WPC PRE-CONFERENCE SHORT COURSES
Monday, June 12, 12:00 - 3:00 pm
SC1: Introduction to Allosteric Modulators and Biased Ligands of GPCRs
Allosteric modulators and pathway-biased ligands represent novel therapeutic approaches for achieving more selective actions with regards to G protein-coupled receptors (GPCRs). However the identification and characterization of such compounds can be challenging due in part to 'context-dependent phenomena.' Aimed at scientists working on GPCRs this course will provide information on the identification and validation of allosteric, pathway-biased drugs including emerging screening approaches, practical tips and tools for identification and validation, and the structural basis underlying such drugs.
Annette Gilchrist, Ph.D., Professor, Pharmacology, Midwestern University
Sid Topiol, Ph.D., CSO, 3D-2drug, LLC; Professor and Director, Structural and Computational Drug Discovery, Stevens Institute of Technology
SC2: Drug Metabolism and Its Impact on Decisions in Lead Discovery - Part 1
This short course will focus on concepts important for those wanting to understand how drug metabolism is applied to drug discovery. Topics will include how drugs are metabolized, what enzymes are involved, common assays for predicting clearance and drug-drug interactions and how drug metabolism concepts are applied during lead optimization. Those scientists involved in medicinal chemistry, pharmacology and drug metabolism will benefit from this overview.
John Erve, Ph.D., Consultant
Adrian J. Fretland, Ph.D., Associate Director, DMPK Oncology iScience, AstraZeneca
Monday, June 12, 3:30 - 6:30 pm
SC3: Drug Metabolism and Its Impact on Decisions in Drug Development - Part 2
This short course will focus on concepts important for those wanting to understand how drug metabolism is applied to drug development. Topics will include how drug metabolites are identified in pre-clinical studies and human clinical trials, the role of bioactivation and the growing importance of transporters in drug disposition and safety. Those scientists involved in medicinal chemistry, pharmacology and drug metabolism will benefit from this overview.
John Erve, Ph.D., Consultant
Mingxiang Liao, Ph.D., Senior Scientist I, DMPK, Takeda Pharmaceutical Intl. Company
SC4: Understanding and Dealing with Drug Disposition in CNS
This course will aim to discuss compound selection in CNS drug discovery by modeling and simulation, factors affecting disposition of biologics, kinetic relationship between systemic circulation and CNS and understanding factors that affect brain ISF/CSF production and clearance and its implications.
Qin Wang, Ph.D., Principal Scientist, Translational Sciences, Biogen
SC5: Convergence of Immunotherapy and Epigenetics for Cancer Treatment
In recent years the understanding of both the immunotherapy and epigenetics of cancer has increased. This course will provide some details of how immunotherapy and epigenetic pathways interact and how they can be exploited to enhance the efficacy of current cancer treatments. The instructors will review recent scientific evidence and pre-clinical data that support the development of combination therapies and offer their perspectives on challenges that may have to be tackled along the way.
Alejandro Villagra, Ph.D., Assistant Professor, Department of Biochemistry and Molecular Medicine, School of Medicine and Health Sciences, The George Washington University
Katherine Bakshian Chiappinelli, Ph.D., Assistant Professor, Department of Microbiology, Immunology, and Tropical Medicine, The George Washington University Cancer Center
Additional Instructors to be Announced
Monday, June 12, 7:00 - 9:30 pm (Dinner Provided)
SC6: How to Best Utilize 3D Spheroids and CRISPR Assays in Oncology
The course will provide an overview of 3D cell culture models, their strengths and weaknesses. The instructors will share their experiences on the challenges they faced from experimental design to data analysis while developing and optimizing these 3D spheroid models for CRISPR-based functional screening. The focus of their presentations will be in the area of oncology research, utilizing either low or high throughput screening approaches.
