G protein-coupled receptors (GPCRs) act as membrane gatekeepers and are the pleiotropic mediators of cellular signaling. GPCRs are the largest receptor superfamily in the human genome and play indispensable roles in almost all known physiological processes. As a result, almost half of the currently prescribed drugs work by targeting GPCRs. Our lab focuses on understanding the underlying molecular basis of GPCR functioning in many physiological and pathophysiological processes. We employ multiple orthogonal and combinatorial approaches ranging from biochemical, biophysical, chemogenetic, and pharmacological methods in our studies. Leveraging this molecular information will enable us to design better and safer GPCR therapeutics.