Smoothened Receptor Antagonists

Smoothened (Smo) receptors are non-classical G-protein-coupled receptors that belong to the Frizzled family. Smoothened receptors lack the ability to directly interact with their endogenous ligand, Hedgehog (Hh). In the resting state, Smo receptors are bound to and repressed by patched (Ptc).

Upon Hh-Ptc interaction, Smo receptors are liberated and phosphorylated (activated). This initiates a signaling cascade that controls the activity of transcription factors belonging to the Gli family ...