Give a Day of Service to San Diego at EB 2016

7:00 am-3:00 pm 

Since 2009, ASPET members attending Experimental Biology (EB) have given a day of volunteer service in the local communities  such as New Orleans, Pasadena, Washington DC, and San Diego.

Volunteer activities have ranged from home construction to painting, cleaning, stocking, food preparation, and food service. ASPET's division for behavioral pharmacology is again sponsoring a volunteer opportunity at EB 2016 in San Diego.

For the third time, we will 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 your earliest convenience.

Email: france@uthscsa.edu
Tel: 210 567 6969

Space is limited and further details will be provided to those who volunteer.  

Securing NIH Intramural Fellowships to Enhance Your Pharmacology Training

San Diego Convention Center
9:30 am–12:00 pm

Chairs:
Janet E. Clark—Nat’l Inst. of Mental Hlth./NIH 
A. Reid—Nat’l Inst. of Mental Hlth./NIH

This session will provide an overview of how the NIH is organized, the research institutes it comprises, differences between the intramural and extramural research programs, and an outline of the fellowship opportunities available on the NIH campuses in the intramural programs. Following this summary of fellowship opportunities, NIH training directors from NIMH, NINDS, NIAID and NIDCD will present a summary of the unique research being done in their respective institutes, highlighting more specifically where pharmacology is of particular importance. A panel discussion will follow the presentations, where trainees will have time to ask questions and discuss opportunities with the speakers.

Sponsored by the Division for Pharmacology Education. 

Co-Sponsored by the Divisions for:     

• Behavioral Pharmacology    
• Cancer Pharmacology   
• Cardiovascular Pharmacology   
• Drug Discovery and Development    
• Drug Metabolism    
• Translational and Clinical Pharmacology    
• Molecular Pharmacology    
• Neuropharmacology   
• Toxicology    

Fellowship Opportunities at the NIH
Aneka Reid—NIMH/NIH   

NIMH: Opportunities for the Investigation and Treatment of Mental Illnesses Through Basic and Clinical Research
Janet Clark—NIMH/NIH  

NIAID’s Global Health Research Challenge: Emerging, Persisting and Preventing Infectious Diseases
Wendy Fibison—NIAID/ NIH  

An Overview of the NINDS Intramural Research Program from Basic to Clinical Neurosciences
Katherine Roche —NINDS/ NIH  

NIDCD Research Training in the Hearing and Communication Sciences
Elyssa Monzack—NIDCD/ NIH  

2016 Teaching Institute: Developing Mentees Using IDPs

San Diego Convention Center
12:00 pm–2:30 pm

Chairs:
Kelly Karpa—Penn State Univ. Coll. of Med.
Jonathan P. Neiswinger—NIA/NIH

This session will educate attendees about what an individual development plan (IDP) is, the NIH requirements for trainees to develop an IDP, explore the realities of how IDPs are currently being used by identifying barriers and solutions for mentors/mentees, demonstrate the practical utility of existing IDP tools, and hear how IDPs were instrumental in the success of a young trainee.

Sponsored by the Division for Pharmacology Education  

The What and Whys of IDPs for NIH-Supported Trainees
Nancy Desmond—NIMH/NIH 

Using Available Tools to Facilitate IDP Development
Cynthia N. Fuhrmann—Univ. of Massachusetts Medical Sch. 

The Reality of IDP Implementation
Philip S. Clifford—Univ. of Illinois at Chicago 

How an IDP Jump-Started My Career
Asia Klementowicz—Univ. of California, San Francisco 

Graduate Student-Postdoctoral Colloquium

Marriott Marquis San Diego Marina
2:45 pm–5:15 pm

Sponsored by the ASPET Mentoring and Career Development Committee  

Chair:
Lynn Wecker—Univ. South Florida College of Medicine 

Mentoring Your Mentor: Key Skills for Effective Mentoring Relationships with Shared Responsibility
Rick McGee—Northwestern Medicine 

ASPET Business Meeting and Awards Presentation

San Diego Convention Center
6:00 pm–7:30 pm

Hear updates on Society activities and initiatives. Join us in recognizing excellence in pharmacology as we present the ASPET 2016 Scientific Achievement Awards, Travel Awards, and PhRMA Foundation Awards. 

ASPET-PhRMA Foundation Opening and Awards Reception

San Diego Convention Center
7:30 pm–9:30 pm

The opening reception immediately follows the conclusion of the business meeting. ASPET members and pharmacology attendees are welcome to join us as we celebrate our awardees and the 50th Anniversary of the PhRMA Foundation. 

 

Julius Axelrod Award in Pharmacology Lecture

Therapies of Brain Diseases, Past, Present and Future

8:30 am–9:20 am

Keynote:
Jean Rossier—Neuroscience Paris Seine 

Julius Axelrod Symposium

New Vistas on Drug and Gene Therapies of Cognitive Deficits in Down Syndrome, Autism, Leucodystrophies and Alzheimer's Disease

Supported by the John V. Croker Fund 

9:30 am–12:00 pm 

Chair: J. Rossier—Neuroscience Paris Seine 

This symposium should give to the audience hopes that new drug or gene therapies for Central Nervous System (CNS) diseases could be developed. At the present time pharmaceutical industries have withdrawn from CNS drug discovery as CNS drugs take longer to develop and have low success rate. The symposium is focused on cognitive disorders and has gathered leaders in their respective field. Dr. Hadjikhani will described the use of the diuretic Bumetanide in autism, Drs. Potier and Rafii will cover the clinical development of new Alpha 5 benzodiazepine inverse agonists in Down’s syndrome and Dr. Cartier will describe the promising preclinical studies on new gene therapies for Alzheimer’s disease.  

Comments on the 1986 Seminal Paper: Benzodiazepine Inverse Agonists Improved Performances in Learning and Memory Tasks
Jean Rossier—Neuroscience Paris Seine 

Treating Cognitive Deficits in a Mouse Model of Down Syndrome Using GABA-A Alpha 5 Inverse Agonists
Marie Claude Potier—Institut du Cerveau et de la Moelle Epinière, Paris 

Alpha 5 Benzodiazepine Inverse Agonists Clinical Studies for the Treatment of Cognitive Deficits in Down Syndrome Patients
Michael S. Rafii—Univ. of California, San Diego 

The Diuretic Bumetanide Improves Social Processing in Individuals with Autism
Nouchine Hadjikhani—Harvard Medical Sch., Boston 

Gene Therapy Strategy for Alzheimer's Disease: The Cholesterol Connection
Nathalie Cartier—INSERM Mircen CEA, Fontenay-aux-Roses, France 

Correcting Memory deficits in Fragile X Syndrome by Targeting Rac1/PAK1 Signaling
Luis Martinez—Univ. of Houston

Chronic Antagonism of p38α MAPK Normalizes Serotonin Clearance, Serotonin Receptor Hypersensitivity and Social Behavior Deficits in a Genetic Murine Model of Autism Spectrum Disorder
Matthew Robson—Vanderbilt Univ.

Emerging Roles for the Ubiquitin-Proteasome System in Therapeutics

9:30 am–12:00 pm

Chairs:
B. Sjogren—Michigan State Univ.
H.L. Paulson—Univ. of Michigan Health System

The ubiquitin-proteasome system (UPS) serves a crucial role in virtually all aspects of cellular functions, including degradation of misfolded proteins as well as cell cycle progression, cell differentiation and apoptosis. Dysregulation of this system can lead to severe consequences such as accumulation of misfolded proteins and cell cycle arrest. Thus pathophysiology, including cancer, neurodegenerative diseases, and cardiovascular disease can, in many cases, be related to defects in the UPS. This symposium elaborates on the importance of the UPS as a therapeutic target and provides an update on the progress of drug discovery and development both basic and clinical.

Sponsored by the Division for Drug Discovery and Development. Co-sponsored by the Divisions for:  

• Molecular Pharmacology 
• Neuropharmacology 
• Cancer Pharmacology 

The Ubiquitin-Proteasome System in Health and Disease
Raymond J. Deshaies—HHMI and California Institute of Technology 

The Role of the Ubiquitin-Proteasome System in Neurodegenerative Disease
Henry L. Paulson—Univ. of Michigan Health System 

Clinical Development of MDM2 E3 Ligase Antagonists in Cancer Treatment
Gwen L. Nichols—Roche Pharma Research and Early Development 

Targeting Degradation of Regulator of G Protein Signaling Proteins in Therapeutics
Benita Sjogren—Michigan State Univ. 

Ubiquitin Plays an Atypical Role in GPCR-induced p38 MAP Kinase Activation on Endosomes
Neil Grimsey—Univ. of California, San Diego

Drugs of Abuse and Antiretrovirals: Interactions and Toxicities

9:30 am–12:00 pm

Chairs:
S. Kumar—Univ. of Missouri-Kansas City
K. Jordan-Sciutto—Univ. of Pennsylvania

Drugs of abuse are an important comorbidity in HIV-infected populations. Thus interactions between antiretroviral therapy (ART), drugs of abuse, and drugs used to treat other comorbidities are serious challenges in treating the HIV+ patients. Drug interactions and toxicities by ART and drugs of abuse are not only limited to peripheral cells but also severely affect brain cells, leading to exacerbated HIV-associated neurocognitive disorder. This symposium will focus on such drug interactions and drug-mediated toxicities. The attendees will learn the impact of drug interactions/toxicities during HIV infection and appreciate the importance for developing precise medication for these patients.  

Sponsored by the Division for Drug Metabolism. Co-sponsored by the Divisions for:  

• Neuropharmacology 
• Toxicology 
• Pharmacology Education 
• Molecular Pharmacology 

Antiretroviral Drugs Induce Oxidative Stress and Neuronal Damage in the Central Nervous System
Kelly Jordan-Sciutto—Univ. of Pennsylvania 

Drug-Drug Interactions in HIV-Infected Patients Who Have Other Comorbid Conditions
Walter Royal—Univ. of Maryland Sch. of Med. 

