2018 Short Courses*
MONDAY, APRIL 2, 2:00 - 5:00 PM
SC1: Ligand-Receptor Molecular Interactions and Drug Design - Learn More
Instructor: Maricel Torrent, PhD, Senior Scientist, AbbVie
- Drug design principles generally applicable to all medicinal chemistry programs
- Interpretation of atomic-level protein X-ray and modeled structures of binding model
- Understanding the relative amounts of potency gain from different interactions
- Case studies illustrate all the design strategies
SC2: Advancing Tools and Technology for Fragment-Based Design - Learn More
Instructors: Daniel A. Erlanson, PhD, Co-Founder, Carmot Therapeutics, Inc.
Mary Harner, Ph.D., Research Investigator II, Mechanistic Biochemistry, Bristol-Myers Squibb R&D
- Why fragments – pros and cons
- What makes a good fragment, and a good fragment library
- Finding, validating and characterizing low affinity ligands
- The importance of using orthogonal screening methods
- What to do with a fragment – growing, linking, and more
SC3: Drug Metabolism and Its Impact on Decisions in Lead Discovery and Drug Development - Learn More
Instructor: John C. L. Erve, PhD, DABT, Consultant, Jerve Scientific Consulting, Inc.
- Applying drug metabolism concepts to lead optimization
- Impact of drug structures on important PK parameters
- Common assays for predicting clearance and metabolism-based drug-drug interactions
- Growing application of in silico tools in drug metabolism
- Role of bioactivation in drug toxicity
SC4: Diversity-Oriented Platforms for Ligand Discovery - Learn More
Instructors: Sepideh Afshar, PhD, Principal Research Scientist, Department of Protein Engineering, Eli Lilly and Company
Svetlana Belyanskaya, PhD, Encoded Library Technologies, R&D Platform Technology & Science, GSK Boston
Pros and cons of affinity based screening platforms in drug discovery:
- Phage display
- mRNA display
- DNA-encoded libraries
MONDAY, APRIL 2, 6:00 - 9:00 PM
SC5: Immunology Basics for Chemists - Learn More
Instructors: Songqing Na, PhD, Senior Scientist, Biotechnology & Autoimmunity Res-AME, Eli Lilly and Company
Thomas Sundberg, PhD, Senior Research Scientist I, Center for Development of Therapeutics, Broad Institute of MIT and Harvard
- Review of immune system’s cellular players
- Review of inflammatory process
- Autoimmune & inflammation-related diseases
- Current treatment landscape and promising drug targets
- Principles in immune-oncology (e.g., checkpoint blockade)
SC6: Introduction to Allosteric Modulators and Biased Ligands of GPCRs - Learn More
Instructor: Terry Kenakin, PhD, Professor, Department of Pharmacology, University of North Carolina School of Medicine
- Overview of allosteric modulators and pathway biased ligands
- Approaches for screening and validation
- Fitting functional allosteric data to obtain allosteric drug parameters
SC7: Introduction to Targeted Covalent Inhibitors - Learn More
Instructor: Mark Schnute, PhD, Associate Research Fellow, Biotherapeutics Chemistry & Immunoscience Research, Pfizer Global R&D
- Overview of covalent drugs, irreversible and reversible inhibitors including recent clinical examples
- Biochemical analysis of covalent inhibitors
- Design considerations for targeted covalent inhibitors
- De-risking covalent inhibitors
SC8: Introduction to the Ubiquitin Proteasome System - Learn More
Instructor: Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston
- Mechanisms of E1, E2, E3, and DUB enzymes
- Technologies available and experimental controls
- Discovered inhibitors and emerging biology
WEDNESDAY, APRIL 4, 6:30 - 9:00 PM
SC9: Impact of Convergence of Immunotherapy and Epigenetics on Drug Discovery - Learn More
Instructors: Katherine Chiappinelli, PhD, Assistant Professor, Department of Microbiology, Immunology, and Tropical Medicine, The George Washington University Cancer Center
Alejandro Villagra, PhD, Assistant Professor, Department of Biochemistry and Molecular Medicine, School of Medicine and Health Sciences, The George Washington University
Wayne W. Hancock, MD, PhD, Professor of Pathology and Chief of Transplant Immunology, Children's Hospital of Philadelphia and University of Pennsylvania
- Epigenetic pathways that intersect and interact with the immune system
- Effect of epigenetic therapies on the tumor and host immune system
- Exploiting immunoepigenetics to enhance the efficacy of current drug treatments
- Case studies highlighting promises and challenges
SC10: Enabling Macrocyclic Compounds for Drug Discovery: Opportunities, Challenges and Strategies - Learn More
Instructors: Eric Marsault, PhD, Professor, Medicinal Chemistry and Pharmacology, University of Sherbrooke
Mark Peterson, PhD, COO, Cyclenium Pharma, Inc.
- Unique characteristics of macrocycles
- Factors affecting cell permeability and PK/ADME properties
- Synthetic strategies for macrocyclic compound libraries & macrocyclization challenges
- Drug discovery and development examples and future perspectives
SC11: Trends in Physical Properties of Drugs - Learn More
Instructors: Terry Stouch, PhD, President, R&D, Science for Solutions, LLC
Robert Fraczkiewicz, PhD, Team Leader, Simulations Plus, Inc.
Max Totrov, PhD, Principal Scientist, MolSoft, LLC
- Properties important for enhanced efficacy, delivery, and formulation
- pKa, tautomerism, crystallization, others
- Computational prediction: What works - what doesn’t
- Experimental best practices
SC12: Covalent Fragments: Applications in Target-Based and Phenotypic Screens - Learn More
Instructor: Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston
- Design principles of covalent fragment libraries, target-based and phenotypic screens using covalent fragments
- Strategies to grow fragments into drug leads, and case studies
- Coupling covalent fragment growth with selectivity profiling in cells
*Separate registration required