Structure-based drug discovery for G Protein Coupled Receptors
G-protein coupled receptors (GPCRs) represent the largest family of membrane proteins in the human genome, and the largest class of targets for drug discovery. More than 30% of FDA approved drugs target GPCRs. They mediate the majority of cellular response to hormones and neurotransmitters. Clinical indications for GPCRs include cardiovascular, pulmonary, metabolic and psychiatric disorders, as well as inflammation, cancer and HIV infection. ConfometRx is developing a platform of structure-based drug discovery technologies to facilitate lead identification and lead optimization for G-protein coupled receptors.
This platform includes:
- the production of pure, functional GPCRs for high-resolution structure determination by crystallography or Cryo-EM
- biophysical technologies for characterizing ligand-induced structural changes in GPCRs
- the generation of GPCR-specific, functional antibodies for target validation, therapeutics and protein crystallography
Brian Kobilka, M.D.
Dr. Kobilka is Professor of Medicine, and Molecular and Cellular Physiology at Stanford University. He has been working in the G protein coupled receptor field for over 30 years. Dr. Kobilka's lab has pioneered the use of biophysical methods to study the structure and mechanism of activation of GPCRs. His lab was the first to obtain a high-resolution crystal structure of a non-rhodopsin GPCR. He has served as a member of the scientific advisory boards of Acadia Pharmaceuticals, Theravance, and 7TM Pharma. Dr. Kobilka has a BS degree in Biology and Chemistry from the University of Minnesota, and a MD degree from Yale University.
Tong Sun Kobilka, M.D., Chief Executive Officer
Dr. Kobilka is a practicing physician and a research scientist in the Kobilka academic lab at Stanford University. She has extensive research experience in GPCRs including the cloning of several GPCRs, structure/function analysis of the β2 adrenergic receptor, and purification of GPCRs for crystallography. Dr. Kobilka has a BS degree in Biology from the University of Minnesota, Masters degrees in Microbiology from Iowa State University and East Asian Studies from Yale University, and a MD degree from Stanford University.