Differential Drug Interactions Between Antiretroviral Drugs and Methamphetamine in Human and Rhesus Monkey
Anil Kumar—Univ. of Missouri-Kansas City 

Interactions of HIV and Drugs of Abuse: The Importance of Glia, Neural Progenitors, and Host Genetic Factors
Pamela Knapp—Virginia Commonwealth Univ. 

Drug Interactions and Toxicity between ART and Alcohol in Monocytes and Astrocytes: Implications with HIV Pathogenesis
Santosh Kumar—Univ. of Tennessee Hlth. Sci. Ctr. 

Tobacco Smoking and HIV Pathogenesis: Potential Role of Cytochrome P450 Pathway
PS Shantanu Rao—Univ. of Findlay 

Newly Recognized GPCRs in Health, Disease and as Therapeutic Targets

9:30 am–12:00 pm 

Chairs:
Ross Corriden—Univ. of California, San Diego
Paul A. Insel— Univ. of California, San Diego

G protein-coupled receptors (GPCRs), the largest family of signaling receptors in the human genome, are also the largest class of targets of approved drugs. Despite this utility of GPCRs as therapeutic targets, one can ask: Are the optimal GPCRs (in terms of efficacy and safety) targeted by current therapeutic approaches? This question derives in part from the therapeutic targeting of only a fraction of the known GPCRs. Especially given the ~120 orphan GPCRs (without known physiologic agonists), previously unrecognized GPCRs likely regulate cellular functions and can be targeted therapeutically. This session highlights research that has identified such new GPCR targets.

Sponsored by the Division for Translational and Clinical Pharmacology.  Co-sponsored by the Divisions for:  

• Molecular Pharmacology 
• Cardiovascular Pharmacology 
• Neuropharmacology 

GPCRs and the Druggable Genome
Bryan Roth—Univ. of North Carolina-Chapel Hill Sch. Of Med. 

Chemosensory GPCRs as Targets for Endogenous Ligands
Jennifer Pluznick—Johns Hopkins Univ. Sch. of Med. 

GPCRs as Regulators of Neutrophil Function
Ross Corriden—Univ. of California, San Diego 

Orphan GPCRs and Psychiatric Disorders: GPR88
Brigitte Kieffer—McGill Univ.  

The Extent of Vascular Remodeling is Dependent on the Balance Between ERα and GPER(GPR30)
Robert  Gros—Robarts Research Inst., Western Univ.

Identification of a First-In-Class Adhesion G protein-Coupled Receptor Orthosteric Antagonist
Hannah Stoveken—Univ. of Rochester Med. Ctr.

Advances in Toxicogenetics of Metals

9:30 am–12:00 pm 

Chairs:
J. Kim—Northeastern Univ.
T. Maher—MCPHS Univ.

The body maintains the optimal levels of individual essential metals by a variety of proteins, including metal transporters, receptors and enzymes, which are tightly regulated at the levels of transcription and translation. However, several non-essential heavy metals share similar metabolic systems with essential metals, resulting in increased toxicities. Despite rapid progress in understanding of metal biology, less is known about how genetic, nutritional, pharmaceutical and environmental factors can modify the transport and toxicities of metals. The symposium will discuss and address the emerging issues on the molecular mechanisms and pathophysiology of gene-metal interactions.

Sponsored by the Division for Toxicology. Co-sponsored by the Divisions for: 

• Behavioral Pharmacology 
• Cancer Pharmacology 
• Molecular Pharmacology 

Influence of Brain Iron Overload on Behavioral and Neurochemical Toxicity
Jonghan Kim—Northeastern Univ. 

Neurobehavioral Effects of Lead (Pb) and Manganese Individually and in Combination in Developmentally-Exposed Rats
Timothy Maher—MCPHS Univ. 

A Novel Molecular Mechanism of Arsenic in Modulating Autophagy and Nrf2 Stress Responses
Donna Zhang—Univ. of Arizona 

Mechanisms of Cisplatin Nephrotoxicity
Navjot Singh Pabla—The Ohio State Univ. 

Ferroportin Deficiency Impairs Manganese Metabolism in Flatiron Mice
Marianne Wessling-Resnick—Harvard T.H. Chan Sch. of Public Health 

Undergraduate Research: Cultivating the Next Generation of Researchers through SURF and Beyond

9:30 am–12:00 pm 

Chairs:
Catherine Fry—ASPET
Catherine Davis—Johns Hopkins Univ. Sch. of Med.
Lauren Aleksunes—Rutgers Univ.

Participating in research has widely-established benefits for students. Yet, despite the increased prevalence of undergraduate research programs, there are limited opportunities for faculty and students to come together to share strategies, successes, and challenges related to student research. This symposium is structured around ASPET's SURF program, but it is intended to be broadly useful to any faculty who mentor undergraduate researchers as well students either currently participating or interested in research. Panels will be followed by interactive discussions to generate insights and feedback both for the participants and for ASPET in order to better cultivate the next generation of researchers.

Introduction and Overview
Catherine Fry—ASPET 

Faculty Perspectives on Undergraduate Research
Lauren Aleksunes—Rutgers Univ.
Stella Tsirka—Stony Brook Univ.
Kevin Murnane—Mercer Univ. 

Student Perspectives on Undergraduate Research
Natalie Arabian—Univ. of Southern California
Chelesa Fearce—Spelman Coll.
Michael Little—UNC Chapel Hill 

Interactive Table Discussions 

 

ASPET Poster Presentations

12:30 pm–2:30 pm 

Goodman and Gilman Award in Receptor Pharmacology Lecture

Towards an Atomic-level Understanding of Psychoactive Drug Actions

2:00 pm–2:50 pm 

Keynote:
Bryan L. Roth—University of North Carolina, Chapel Hill   

ASPET Presidential Symposium: Precision Medicine in Anti-Cancer Pharmacology

3:00 pm–5:30 pm 

Chairs:
Ken Thummel—Univ. of Washington
Susan P.C. Cole—Queen’s Univ. Cancer Res. Inst.

Co-sponsored by the Divisions for:   

• Cancer Pharmacology 
• Cardiovascular Pharmacology 
• Translational and Clinical Pharmacology 

Overview of Precision Medicine
Ken Thummel—Univ. of Washington  

Pharmacogenomics: A Foundation of Precision Medicine for Leukemia
William Evans—St. Jude Children's Research Hosp.  

Genome Wide Studies of Chemotherapeutic Associated Toxicities
Eileen Dolan—Univ. of Chicago 

Use of Tumor Genomics to Customize Drug Treatment in Women with Triple Negative Breast Cancer
Anthony Blau—Univ. of Washington 

Breast Cancer Pharmacogenomics: Application of PDX Model
Liewei Wang—Mayo Clinic  

Sex Differences in Cardiovascular and Renal Pharmacology

3:00 pm–5:30 pm 

Chairs:
S.H. Lindsey—Tulane Univ.
E. Gohar—Univ. of Alabama at Birmingham

Cardiovascular disease is the number one cause of death for both men and women, but many of the molecular mechanisms involved in its development and progression disease differ by sex. Preferential use of male experimental animals expands the gap in understanding how sex affects cardiac, vascular, and renal outcomes. Although the number of animal and clinical studies which include females is steadily increasing, sex is still not considered when prescribing lifestyle or pharmacological interventions. This symposium will address important sex differences in the heart, vasculature, and kidney and discuss how pharmacological treatments exert disparate effects in men versus women.

Sponsored by the Division for Cardiovascular Pharmacology. Co-sponsored by the Division for Molecular Pharmacology.    

Sex-specific Immune Mechanisms in Vascular Disease
Kathryn Sandberg—Georgetown Univ. Medical Ctr.  

Double-edged Sword: Sex Hormones in Renal Health
Margaret Zimmerman—Tulane Univ.  

Sexual Dimorphism in Nicotine Interaction with Baroreflex Control of Heart Rate
Mahmoud El-Mas—Alexandria Univ., Egypt 

Sex Hormones and Vascular Protection: Clinical Implications
Fadi Hage—Univ. of Alabama at Birmingham 

Sex Specific Differences In Key Signaling Pathways Involved In Sympathetic Nervous System Control Within The Dorsal Medulla Of Adult Sheep With Fetal Betamethasone Exposure
Alexa Hendricks—Wake Forest Sch. of Med.

Sex-based Differences in the Aortic Function of UCD-T2DM Rats: A Novel Rat Model of Type 2 Diabetes Mellitus
Farjana Akther—Univ. of the Pacific

The Effects of Sex and Genotype on the Population Pharmacokinetics and Pharmacodynamics Modeling and Simulation of Low Dose Epinephrine and Cardiac Output
Andy R. Eugene—Mayo Clinic

Cannabinoid Signaling in Pain and Addiction: Translating Preclinical Basic Research to the Clinic

3:00 pm–5:30 pm 

Chairs:
D. Morgan—Penn State Univ. Col. of Med.
J. Guindon—Texas Tech Univ. Health Sciences Ctr.

This symposium will highlight recent advances in our understanding of how cannabinoid signaling modulates pain and addiction and will feature topics ranging from the molecular neuropharmacology of cannabinoid signaling to the clinical uses of cannabinoids. Other topics that will be discussed include the role of the circulating endocannabinoids in pain, mechanisms of cannabinoid tolerance, and the role of cannabinoid signaling in addiction. This timely symposium will shed new insight on the potential therapeutic uses of cannabinoid drugs in the treatment of chronic pain as well as some of their clinical limitations including tolerance and addiction.  

Sponsored by the Division for Neuropharmacology. Co-sponsored by the Divisions for:    

• Behavioral Pharmacology 
• Molecular Pharmacology 
• Drug Discovery and Development 
• Translational and Clinical Pharmacology 

Allosteric Modulators of Cannabinoid Receptor Function
Ken Mackie—Indiana Univ.  

Cannabidiol as an Anti-Inflammatory/Analgesic and Potential Anti-Addictive Treatment
Ethan Russo—Phytecs 

Endocannabinoids in Circulation and Pain
Cecilia Hillard—Medical Col. of Wisconsin 

Insights Into the Mechanisms of Tolerance for Cannabinoid Drugs
Josee Guindon—Texas Tech Univ. Health Sciences Ctr.  

