Gli proteins are the effectors of Hedgehog (Hh) signaling and have been shown to be involved in cell fate determination, proliferation and patterning in many cell types and most organs during embryo development. The Gli transcription factors activate/inhibit transcription by binding to Gli responsive genes and by interacting with the transcription complex. The Gli transcription factors have DNA binding zinc finger domains which bind to consensus sequences on their target genes to initiate or suppress transcription. Research showed that mutating the Gli zinc finger domain inhibited the proteins effect proving its role as a transcription factor. Gli proteins have an 18-amino acid region highly similar to the α-helical herpes simplex viral protein 16 activation domain.
||GANT 61 is an inhibitor of Gli1 and Gli2, used for cancer research.
||GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM.
||Glabrescione B (GlaB) is a small molecule binding to Gli1 zinc finger and impairing Gli1 activity by interfering with Gli1/DNA interaction, inhibits Hh signaling by impairing Gli1 function.
||A novel, synthetic small molecule that efficiently interferes with Gli/TAF9 interaction and downregulate Gli/TAF9-dependent transcriptional activity (at 15 uM).
||Hedgehog-IN-7d is a potent, cell-permeable Hedgehog (Hh) pathway inhibitor that inhibits Gli transcription activity with an IC50 value of 70 nM.