Short Courses*

Monday, April 18, 2016
Morning Courses | 10:00 am – 1:00 pm

SC1: Trends in Physical Properties of Drugs


Terry Stouch, Ph.D., President, R&D, Science for Solutions, LLC

Robert Fraczkiewicz, Ph.D., Team Leader, Simulations Plus, Inc.

John Comer, Ph.D., CSO, Sirius Analytical Ltd.

  • Properties important for enhanced efficacy, delivery, and formulation
  • pKa, tautomerism, crystallization, others
  • Computational prediction: What works - what doesn’t
  • Experimental best practices

SC2: GPCR Structure-Based Drug Discovery


Matthew Eddy, Ph.D. Postdoctoral Fellow, Ray Stevens Laboratory, The Bridge Institute, University of Southern California

Huixian Wu, Ph.D., Senior Scientist, Groton Center of Chemistry, Pfizer Inc. 
  • Review of recent GPCR structures and their lessons
  • Approaches for crystallization of GPCRs
  • GPCR conformational dynamics
  • Application of nuclear magnetic resonance (NMR) to study GPCR structure and dynamics

SC3: Designing Peptide Therapeutics for Specific PPIs


Nir Qvit, Ph.D., Postdoctoral Associate, Chemical & Systems Biology Operations, Stanford University School of Medicine
Opher S. Kornfeld, Ph.D. Candidate, Department of Chemical and Systems Biology, Stanford University School of Medicine

  • Designing novel modulators of protein interactions based on sequence homology, domain conversation and protein structure
  • Synthesis of novel inhibitors to target specific protein-protein interactions
  • Development of peptidomimetics that derive from an active site to improve stability, activity and bioavailability

Afternoon Courses | 2:30 – 5:30 pm

SC4: Immunology Basics for Chemists


Seng-Lai “Thomas” Tan, Ph.D., Senior Director, Immunology, FORMA Therapeutics

Songqing Na, Ph.D., Senior Scientist, Biotechnology & Autoimmunity Res-AME, Eli Lilly and Company

  • Review of immune system’s cellular players
  • Review of inflammatory process
  • Autoimmune & inflammation-related diseases
  • Current treatment landscape and promising drug targets

SC5: Phenotypic Screening and Chemical Probe Development

Instructor: Samarjit Patnaik, Ph.D., Research Scientist, Probe Development Center, NCATS, NIH

  • Overview of modern phenotypic drug discovery using examples from literature and NCATS
  • Screening assay designs and phenotypic systems
  • Strategies to elucidate MOA and options for de-convoluting molecular targets
  • Development of chemical probes at NCATS

Dinner Courses | 6:00 – 9:00 pm

SC7: Ligand-Receptor Molecular Interactions and Drug Design

Instructor: Maricel Torrent, Ph.D., 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 modes
  • Understanding the relative amounts of potency gain from different interactions
  • Case studies illustrate all of the design strategies

SC8: Inhibitor Design using MOE SBDD Applications

Daniel Chang, Ph.D., Applications Scientist, Chemical Computing Group

Alain Ajamian, Ph.D. Director Chemical Computing Group

  • Analyzing protein active sites with molecular surfaces and maps
  • Generating pharmacophore models to capture essential ligand binding features
  • Application of docking to determine ligand poses in the active site  
  • Fragment-based design applications for scaffold replacement
  • A virtual reaction-based combinatorial approach for R-group screening

Wednesday, April 20, 2016
Dinner Courses | 6:30 – 9:30 pm

SC10: Enabling Macrocyclic Compounds for Drug Discovery: Opportunities, Challenges and Strategies


Mark L. Peterson, Ph.D., COO, Cyclenium Pharma, Inc.

Eric Marsault, Ph.D., Professor, Medicinal Chemistry and Pharmacology, University of Sherbrooke

  • 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: Advancing Tools and Technologies for Fragment-Based Design

Instructors: Daniel A. Erlanson, Ph.D., Co-Founder, Carmot Therapeutics, Inc.

Ben Davis, Ph.D., Research Fellow, Biology, Vernalis Research

  • 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

SC12: Introduction to Targeted Covalent Inhibitors

Instructors: Mark Schnute, Ph.D., Associate Research Fellow, Biotherapeutics Chemistry & Immunoscience Research, Pfizer Global R&D

Christoph Zapf, Ph.D., Senior Principal Scientist, Worldwide Medicinal Chemistry, Pfizer Research Labs

  • 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
  • Mechanism of drug resistance

*Separate Registration Required