and discussed.
Circulating mitochondrial fragments as a novel signaling mechanism that induces systemic inflammation
Kiyoshi Itagaki, Beth Israel Deaconess Med. Ctr. and Harvard Med. Sch.
Mitochondrial dysfunction and myocardical ischemia/reperfusion
Charles L. Hoppel, Case Western Res. Univ.
Mitochondrial oxidative stress and atherosclerosis
Qi-An Sun, Univ. of North Carolina-Chapel Hill
Evolutionary selection and mitochondrial genetics: Implications on cardiovascular disease susceptibility
Scott Ballinger, Univ. of Alabama
The role of placenta-derived mitochondrial fragments in the development of preeclampsia
Styliani Goulopoulou, Georgia Regents Univ.
Mitochondrial N-formyl peptides cause hypotension via formyl peptide receptor activation
Camilla Ferreira Wenceslau, Georgia Regents Univ.
Junior Speaker: Chronic Bendavia therapy improves post-infarction cardiac function and prevents adverse left ventricular remodeling in rats
Wangde Dai, Good Samaritan Hosp.
Drug Metabolism Division James Gillette Award and Platform Session
San Diego Convention Center, Room 5A
3:00 PM – 5:30 PM
Chairs: Jeffrey P. Jones, Washington State Univ. and Larry C. Wienkers, Amgen Inc.
CYP3A5 genotype impacts maraviroc pharmacokinetics in healthy volunteers
Yanhui Lu, Johns Hopkins Univ.
Application of physiologically-based pharmacokinetic modeling in hepatic impairment populations
Jennifer E. Sager, Univ. of Washington
Gestational age-dependent maternal-fetal glyburide disposition in pregnant mice
Diane L. Shuster, Univ. of Washington
The orally active male contraceptive agent H2-gamendazole interacts with Organic Anion Transporting Polypeptides (OATPs) expressed in human hepatocytes
Jessica Shoop, Univ. of Kansas Med. Ctr.
The potent inhibition of human SULT1A1 by 17β-ethinylestradiol (EE2) is due to interactions with ILE89 in loop 1
Katie Jo Rohn-Glowacki, Univ. of Alabama at Birmingham
Intracellular chloride concentration and its impact on dichloroacetate metabolism
Stephan Jahn, Univ. of Florida
James Gillette Best Paper Award: Genetic variation in aldo-keto reductase 1D1 (AKR1D1) affects the expression and activity of multiple cytochrome P450s
Amarjit S. Chaudhry, St. Jude Children's Research Hosp.
James Gillette Best Paper Award: Analysis of the repaglinide concentration increase produced by gemfibrozil and itraconazolebased on the inhibition of the hepatic update transporter and metabolic enzymes
Toshiyuki Kudo, Musashino Univ.
Molecular Pharmacology Division Postdoctoral Award Finalists
San Diego Convention Center, Room 5B
3:00 PM – 5:30 PM
Keynote Speaker: Richard A. Heyman, Seragon Pharmaceuticals
Alveolar type II cell-localized p120-catenin is an essential regulator of lung barrier function and innate immunity
Andreia Chignalia, Univ. of Illinois at Chicago
G protein-coupled receptor kinase selective small molecule inhibitors
Kristoff Homan, Univ. of Michigan
GPCRs and heterotrimeric G proteins directly regulate member type-1 matrix metalloprotease
Aaron Overland, Univ. of California at San Diego
Keynote Address: Nuclear receptors: Integrating molecular endocrinology and drug discovery
Richard A. Heyman, Seragon Pharmaceuticals
Neuropharmacology Division Postdoctoral Scientist Award Finalists
San Diego Convention Center, Room 2
3:00 PM – 5:30 PM
Keynote Speaker: Athina Markou, Univ. of California at San Diego
Characterization of the kappa opioid receptor-mediated G protein signaling in mouse striatum using [35S]GTPγS binding assay
Lei Zhou, The Scripps Research Inst.
Analysis of functional selectivity at the nociception opioid receptor
Steven Chang, Washington Univ. in St. Louis
VTA GABA(A) receptors mediate maladaptive disinhibition of dopamine release in the NAc — a potential mechanism for increased risk taking behavior following adolescent voluntary alcohol intake
Abigail Schindler, Univ. of Washington
μ opioid receptor activity is regulated by endothelin converting enzyme-2
Erin Bobeck, Icahn Med. Sch. at Mt. Sinai
Identification of a novel, highly potent D3 dopamine receptor-selective agonist
Amy Moritz, NINDS, NIH
Influence of M1 muscarinic acetylcholine receptor activation on arousal and cognitive performance using electroencephalography and novel touchscreen cognition assessment
Robert Gould, Vanderbilt Univ.
