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0026-895X/04/6506-1323-1332$20.00
Mol Pharmacol 65:1323-1332, 2004

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Probing Receptor Structure/Function with Chimeric G-Protein-Coupled Receptors

Dezhong Yin, Shai Gavi, Hsien-yu Wang, and Craig C. Malbon

Departments of Molecular Pharmacology (D.Y., S.G., C.C.M.) and Physiology & Biophysics (H.W.), Diabetes & Metabolic Diseases Research Program (H.W.), University Medical Center, Stony Brook University, Stony Brook, New York

Owing its name to an image borrowed from Greek mythology, a chimera is seen to represent a new entity created as a composite from existing creatures or, in this case, molecules. Making use of various combinations of three basic domains of the receptors (i.e., exofacial, transmembrane, and cytoplasmic segments) that couple agonist binding into activation of effectors through heterotrimeric G-proteins, molecular pharmacology has probed the basic organization, structure/function relationships of this superfamily of heptahelical receptors. Chimeric G-protein-coupled receptors obviate the need for a particular agonist ligand when the ligand is resistant to purification or, in the case of orphan receptors, is not known. Chimeric receptors created from distant members of the heptahelical receptors enable new strategies in understanding how these receptors transduce agonist binding into receptor activation and may be able to offer insights into the evolution of G-protein-coupled receptors from yeast to humans.

Received December 29, 2003; accepted February 26, 2004

Address correspondence to: Craig Malbon, Department of Pharmacology, HSC, Stony Brook University, Stony Brook, NY 11794-8651. E-mail: craig{at}pharm.sunysb.edu




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