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Fig. 1 | Journal of Experimental & Clinical Cancer Research

Fig. 1

From: Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer

Fig. 1

Evaluation of BRD4-PROTACs (MZ1 and ARV-825) efficacy in comparison with BET inhibitors (JQ1 and OTX-015) in MDA-MB-231 and MDA-MB-231-derived JQ1-resistant cells (MDA-MB-231R). a. MDA-MB-231 and MDA-MB-231R were treated with JQ1, MZ1, and ARV-825 for 12, 24, or 48 h (0.4 μM). Then, cells were lysed and 25 μg of total protein extract were analyzed by Western-blot with anti-BRD4 and anti-BRD2 antibodies. Calnexin was used as loading control.b.Parental and resistant-derived models were treated with JQ1, MZ1, OTX-015 and ARV-825 (0.2,0.4 and 1 μM). The inactive stereoisomer Cis-MZ1 was used as negative control. Cell viability was evaluated by metabolization of MTT after 48 or 96 h.c. MDA-MB-231 and MDA-MB231R were seeded in a semi-solid matrigel matrix the day prior the beginning of the treatments. Then, matrigel invasion capacity following a 72 h treatment with JQ1, MZ1, and ARV-825 (0.4 μM) was assessed and invading 3D structures were measured. Diameter scores are shown as arbitrary units. Scale bar = 100 μm. d. Colony formation ability after 12 h exposure to JQ1, MZ1, or ARV-825 (0.4 μM). Following the treatments, cells were seeded at low density (500 cells/well) and, 10 days later, fixed, stained with crystal violet, and counted. *p < 0.05; **p < 0.01; ***p < 0.001

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