Keynote address: Glutamate and nictoine dependence: The route to medication development with advise from Chiron, the centaur
Athina Markou, Univ. of California at San Diego
Behavioral Pharmacology and Neuropharmacology Divisions Joint Mixer
Marriott Marquis & Marina, Point Loma
6:45 PM – 8:45 PM
Drug Metabolism and Toxicology Divisions Joint Mixer
Marriott Marquis & Marina, Chicago/Atlanta
7:30 PM – 9:30 PM
Molecular Pharmacology Division Mixer
Marriott Marquis & Marina, Marriott Hall I
7:30 PM – 9:30 PM
Pharmacology Education, Drug Discovery and Development, & Integrative Systems, Translational and Clinical Pharmacology Divisions Joint Mixer
Marriott Marquis & Marina, New York
7:30 PM – 9:30 PM
Y.E.S. Young Experimental Scientist Mixer
Marriott Marquis & Marina, Marriott Hall 3/4
9:00 PM – 11:00 PM
*21 & older must have ID to receive drink tickets
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ASPET Networking Walk
Marriott Marquis & Marina, 7:00 AM – 9:00 AM
Meet at the ASPET Office (Rancho Santa Fe 3).
12-lipoxygenase and disease: New insights into regulation and inhibition of a critical enzyme
San Diego Convention Center, Room 2
9:30 AM – 12:00 PM
Sponsored by the Divisions for Integrative Systems, Translational and Clinical Pharmacology; Cardiovascular Pharmacology; Drug Discovery and Development; and Molecular Pharmacology
Chair: Michael Holinstat, Thomas Jefferson Univ.
The enzyme 12-lipoxygenase is known to affect a number of disease conditions including thrombosis, diabetes mellitus, and cardiovascular disease. Understanding the mechanism by which this enzyme and its bioactive lipid products regulate these systems is crucial in order to develop viable therapeutic strategies while minimizing off-target effects. This symposium focuses on the evolution of this field and highlights 12-lipoxgenase as a preferred therapeutic target for treatment of these pathophysiological conditions.
12-lipoxygenase-mediated fatty acid regulation of hemostasis and thrombosis
Michael A. Holinstat, Thomas Jefferson Univ.
Development of novel inhibitors to human lipoxygenases
Theodore R. Holman, Univ. of California-Santa Cruz
12-lipoxygenase regulation of diabetes mellitus
Jerry L. Nadler, Eastern Virginia Med. Sch.
Junior Speaker: Deletion of soluble epoxide hydrolase modulates coronary reactive hyperemia in isolated mouse hearts
Ahmad Hanif, West Virginia Univ.
Emerging integrative approaches to predicting host response to antimicrobials
San Diego Convention Center, Room 5B
9:30 AM – 12:00 PM
Sponsored by the Divisions for Integrative Systems, Translational and Clinical Pharmacology; Drug Metabolism; and Toxicology
Chair: Namandjé N. Bumpus, Johns Hopkins Univ. School of Med.
Therapeutic responses to antiviral drugs can be challenging to predict due, in part, to the fact that robust in vitro models of viral replication and animal models that are susceptible to certain human viruses are largely lacking. The purpose of this symposium is to bring together researchers who will share their progress in investigating host responses to antiviral therapy against a wide range of viruses through application of systems biology, metabolomics, and novel modeling approaches based upon the use of innovative in vitro and in vivo systems.
Introduction
Namandjé N. Bumpus, Johns Hopkins Univ. School of Med.
A ‘GoogleMAP’-type molecular view of microbes — From culture to people
Pieter C. Dorrestein, Univ. of California-San Diego
Developmental clinical pharmacology — Integrating enzyme maturation, pharmacokinetics, pharmacogenetics and pharmacodynamics
Courtney V. Fletcher, Univ. of Nebraska Med. Ctr. Col. of Pharmacy
Determinants of efavirenz pharmacokinetics and host response
Zeruesenay D. Desta, Indiana Univ. Sch. of Med.
Junior Speaker: Effects of HIV-1 Tat and morphine on the biophysical properties of sodium channels
Sylvia Fitting, Virginia Commonwealth Univ.
