Smoothened
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Smoothened is a protein that in humans is encoded by the SMO gene. Smoothened is not a G protein-coupled receptor[1] (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.[2]
Contents
Function
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.[3] 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.[4]
SMO can function as an oncogene. Activating SMO mutations can lead to unregulated activation of the hedgehog pathway and cancer.[5]
Agonists
Antagonists
- Cyclopamine
- Itraconazole
- Vismodegib (Erivedge), a smoothened receptor inhibitor for the treatment of basal-cell carcinoma, being investigated for the treatment of other types of cancer
See also
References
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Further reading
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External links
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- SMO protein, human at the US National Library of Medicine Medical Subject Headings (MeSH)
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