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Identification of Novel Smoothened Ligands Using Structure-Based Docking

Fig 6

New Smo antagonists compete for BODIPY-cyclopamine binding.

(A) and (B) Dose-response analysis of BODIPY-cyclopamine displacement in HEK293 cells overexpressing mSmo-mCherry for compound 44 (A) and compound 45b (B). Left: average cell fluorescence was measured by flow cytometry and plotted against antagonist concentration. Representative curve are shown. Right: representative images of BODIPY-cyclopamine displacement by antagonists in HEK293 cells overexpressing mSmo-mCherry. Cells were incubated with 5 nM BODIPY-cyclopamine and compounds 44 or 45b for 2 hours. (C) Specificity of 45b towards Smo is demonstrated by the lack of inhibition of the TOPFLASH Wnt-ß-catenin reporter by compound 45b (10 μM) and vismodegib (100 nM). n = 3, combined experiments, error bars: standard deviation.

Fig 6