Not just a glue: Pharmacology, Physiology, and Pathology of Transglutaminases (focus on the Vasculature)
San Diego Convention Center, Room 3
9:30 AM – 12:00 PM
Supported by funding from Zedira
Sponsored by the Divisions for Cardiovascular Pharmacology & Molecular Pharmacology
Chairs: Stephanie Watts, Michigan State Univ. and Erik Bakker, Univ. of Amsterdam
The focus of this symposium will be on the novel and compelling functions of the transglutaminase (TG) family of enzymes in the cardiovascular system, an untapped area of research relative to TG function. TGs typically carry out a protein-protein bond, but recent evidence suggests that TGs attach primary amines – 5-HT, NE, DA and E – to a protein via a covalent modification that can change the function of the protein. Classic receptor activation does not appear to be necessary for this function, so this adds a new and exciting layer of complexity for how amines signal, not only in the cardiovascular system, but elsewhere.
Inhibition of transglutaminase
Jeffrey W. Keillor, Univ. of Ottawa
Transglutaminase in arterial remodeling
Erik Bakker, Univ. of Amsterdam
Transglutaminase-mediated amidation of proteins by monoamines
Kyle B. Johnson, Concordia Univ.
Vascular aging and transglutaminase
Lakshmi Santhanam, Johns Hopkins Univ.
Junior Speaker: Cerebral arterial wall remodeling following subarachnoid hemorrhage
Nadia Lachkar, Academic Med. Ctr. Amsterdam
Junior Speaker: Vascular oxidative stress promotes aortic stiffening
Jing Wu, Vanderbilt Univ.
Role of (drug) transporters in imaging in health and disease
San Diego Convention Center, Room 5A
9:30 AM – 12:00 PM
Sponsored by the Division for Drug Metabolism
Chair: Bruno Stieger, Univ. Hospital Zurich
The role of transporters in drug development is now widely recognized but the role of transporters in diagnosis is less appreciated. Since many of the widely used imaging probe substances need transporters to enter cells, it is important to understand how transporters function in disease states. Several groups are now working on developing imaging methodology and in particular imaging probes in conjunction with microdosing. This session will highlight the role of transporters in clinical diagnosis with a focus on imaging and the development of new tools for the application of microdosing in drug development.
Introduction
Bruno Stieger, Univ. Hospital Zurich
The Role of Transporters for Diagnostic Probes
Bruno Stieger, Univ. Hospital Zurich
Quantification of drug transporters to understand interindividual variability in drug disposition and drug response
Jashvant Unadkat, Univ. of Washington
PET imaging of ABC efflux transporters at the blood-brain barrier in humans and animal models
Oliver Langer, Med. Univ. of Vienna
Junior Speaker: New radiopharmaceuticals for PET renography utilizing OAT1
Hariprasad Gali, Univ. of Oklahoma Col. of Pharmacy
Transporters in glial cells as new therapeutic targets
San Diego Convention Center, Room 4
9:30 AM – 12:00 PM
Sponsored by the Divisions for Neuropharmacology; Cardiovascular Pharmacology; Drug Discovery and Development; and Molecular Pharmacology
Chair: Lucio Annunziato, Federico II Univ. of Naples Sch. of Med.
Glial cells constitute the large majority of cells in the nervous system and account for the majority of cells in the human brain. During recent years, a large number of studies have critically attributed to glia a new role which no longer reflects the long-held view that glia constitute solely a silent and passive supportive scaffolding for brain cells but credits them with a much more active role in brain function. Glial transporters, responsible for maintaining intraglial ionic homeostasis in ischemic brain injury, are potential candidates in stroke intervention. This symposium will discuss how targeting these transporters may make it possible to modulate regenerative processes occurring after stroke and in other neurodegenerative disorders.
NCX expression and activity in microglia and oligodentrocytes after stroke
Lucio Annunziato, Federico II Univ. of Naples Sch. of Med.
Protective role of microglia and its mechanism under stroke: Na+/Ca2+ exchange dependent microglial migration
Mami Noda, Kyushu Univ.
Na+/H+ exchange in microglia-mediated oxidative stress: Support of NADPH oxidase function
Dandan Sun, Univ. of Pittsburgh Med. Sch.
