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|Title:||Pharmacophore-Based Virtual Screening for Identification of Negative Modulators of GLI1 as Potential Anticancer Agents||Authors:||Manetti, Fabrizio
|Keywords:||Pharmacophore-based virtual screening, Hedgehog pathway, GLI-1 modulators, anticancer agents, melanoma, medulloblastoma||Issue Date:||2020||Project:||None||Journal:||ACS MEDICINAL CHEMISTRY LETTERS||Abstract:||
Starting from known GLI1 inhibitors, a pharmacophore-based virtual screening approach was applied to databases of commercially available compounds with the aim of identifying new GLI1 modulators. As a result, three different chemical scaffolds emerged that were characterized by a significant ability to reduce the transcriptional activity of the endogenous Hedgehog-GLI pathway and GLI1 protein level in murine NIH3T3 cells. They also showed a micromolar antiproliferative activity in human melanoma (A375) and medulloblastoma (DAOY) cell lines, without cytotoxicity in non-neoplastic mammary epithelial cells.
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