Role of the Endocannabinoid System in Addiction
Rafael Maldonado—Universitat Pompeu Fabra 

Division for Pharmacology Education Symposium: Meet the New POPS—They'll Flip Your Teaching

3:00 pm–5:30 pm 

Chairs:
M.A. Simmons—Univ. of Maryland Eastern Shore
R. Theobald—A.T. Still Univ.—Kirksville Col. of Osteo. Med.

This workshop will be the roll out of the newly-revised patient-oriented problem-solving system in Pharmacology. The POPS are small group exercises covering various aspects of pharmacology. The POPS provide a platform for pharmacology-focused activities and are designed to meet the needs of pharmacology educators to offer problem-solving exercises, active learning, peer-to-peer teaching and interprofessional education. Participants will be split into groups. Each group will work through one of the exercises. Authors of the revised POPS will serve as facilitators of the groups. Once the exercises have been completed, the audience will reassemble for a summary and discussion. Please bring your laptop.

Sponsored by the Division for Pharmacology Education.   

A Brief History of the POPS and Presentation of Their Current Structure.
Mark A. Simmons—Univ. of Maryland Eastern Shore 

Treatment of Essential Hypertension
Mark A. Simmons—Univ. of Maryland Eastern Shore 

Treatment of Cardiac Arrhythmias
June Yun—Northeast Ohio Med. Univ 

Drug Treatment of Heart Failure
Rob Rockhold—Univ. of Mississippi Medical Ctr.  

Therapy of Diabetes Mellitus
Jayne Reuben—Univ. of South Carolina Sch. of Med. Greenville  

Treatment of Psychosis
Gagani Athauda—Florida Intl. Univ. 

Drug Overdose Toxicity
Robert Theobald, Jr.—A.T. Still Univ., Kirksville Col. of Osteo. Med.  

From Ligands to Signaling: Recent Advances in Adhesion GPCR Pharmacology and Biology

3:00 pm–5:30 pm 

Chairs:
X. Piao—Boston Children's Hospital
R.A. Hall—Rollins Res. Ctr.

The goal of this symposium is to capitalize on new breakthroughs in the emerging research areas of structure, signaling, as well as natural ligand and synthetic molecule modulation of adhesion G protein-coupled receptors (aGPCRs). Numerous recent reports have demonstrated that aGPCRs play critical roles in brain development, myelination, blood brain barrier formation, and cancer progression. Moreover, mutations in multiple members of the aGPCR class cause human diseases. This symposium brings together established and emerging leaders in the aGPCR field to discuss recent advances in our understanding of the signaling mechanisms, structural organization, biological functions, and pharmacological properties of aGPCRs.

Sponsored by the Division for Molecular Pharmacology. Co-sponsored by the Divisions for:    

• Drug Discovery and Development 
• Neuropharmacology 
• Cancer Pharmacology 
• Cardiovascular Pharmacology 

Signaling and Regulation of the BAI Subfamily of Adhesion GPCRs
Randy A. Hall—Emory Univ. School of Medicine  

Structural Organization of the Extracellular Domains of Adhesion GPCRs
Demet Arac-Ozkan—Univ. of Chicago 

Adhesion GPCRs are Turned on by Tethered Ligands
Torsten Schöneberg—Univ. Leipzig 

Adhesion GPCR Activation by Tethered Agonist Decryption and Small Molecule Antagonism
Gregory Tall—Univ. of Rochester Medical Ctr.  

In Vivo Small Molecule Screens Define Modulators of Adhesion GPCR Signaling
Sarah C. Petersen—Washington Univ.—St. Louis 

GPR56 and its Ligand in Oligodendrocyte Development and Myelination
Xianhua Piao—Boston Children's Hospital 

Dose Selection Using Physiologically Based Modeling

3:00 pm–5:30 pm 

Chair: J. Wahlstrom—Amgen, Inc.

The accurate prediction of pharmacokinetics (PK) is fundamental to underwriting safety and efficacy in clinical trials. Physiologically based pharmacokinetic (PBPK) modeling is an emerging technique that can integrate intrinsic (population and physiological) and extrinsic (drug specific) characteristics to model and simulate PK based on in vitro, preclinical and clinical data. PBPK can also simulate scenarios involving complex physiology such as disease states or age-dependent changes in PK observed for pediatrics. This session will focus on how physiological or physicochemical data is incorporated into PBPK models and how PBPK may be used to impact decision making in drug discovery and development.

Sponsored by the Division for Drug Metabolism. Co-sponsored by the Division for Pharmacology Education.  

Translation of Preclinical Information to Clinical Dose Selection Using PBPK Approaches
Hannah Jones—Pfizer Worldwide R&D 

Mechanistic Insights to the Prediction of Nonlinear Pharmacokinetics
Jan Wahlstrom—Amgen, Inc.  

Modeling and Simulation to Support Pediatric Drug Development
Andrea Edginton—Univ. of Waterloo 

Predicting the Effects of Cytokine Modulation on Pharmacokinetics Using PBPK
Yang Xu—Amgen, Inc. 

Simulating Biodistribution and Pharmacokinetics for Protein Therapeutics Using PBPK
Patrick Glassman—University at Buffalo 

Student/Postdoc Poster Competition

6:30 pm–8:30 pm 

ASPET Divisions award prizes to undergraduates, graduate students, and postdocs making the best poster presentations at this event. Only ASPET members are eligible. You must submit an abstract to EB by November 5th and apply to compete through the ASPET online awards portal by November 23rd.  

Student/Postdoc Mixer

8:30 pm–11:00 pm 

A little dancing, a little networking…a high-energy event designed for students and postdocs to mingle.  

 

John J. Abel Award in Pharmacology Lecture

Epithelial-Mesenchymal Plasticity in Carcinoma

8:20 am–9:20 am 

Keynote:
Rita J. Valentino—Children’s Hosp. of Philadelphia / Univ. of Pennsylvania

Hear It from the Editors: Navigating the Course through Journal Submission and Publication

9:30 am–12:00 pm 

Chairs:
M. Vore—Univ. of Kentucky
E. Morgan—Emory Univ.

This symposium is intended as a practical guide for early-career scientists to enhance their writing and analytical skills, with a focus on publishing in ASPET journals. Attendees will learn about key elements of generating a competitive manuscript. They will leave with an enhanced knowledge of how to effectively deal with rejection and revision decisions, and with increased awareness of publication ethics and accountability. They will also receive specific information about the ASPET journals and individual journal editorial policies & initiatives.

Co-sponsored by all of ASPET’s Divisions  

How to Choose a Journal for Your Manuscript?
Mary Vore—Univ. of Kentucky 

How to Write a Competitive Manuscript
Michael Jarvis—AbbVie, Inc.  

Communicating Experimental Design and Analysis Considerations
Edward Morgan—Emory Univ.  

The Peer—Review Process: Rejection, Revision, and Acceptance
Steven Traynelis—Emory Univ.  

Authorship, Accountability, and Ethics
Richard Dodenhoff—ASPET 

Panel Discussion
Moderator: David R. Sibley—ASPET Board of Publications Trustees 

Beyond Traditional Assessments of Pain: Implications for Drug Discovery of Novel Pain Therapeutics

9:30 am–12:00 pm 

Chairs:
Carol A. Paronis – McLean Hosp.
Harshini Neelakantan – Univ. of Texas Med. Branch Galveston

Sponsored by the Division for Behavioral Pharmacology. Co-sponsored by the Divisions for:   

• Neuropharmacology 
• Drug Discovery and Development 

Pain is a common, debilitating clinical condition with unmet therapeutic need. Traditional reflexive pain models have shown good predictive validity in the discovery of pain therapeutics, yet lack the translational ability to capture important facets of human pain conditions. Development of translational and non-traditional assays to measure pain has been a current topic of research. Speakers in this symposium will present diverse approaches to quantitatively measure multiple dimensions of pain, including successes and failures, while highlighting the responsiveness of such behavioral measures to pharmacological manipulations.

Analgesic Medication Development: Finding the Appropriate Assay to Identify New Therapeutics
Robert P. Yezierski—Univ. of Florida  

Novel Methods of Assessing Nociception and Antinociception in Nonhuman Primates
Brian Kangas—Harvard Medical School, McLean Hosp.  

Pharmacological Responses in Spontaneous Pain
Jeffrey Mogil—McGill Univ. 

Distinguishing Nonopioid Mediators of Pain Suppression
Andrea Hohmann—Indiana Univ. 

Depression of Home Cage Wheel Running: A Novel Method to Assess Spontaneous Migraine Pain
Ram Kandasamy—Washington State Univ.

Neuropathic Pain Unmasks Delta Opioid Receptor-Mediated Analgesia
Edmund Ong—Queen's University

Substrate Modulation of Organic Anion and Cation Transporters

9:30 am–12:00 pm 

Chairs:
B. Hagenbuch—Univ. of Kansas Medical Ctr.
J. Lampe—Univ. of Kansas Medical Ctr.

In this session, attendees will learn about substrate-dependent activity modulation of the OCT1, MATE, OATP1B1, and OATP1B3 classes of transporters. This is an important phenomenon because recent findings suggest that these transporters can be modulated (either inhibited or stimulated) in a substrate-dependent manner, questioning the use of a single substrate for interactions studies. An overview of this phenomenon, along with the types of compounds are responsible for it, will be provided for each class of transporter. Additionally, attendees will obtain an industrial prospective on substrate modulation of transporter function and its assessment in the drug development and FDA approval process.

Sponsored by the Division for Drug Metabolism. Co-sponsored by the Division for Molecular Pharmacology.  

Substrate and Inhibitor Modulation of Hepatic OCT1 Transport
Jed Lampe—Univ. of Kansas Medical Ctr.  

Substrate-Dependent Ligand Interaction with MATE Transporters
Stephen Wright—Univ. of Arizona 

Substrate-Dependent Modulation of OATP1B1 and OATP1B3
Bruno Hagenbuch—Univ. of Kansas Medical Ctr.  