Madhu Lal-Nag, Ph.D., Group Leader, Trans-NIH RNAi Facility, National Center for Advancing Translational Sciences, National Institutes of Health
Geoffrey Bartholomeusz, Ph.D., Associate Professor and Director, Target Identification and Validation Program, Department of Experimental Therapeutics, Division of Cancer Medicine, The University of Texas M.D. Anderson Cancer Center
SC7: Evaluating and Characterizing in vitro Models of Drug Toxicity
This short course will focus on ways to evaluate and characterize which in vitro model of drug toxicity is best suited to understand the mechanism and extent of drug toxicity involved. Topics will include a general overview of the different types of in vitro models available to assess drug toxicity, what are some of their inherent strengths and limitations, and what factors need to be considered when deciding which model to use. Those scientists involved in medicinal chemistry, DMPK, safety pharmacology and toxicology will benefit from this overview by understanding some aspects of how safety assessments are made.
Terry Van Vleet, Ph.D., DABT, Head of Molecular and Computational Toxicology, Department of Preclinical Safety, Abbvie
Will Proctor, Ph.D., Senior Scientist, Head of Investigative Toxicology, Department of Safety Assessment, Genentech
WPC DAY 2 DINNER SHORT COURSES
Wednesday, June 14, 7:00 - 9:30 pm (Dinner Provided)
SC8: Applications of Functional Screening Using CRISPR and RNAi
This course will offer details on how the CRISPR (Clustered Regularly Interspaced Short Palindromic Repeats)/Cas technology works, how to set up CRISPR-based screens and how to complement it with existing RNAi-based screens using proper analysis and follow-up studies. The instructors will share their experiences on how to go about evaluating reagents/libraries, designing and setting up assays, and interpreting results when dealing with complex biology and informatics. The applications of such functional genomics screens for drug discovery and disease modeling will be discussed, along with design and workflows when working with different model systems. Ideas and best practices will be shared in an informal, interactive setting and attendees will walk away with practical advice and resources.
Jennifer Smith, Ph.D., Assistant Director, ICCB-Longwood Screening Facility, Harvard Medical School
John Doench, Ph.D., Associate Director, Genetic Perturbation Platform, Broad Institute of Harvard and MIT
Roderick Beijersbergen, Ph.D., Group Leader, Netherlands Cancer Institute and Head, NKI Robotics and Screening Center
Michael Bassik, Ph.D., Assistant Professor, Department of Genetics, Stanford University
SC9: Importance of Solubility in Drug Discovery and Development Applications
This short course will cover the importance of solubility in achieving proper concentration, as well as techniques and tools for achieving the desired pharmacological response. It will discuss solubility measurements, predicting solubility, parameters that impact solubility, solubility diagnosis in discovery and impact of solubility on absorption and in vitro assays.
Bernard Faller, Director, Discovery ADME, Novartis Institutes for BioMedical Research, Basel
Manuel Sanchez-Felix, Senior Fellow, Chemical & Pharmaceutical Profiling, Novartis Institutes for BioMedical Research, Cambridge
Suzanne Skolnik, Investigator, Analytical Chemistry Group, Novartis Institutes for BioMedical Research, Cambridge
SC10: Humanized Mouse Models for Preclinical Assessment of Cancer Immunotherapy
The development of severely immunodeficient IL2r null mice that support engraftment of functional human immune systems has enabled the in vivo study of human immunity. This presentation will include a general overview of these humanized mouse models, describing currently available strains, the protocols to generate humanized mice, the strengths of each system and a discussion of the application of these models to study human immunology.
Michael Brehm, Ph.D., Associate Professor, The Robert and Sandra Glass Term Chair in Diabetes, Diabetes Center of Excellence, Program in Molecular Medicine, University of Massachusetts Medical School
SC11: 3D Lung Models
Lung disease causes more than 200,000 deaths annually in the United States. These numbers highlight the need for new, physiologically relevant models for translational lung research. Lab-grown 3D lung models can help because they provide a model to screen drugs, understand gene function, and study complex human diseases, such as asthma, COPD, cancer, and respiratory diseases caused by infectious agents and the environment.
Thomas J. Goodwin, Ph.D., NASA (retired) & Sovaris Aerospace
Kambez H. Benam, D.Phil., Technology Development Fellow, Wyss Institute for Biologically Inspired Engineering, Harvard University
Additional Instructors to be Announced
* The program is subject to change without notice, due to unforeseen reason.