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• W1424914904 abstract "Proc Amer Assoc Cancer Res, Volume 46, 2005670 Lung cancer is a very aggressive disease with a poor prognosis where cisplatin-based regimens are the standard care. Heterotrimeric guanine-binding protein-coupled receptors are involved in lung cancer since multiple GPCR agonists fuel tumor growth, invasion, and metastasis. Thus, the therapeutic impact based on single antagonists acting on a given GPCR is very limited since invasive tumor growth is driven by multiple GPCRs. Here, the novel imidazo-pyrazine derivative BIM-46174 is characterized as an inhibitor of several agonist-activated G-protein signaling pathways linked to cAMP generation, calcium translocation, as well as lung cancer cell invasion. An NCI COMPARE analysis of BIM-46174 showed no similar pattern of antiproliferative activity with standard agents supporting the identification of a novel mechanism of tumor growth inhibition. Furthermore, BIM-46174 combined with cisplatin strongly delays the growth of human NSCLC xenografts in athymic mice. These data obtained with BIM-46174 establish heterotrimeric G-protein signaling as a new therapeutic target in lung cancer, especially in combination with cisplatin. This result was previously reported in SCLC." @default.
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• W1424914904 date "2005-05-01" @default.
• W1424914904 modified "2023-10-18" @default.
• W1424914904 title "The novel inhibitor of heterotrimer G-protein signaling, BIM-46174, enhances the anticancer activity of cisplatin in human NSCLC lung tumor xenografts" @default.
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