TESMER LAB RESEARCH SUMMARY

Molecular Basis of Signal Transduction

Our lab studies the molecular basis of G protein-coupled receptor (GPCR)-mediated signal transduction, principally via the technique of X-ray crystallography. GPCRs are responsible for the sensations of sight and smell, for regulation of blood pressure and heart rate, and for many other cellular events. Extracellular signals impinging upon GPCRs in the cell membrane induce a conformational change that allows these proteins to activate specific heterotrimeric G proteins within the cell. The activated G proteins then bind to various effectors that initiate downstream cascades, leading to profound physiological change. Activated GPCRs also specifically interact with GPCR kinases (GRKs), which function to inhibit signaling by heterotrimeric G proteins and to initiate G protein-independent signaling cascades. By determining atomic structures of these signaling proteins both alone and in complex with their various targets, we provide important insights into the molecular basis of signal transduction and of diseases that emerge as a result of dysfunctional signaling.

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Regulation of Effectors by Heterotrimeric G Proteins

G protein-coupled receptor kinases (GRKs)

Structure Based Drug Design