Tuesday April 22, 2014 12:00-3:00pm

SC2: GPCR Structure-Based Drug Discovery*

Instructors:
Vsevolod (Seva) Katritch, Ph.D., Assistant Professor, Integrative Structural and Computational Biology, The Scripps Research Institute

Jan Steyaert, Ph.D., Director, Structural Biology Brussels Research Center, Vrije University Brussels

This course will review the new structural knowledge now available for many G Protein-Coupled Receptors (GPCRs) based on their recently elucidated crystal structures. The instructors will explore with participants, how new findings are impacting rational drug design approaches for GPCRs. There will also be a focus on tools now showing progress against GPCRs such as fragment-based approaches and using antibodies to probe GPCR structure for extracting information that enables the medicinal chemist to more efficiently design GPCR-targeted ligands.

  • Review of recent structures and their lessons
  • Working with fragments
  • Dealing with conformational states
  • Antibodies as probes for structure

Instructor Biographies:

Vsevolod KatritchVsevolod (Seva) Katritch, Ph.D., Assistant Professor, Integrative Structural and Computational Biology, The Scripps Research Institute. 

Dr. Katritch received Ph.D. in Biophysics & Molecular Biology from Moscow Institute of Physics and Technology. Following postdoctoral training at the Chemistry Department of Rutgers University, Dr. Katritch held a position as a Director of Computational Biology at SiGA Technologies Inc. Upon return to academia in 2009, Dr. Katritch joined the faculty of the UCSD School of Pharmacy, and then the Department of Integrative Structural and Computational Biology at The Scripps Research Institute. His current research is focused on development and application of 3D molecular modeling and bioinformatics tools to explore structure, function and pharmacology of membrane proteins and specifically of the GPCR superfamily.

Jan SteyaertJan Steyaert, Ph.D., Director, Structural Biology Brussels Research Center, Vrije University Brussels 

Jan Steyaert is a full professor at the Vrije Universiteit Brussel. He teaches biochemistry and protein engineering for chemists, biologists and bio-engineers. Jan Steyaert made his Ph.D. at the protein engineering department of Plant Genetic Systems (currently Bayer Crop science). After a postdoc at the International Livestock Research Institute (Nairobi, Kenya), he joined the laboratory of Structural Biology of Lode Wyns. His research team focuses on the investigation of the structure and function of proteins and their therapeutic applications. Recent work involves the use of single domain antibodies (nanobodies) derived from camels to rigidify flexible regions and obscure aggregative surfaces on proteins. Stable complexes with nanobodies warrant conformationally uniform samples that are key to protein structure determination by X-ray crystallography.



*Separate registration is required