Substrate Modulation of Drug Transporters: An Industry Perspective
Caroline Lee—Ardea Biosciences 

Organic Cation Transporters in Drug Interactions with Methamphetamine and Metabolites
David Wagner—Univ. of Washington

Wnt Signaling: From Disease Mechanisms to Therapeutic Interventions

9:30 am–12:00 pm 

Chairs:
R. Gosens—Univ. of Groningen
W.M. Blankesteijn—Cardiovascular Research Institute Maastricht

Wnt signaling is crucial during development but also has been found to play a pivotal role in a rapidly growing number of diseases. In this symposium, we will start off with an overview of the highlights of 30 years of Wnt research, followed by a lecture on the specificity of Wnt-frizzled interactions. Subsequently, presentations on the role of Wnt signaling in cancer, stem cell biology, respiratory disease and cardiovascular disease will be delivered by experts in their fields. By attending this Symposium, the audience will be informed on the latest developments concerning this fascinating signal transduction pathway.

Sponsored by the Division for Molecular Pharmacology. Co-Sponsored by the Divisions for:   

• Cardiovascular Pharmacology 
• Cancer Pharmacology 
• Translational and Clinical Pharmacology 
• Drug Discovery and Development 

Evolution of Wnt Signaling: From Developmental Biology Towards Therapeutic Application
W. Matthijs Blankesteijn—Cardiovascular Research Institute Maastricht 

Receptor-Ligand Selectivity of Wnt/Frizzled Signaling
Gunnar Schulte—Karolinska Institute 

Wnt Signal Transduction Pathways in Stem Cells and Cancer
Satdarshan (Paul) S. Monga—Univ. of Pittsburgh, Sch. of Med. 

Wnt Signaling in Respiratory Diseases
Hoeke Baarsma—CPC Großhadern

Targeting Wnt Signaling in Cardiovascular Diseases
Arjun Deb—Univ. of California, Los Angeles 

Tankyrases are Druggable Targets for the Treatment of Metabolic Disorders
Obinna Obianom—Univ. of Maryland

A Novel Activator of Canonical Wnt Signaling
Jugajyoti Baruah—Univ. of Illinois Chicago

Structure-Activity Relationship of Peptide Inhibitors of the Wnt/Frizzled Interaction
W. Matthijs Blankesteijn—Maastricht Univ.

A Pharmacokinetics Primer: From Equations to Application

9:30 am–12:00 pm 

Chair: Reza Mehvar—Chapman Univ.

This conceptual, less-mathematical pharmacokinetics primer is designed for a general audience with a background in Pharmacology or Biomedical Sciences, who use or plan to use pharmacokinetics in their research or as part of their instructional responsibilities. In part one, designed for both researchers and educators, fundamental concepts behind the major pharmacokinetic parameters, including their estimation and application will be discussed. Part two will be a more hands-on session, utilizing simulations and other exercises, which will be more useful to pharmacology educators. A variety of resources will be shared with the audience who may incorporate them into their own instructional plans.

Sponsored by the Division for Pharmacology Education. Co-sponsored by the Divisions for:   

• Molecular Pharmacology 
• Drug Discovery and Development 
• Drug Metabolism 
• Cardiovascular Pharmacology 
• Translational and Clinical Pharmacology 

Fundamental Concepts in Pharmacokinetics: Applications in Research and Education
Reza Mehvar—Chapman Univ. 

Active Learning Exercises in Pharmacokinetics Using Simulations and Other Resources
Reza Mehvar—Chapman Univ. and Dion Brocks—Univ. of Alberta 

Pharmacometabolomics Enabling Tools for Systems Pharmacology and Precision Medicine

9:30 am–12:00 pm 

Chairs:
Rima Kaddurah-Daouk—Duke Univ. Medical Ctr.
Richard Weinshilboum—Mayo Clinic

Metabolomics, the study of metabolism at an “omic” level, has the potential to transform our understanding of mechanisms of drug action and the molecular basis for variation in drug response. It is now possible to define metabolic signatures of drug exposure that can identify pathways involved in both drug efficacy and adverse drug reactions capturing effects of genome, environment and gut microbiome. In addition, the “metabotype,” the metabolic “signature” of a patient, is a unique identity that contains information about drug response and disease heterogeneity. The application of metabolomics for the study of drug effects and variation in drug response is creating “pharmacometabolomics,” a discipline that will contribute to establishing “Quantitative Systems Pharmacology”. This field has the potential to transform pharmacology in several significant ways and establish foundations for Precision Medicine.

Sponsored by the Division for Translational and Clinical Pharmacology. Co-sponsored by the Divisions for:   

• Molecular Pharmacology 
• Cardiovascular Pharmacology 

Pharmacometabolomics Enabling Tools for and Systems Pharmacology and Precision Medicine
Rima Kaddurah-Daouk—Duke Univ. Medical Ctr.  

Pharmacometabolomics Informs and Compliments Pharmacogenomics
Richard Weinshilboum—Mayo Clinic 

Gut Microbiome and Host Metabolic Interactions—Implications for Drug Metabolism and Drug-Induced Toxicity
Wei Jia—Univ. of Hawaii Cancer Ctr.  

Integrating Multiple Omics Reveals Novel Signatures Associated with Thiazide Diuretics Blood Pressure Response
Mohamed Shahin—Univ. of Florida 

Stable Isotope Resolved Metabolomics (SIRM) on Fresh Human Tissues as a Preclinical Drug Testing Platform
Andrew N. Lane—Univ. of Kentucky College of Med.

 

ASPET Poster Presentations

12:30 pm–2:30 pm 

Bernard B. Brodie Award in Drug Metabolism

Phenobarbital Induction of Drug Metabolism and Beyond

2:00 pm–2:50 pm 

Sponsored by the Division for Drug Metabolism 

Keynote:
Masahiko Negishi—National Institute of Environmental Health Sciences, NIH  

P.B. Dews Lifetime Achievement Award for Research in Behavioral Pharmacology

Behavioral Mechanisms of Drug Action: Peter Dew’s Legacy

2:00 pm–2:50 pm 

Sponsored by the Division for Behavioral Pharmacology 

Keynote:
Travis Thompson—Univ. of Minnesota 

Diversity 3.0: From Fairness to Excellence

2:00 pm–2:50 pm 

Sponsored by the ASPET Mentoring and Career Development Committee 

Speaker
Marc A. Nivet—Association of American Medical Colleges 

This talk will describe the needed evolution from thinking about diversity as competing with excellence to being a core driver and marker of excellence. Through vivid narrative and illustrative examples from other industries, be prepared and open to a new vision on how we harness diversity and its necessary inclusion to advance our profession.  

» View Flyer (PDF) 

Division for Behavioral Pharmacology Symposium: Quantitative Pharmacological Analysis of In Vivo Data and Its Implications in CNS Drug Discovery

3:00 pm–5:30 pm 

Chairs:
Jun-Xu Li—Univ. at Buffalo
Lisa Gerak—Univ. of Texas Hlth. Sci. Ctr. at San Antonio

Understanding drug-receptor and drug-drug interactions are crucial for predicting the therapeutic effectiveness and therapeutic window of candidate drugs; however, quantitative approaches that can characterize these interactions are often lacking in preclinical and clinical research. This symposium aims to revitalize and emphasize the importance of quantitative pharmacological analyses in drug discovery, with special emphasis on applying these approaches to in vivo studies examining the effects of drugs acting in the central nervous system.

Sponsored by the Division for Behavioral Pharmacology 

Understanding the Actions of GABA_A Receptor Modulators in Vivo Using Schild Analyses in Rhesus Monkeys
Lisa Gerak—Univ. of Texas Hlth. Sci. Ctr. at San Antonio 

Combining Imidazoline I2 Receptor Ligands and Opioids for Pain Management: A Composite Additive Curve Analysis
Jun-Xu Li—Univ. at Buffalo 

Predicting Additivity: Abuse—Related Effects of “Bath-Salt” Mixtures
Gregory Collins—South Texas Veterans Hlth. Care Syst.—Audie L. Murphy VA Hosp.  

PK/PD Modeling of Opioid Modulation: Application in the Development of a Novel Treatment for Depression
Ryan Turncliff—Alkermes, Inc. 

Comparison of Heroin- and Δ9-Tetrahydrocannabinol-Induced Antinociception and Physical Dependence in Monkeys
Huiping Ding—Wake Forest University School of Medicine

Novel Platelet Therapies: Attacking Them from the Inside and Out

3:00 pm–5:30 pm 

Chair:
MarvinT. Nieman—Case Western Reserve Univ.

Cardiovascular disease is a major health problem in the developed world. The mainstay of treatment for acute coronary syndrome (ACS) and thrombosis is antiplatelet therapy. The major obstacle in antiplatelet therapies is for agents to be effective without causing bleeding complications. This symposium will describe the interactions within the plasma membrane that govern the physiological response of platelets endogenous agonist. We then will discuss novel approaches for targeting platelet receptors with antibodies and intracellular allosteric modulators. Finally, we will present methods for harnessing platelet receptors for the development of synthetic hemostats from a bioengineering approach.

Sponsored by the Division for Cardiovascular Pharmacology. Co-sponsored by the Division for Translational and Clinical Pharmacology  

The Neighborhood Matters: How Interactions Within the Membrane Influence Therapeutic Response
Marvin T. Nieman—Case Western Reserve Univ. 

Characterization of Function Blocking Antibodies Targeting Platelets
Zubair Karim—Western Univ. of Health Sciences 

Targeting G-protein Coupled Receptors from the Inside with Small Molecules
Robert Flaumenhaft—Beth Israel Deaconess Medical Ctr. 

Platelet-Inspired Synthetic Hemostats: Mimicking Platelet Functions on Engineered Biomaterial Systems to Treat Bleeding
Anirban Sen Gupta—Case Western Reserve Univ. 

Nanogel Drug Carriers Presenting Platelet GPIbα Mimic and Enhance Platelet Adhesion
Jacob Myerson—Univ. of Pennsylvania

Loss of Serotonin Transporter Function Alters ADP-mediated αIIbβ3 Activation through Disregulation of 5HT2A Receptor
Kendra H. Oliver—Vanderbilt Univ.

