SC5: GPCR Structure-Based Drug Discovery
Monday, September 19, 2016 | 12:00 - 3:00 pm
Instructors:
Matthew Eddy, Ph.D. Postdoctoral Fellow, Ray Stevens Laboratory, The Bridge Institute, University of Southern California
Huixian Wu, Ph.D., Senior Scientist, Structural Biology and Biophysics, Groton Center of Chemistry, Pfizer Inc.
Recent breakthroughs in obtaining high resolution structures of G Protein-Coupled Receptors (GPCRs) are rapidly impacting the pharmaceutical industry. This course will review the most recently elucidated GPCR crystal structures and explore how new structural information is guiding rational drug design approaches for targeting GPCRs. This course will also review the role of conformational dynamics in GPCR function and cover structural biology techniques, including the burgeoning field of applying nuclear magnetic resonance (NMR), to study GPCR structure and dynamics.
Topics to be covered:
Huixian Wu will cover:
- Overview of GPCRs and their impact in the pharmaceutical industry
- Approaches for crystallization of GPCRs
- Review of GPCR structures and their lessons
Matthew Eddy will cover:
- GPCR conformational dynamics: roles in function and drug discovery
- Application of nuclear magnetic resonance (NMR) to study GPCR structure and dynamics
- Review of recent studies of GPCR dynamics and their lessons
Instructors:
Matthew Eddy, Ph.D. Postdoctoral Fellow, Ray Stevens Laboratory, The Bridge Institute, University of Southern California
Dr. Matthew Eddy is a physical chemist who specializes in the investigation of the structure and conformational dynamics of membrane proteins, including G Protein-Coupled Receptors, using nuclear magnetic resonance (NMR). Dr. Eddy received his Ph.D. from the Massachusetts Institute of Technology, working in the laboratory of Professor Robert Griffin. During his Ph.D., Dr. Eddy developed new methodologies for applying solid state NMR to study the structure and dynamics of membrane proteins, focusing on discovering the mechanism of ion selectivity of the human mitochondrial membrane protein VDAC. After completing his Ph.D, Dr. Eddy joined the laboratory of Professor Ray Stevens at The Scripps Research Institute. There, he began working in collaboration with Professor Kurt Wüthrich to investigate the conformational dynamics of G Protein-Coupled Receptors with solution nuclear magnetic resonance. Dr. Eddy has authored or coauthored over 21 publications and is currently an American Cancer Society postdoctoral fellow in Professor Stevens’ laboratory at the University of Southern California.
Huixian Wu, Ph.D., Senior Scientist, Structural Biology and Biophysics, Groton Center of Chemistry, Pfizer Inc.
Dr. Huixian Wu is interested in using x-ray crystallography to understand the structures of important drug targets and their interaction with small molecule compounds, with particular specialization in membrane proteins. Dr. Wu received her Ph.D. in Structural Biology and Chemistry from The Scripps Research Institute (TSRI) working with Prof. Ray Stevens focusing on G Protein-Coupled Receptor (GPCR). While in Stevens laboratory, Dr. Wu determined the crystal structures of several important human GPCRs, including the kappa opioid receptor, the first class C GPCR, metabotropic glutamate receptor, the first class F GPCR, smoothened receptor, and authored multiple Nature and Science papers. After completing her Ph.D., Dr. Wu joined Prof. Stuart L. Schreiber’s group in The Broad Institute (Cambridge, MA) as a post-doctoral Associate, working on structure-based drug discovery targeting the inflammatory bowel diseases. Currently, Dr. Wu is a Senior Scientist in Groton Center of Chemistry, Pfizer Inc. working on structure-based drug discovery targeting GPCRs.