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- W1600219771 abstract "The adrenergic receptors (AR) are members of the superfamily of G protein-coupled receptors (GPCRs) which transduce signals across the cell membrane. Mutational analysis of several GPCRs has revealed that the transmembrane domains (TMDs) contribute to the formation of the ligand binding pocket, whereas the amino acid sequences of the intracellular loops appear to mediate receptor-G-protein coupling. A conservative substitution (A293E) in the C-terminal portion of the third intracellular loop of the α1B-AR results in its constitutive (agonist-independent) activity. GPCRs can undergo an allosteric transition between at least two different states, R and R*. In the absence of ligand the inactive state R predominates, possibly because a structural constraint might prevent sequences of the intracellular loops to interact with the G proteins. The release of such constraint would trigger the conversion into the active state R*, which couples to G proteins. A novel strategy is proposed to explore the structural and dynamic properties of the active state of a GPCR and the potential molecular changes correlate with the transition from R to R*." @default.
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- W1600219771 date "1997-01-01" @default.
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- W1600219771 title "Constitutively active α1B-adrenergic receptor mutants: Potential mechanisms underlying receptor activation" @default.
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- W1600219771 doi "https://doi.org/10.1016/s0165-7208(97)80083-9" @default.
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