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.

Monday, April 8, 10:00 am – 1:00 pm

SC1: Covalent Fragments: Applications in Target-Based and Phenotypic Screens

Topics include: design principles of covalent fragment libraries; target-based and phenotypic screens using covalent fragments; strategies to grow fragments into drug leads; case studies of coupling covalent fragment growth with selectivity profiling in cells.
Instructor:
Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston

SC2: Trends in Physical Properties of Drugs

Topics include: Properties that impact drug efficacy, development, delivery and formulation; including pKa, tautomerism, crystal structure interpretation among others. Use of computational tools.
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

SC3: Introduction to GPCR-Based Drug Discovery

Topics include: GPCR pharmacology, including allosteric modulation; biased signaling, persistent signaling, and accessory proteins; emerging GPCR screening methods, including cellular redistribution assays; affinity mass spectrometry and biosensors.
Instructor:
Annette Gilchrist, PhD, Professor, Department of Pharmacology, Midwestern University

Monday, April 8, 2:00 – 5:00 pm

SC5: Ligand-Receptor Molecular Interactions and Drug Design

Topics include: medicinal chemistry drug design principles illustrated via case studies such as interpretation of atomic-level protein X-ray and modeled structures of binding model; understanding the relative amounts of potency gain from different interactions; and case studies to illustrate all the design strategies.
Instructor:
Maricel Torrent, PhD, Senior Scientist III, Molecular Modeling, AbbVie

SC6: Methodologies for Optimizing Drug Clearance and Drug-Drug Interactions

Topics include: drug metabolism; CYP regulation; the role of bioactivation and how each affects lead optimization; and common assays and methodologies for predicting clearance and drug-drug interactions.
Instructors:
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.

SC7: Emerging Targets for Cancer Immunotherapy

Topics include: recently published data on immunology (STING, RIG- 1), epigenetic (HDAC, HAT), ubiquitin (DUBs, ligases) and autophagy targets; resulting strategies for development of new standalone or combination therapies for many types of cancers.
Instructors:
Wayne W. Hancock, MD, PhD, Professor of Pathology and Chief of Transplant Immunology, Children's Hospital of Philadelphia and University of Pennsylvania
Aditya Murthy, PhD, Scientist, Cancer Immunology, Genentech, Inc.
Additional Instructors to be Announced

Monday, April 8, 6:00 – 9:00 pm

SC9: Advancing Tools and Technologies for Fragment-Based Design

Topics include: pros and cons of fragment-based approaches; what makes a good fragment; properties of a good fragment library; finding, validating and characterizing low affinity ligands; the importance of using orthogonal screening methods; and what to do with a fragment – growing, linking, and more.
Instructors:
Daniel A. Erlanson, PhD, Co-Founder, Carmot Therapeutics, Inc.
Ben Davis, PhD, Research Fellow, Biology, Vernalis Research

SC10: Diversity-Oriented Platforms for Ligand Discovery

Topics include: introduction to and comparison of these affinity-based drug discovery screening platforms: phage display, mRNA display and DNA-encoded libraries.
Instructor:
Svetlana Belyanskaya, PhD, Encoded Library Technologies, R&D Platform Technology & Science, GSK Boston
Additional instructor to be Announced

SC11: Targeted Protein Degradation Using PROTACs and Molecular Glues

Topics include: basic understanding of proteolysis-targeting chimeric molecules (PROTACs); applying PROTACS to target and degrade specific proteins of interest; case studies from instructors’ research.
Instructors:
Lara Gechijian, PhD, Scientist/Project Lead, Jnana Therapeutics; Former Graduate Student, Laboratory of Drs. James Bradner/Nathanael Gray, Harvard Medical School
Eric Fischer, PhD, Assistant Professor, Cancer Biology, Dana-Farber Cancer Institute/Harvard Medical School
Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston

Wednesday, April 10, 6:30 – 9:00 pm

SC13: Biochemistry and Pharmacology of the Ubiquitin-Proteasome System

Topics include: basic mechanistic biochemistry and pharmacology of the ubiquitin proteasome system, including E1, E2, E3, and deubiquitinating enzymes; signaling pathways regulated by UPS; the effect of small molecules on UPS-regulated pathways; assays and technologies for discovering enzyme inhibitors of the UPS system.
Instructor:
Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston

SC14: Immunology Basics for Chemists

Topics include: review of the immune system’s cellular players; review of the inflammatory process; autoimmune and inflammation-related diseases; current treatment landscape; promising drug targets; and principles in immuno-oncology (e.g., checkpoint blockade).
Instructors:
Songqing Na, PhD, Senior Scientist, Biotechnology & Autoimmunity Res-AME, Eli Lilly and Company
Additional Instructor to be Announced

SC15: Macrocyclic Compounds for Drug Discovery: Opportunities, Challenges and Strategies

Topics include: unique characteristics of macrocycles; factors affecting cell permeability and PK/ADME properties; synthetic strategies for macrocyclic compound libraries and macrocyclization challenges; and drug discovery and development examples.
Instructors:
Eric Marsault, PhD, Professor, Medicinal Chemistry and Pharmacology, University of Sherbrooke
Mark Peterson, PhD, COO, Cyclenium Pharma, Inc.

SC16: GPCR Structure-Based Drug Discovery

Topics include: methodologies for the characterization and crystallization of GPCRs; a review of X-ray crystallographic and cryoEM GPCR structures and their lessons; biophysical tools (NMR, fluorescence spectroscopy, EPR, SPR and computational approaches) for observing function-related conformational dynamics of GPCRs; implications of structural knowledge on drug discovery especially related to allosteric modulation by small molecules, ions, and engineered partner proteins.
Instructors:
Matthew Eddy, PhD, Assistant Professor, Chemistry, University of Florida
Additional Instructor to be Announced


*Separate registration required

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