D3-βArr is a positive allosteric modulator of TSHR (thyrotropin receptor) for β-Arr 1-mediated signaling that initiates translocation of β-Arr 1 by direct TSHR activation, while showing no agonistic effect on cAMP production. D3-βarr is a positive allosteric modulator for TSH-enhanced osteoblast differentiation.
positive allosteric modulator of TSHR (thyrotropin receptor) for β-Arr 1-mediated signaling
The Journal of pharmacology and experimental therapeutics, 364(1), 38-45 (2017-11-02)
Recently, we showed that TSH-enhanced differentiation of a human preosteoblast-like cell model involved a β-arrestin 1 (β-Arr 1)-mediated pathway. To study this pathway in more detail, we sought to discover a small molecule ligand that was functionally selective toward human
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