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説明

Hedgehog proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of Smoothened. In vertebrates, this ultimately leads to the activation of the zinc-finger transcription factors of the GLI family. Overactivation of this pathway contributes to certain cancers, including glioblastoma, for which the GLI proteins are named. GANT 61 is a GLI antagonist, inhibiting GLI1 activation of gene expression with an IC50 value of 5 μM. It does not affect signaling through NF-κB, glucocorticoid receptor, MAPK, HGF, C/EBPα, or HIF-1, supporting specificity for the Hedgehog pathway. GANT 61 has been shown to inhibit the in vitro proliferation of PANC-1 and 22Rv1 cancer cells, which have elevated GLI1 levels, and prevent the development of 22Rv1 tumors in mice.