The Sur1-Trpm4 channel in glial cells in CNS injury
J. Marc Simard, Univ. of Maryland Sch. of Med.
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Career Development Workshop: Establishing Individual Development Plans (IDPs) in your Graduate and Postdoctoral Training Programs: The Ins and Outs of Successful IDPs for Career Development
San Diego Marriott Marquis & Marina, Marriott Hall, Salon 2
1:00 PM – 3:00 PM
Chair: Susan L. Ingram, Oregon Hlth. & Sci. Univ.
A goal without a plan is just a wish
Philip Clifford, Univ. of Illinois at Chicago
The IDP: A strategic personal career plan
Lynn Wecker, Univ. of South Florida Col. of Med.
Cardiovascular Pharmacology Division Trainee Showcase
San Diego Convention Center, Room 3
2:30 PM – 4:30 PM
Chair: Amy C. Arnold, Vanderbilt Univ
Membrane cholesterol and caveolar modulation of cardiac function, ischemic tolerance and opioidergic protection
Louise See Hoe, Griffith Univ.
Contribution of guanine nucleotide exchange factor Vav2 to homocysteine-induced NLRP3 inflammasome activation in mouse podocytes
Justine Abais, Virginia Commonwealth Univ.
PSD95 scaffolding of the Shaker-type K+ channel enables PKA-dependent phosphorylation and vasodilation of cerebral arteries
Christopher Moore, Univ. of Arkansas for Med. Sci.
Short-term Toll-like receptor 9 stimulation increases blood pressure and vascular dysfunction via attenuated NO and exacerbated ROS generation
Cameron McCarthy, Georgia Regents Univ.
New insights on endothelial CaMKII in angiotensin II-induced hypertension
Chimene Charbel, Univ. de Montréal
Mitochondrial processing peptidases as a target therapy for vascular endothelial dysfunction in atherosclerosis
Deepesh Pandey, Johns Hopkins Univ.
Novel roles of chromogranin A and its peptide, catestatin, in cardioprotection
Jan Schilling, Univ. of California at San Diego
Drug Discovery and Development Division Symposium: Productive public private partnerships for pharmacological progress
San Diego Convention Center, Room 4
3:00 PM – 5:30 PM
SPONSORSHIP OPPORTUNITY AVAILABLE
Chair: John S. Lazo, Univ. of Virginia
Introduction to public private partnerships
John S. Lazo, Univ. of Virginia
The role of the NCATS in fostering public-private partnerships in translation
Christopher P. Austin, Natl. Ctr. for Advancing Translational Sci. (NCATS), NIH
We have to work together to catalyse the discovery of new medicines
Chas Bountra, Univ. of Oxford
Pfizer's strategies to access external innovation through partnerships with academia
Robert Abraham, Pfizer Pharmaceuticals
Allosteric modulators of GPCRs as a novel approach to treatment of CNS disorders
Carrie K. Jones, Vanderbilt Univ. Med.Sch.
Inhibitory G protein-coupled receptors as therapeutic targets for obesity and type 2 diabetes
San Diego Convention Center, Room 2
3:00 PM – 5:30 PM
Sponsored by the Divisions for Molecular Pharmacology; Cardiovascular Pharmacology; Drug Discovery and Development; and Integrative Systems, Translational and Clinical Pharmacology
Chair: Michelle E. Kimple, Univ. of Wisconsin-Madison
Obesity and the potential for insulin resistance are the biggest risk factors for type 2 diabetes (T2D). Thus, there is a pressing need for more effective treatments for type 2 diabetes, as well as those that might halt or reverse obesity itself. Current T2D therapeutics that act via beta-cell GPCRs mainly target the glucagon-like peptide 1 (GLP-1) receptor, which is coupled to Gs and stimulates cyclic AMP accumulation. These drugs have been used clinically for the past decade and are effective anti-hyperglycemic agents in many individuals. Yet, there exists a subset of individuals that remain resistant to the effects of these drugs. The existence of endogenous signaling pathways that are dysfunctionally up-regulated in T2D and act to inhibit cAMP accumulation might explain the lack of response in certain individuals, as well as provide a new physiological target for T2D. This program will summarize the current state of research in Gi-coupled GPCRs as therapeutic targets for type 2 diabetes and obesity.
Introduction
The Gz-coupled EP3 receptor as a therapeutic target for diabetic beta-cell dysfunction
Michelle E. Kimple, Univ. of Wisconsin-Madison
The PGE2 EP3 receptor in metabolic syndrome: The good, the bad, and the ugly
Richard Breyer, Vanderbilt Univ. Med. Ctr.
