Article
Mutations that silence constitutive signaling activity in the allosteric ligand-binding site of the thyrotropin receptor.
Cellular and molecular life sciences : CMLS - 1 Jan 2011
Haas Ann-Karin, Kleinau Gunnar, Hoyer Inna, Neumann Susanne, Furkert Jens, Rutz Claudia, Schülein Ralf, Gershengorn Marvin C, Krause Gerd
Abstract excerpt
The thyrotropin receptor (TSHR) exhibits elevated cAMP signaling in the basal state and becomes fully activated by thyrotropin. Previously we presented evidence that small-molecule ligands act allosterically within the transmembrane region in contrast to the orthosteric extracellular hormone-binding sites. Our goal in this study was to identify positions that surround the allosteric pocket and that are sensitive...
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