Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/7322
Title: Pharmacophore-Based Virtual Screening for Identification of Negative Modulators of GLI1 as Potential Anticancer Agents
Authors: Manetti, Fabrizio 
Stecca, Barbara
Santini, Roberta
Maresca, Luisa
Giannini, Giuseppe
Taddei, Maurizio 
Petricci, Elena 
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.
Description: 
208947
URI: http://hdl.handle.net/20.500.12779/7322
ISSN: 1948-5875
DOI: 10.1021/acsmedchemlett.9b00639
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