Projects

Class A G Protein-Coupled Receptor (GPCR) Projects

  • Use of photoaffinity labeling and mutagenesis to explore the molecular basis of natural cholecystokinin (CCK) ligand binding to its receptor and refine our understanding of the structure of ligand-receptor complexes in active and inactive states (as well as molecular modeling of these complexes).
  • Use of fluorescence to probe microdomains involved in CCK ligand binding, as well as conformational changes associated with receptor activation.
  • Structure-based rational design and optimization of CCK receptor-active drugs, including both orthosteric and allosteric ligands.
  • Analysis of the impact of the lipid microenvironment on CCK receptor structure and function.
  • Applications of CCK receptor-active drugs for the control of appetite and obesity.

Class B G Protein-Coupled Receptor (GPCR) Projects

  • Use of photoaffinity labeling and mutagenesis to explore the molecular basis of natural secretin ligand binding and activation of its receptor (as well as molecular modeling of these complexes).
  • Use of fluorescence to probe microenvironments involved in secretin ligand binding, as well as conformational changes associated with receptor activation.
  • Analysis of the quaternary structure of receptor complexes, including dimerization and oligomerization, as well as association with other regulatory proteins.
  • Evaluation of the molecular basis of drug action and definition of "druggable" pockets within class B GPCRs.
  • Application of class B GPCRs and receptor-active drugs for the management of diabetes and obesity.