Division for Drug Metabolism James Gillette Award and Platform Session

3:00 pm–5:30 pm 

Chairs:
E.E. Scott—Univ. of Kansas
T.J. Carlson—Amgen, Inc. 

Predicting Fetal Exposure to Drugs Throughout Pregnancy Using a PBPK Model
Zufei Zhang—Univ. of Washington

Implications of In Vitro System Conditions for CYP2C9 and CYP3A4: Impact of pH on Clearance and Enzyme Inhibition
Luc Rougee—Eli Lilly and Company

Effect of Ethanol on the Metabolism of Antiretroviral Drugs Elvitegravir and Darunavir in the Presence and Absence of their Pharmacoenhancers in Microsomes
Narasimha Midde—Univ. of Tennessee Hlth. Sci. Ctr.

SULT4A1 Deletion in Zebrafish Alters Expression of Genes Implicated in Neurological Disorders
Patrick Garcia—Univ. of Alabama at Birmingham

Induction of CYP2A6 by Metronidazole in Primary Human Hepatocytes
Stephani Stancil—Children's Mercy Hospital

Endogenous Substrates for Tumor-Specific Human Cytochrome P450 CYP2W1
Yan Zhao—Univ. of California, San Francisco

Dose of Phenobarbital and Age of Treatment at Early Life are Two Key Factors for the Persistent Induction of Cytochrome P450 Enzymes in Adult Mouse Liver
Xiaobo Zhong—Univ. of Connecticut Sch. of Pharmacy

Modulation of P-glycoprotein at the Human Blood-Brain Barrier by Quinidine or Rifampin Treatment: A Positron Emission Tomography Imaging Study
Jashvant Unadkat—Univ. of Washington

Division for Translational and Clinical Pharmacology: Young Investigator Awards Platform Session

3:00 pm–5:30 pm 

Chair:
Ben T. Green—USDA, ARS

Introduction
Ben T. Green—USDA, ARS

Immunogenetic role of G Protein Signaling Modulator 3 (GPSM3) in the Pathogenesis of Rheumatoid Arthritis
Bryan Gall—West Virginia Univ.

Systems Pharmacology Approach to Identify Potential Therapeutic Small-Molecules for Treatment of Diabetic Peripheral Neuropathy
Brett McGregor—Univ. of North Dakota

Doxorubicin Acutely Inhibits Lymph Flow in Rat Mesenteric Lymph Vessels
Amanda J. Stolarz—Univ. of Arkansas for Medical Sciences

Preclinical Evaluation of Flt3 Ligand to Improve T Cell Adaptive Immune Response During Sepsis
Naeem K. Patil—Vanderbilt Univ. Medical Center

Microbiota-derived Metabolites Associated with Metabolic Improvements after Gastric Bypass Surgery and their Effects on Intestinal Cells in Vitro
Matthew L. Jennis— Janssen Pharmaceutica

Awards  

Division for Molecular Pharmacology Postdoctoral Scientist Award Finalists

3:00 pm–5:30 pm 

β2‐Adrenergic Receptors Regulate Innate Immune Responses Through β‐Arrestin Dependent Pathways
Laurel Grisanti—Temple Univ.

Structural and Functional Characterization of the Metastatic RhoGEF P-Rex1 and its Regulation by PtdIns(3,4,5)P3: Towards Inhibitory Small Molecule Development
Jennifer N. Cash—Univ. of Michigan

Structurally Diverse Positive Allosteric Modulators of the D1 Dopamine Receptor Potentiate G-protein and β-arrestin-mediated Signaling
KathrynD. Luderman—NINDS / NIH

Signaling by G Proteins and Phospholipase C: Yes It’s Still Exciting!
Keynote:  AlanV. Smrcka—Univ. of Rochester Sch. of Med. & Dentistry

Division for Translational and Clinical Pharmacology: Early Career Faculty Showcase

5:30 pm–6:00 pm 

Chair:  Pam Hornby—Janssen Pharmaceutical Companies of J&J

Structure-based Ligand Discovery for Nutrient Transporters
Avner Schlessinger—Tisch Cancer Institute

Novel Mechanisms Regulating Platelet and Pancreatic Beta Cell Function in Type 2 Diabetes Mellitus
Michelle E. Kimple—Univ. of Wisconsin-Madison

 

Invited Lecture: RhoA in Focus: Pathways from GPCRs to Disease

8:30 am–9:20 am 

Sponsored by the Divisions for Cardiovascular Pharmacology and Molecular Pharmacology 

Keynote: Joan Heller Brown—Univ. of California, San Diego 

Invited Symposium: GPCR and RhoA as Mediators of Disease

9:30 am–12:00 pm 

Chairs:
Rick Neubig—Michigan State Univ.
Shigeki Miyamoto—Univ. of California, San Diego

Signaling through the Rho GTPase family serves as a nodal point for signals that regulate a range of cellular functions, including cell proliferation and migration, cell survival and tissue fibrosis. In light of the complex downstream signals from RhoA, it is not surprising that its role in physiology and pathophysiology has remained obscure. Recently emerging evidence has revealed previously unrecognized aspects of RhoA action. This symposium will introduce the importance of transcriptional signals downstream of Rho activation activated by GPCRs in cancer, tissue fibrosis, and brain development as well as preservation of integrity of mitochondria in disease models.

Sponsored by the Divisions for Cardiovascular Pharmacology and Molecular Pharmacology   

GPCR and RhoA Signaling in Fibrosis
Rick Neubig—Michigan State Univ.  

GPCR and RhoA Signaling in Cancer
Silvio Gutkind—Univ. of California, San Diego 

GPCR and RhoA Signaling in the Nervous System
Xianhua Piao—Boston Children's Hosp.  

GPCR and RhoA Signaling in Cardioprotection
Shigeki Miyamoto—Univ. of California, San Diego 

GPCR and RhoA Signaling in Hypertension
Christopher P. Mack—Univ. of North Carolina

Nicotinic Agonist/Antagonist Drug Development: Implications for Treatment of Neurodegenerative and Addictive Disorders

9:30 am—12:00 pm 

Chairs:
Annette Fleckenstein—Univ. of Utah
M. Quik—SRI International

Increasing interest has focused on the development of nicotinic agonists/antagonists as treatments for a wide spectrum of disorders ranging from Parkinson's disease to Alzheimer's disease to substance abuse disorders. This symposium will highlight recent advancements in understanding the mechanistic role of nicotine, and the different nicotinic receptor subtypes involved in these disorders. Such work is essential for the development of targeted therapies with optimal beneficial and minimal adverse effects.

Sponsored by the Division for Behavioral Pharmacology. Co-sponsored by the Divisions for:    

• Neuropharmacology 
• Molecular Pharmacology 
• Drug Discovery and Development 
• Translational and Clinical Pharmacology 

Chronic Nicotine Protects Against Methamphetamine-Induced Behavioral and Dopaminergic Deficits
Annette Fleckenstein—Univ. of Utah 

Nicotinic Receptors as Targets for Treating Parkinson's Disease: Relevance to Parkinson's Disease Therapy
Tanuja Bordia—SRI Intl.  

Nicotinic Receptors as Targets for Treating Alzheimer's Disease
Kelly Dineley—Univ. of Texas, Medical Branch 

Nicotine and Interoceptive Conditioning: Implications for Treating Nicotine Dependence
Rick Bevins—Univ. of Nebraska-Lincoln 

Acute Tolerance to the Discriminative Stimulus Effects of Nicotine in Monkeys
Megan Moerke—Univ. of Texas Health Science Center

A Novel Structural Landscape for Ligand Binding to the α7 Nicotinic Acetylcholine Receptor
Gisela Camacho-Bustamante—Univ. of California, San Diego

Central Mechanisms Contributing to Novel Antidepressant Efficacy

9:30 am–12:00 pm 

Chair: D. Lodge—UT Health Science Ctr., San Antonio

Depression in the most common single psychiatric disease throughout the world. Unfortunately current therapeutic approaches are far from adequate. While novel treatments are currently being evaluated clinically, the neurobiological basis for their beneficial effects have not been completely delineated. This session will discuss potential mechanisms contributing to novel antidepressant activity, with an emphasis on ketamine and BDNF. By better understanding such mechanisms, it is our hope that future studies can specifically engage these targets to develop novel therapies with increased efficacy and improved side effect profiles.

Sponsored by the Division for Neuropharmacology. Co-sponsored by the Divisions for:    

• Molecular Pharmacology 
• Translational and Clinical Pharmacology 
• Behavioral Pharmacology 

Antidepressant Efficacy of Ketamine in Depressed Patients
Gerard Sanacora—Yale Univ.  

The vHipp-mPFC Pathway Mediates the Sustained Antidepressant Response to Ketamine
Dan Lodge—UT Health Science Ctr., San Antonio 

Development of Prophylactics Against Stress-induced Depressive-like Behavior
Christine Ann Denny—Columbia Univ. 

BDNF Receptor Signaling is Differentially Altered by Novel Antidepressants
Flavia Carreno—UT Health Science Ctr., San Antonio 

Evaluation of Molecular Biomarkers in an Adolescent Chronic Restraint Stress Model of Depression
Martha Graham—Mercer Univ. Coll. Of Pharmacy

Chronic isolation stress alters antidepressant-like behaviors in animals lacking RGS4
Jeffrey N. Talbot—Roseman University of Health Sciences

Chronopharmacology in Cancer: Does Time Really Matter?

9:30 am–12:00 pm 

Chair: Shobhan Gaddameedhi—Washington State Univ.

This session will highlight the circadian clock role in modulating the response to cancer pharmacology and anti-cancer therapeutics. Although circadian variability of anti-cancer drug exposure and disposition following drug administration at different times of day has been known for 30 years, it has had limited impact on clinical practice. This was due to a lack of understanding of the molecular mechanisms behind these experimental observations, aside from some influence on cancer chemotherapy. The molecular connection between the circadian clock and these drug targets in anti-cancer therapy will be considered and the therapeutic potential of the pharmacological modulation of the circadian clock will be discussed.

