Short Courses*

Short courses at Drug Discovery Chemistry are designed to be instructional and interactive. The class size allows for one-on-one interactions between the instructors and attendees. Time is also built into the schedule for Q&A throughout. The courses include introductions for those new to the field, as well as explanations on more technical aspects than time allows during our main conference presentations. Instructors are drawn from industry and academics alike, many of whom are recognized authorities in their fields or have teaching experience.

Morning Short Courses

Monday, April 13 | 10:00 am - 1:00 pm

SC1: Biochemistry and Pharmacology of the Ubiquitin-Proteasome System


Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston

  • Mechanisms of E1, E2, E3, and deubiquitinating enzymes (DUBs)
  • Assays and technologies, enzyme inhibitors
  • PROTACs and molecular glues

SC2: Immunology Basics for Chemists


Timothy Bauler, PhD, Assistant Professor, Biomedical Sciences, Western Michigan University School of Medicine

  • Organization of the immune system
  • Inflammation and innate immunity
  • Functions of T cells and B cells
  • Molecular basis of pathogenic immune responses

SC3: Pharmacology Tricks of the Trade: Identifying Highly Active Compounds and Avoiding Assay Artifacts


Sam Hoare, PhD, Founder, Pharmechanics LLC

  • Designing assays for successful lead optimization and discovery
  • Assay properties discussed: binding kinetics, buffer compositions, target concentration, artificial signaling systems

Afternoon Short Courses

Monday, April 13 | 2:00 - 5:00 pm

SC4: Fragment-Based Drug Design: Tools and Techniques


Daniel Erlanson, PhD, Vice President, Chemistry, Frontier Medicines

Ben Davis, PhD, Research Fellow, Vernalis Research

  • Pros and cons of fragment-based approaches
  • Properties of a good fragment and a good fragment library
  • Finding, validating, and characterizing low-affinity ligands
  • What to do with a fragment: growing, linking, and more
  • Orthogonal screening methods

SC5: Macrocyclic Compounds for Drug Discovery: Opportunities, Challenges, and Strategies


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 and macrocyclization challenges
  • Drug discovery and development examples

SC6: Emerging Chemical Tools for Phenotypic Screening and Target Deconvolution


Paul Brennan, PhD, Associate Professor, Medicinal Chemistry, University of Oxford; Principal Investigator, Target Discovery Institute, Structural Genomics Consortium

Robert Kyne, PhD, Senior Scientist, Chemical Biology, Celgene

Hua Xu, PhD, Associate Research Fellow, Medicine Design, Pfizer

  • Chemical biology tools and probes for MoA studies
  • Constructing annotated chemical sets for effective screening
  • Case studies highlighting use of small molecules for target identification and validation

Dinner Short Courses

Monday, April 13 | 6:00 - 9:00 pm

SC8: Targeted Protein Degradation Using PROTACs, Molecular Glues, and More


Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston

Additional Instructors to be Announced

  • Molecular events required for PROTAC-mediated degradation
  • New screening technologies available to discover PROTAC and molecular glues for E3 ligases
  • Applying enzymology concepts to the optimization of targeted protein degraders
  • Protein degradation beyond bifunctional degraders

SC9: GPCR Structures and Enabling Biophysical Tools


Matthew Eddy, PhD, Assistant Professor, Chemistry, University of Florida

  • Structurally characterizing GPCRs (X-ray crystallography, cryoEM, NMR)
  • Review of GPCR structures and their implications for drug discovery
  • Biophysical tools for membrane proteins (NMR, fluorescence spectroscopy, EPR, and SPR)

SC10: Trends in Physical Properties of Drugs


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 impacting drug efficacy, development, delivery, and formulation including:

  • Position and intensity of pKa throughout molecules
  • Bioisosteres in medicinal chemistry
  • Crystal structure interpretation, PAINS, tox alerts, and other physical chemical properties

Dinner Short Courses

wednesday, April 15 | 6:30 - 9:30 pm

SC12: DNA-Encoded Libraries & Affinity Selection Methods for Small and Large Molecules


Svetlana Belyanskaya, PhD, Encoded Library Technologies, R&D Platform Technology & Science, GSK Boston

Jonas Schaefer, PhD, Laboratory Head, Encoded Library Technologies, Novartis Institutes for Biomedical Research, Chemical Biology & Therapeutics (CBT), Novartis Pharma AG

  • Overview, comparison, and challenges of affinity-based screening methods for small molecules, peptides, alternative scaffolds, and antibodies
  • Platforms discussed: Phage, Yeast, Ribosome, and mRNA Display
  • DNA-Encoded Libraries (DEL): chemistry and library synthesis, selection methods, data analysis, basic chemistry follow-up, comparison of different platforms, case studies

SC13: Principles of Immuno-Oncology


Timothy Bauler, PhD, Assistant Professor, Biomedical Sciences, Western Michigan University School of Medicine

Thomas Sundberg, PhD, Senior Group Leader, Center for Development of Therapeutics, Broad Institute of MIT and Harvard

  • Basic principles of anti-tumor immune responses
  • Strategies to enhance anti-tumor T/NK cell activity (e.g., CAR-T, checkpoint blockade)
  • Activation of innate cells to initiate anti-tumor immunity
  • Small molecule immuno-oncology targets

SC14: Ligand-Receptor Molecular Interactions and Drug Design


Maricel Torrent, PhD, Principal Research Scientist, Molecular Modeling, AbbVie

  • Medicinal chemistry drug design principles
  • Interpretation of atomic-level protein X-ray and modeled structures of binding mode
  • Understanding the relative amounts of potency gain from different interactions
  • Case studies to illustrate all the design strategies

SC15: Methodologies for Optimizing Drug Clearance and Drug-Drug Interactions


Zhengyin Yan, PhD, Principal Scientist, Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc.

Donglu Zhang, PhD, Principal Scientist, Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc.

  • Applications of drug metabolism in lead optimization
  • In vitro methods for detecting and characterizing bioactivation and soft-spot metabolites
  • Common in vitro assays and methodologies for predicting metabolic clearance
  • CYP regulation and induction
  • Methodologies for predicting drug-drug interactions

*Best Value or separate registration required.

* The program is subject to change without notice, due to unforeseen reason.

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