Alpha 2A adrenergic receptors and beta cell secretion
Erik Renström, Skåne Univ. Hosp. Malmö
Peripheral CB1 receptors as emerging therapeutic targets in diabetes and obesity
George Kunos, NIAAA/NIH
Junior Speaker: Protein and Gene Expression of Angiotensin II Receptors (AT1 and AT2) in Aorta of Diabetic and Hypertensive Rats
Rodrigo Romero, Escuela Superior de Med. IPN
Wrap-up
Integrative Systems, Translational and Clinical Pharmacology Division Young Investigator Awards Platform Session
San Diego Convention Center, Room 5A
3:00 PM – 5:30 PM
Chairs: Michael A. Holinstat, Thomas Jefferson Univ. and Ross Corriden, Univ. of California at San Diego
Introduction
Evidence for an angiotensin-(1-7) neuropeptidase in the brain medulla of sheep
Allyson Marshall, Wake Forest Univ. Sch. of Med.
Effect of HIV-1 Tat on enteric neuropathogenesis
Joy Ngwainmbi, Virginia Commonwealth Univ.
Enhanced in vitro cancer cell cytotoxicity of dual ligand-targeted liposomes
Shravan Sriraman, CPBN, Northeastern Univ.
Effects of selective inhibitors of the isoprenoid biosynthetic pathway on androgen-dependent and independent prostate cancer cells
Jacqueline Reilly, Univ. of Iowa
Targeting GUCY2C for anti-obesity pharmacotherapy
Gilbert Kim, Thomas Jefferson Univ.
Rgs16 is an early marker of pancreatic ductal adenocarcinoma
Ozhan Ocal, UT Southwestern Med. Ctr.
PAR4 Mediates an Elevated Risk for Thrombosis in Blacks Relative to Whites
Benjamin Tourdot, Thomas Jefferson Univ.
Toxicology Division Symposium: Macrophages and tissue injury: Agents of defense or destruction?
San Diego Convention Center, Room 5B
3:00 PM – 5:30 PM
Chair: Debra L. Laskin, Rutgers Univ.
Pathologic and protective role of macrophages in drug-induced hepatotoxicity
Debra L. Laskin, Rutgers Univ.
Macrophage subpopulations in kidney injury and repair
Jeremy S. Duffield, Univ. of Washington
Macrophage heterogeneity in cardiovascular disease
Filip K. Swirski, Mass General Hosp./Harvard Med. Sch.
Macrophages are required to maintain type 2-dependent inflammation, immunity, and fibrosis
Luke Barron, NIH/NIAID
 "Sue Duckles")
PAUL M. VANHOUTTE AWARD LECTURE IN VASCULAR PHARMACOLOGY
San Diego Convention Center, Room 3
4:30 PM – 5:30 PM
Sue P. Duckles, Univ. of California-Irvine Col. of Med.
Vascular Mysteries: More than the Sum of the Part
Cardiovascular Pharmacology Division Mixer
Marriott Marquis & Marina, Presidio I/II
6:30 PM – 8:00 PM
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RAY FULLER AWARD LECTURE
San Diego Convention Center, Room 2
8:30 AM – 9:20 AM
Jeffrey M. Witkin, Lilly Research Labs
AMPA receptor potentiation: Implications for the discovery of medicines for treatment-resistant depression
RAY FULLER SYMPOSIUM: Treatment-resistant depression (TRD): Biological bases and treatments
San Diego Convention Center, Room 2
9:30 AM – 12:00 PM
Chair: Jeffrey M. Witkin, Lilly Research Labs
The Ray Fuller symposium will complement the Ray Fuller Lecture by addressing new approaches to attacking the problem of treatment resistance depression by focusing on both novel clinical approaches as well as new developments in preclinical modeling.
Introduction
Jeffrey M. Witkin, Lilly Research Labs
Neurostimulation
Paul E. Holtzhiemer, Dartmouth Hitchcock Med. Ctr.
The cholinergic hypothesis
Christian C. Felder, Lilly Research Labs
The glutamate hypothesis
Phil Skolnick, NIDA
Kappa opioid receptors
Irwin Lucki, Univ. of Pennsylvania
Arginase as an emerging therapeutic target
San Diego Convention Center, Room 5B
9:30 AM – 12:00 PM
Sponsored by the Divisions for Drug Discovery and Development; Cardiovascular Pharmacology; Integrative Systems, Translational and Clinical Pharmacology; and Molecular Pharmacology
Chair: R. William Caldwell, Med. Col. of Georgia, Georgia Regents Univ.
