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Biological membranes act as selective barriers that separate the interior of cells from their outside environment. Membrane proteins play crucial roles in a wide range of biological and physiological processes and are targeted by a large number of pharmacologically active compounds including ~ 50% of the drugs in use today. Lack of high-resolution structural information has become a bottleneck for the mechanistic understanding of membrane proteins and hinders potential drug development. Our research interest lies primarily in understanding the mechanism and regulation of these dynamic membrane proteins, and developing small molecule modulators based on their structures and functions. We are taking a multi-disciplinary approach, employing structural methods to capture the high-resolution picture of different states, functional assays and biophysical methods to dissect the information inferred from the structure and computational approaches to understand their dynamics and kinetics.