Sponsored by the Division for Cancer Pharmacology. Co-sponsored by the Divisions for:    

• Drug Metabolism 
• Pharmacology Education 

Chronopharmacology: Temporal Targets of Drug Action and Therapeutic Implications
John B. Hogenesch—Univ. of Pennsylvania 

Unraveling the Potential of Chronopharmacology through Genotoxic Stress Mediated Anti-Cancer Drug Effect in Cancer
Shobhan Gaddameedhi—Washington State Univ.  

Tamoxifen Resistance in Breast Cancer: The Melatonin Connection
Steven M. Hill—Tulane Univ. Sch. of Med.  

Cancer Chronotherapy: Clinical Perspectives and Outcomes
Francis Levi—Warwick Medical Sch., UK 

A Multi-Scale Systems Pharmacology Approach for Personalizing Irinotecan Chronotherapy
Annabelle Ballesta—Univ. of Warwick

Patient-Specific Stem Cells as Models for Gene-Disease, Drug, and Environment Interactions

9:30 am–12:00 pm 

Chair: J. Richardson—Northeast Ohio Medical Univ.

Sponsored by the Division for Toxicology. Co-sponsored by the Divisions for:    

• Neuropharmacology 
• Translational and Clinical Pharmacology 
• Drug Discovery and Development 

There is increasing interest in the use of human stem cells as screens for drug and chemical toxicity and drug efficacy. Additionally, this technology is being used to research individual differences in these outcomes based on genetics. By using a patient's own stem cells increased understanding of disease pathophysiology and personalized approaches for therapeutic intervention may be attainable. Using the powerful tools of genetics and iPSC technology, this participants in this symposium will discuss new and cutting edge research that provides examples of probing disease pathophysiology gene-environment interactions, susceptibility to carcinogenicity and disease effects on drug efficacy. 

Modeling Gene-Environment Interactions in Alzheimer Disease
Jason Richardson—Northeast Ohio Medical Univ. 

Alterations of Manganese Biology in Huntington's Disease
Aaron Bowman—Vanderbilt Univ. 

Stem Cells in Inorganic Carcinogenesis
Erik Tokar—Natl. Inst. Of Environmental Health Sciences 

Leveraging Novel Technologies for Human iPSC-based Screening for Parkinson’s Disease
Xianmin Zeng—The Buck Institute 

Current Trends in Antibody Drug Conjugates: From Discovery to the Clinic

9:30 am–12:00 pm 

Chairs:
T. Esbenshade—Abbvie, Inc.
L.C. Wienkers—Amgen

Sponsored by the Divisions for Drug Discovery and Development and Drug Metabolism. Co-sponsored by the Divisions for:    

• Molecular Pharmacology 
• Cancer Pharmacology 
• Translational and Clinical Pharmacology 

Therapeutic antibody-drug conjugates or ADCs combine a target specific monoclonal antibody or mAb with the cell-killing activity of a small molecule drug and deliver the combined agent directly to specifically targeted cancer cells. Currently, there is considerable effort within the biopharmaceutical industry to advance ADC drug discovery with a large number of ADCs in various stages of preclinical/clinical development.  This symposium is designed to cover a spectrum of ADC drug discovery efforts which will include ADC design considerations, associated pharmacology/biology, and drug disposition. The science described in the session should provide greater understanding of antibody-drug conjugate pharmacological activity and disposition. 

Advances in Drug-linker Design to Improve the Stability, Homogeneity, and Pharmacokinetics of Antibody-drug Conjugates
Robert Lyon—Seattle Genetics  

Considerations for ADC Catabolism and Catabolite Disposition
Dan Rock—Amgen, Inc. 

Analysis of Antibody-Auristatin Conjugates for Cancer Therapy
Shawna Hengel—Seattle Genetics 

Leveraging Clinical Learnings and Patient Tailoring to Enable Next Generation Conjugate Success: Hsp90 Inhibitor Drug Conjugates (HDCs)
Alan Rigby—Synta Pharmaceuticals Inc. 

 

ASPET Poster Presentations

12:30 pm–2:30 pm 

Meet-the-Experts in Translational and Clinical Pharmacology Luncheon

12:30 pm–2:30 pm 

Pre-registration required. First come, first served.   

Division for Cardiovascular Pharmacology Trainee Showcase

2:30 pm–4:30 pm 

Chairs: 
Cam McCarthy—Augusta Univ.
Jan M. Schilling—UCSD

Inhibiting Fibronectin Improves Cardiac Function in a Mouse Model of Heart Failure
Inigo Valiente-Alandi—Cincinnati Children's Hospital Medical Center

Kruppel-Like Factor 15: A Critical Transcriptional Regulator Of Hypoxia Induced Endothelial Arginase 2
Deepesh R. Pandey—John Hopkins Univ.

Nanogel Drug Carriers Presenting Platelet GPIbα Mimic and Enhance Platelet Adhesion
Jacob W. Myerson—Univ. of Pennsylvania

Reversal of Stem Cell Mobilopathy and Enhanced Vascular Repair by Angiotensin-(1-7) in Diabetes
Goutham Vasam—North Dakota State Univ.

MSC Exosomes Deliver Cardioprotective miR-21
Kristin Luther—Loyola Univ. Chicago

Human Perivascular Adipose Tissue Contains an Adrenergic System
Nadia Ayala-Lopez—Michigan State Univ.

Division for Cancer Pharmacology: Cell Signaling in Cancer Biology and Therapeutics

3:00 pm–5:30 pm 

Chairs:
R. Kip Guy—St. Jude Children's Research Hospital
Jack C. Yalowich—Ohio State Univ. 

Proteinases, Proteinase-Activated Receptors (PARs) and Transient Receptor Potential (TRP) Ion Channels: Driving Tumorigenesis in the Bladder Cancer Microenvironment
Stacy G. Gibson—Univ. of Calgary

Epac1 Links Prostaglandin E2 to β-catenin Transcriptional Activity During Epithelial-to-Mesenchymal Transition in A549 Cells
Sepp Jansen—Univ. of Groningen

Electrophilic Nitroalkenes Inhibit Triple Negative Breast Cancer Metastasis
Chen-Shan Woodcock—Univ. of Pittsburgh, Sch. of Med.

Treatment of Triple Negative Breast Cancer-Derived Cells with Polyisoprenylated Cysteinyl Amide Inhibitors Activates Caspase 3/7 and Disrupts F-actin Organization leading to Apoptosis and Diminished Cell Motility
Olufisayo Salako—Florida A&M Univ.

A Dock-Derived PEDF Mimic Targeting Laminin Receptor Downregulates VEGF Receptor
Charles Umbaugh—Purdue Univ.

Synergism between Bioengineered miR-34a Prodrugand Doxorubicin in Suppressing Osteosarcoma Cell Proliferation and Xenograft Tumor Growth
Meijuan Tu—Univ. of California Davis

Division for Neuropharmacology Postdoctoral Scientist Award Finalists

3:00 pm–5:30 pm 

Chairs:
B. Greenwood-Van Meerveld—Oklahoma Center for Neuroscience
M. Wood—AstraZeneca Pharmaceuticals LP 

Path to Becoming a Neuropharmacologist and the Search for Novel Psychotherapeutic Drug Targets
Lynette C. Daws—Univ. of Texas Health Science Ctr.

Chronic Cocaine Exposure Alters D1 Medium Spiny Neuron Activity to Promote Relapse
Erin Calipari—Icahn Sch. of Med. at Mount Sinai

Chronic Antagonism of p38α MAPK Normalizes Serotonin Clearance, Serotonin Receptor Hypersensitivity and Social Behavior Deficits in a Genetic Murine Model of Autism Spectrum Disorder
Matthew J. Robson—Vanderbilt Univ.

Cocaine-induced Chromatin Modifications are Associated with Increased Gene Expression and DNA-DNA Interactions of AUTS2 and CALN1
Olivia Engmann—Friedman Brain Inst. at Mount Sinai Sch. of Med.

Rapid Antidepressant-like Effects of the “Uptake-2” Blocker, Decynium 22 in the Flinders Sensitive Line Rat Model of Depression
Rheaclare Fraser-Spears—Univ. of Texas Health Science Center at San Antonio

Impact of Chronic Ethanol Self-Administration on Kappa Opioid Receptor Regulation of Dopamine Signaling in Nonhuman Primates
Cody Siciliano—Wake Forest Univ. School of Medicine

GPR171 in the Basolateral Amygdala Regulates Stress and Reward-related Behaviors
Erin Bobeck—Mount Sinai School of Medicine

Division for Toxicology: Fortuitous Protein Modification in Disease Pathogenesis and Treatment

3:00 pm–5:30 pm 

Chair:
Serrine S. Lau—Wayne State Univ.

Biologically reactive intermediates formed as endogenous products of various metabolic processes are important factors in human diseases. Chemical-induced toxicities have long been known to be associated with the ability of electrophilic metabolites to react with cellular targets, including their covalent adduction to nucleophilic resides in proteins. Identifying specific sites within adducted proteins can provide the initial information necessary to determine whether such adventitious posttranslational modifications (PTM) significantly alter either protein structure and/or function. This symposium addresses our current understanding of exogenous and endogenous PTM and their impact on disease pathogenesis. Topics include carcinogenesis (Turesky); Parkinson’s Disease (Monks); Retinal Diseases (Sparrow); Type 2 Diabetes (Lau) and Insulin Resistance (Yi). 

Introduction
Serrine S. Lau—Wayne State Univ. 
 

Characterization of Blood Protein Adducts Formed with Cooked Meat Carcinogens and Approaches of Human Biomonitoring by Ion Trap Mass Spectrometry
Robert Turesky—Univ. of Minnesota  

Dopamine Adduction to α-Synuclein and Parkinson’s Disease
Terrence J. Monks—Univ. of Arizona  

Visual Cycle Adducts and Diseases of Retina
Janet R. Sparrow—Columbia Univ.    

Dicarbonyl Protein Modification, Diabetic Complications and Metformin Therapy
Serrine S. Lau—Wayne State Univ. 
 

