Understanding Allosteric Modulation and Functional Selectivity at G Protein-Coupled Receptors

GPCRs are the most important class of receptors in the human genome and are involved in virtually all
physiological processes. They are key players in the major health burdens of the 21st century, including
mental illness, obesity & diabetes, cardiovascular disease, cancer and inflammation. This project seeks to
gain a more detailed fundamental understanding of the mechanisms of GPCR function by small molecule
ligands. More specifically, our research will address two novel and exciting biological paradigms that have
emerged in recent years, GPCR allosteric modulation and functional selectivity, and provide novel chemical
tools and optimized biological assays for detecting and quantifying these phenomena