Smoothened
Smoothened is a protein that is not a G protein-coupled receptor (it is instead a GPCR-like receptor) that is a component of the hedgehog signaling pathway and is conserved from flies to humans. It is the molecular target of the teratogen cyclopamine. Cellular localization plays an essential role in the function of SMO. Stimulation of the patched receptor by the sonic hedgehog ligand leads to translocation of SMO to the primary cilium. Furthermore, SMO that is mutated in the domain required for ciliary localisation cannot contribute to pathway activation. SMO has also been shown to bind the kinesin motor protein Costal-2 and play a role in the localization of the Ci (Cubitus interruptus transcription factor) complex.
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MRT 10是Smoothened (Smo) 拮抗剂。
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IHR 1是活性的 Smo(Smoothened) 拮抗剂。
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Purmorphamine与Smo拮抗剂竞争性结合到Smoothened，并激活Smoothened，IC50约为1.5 μM，也诱导成骨细胞分化，EC50为1μM。
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LDE225 (NVP-LDE225,Erismodegib)是一种Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，IC50分别为1.3 nM (小鼠)和2.5 nM(人)。
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Cyclopamine是一种特异性的Hedgehog (Hh)信号通路拮抗剂，作用于Smoothened (Smo)，IC50为46 nM。
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