2006
DOI: 10.1210/en.2005-0687
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The Human Thyrotropin Receptor Is Predominantly Internalized by β-Arrestin 2

Abstract: The beta-arrestin-dependent endocytosis of the beta2-adrenergic receptor (beta2AR) has been demonstrated by confocal fluorescence microscopy. Furthermore, a constitutively activated beta2AR is also constitutively desensitized and down-regulated. To clarify the function of beta-arrestin 1 or 2 for TSH receptor (TSHR) desensitization and examine whether constitutively activated TSHR mutants are internalized in a different way, we investigated the TSHR trafficking in association with beta-arrestins in cotransfect… Show more

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Cited by 58 publications
(43 citation statements)
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“…8). There was no apparent TSHR internalization in HEK-TSHR cells or in HEK-TSHR cells expressing K44A (data not shown) but robust internalization in HEK-TSHR cells expressing ␤Arr2, as has been reported previously (Frenzel et al, 2006;Neumann et al, 2010a). However, G␣ q -YFP remained at the surface of all cells including cells expressing ␤Arr2 (Fig.…”
Section: Resultssupporting
confidence: 84%
“…8). There was no apparent TSHR internalization in HEK-TSHR cells or in HEK-TSHR cells expressing K44A (data not shown) but robust internalization in HEK-TSHR cells expressing ␤Arr2, as has been reported previously (Frenzel et al, 2006;Neumann et al, 2010a). However, G␣ q -YFP remained at the surface of all cells including cells expressing ␤Arr2 (Fig.…”
Section: Resultssupporting
confidence: 84%
“…Desensitization, internalization, and functional importance of the arrestin proteins have been demonstrated for other LGR GPCRs: TSHR, LHR, and FSHR. These receptors undergo ␤-arrestin 1 and 2-dependent desensitization with enhanced internalization by ␤-arrestin 2 (20 -22), TSHR has a higher affinity to ␤-arrestin 2 than ␤-arrestin 1 (22). We investigated the desensitization and down-regulation of signaling of RXFP1 after relaxin treatment.…”
Section: Discussionmentioning
confidence: 99%
“…Since constitutively active mutant GPCRs may or may not exhibit constitutive desensitization and down-regulation, depending on the particular receptor and the location of the activating mutation (Frenzel et al, 2006;Pei et al, 1994;Quellari et al, 2003), we studied the kinetics of desensitization and internalization of the N431I mutant FSHR. For this purpose, HEK-293 transiently transfected with the WT and mutant FSHR cDNAs were incubated with increasing concentrations of FSH for 2 h and then exposed to high concentrations of agonist for 30 min.…”
Section: Desensitization and Internalization Of The N431i Mutant Fshrmentioning
confidence: 99%