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Modeling activated states of GPCRs: the rhodopsin template.


ABSTRACT: Activation of G Protein-Coupled Receptors (GPCRs) is an allosteric mechanism triggered by ligand binding and resulting in conformational changes transduced by the transmembrane domain. Models of the activated forms of GPCRs have become increasingly necessary for the development of a clear understanding of signal propagation into the cell. Experimental evidence points to a multiplicity of conformations related to the activation of the receptor, rendered important physiologically by the suggestion that different conformations may be responsible for coupling to different signaling pathways. In contrast to the inactive state of rhodopsin (RHO) for which several high quality X-ray structures are available, the structure-related information for the active states of rhodopsin and all other GPCRs

SUBMITTER: Niv MY 

PROVIDER: S-EPMC4030242 | biostudies-literature | 2006 Jul-Aug

REPOSITORIES: biostudies-literature