Wide-Spread Insulin Resistance in Tyrosine Phosphorylation in Type 2 Diabetic Patients
Zhengping Yi—Wayne State Univ.  

Division for Drug Discovery and Development: Chemical Biology as an Engine for Drug Discovery

3:00 pm–5:30 pm 

Chairs:
J.S. Lazo—Univ. of Virginia Sch. of Med.
C. Beeson—Medical Univ. of South Carolina 

Chemical Biology has emerged as an important and dynamic approach for pharmacological studies being practiced in the pharmaceutical sector and in academia. The goal of this timely symposium is to highlight recent advances in chemical biology as they relate to pharmacological questions in drug discovery. Topics include therapeutics targets, strategies for modulating targets, drug design and the role of natural products in drug discovery. The symposium should be of interest to members of all of the ASPET Divisions as well as EB attendees from other societies. 

Introduction to the Symposium
John S. Lazo—Univ. of Virginia 

Developing Novel Chemical Biology Strategies to Synthetically Disrupt Protein: Protein Interactions
Eileen J. Kennedy—Univ. of Georgia 

Getting What You Screen For: Modulating p97 Proteostasis Networks
Michelle Arkin—Univ. of California, San Francisco 

Targeted Protein Degradation—What it Provides and How to Achieve It
Craig M. Crews—Yale Univ.  

Precision Biosynthesis of Natural Product Drug Leads
Bradley Moore—Univ. of California, San Diego 

Summary and Concluding Remarks
Craig Beeson—Medical Univ. of South Carolina 

2014 Tang Prize in Biopharmaceutical Science (EB-wide lecture for all societies)

3:15 pm–5:15 pm 

Keynote:
Tasuko Honjo—Kyoto Univ.

The Tang Prize in Biopharmaceutical Science recognizes original biopharmaceutical or biomedical research that has led to significant advances towards preventing, diagnosing and/or treating major human diseases to improve human health.

In 2014, the Tang Prize in Biopharmaceutical Science was awarded to James P. Allison and Tasuku Honjo for the discoveries of CTLA-4 and PD-1 as immune inhibitory molecules that led to their applications in cancer immunotherapy. Tasuku Honjo will join EB 2016 and present the Tang Prize Lecture.  

Paul M. Vanhoutte Distinguished Lectureship in Vascular Pharmacology

Capillaries as Decoders of the Neural Rhythm of the Brain: Translating Thought into Blood Flow

4:30 pm–5:30 pm 

Keynote:
Mark T. Nelson—University of Vermont 

 

Ray Fuller Lecture in the Neurosciences

Sex Biased Stress Signaling

8:30 am–9:20 am 

Keynote: Rita J. Valentino—Children’s Hosp. of Philadelphia / Univ. of Pennsylvania 

Ray Fuller Symposium

Sex Differences in Biology: Challenges and Opportunities for Drug Development

9:30 am–12:00 pm 

Chair: Rita J. Valentino—Children’s Hosp. of Philadelphia / Univ. of Pennsylvania

Sex differences exist at many biological levels that can create distinctions in the pharmacodynamic and pharmacokinetic properties of drugs. Many diseases exhibit sex biases in prevalence and severity, underscoring the potential for individualized therapy based on sex. Importantly, sex differences in biological or pharmacological responses are invaluable tools that can be used to elucidate underlying mechanisms. This symposium highlights research on sex differences in biology and pharmacology that is advancing our understanding of biological phenomena, diseases and drug actions.  

Estrogens Enhance Female Vulnerability to Drug Addiction
Paul Mermelstein—Univ. of Minnesota 

Social Defeat Stress in Males and Female: Role of Kappa Opioid Receptors
Brian Trainor—Univ. of California, Davis 

Sex Differences in Ketamine's Antidepressant-like Effects
Mohamed Kabbaj—Florida State Univ.  

Sex Differences in the Brain are Established Early and Enduringly
Margaret McCarthy—Univ. Maryland Sch. of Med.  

Drug Transporter Protein Quantification by LC-MS/MS for In Vitro to In Vivo Extrapolation (IVIVE) and Prediction of Interindividual Variability of Transporter Mediated Drug Disposition

9:30 am–12:00 pm 

Chairs:
B. Prasad—Univ. of Washington
Y. Lai—Bristol-Myers Squibb

Over the past few years, LC-MS/MS proteomics has emerged as a viable and reproducible technique to quantify drug transporters. The transporter quantification data are crucial to elucidate inter-individual variability and to generate physiologically relevant scaling factors for translating kinetic parameters between in vitro systems and for in vivo prediction. The symposium will benefit scientists both from industry and academia through accommodating speakers in the area of quantitative transporter proteomics and physiological modeling to provide the overview of membrane proteomics, its application, data interpretation and transporter expressions in various tissues as a factor for establishing the in vitro to in vivo extrapolation.

Sponsored by the Division for Translational and Clinical Pharmacology. 
Co-sponsored by the Divisions for:   

• Cardiovascular Pharmacology 
• Drug Metabolism 

Blood-Brain Barrier (BBB) Pharmacoproteomics: Reconstruction of In Vivo Brain Drug Distribution in Mouse, Monkey and Diseased Models
Tetsuya Terasaki—Tohoku Univ.  

Quantitative Proteomics for IVIVE of Transporter Mediated Drug Clearance
Yurong Lai—Bristol-Myers Squibb 

QNo Escape from Models in Translating LCMS-Derived Abundance Values!
Amin Rostami—Univ. of Manchester 

Effect of Ontogeny and Pharmacogenomics on Transporter Mediated Interindividual Variability in Drug Disposition
Bhagwat Prasad—Univ. of Washington, Seattle 

Chronic Paroxetine Treatment in Mice Leads to Adiposity and Glucose Intolerance
Weibin Zha—Univ. of Washington

Intracellular GPCR and Lipid Signaling

9:30 am–12:00 pm 

Chairs:
A. Marchese—Loyola Univ. Chicago
A. Smrcka—Univ. of Rochester Medical Ctr.

GPCR signaling is classically known to initiate at the plasma membrane, but it is now appreciated that GPCRs can also signal from intracellular compartments, such as endosomes and Golgi. This is functionally relevant because this spatial and temporal segregation of signaling may lead to discrete cellular and biological outcomes. Importantly, this may also be linked to dysregulation of GPCR signaling in disease. Yet the mechanisms governing intracellular GPCR signaling remain poorly understood. This session will focus on recent advances in our understanding of GPCR and lipid signaling from intracellular compartments.

Sponsored by the Division for Molecular Pharmacology. 
Co-sponsored by the Divisions for:   

• Cardiovascular Pharmacology 
• Neuropharmacology 
• Translational and Clinical Pharmacology 

GPCR Promoted Akt Signaling from Early Endosomes
Adriano Marchese—Loyola Univ. Chicago 

Ubiquitin Regulates GPCR-induced p38 MAPK Signaling from Endosomes 
JoAnn Trejo—Univ. of California, San Diego 

Phosphatidylinositol 4-phosphate: A Lipid's Journey to Fame
Tamás Balla—NICHD / NIH 

Lipid Signaling from the Golgi
Alan Smrcka—Univ. of Rochester Medical Ctr.  

Structural and Functional Characterization of the Metastatic RhoGEF P-Rex1 and its Regulation by PtdIns(3,4,5)P3: Towards Inhibitory Small Molecule Development
Jennifer Cash—Univ. of Michigan

Spatial Encoding of Cyclic AMP Signaling Specificity by GPCR Endocytosis
Nikoleta Tsvetanova—Univ. of California, San Francisco

Novel Targets for Treatment of Cardiometabolic Diseases

9:30 am–12:00 pm 

Chairs:
J. Ren—Univ. of Wyoming
S. Nair—Univ. of Wyoming

Type 2 diabetes and associated metabolic disorders are global public health problems. Heart disease is the leading cause of death and disability among people with type-2 diabetes. However, the molecular signals that contribute to cardiovascular disease in diabetics are yet unclear. Altered insulin signaling, excessive mineralocorticoid activity abnormal glucose and lipid metabolism, oxidative/nitrosative stress, endoplasmic reticulum stress, apoptosis, autophagy and mitochondrial damage have been identified as potential causes and/or consequences of cardiometabolic disease in diabetic subjects. Identifying and characterizing these molecular pathways is paramount to designing novel strategies for the treatment of cardiometabolic diseases, which is the focus of this session.

Sponsored by the Division for Cardiovascular Pharmacology. 
Co-sponsored by the Divisions for:  

• Molecular Pharmacology 
• Translational and Clinical Pharmacology 
• Drug Discovery and Development 

Interplay of Oxidative Stress, Inflammation, and Cell Death, in Diabetic Cardiomyopathy
Pal Pacher—NIAAA/NIH 

Mineralocorticoid Receptor Signaling and Cardiovascular Stiffness in Insulin Resistance
James D. Sowers—Univ. of Missouri Sch. of Med.  

Self-Renewal of Cardiomyocyte: Metabolic Signals as Regulators of Protein Turnover
Heinrich Taegtmeyer—The Univ. of Texas Health Sciences Ctr.  

Targeting Cathepsin K in Heart Failure
Sreejayan Nair—Univ. of Wyoming

Metabolic Syndrome Perivascular Adipose Tissue Impairment of Aortic Reactivity Post Stroke, Improved by NOX2 Inhibition
Evan DeVallance—West Virginia Univ.

Mitochondrial Function of Cerebral Vasculature in Insulin Resistant Zucker Obese Rats
Ivan Merdzo—Tulane Univ.

Cancer Stem Cells as Pharmacological Targets

9:30 am–12:00 pm 

Chairs:
J.S. Gutkind—Univ. of California, San Diego
T. Reya—Univ. of California, San Diego

Sponsored by the Division for Cancer Pharmacology. 
Co-sponsored by the Divisions for:   

• Molecular Pharmacology 
• Translational and Clinical Pharmacology 
• Drug Discovery and Development 

Targeting the Cancer Cell Cycle:  The Development of Palbociclib in Breast Cancer
Robert T. Abraham—Pfizer Inc.  