While part of the hepatic urea cycle, arginase is widely distributed and is expressed in many non-hepatic cell types that lack urea cycle function. Overactive arginase has been implicated in neurovascular injury, abnormal vascular growth and remodeling, tissue fibrosis during vascular disease and tumor growth. This symposium will cover the various cellular and molecular effects of elevated arginase activity and the implications for the development of novel therapeutic interventions.
Recent advances in arginine metabolism: Role and regulation of arginase isoforms
Sidney M. Morris, Jr., Univ. of Pittsburgh Sch. of Med.
Role of arginase in retinovascular disease
Ruth B. Caldwell, Med. Col. of Georgia, Georgia Regents Univ.
Role of arginases in atherosclerotic vascular disease and age-related vascular dysfunction
Dan E. Berkowitz, Johns Hopkins Univ. Sch. of Med.
Involvement of arginase in cancer biology
Augusto Ochoa, LSU Hlth New Orleans
Junior Speaker: Arginase 1 Regulates SIRT1 Activity and Endothelial Senescence in Diabetes
Haroldo Toque, Georgia Regents Univ.
Chemical biology in drug discovery
San Diego Convention Center, Room 4
9:30 AM – 12:00 PM
Sponsored by the Divisions for Molecular Pharmacology & Drug Discovery and Development
Chairs: Haian Fu, Emory Univ.
Recent NIH initiatives and an expanding number of academic chemical biology centers have fueled the rapid discovery of small molecule modulators for many therapeutically associated molecular pathways and the large scale profiling of therapeutic agents for their efficacy as well as toxicity. All together, these activities enhance our understanding of the mechanism of actions and toxicity of currently used therapeutic agents, accelerate the discovery of new leads for therapeutic development, and bridge the pharmacology discipline with a broad field of chemical biology, genomics, and systems biology. This session will highlight recent research activities in the broad area of chemical biology field that enhance the discovery and development of therapeutic agents and how these two fields merge to generate a synergistic impact on the development of the next generation of therapeutic agents to improve human health. Major goals of some national initiatives will also be presented.
Brief introduction
Haian Fu, Emory Univ.
Interrogating protein-protein interactions in cancer
Haian Fu, Emory Univ.
Targeting menin mediated epigenetic regulation for therapeutic discovery
Jolanta Grembecka, Uni. of Michigan
Discovery of new ligands based on the cholinergic modulation in neurodegenerative diseases
Hongzhuan Chen, Shanghai Jiaotong Univ. Sch. of Med.
Systems and target-based ligand discovery for GPCRs
Brian K. Schoichet, Univ. of California San Francisco
G protein-coupled receptor kinase selective small molecule inhibitors
Kristoff Homan, Univ. of Michigan
Scientists versus street chemists: The toxicity of designer marijuana
San Diego Convention Center, Room 3
9:30 AM – 12:00 PM
Supported by funding from Cayman Chemical Company
Sponsored by the Divisions for Toxicology; Behavioral Pharmacology; Integrative Systems, Translational and Clinical Pharmacology; and Neuropharmacology
Chairs: Laura P. James, Arkansas Children's Hosp. and Jeffery H. Moran, Univ. of Arkansas for Med. Sciences
K2, also known as Spice, is the most common term for "synthetic marijuana" products being sold in the US. These preparations typically contain high-efficacy synthetic cannabinoids, making them much more powerful than marijuana itself. Recent clinical and forensic reports demonstrate that some of the constituents of these synthetic marijuana preparations have unique toxicity, and morbidity and mortality reports are increasingly being associated with K2 use. Cardiac, neurologic, and psychiatric complications are common with K2 exposure, and metabolic, behavioral, and pharmacological studies are beginning to unravel the underlying mechanisms for these adverse effects. This symposium will review the known pharmacology and toxicology of K2 including perspectives of scientists that are working in the areas of public health, chemical analysis, receptor signaling, behavioral effects, and clinical case collection.
An analytical chemist's approach to public health problems
Jeffery H. Moran, Arkansas Dept. of Health
Atypical in vitro pharmacodynamic and metabolic characteristics of K2 synthetic cannabinoids: Keys to toxicity?
