GPCRs control a multitude of cellular processes by coupling to a variety of intracellular proteins, including arrestins, kinases and G proteins. A major current direction in drug discovery involves a search for functionally selective or biased ligands that promote signaling of a given GPCR through desired pathways while avoiding signaling through undesired pathways, by causing the GPCR to trigger selective activation of a particular intracellular protein. To enable these efforts, we are using atomic-level simulations, together with complementary experimental data, to determine how GPCRs cause the structural changes in various intracellular proteins that lead these proteins to activate and signal.<br/>

One receptor, many partners: How do GPCRs stimulate diverse signaling proteins?

255th National Meeting (2018)

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