Drug Treatment or Cellular Stress Drives Tumor Reprogramming, Progression and Drug Resistance
David Cheresh—UC San Diego Dept. of Pathology 

Heterotrimeric G-protein α Subunit Chaperone Ric-8A as a Novel Target for Cancer Therapeutics
Bharti Patel—Univ. of Rochester Med. Ctr.

mTOR Co-targeting Strategies Against Oral Malignancies and their Cancer Initiating Cells
Zhiyong Wang—Univ. of California, San Diego

Lung Stem Cell Approaches to Understanding Differentiation, Disease and Therapy
Carla Kim—The Harvard Stem Cell Inst. 

Understanding Metastatic Breast Cancer Stem Cell Properties Using Patient-derived Circulating Tumor Cells
Min Yu—Univ. of Southern California

Keep Calm and Target Peptides: Modulation of Stress-Related Behaviors by Neuropeptide Systems

9:30 am–12:00 pm 

Chairs:
S. Clark—Univ. at Buffalo, SUNY
V. Sabino—Boston Univ. Sch. of Med.

Stress-related disorders have a devastating impact on society, and many of them are known to stem from an individual's inability to cope with stressful life events. To identify novel therapeutic targets it is vital to gain a deeper understanding of the endogenous systems that modulate the stress response and how they are dysregulated in neuropsychiatric disorders involving abnormal responses to stress. Neuropeptide systems are powerful regulators of the stress response, and therefore hold great therapeutic promise. This symposium will present recent data on established as well as newly discovered neuropeptide systems, highlighting their potential for treating anxiety- and trauma-related disorders.

Sponsored by the Division for Behavioral Pharmacology.
Co-sponsored by the Divisions for:   

• Neuropharmacology 
• Molecular Pharmacology 
• Drug Discovery and Development 

Genetic Dissection of the CRF-System in the Extended Amygdala
Alon Chen—Max Plank Institute of Psychiatry 

Role of Extended Amygdala PACAP in the Behavioral Response to Acute and Chronic Stress
Valentina Sabino—Boston Univ. Sch. of Med.  

Neuropeptide Y in the Basolateral Amygdala: Role in Stress Resilience
Janice H. Urban—Franklin Univ. of Med. and Sci.  

ProSAAS-Derived Peptides: Major Brain Neuropeptides Implicated in the Regulation of Stress and Reward-Related Behaviors
Lakshmi Devi—Mount Sinai Univ.  

Amygdaloid Corticotropin Releasing Factor as the Key Mediator of Chronic Visceral Pain in Females with a History of Early Life Stress
Dawn Prusator—Univ. of Oklahoma Health Science Center

Development of Neuropeptide S Receptor Targeted Compounds as Potential Therapies for Anxiety-Related Disorders
Stewart Clark—Univ. at Buffalo, SUNY 

 

ASPET Poster Presentations

12:30 pm–2:30 pm 

Translating MicroRNA Cancer Biology to Therapy

3:00 pm–5:30 pm 

Chairs:
A. Yu—UC Davis Sch. of Med.
A.G. Bader—Mirna Therapeutics, Inc.

MicroRNAs (miRNAs or miRs) are small, genomically-encoded noncoding RNAs that control expression of numerous target genes in cells, and modulate various cancer cellular processes. The advances in miRNA cancer biology offer clues to developing novel miRNA-based cancer treatments. This symposium session brings together a number of leading investigators to present their new and most recent research on miRNA cancer pharmacology and therapy. The attendees will have a better understanding of (1) mechanistic functions of miRNAs in the regulation of cancer cellular processes, (2) approaches and strategies in studying miRNA cancer pharmacology and therapy, and (3) new strategies to investigate miRNA cancer pharmacology and develop miRNA therapeutics.

Sponsored by the Division for Cancer Pharmacology. Co-sponsored by the Divisions for: 

• Drug Discovery and Development 
• Translational and Clinical Pharmacology 

MicroRNA Replacement Therapy
Andreas G. Bader—Mirna Therapeutics, Inc.  

Modulating MicroRNAs to Improve Cancer Therapy
James W. Welsh—The Univ. of Texas MD Anderson Cancer Ctr.  

A Combinatorial MicroRNA Therapeutics Approach to Suppressing Cancer Growth
Andrea Kasinski—Purdue Univ.  

Recombinant MicroRNAs as Novel Cancer Therapeutics
Aiming Yu—UC Davis Sch. of Med.  

miR-186 Suppresses Cell Proliferation and Anchorage-independence in a Metastatic Prostate Cancer Cell Line
Dominique Z. Jones—Univ. of Louisville

Modulation of BSEP and MDR3 in Drug-Induced Liver Injury (DILI)

3:00 pm–5:30 pm 

Chairs:
K. He—Biotranex LLC
P. Watkins—The Hammer Institutes for Health Sciences

Beyond bile salt export pump (BSEP) inhibition, it is now recognized that additional factors have to be considered when attempting to predict and model drug-induced liver injury (DILI). For example, drugs can inhibit nuclear hormone receptors (e.g., farnesoid X receptor), which regulate bile acid transporter expression, and impact the adaptive response of the liver under cholestatic conditions. Likewise, phospholipid-transporting multidrug resistance 3 (MDR3) is equally important in bile formation and its inhibition can also trigger cholestasis. Symposium attendees will hear from leading researchers regarding the burgeoning topics of DILI modeling, regulation of transporter expression and the inhibition of MDR3.

Sponsored by the Division for Toxicology. Co-sponsored by the Divisions for: 

• Drug Metabolism 
• Drug Discovery and Development 
• Molecular Pharmacology 

Integration of BSEP Inhibition Data in DILIsym®: Perspectives from System
Paul Watkins—The Hamner Institutes for Health Sciences 

BSEP Inhibition in Drug Discovery Screening
Ryan Morgan—Amgen, Inc.  

Novel BSEP and MDR3 Assays Using Primary Hepatocytes for Screening DILI Drugs and Species Differences
Kan He—Biotranex LLC 

The Role of Bile Salt Export Pump Gene Repression in Drug-Induced Cholestatic Liver Toxicity
Brandy Garzel—Univ. of Maryland Sch. of Pharmacy 

BSEP and MDR3 Inhibition by DILI Drugs and the Implications with Systems Biology Analysis
Jie Zhang—Natl. Ctr. for Toxicological Research 

New Twists on Neurotransmitter Transport: Unraveling Novel Therapeutic Targets for Addiction and Psychiatric Disorders

3:00 pm–5:30 pm 

Chairs:
L.C. Daws—Univ. of Texas Hlth. Sci. Ctr. at San Antonio
H.H. Sitte—Medical Univ. Vienne

The dopamine transporter has long been considered the primary target for amphetamine and cocaine. Here we present new data showing that the actions of amphetamine and cocaine can be mediated via previously unsuspected targets, including organic cation transporter 3, EAAT3 and immune responses. Data will be discussed in terms of consequences for addiction and development of new therapeutics for the treatment of drug abuse.

Sponsored by the Division for Neuropharmacology. Co-sponsored by the Divisions for:  

• Molecular Pharmacology 
• Behavioral Pharmacology 

Integrating Organic Cation Transporter 3 Into Models of Dopamine Clearance and Cocaine Addiction
Paul J. Gasser—Marquette Univ. 

Organic Cation Transporter 3: An Unsuspected Player in the Actions of Amphetamine and a New Target for Psychotherapeutic Drug Development
Lynette C. Daws—Univ. of Texas Hlth. Sci. Ctr. At San Antonio 

Transporters as Clinical Targets of Drugs: Amphetamines, New Psychoactive Substances and the Monoamine Transporter Cycle
Harald H. Sitte—Medical Univ. Vienne 

DAT and EAAT3 Trafficking Regulation by Amphetamine: Integration of Dopaminergic and Glutamatergic Signaling
Suzanne M. Underhill—NIH 

Sick, Stressed, Depressed, and Addicted: Immune Modulation of Cocaine Targets
Nicole L. Baganz—Vanderbilt Univ.  

The Biology and Translational Potential of Hydrogen Sulfide: One Person's Trash is Another Person's Treasure

3:00 pm–5:30 pm 

Chairs:
J.L. Wallace—Univ. of Calgary 
A. Papapetropoulos—Univ. of Athens

Hydrogen sulfide (H2S) is now recognized as an important signaling molecule that regulates a vast array of physiological and pathophysiological processes. It also shows considerable promise as a target molecule for novel therapeutics for a broad range of disorders. This symposium will feature lectures that cover a broad range of the important aspects of H2S biology, focusing on the translational potential of this gaseous mediator. The lectures will be given by investigators at the cutting edge of research and drug development related to hydrogen sulfide.

Sponsored by the Division for Drug Discovery and Development. Co-sponsored by the Divisions for:  

• Molecular Pharmacology 
• Cancer Pharmacology 
• Translational and Clinical Pharmacology 

H2S Actions and Interactions with NO in the Cardiovascular System
Andreas Papapetropoulos—Univ. of Athens 

Diet, H2S and Longevity
James R. Mitchell—Harvard Sch. of Public Health 

Modulation of H2S as an Anti-Cancer Strategy
Csaba Szabo—The Univ. of Texas Medical Branch at Galveston 

H2S and Glucose Metabolism
Lingyun (Lilly) Wu—Lakehead Univ.  

Development of H2S-Releasing, GI-Safe Anti-Inflammatory Drugs
John L. Wallace—Antibe Therapeutics Inc.  

Transdermal Detection of Low Concentrations of Hydrogen Sulfide
Lynnette Rios—Univ. of New Mexico

Sodium Hydrosulfide Alleviates Cecal Ligation and Puncture (CLP) - Induced Sepsis and Elevates the Regional Blood Flow in Septic Shock
Akbar Ahmad—Univ. of Texas Medical Branch

ASPET Closing Reception

6:00 pm–8:00 pm 

Drug Discovery Colloquium

Drug Discovery in Academia: Recent Successes and Emerging Opportunities

8:00 am–8:00 pm