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• W2982030496 endingPage "105105" @default.
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• W2982030496 abstract "Deepening understanding of how Bcl-2 family proteins protect cancer cells from apoptosis has driven the development of 'BH3 mimetic' drugs that target various anti-apoptotic Bcl-2-like proteins by mimicking their natural inhibitors, the BH3-only proteins. The proof of target engagement and an on-target mechanism validation are critical for evaluating drug development potential. To evaluate target engagement of BH3 mimetics in cells, we measured binding potency of ABT-199, A-1210477 and ABT-737 to Bcl-2 and Mcl-1 proteins by using a dose-response cellular thermal shift assay (CETSA), similar affinity rank-order and selectivity were obtained in comparison with in vitro binding assays. A proof of direct target engagement for S1 and AT-101 was obtained through CETSA assay. By using a previously established mathematical model, we simulated individual death response of various cancer cell lines to ABT-199, S1 or AT-101 in comparison with experimental data. A positive correlation between model predictions and experimental data for ABT-199 and S1 showed that dual Bcl-2 and Mcl-1 target engagement underlies their anticancer efficacy. In contrast, an off-target effect was determined for AT-101." @default.
• W2982030496 created "2019-11-01" @default.
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• W2982030496 date "2020-01-01" @default.
• W2982030496 modified "2023-10-15" @default.
• W2982030496 title "Using CETSA assay and a mathematical model to reveal dual Bcl-2/Mcl-1 inhibition and on-target mechanism for ABT-199 and S1" @default.
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• W2982030496 doi "https://doi.org/10.1016/j.ejps.2019.105105" @default.
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