GANT 58 is a GLI-1 and GLI-2 (GLI) antagonist and an inhibitor of GLI induced transcription. Reported to inhibit the hedgehog (Hh) signaling pathway downstream of SUFU and SMO thereby affecting GLI1 nuclear accumulation. It also displays antiproliferative and antitumor activity in vivo.
1. Lauth, Matthias., et al., 2007. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proceedings of the National Academy of Sciences of the United States of America. 104(20): 8455-60. PMID: 17494766
2. Beauchamp, Elspeth., et al., 2009. GLI1 is a direct transcriptional target of EWS-FLI1 oncoprotein. The Journal of biological chemistry. 284(14): 9074-82. PMID: 19189974
3. Joo, Jay., et al., 2009. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PloS one. 4(10): e7608. PMID: 19859563
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