Paul L. Prather, Univ. of Arkansas for Med. Sciences
Pharmacodynamic and pharmacokinetic factors impacting the in vivo pharmacology and toxicology of K2 synthetic marijuana
William E. Fantegrossi, Univ. of Arkansas for Med. Sciences
Clinical and unexplained idiosyncratic toxicity of K2 exposure
Genevieve L. Buser, Oregon Hlth. Authority
Junior Speaker: Functional Consequences of Synthetic Cannabinoid Metabolites and CYP2C9 Polymorphisms
Catherine Allen, Univ. of Central Arkansas
"Target-site" drug metabolism and transport
San Diego Convention Center, Room 5A
9:30 AM – 12:00 PM
Sponsored by the Divisions for Drug Metabolism; Drug Discovery and Development; Integrative Systems, Translational and Clinical Pharmacology; and Toxicology
Chair: Robert S. Foti, Amgen
Therapeutic entities from systemic circulation, emerging evidence has highlighted the importance of drug metabolizing enzymes and transporters at the site of therapeutic action. Target-site drug metabolism can affect the efficacy, safety, and metabolic properties of a therapeutic drug, with potential outcomes including altered dosing regiments, stricter exclusion criteria, or even the failure of a new chemical entity in clinical trials. This proposed session will focus on the contribution of drug metabolizing enzymes and transporters at the site of action to the overall therapeutic properties of a given drug.
Drug metabolism within the brain changes drug response in vivo
Rachel F. Tyndale, Univ. of Toronto
The SLC22 transporter family: Impact on drug efficacy, drug-drug interactions and pathophysiology
Douglas H. Sweet, Virginia Commonwealth Univ.
Pulmonary metabolism of Resveratrol: In vitro and in vivo evidence
Swati Nagar, Temple Univ. Sch. of Pharmacy
Tumor metabolism of antibody-drug conjugates: Effect on pharmacokinetics and efficacy
Dan A. Rock, Amgen, Inc.
Junior Speaker: The ABC transporter Mrp4/Abcc4 is required for Leydig cell protection from chemotherapeutic drugs
Jessica A. Morgan, St. Jude Children’s Res. Hosp.
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Future therapies for chronic pain: Focus on novel non-opioid targets
San Diego Convention Center, Room 4
3:00 PM – 5:30 PM
Sponsored by the Divisions for Neuropharmacology; Behavioral Pharmacology; Cardiovascular Pharmacology; Drug Discovery and Development; Integrative Systems, Translational and Clinical Pharmacology; and Molecular Pharmacology
Chair: Beverley Greenwood-Van Meerveld, Univ. of Oklahoma-HSC
Chronic pain represents a significant heath burden estimated to affect 40% of all adults in the United States. While previous ASPET symposia have focused on opioid-related therapies through discussing novel targets for G-protein coupled opioid receptors and peripheral mechanisms of opioid analgesia, this symposium will seek to expand the repertoire of potential treatments for chronic pain by highlighting cutting-edge research on non-opioid targets for neuropathic and visceral pain.
Overview of pre-clinical models for the development of novel therapies for treating chronic pain
Robert D. Foreman, Univ. of Oklahoma-HSC
Junior Speaker: Amygdaloid corticosteroid receptors as therapeutic targets for treatment of chronic stress-induced visceral pain
Anthony C. Johnson, Univ. of Oklahoma-HSC
A novel molecular switch regulating transition from acute to chronic pain
Annemieke M. Kavelaars, Univ. of Texas–MD Anderson Cancer Ctr.
Gene transfer for treatment of chronic pain
David J. Fink, Univ. of Michigan
Hydrogen sulfide: From physiological messenger to pharmacological target
San Diego Convention Center, Room 2
3:00 PM – 5:30 PM
Sponsored by the Divisions for Cardiovascular Pharmacology; Integrative Systems, Translational and Clinical Pharmacology; Molecular Pharmacology; and Toxicology
Chairs: Nancy L. Kanagy, Univ. of New Mexico Sch. of Med. and Utpal Sen, Univ. of Louisville Sch. of Med.
Hydrogen sulfide (H2S), a gas with a foul odor known for its toxicity, has recently been recognized, along with nitric oxide (NO) and carbon monoxide (CO), as a novel regulator of cardiovascular function. Many tissues produce H2S in the body, and it is now apparent that it regulates a wide array of physiological processes including angiogenesis, ion-channel activity, glucose metabolism, cell proliferation, and apoptosis as well as ameliorating pathophysiological conditions such as inflammation, ischemic cardiac disease, neurodegeneration, and hypertension. The intent of this symposium is to bring together scientists from diverse backgrounds to share, discuss, and disseminate new findings on the interactions of H2S with other mediators, mechanisms of H2S regulation of cellular function, and mechanisms for its protective effects in diabetes and other diseases.
