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Figure 2 | Molecular Cancer

Figure 2

From: The novel BH3 α-helix mimetic JY-1-106 induces apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein–protein interactions with Bak

Figure 2

JY-1-106 functions as Bcl-xl and Mcl-1 pan-inhibitor. (A) JY-1-106 inhibits the binding of the Bak-BH3 α-helix to Mcl-1, as measured by fluorescence polarization. The sequence of the fluorescently-labeled Bak peptide is FITC-Ahx-GQVGRQLAIIGDDINR-CONH2. (B) 5 × 106 REN cells were exposed to 5 μM JY-1-106, 20 μM ABT-737 or a DMSO control for 12 hours and the cells were then harvested and lysed. Bcl- xL and Bak were immunoprecipitated with specific antibodies. Bak signals and Bcl- xL signals were then detected by western blotting. These experiments were repeated twice. (C) 5 × 106 REN cells were exposed to 5 μM JY-1-106, 20 μM ABT-737 or DMSO control for 12 hours and the cells were then harvested and lysed. Mcl-1 and Bak were immunoprecipitated with specific antibodies. Bak signals and Mcl-1 signals were then detected by western blotting. These experiments were repeated twice.

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Molecular Cancer

ISSN: 1476-4598