Abstract
Methods Specific binding of LDE225 to human and mouse Smo protein was investigated in competitive displacement assays using a labeled small molecule Smo agonist (Hh-Ag 1.5). Inhibition of formation and induction of regression of basaloid tumors was determined in skin punch cultures derived from Ptch ± heterozygous knock-out mice. Inhibition of hair growth and Hh-target gene expression during early anagen phase was assessed after topical application of 0.3 or 1% solutions of LDE225 to depilated back skin of C57/BL6 mice twice daily for 7 days. Moreover, the penetration properties of LDE225 into and through human skin in vitro and pig skin in vitro and in vivo were tested.
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