Hydrogen sulfide: Overview of its production and function
Hideo Kimura, National Inst. of Neuroscience
Hydrogen sulfide: A novel endothelium-dependent dilator
Nancy L. Kanagy, Univ. of New Mexico Sch. of Med.
Hydrogen sulfide as a novel therapeutic agent
Christopher G. Kevil, Louisiana State Univ.
Hydrogen sulfide: A novel mediator of diabetic renovascular remodeling
Utpal Sen, Univ. of Louisville Sch. of Med.
Junior Speaker: Hyperhomocysteinemia aggravates endothelial dysfunction via EDHF impairment in resistant arteries of db/db mice
Zhongjian Cheng, Temple Univ.
Improving maternal therapeutics: Drug metabolism and transport during pregnancy and lactation
San Diego Convention Center, Room 3
3:00 PM – 5:30 PM
Supported by funding from Pregmedic, the Canadian Alliance for the Safe and Effective Use of Medications in Pregnancy and Breastfeeding
Sponsored by the Divisions for Drug Discovery and Development; Drug Metabolism; and Integrative Systems, Translational and Clinical Pharmacology
Chairs: Nina Isoherranen, Univ. of Washington; Hollie Swanson, Univ. of Kentucky Med. Center; and Donald Mattison, Risk Sciences Intl.
Use of prescription and over the counter drugs is very common during pregnancy, but due to changes in drug metabolism and transport during pregnancy, the dosing of drugs cannot be directly extrapolated from non-pregnant women or men. Increased scrutiny by the FDA and NIH on therapy of pregnant women has resulted in a considerable increase in the amount of research generated in the area of drug disposition during pregnancy. This symposium is designed to cover the area of drug disposition during pregnancy and highlight the breadth of tools that are currently used to investigate drug disposition during pregnancy.
General overview
Nina Isoherranen, Univ. of Washington
Prediction of drug disposition during pregnancy by PBPK modeling and simulation
Jashvant Unadkat, Univ. of Washington
Junior Speaker: Mechanisms of CYP2D6 regulation during pregnancy
Hyunyoung Jeong, Univ. of Illinois-Chicago
Adaptive changes in liver and intestinal metabolism and transport function in pregnancy and lactation
Mary Vore, Univ. of Kentucky
Addressing pregnancy-associated changes in pharmacodynamics and pharmacokinetics of anti-malaria drugs
Joel Tarning, Mahidol Univ.
Panel discussion
Donald Mattison, Risk Sciences Intl.
Targeted/individualized therapy: Approaches for the future translational pharmacologist
San Diego Convention Center, Room 5A
3:00 PM – 5:30 PM
Supported by funding from SomaLogic and Metabolon
Sponsored by the Divisions for Integrative Systems, Translational and Clinical Pharmacology; Cardiovascular Pharmacology; Drug Discovery and Development; Molecular Pharmacology; and Toxicology
Chair: Jeffrey Paul, Astellas
Personalized medicine, described as giving the right drug, at the right dose, to the right person, requires certain tools and approaches to deal with the heterogeneity of human disease. The use of various -omic platforms, including genomics, transcriptomics, proteomics, and metabolomics are some of the approaches used to evaluate individualized molecular interventions. The need for bioinformatics and disease pathway identification are necessary tools to interpret the results of the -omics laboratory and to assign translational/therapeutic relevance. The purpose of this symposium is to introduce molecular approaches available to the pharmacologist and to provide current tools for integration with translational bioinformatics, using examples from oncology targeted therapeutics.
Systematic identification of genomic markers of anti-cancer drug sensitivity
Cyril H. Benes, Massachusetts General Hosp.
Metabolomic approaches to translation and drug targeting
Rima Kaddurah-Daouk, Duke Univ.
Proteomics as an approach to understanding drug action
Francisca O. Gbormittah, Northeastern Univ.
Omics information, integration and translational bioinformatics
Nicholas Tatonetti, Columbia Univ.
Junior Speaker: Bile acids and acetaminophen protein adducts in children with acetaminophen overdose
Sudeepa Bhattacharyya, Univ. of Arkansas for Med. Sci.
ASPET Closing Reception
San Diego Marriott Marquis & Marina, Poolside Terrace (weather permitting)
6:00 PM – 8:00 PM
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