Three-Dimensional Structure of the Smoothened Receptor: Implications for Drug Discovery

摘要: The recently described high resolution three-dimensional structures of the transmembrane and extracellular domains human Smoothened (Smo) receptor higlight both conserved unique structural features this G protein-coupled receptor. It enables a better understanding very subtle molecular mechanisms regulating Smo function demonstrates plastic nature which is able to accommodate diverse array small weight ligands through several binding sites. This information should pave way for designing modulators targeting different sites insensitive clinically observed mutations.