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- W2895032130 endingPage "380" @default.
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- W2895032130 abstract "Protein-protein interactions are attractive targets because they control numerous cellular processes. In oncology, apoptosis regulating Bcl-2 family proteins are of particular interest. Apoptotic cell death is controlled via PPIs between the anti-apoptotic proteins hydrophobic groove and the pro-apoptotic proteins BH3 domain. In ovarian carcinoma, it has been previously demonstrated that Bcl-xL and Mcl-1 cooperate to protect tumor cells against apoptosis. Moreover, Mcl-1 is a key regulator of cancer cell survival and is a known resistance factor to Bcl-2/Bcl-xL pharmacological inhibitors making it an attractive therapeutic target. Here, using a structure-guided design from the oligopyridine lead Pyridoclax based on Noxa/Mcl-1 interaction we identified a new derivative, active at lower concentration as compared to Pyridoclax. This new derivative selectively binds to the Mcl-1 hydrophobic groove and releases Bak and Bim from Mcl-1 to induce cell death and sensitize cancer cells to Bcl-2/Bcl-xL targeting strategies." @default.
- W2895032130 created "2018-10-12" @default.
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- W2895032130 date "2018-11-01" @default.
- W2895032130 modified "2023-10-18" @default.
- W2895032130 title "Structure-guided design of pyridoclax derivatives based on Noxa / Mcl-1 interaction mode" @default.
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- W2895032130 doi "https://doi.org/10.1016/j.ejmech.2018.10.003" @default.