Exploring the potential of selective FKBP51 inhibitors on melanoma: an investigation of their in vitro and in vivo effects.

ABSTRACT: FKBP51 is a marker of melanocyte malignancy, correlating with vertical growth phase and lesion thickness. It promotes the typical features of epithelial to mesenchymal transition and sustains apoptosis resistance. The present study aimed to assess in vitro and in vivo the efficacy against melanoma of selective small molecules targeting FKBP51, called SAFits. Our findings reveal differing outcomes for SAFits in vitro compared to in vivo. SAFit increased the doxorubicin and dacarbazine cytotoxicity of cultured melanoma cells and was effective in impairing NF-κB activity and related pro-survival genes. Moreover, SAFit affected TGF-β-signaling and reduced the capability of melanoma cells to migrate through transwell filters and invade the matrigel. Unexpectedly, SAFit was ineffective in reduci

SUBMITTER: Marrone L 

PROVIDER: S-EPMC11969000 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature