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ID: ALA4613300

Journal: ACS Med Chem Lett

Title: Pharmacophore-Based Virtual Screening for Identification of Negative Modulators of GLI1 as Potential Anticancer Agents.

Authors: Manetti F, Stecca B, Santini R, Maresca L, Giannini G, Taddei M, Petricci E.

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.

CiteXplore: 32435392

DOI: 10.1021/acsmedchemlett.9b00639