【摘 要】
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Seven transmembrane receptors are important drug targets and exhibiting multiple functional behaviors in response to natural and synthetic ligands.A traditi
【机 构】
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School of Medicine Shandong University China
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Seven transmembrane receptors are important drug targets and exhibiting multiple functional behaviors in response to natural and synthetic ligands.A traditional agonist bound receptor will stabilize receptor-G protein complex and transducer signal downstreams.Recently, research revealed the multiple ligands can function not only through couple to G protein, but also by forming other receptor effector complexes, including arrestin, GRKs, NHERF and other signaling proteins.Efforts to obtain a ternary complex of ligand-receptor-effector are of great importance but encountered the difficulty of produce receptor in vitro and inherent instability of the complex in detergent solutions.Recently,using beta2-adreno-receptor as a model, by a serial molecular engineering, we reconstituted several ligand-receptoreffector complexes in vitro.These complexes display different binding properties and functional efficacies toward a panel of beta2-adreno-receptor ligands.
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