Publication: Reevaluation of bromodomain ligands targeting BAZ2A
Reevaluation of bromodomain ligands targeting BAZ2A
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Cazzanelli, G., Dalle Vedove, A., Parolin, E., D’Agostino, V. G., Unzue, A., Nevado, C., Caflisch, A., & Lolli, G. (2023). Reevaluation of bromodomain ligands targeting BAZ2A. Protein Science, 32(9), e4752. https://doi.org/10.1002/pro.4752
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BAZ2A promotes migration and invasion in prostate cancer. Two chemical probes, the specific BAZ2-ICR, and the BAZ2/BRD9 cross-reactive GSK2801, interfere with the recognition of acetylated lysines in histones by the bromodomains of BAZ2A and of its BAZ2B paralog. The two chemical probes were tested in prostate cancer cell lines with opposite androgen susceptibility. BAZ2-ICR and GSK2801 showed different cellular efficacies in accordance with their unequal selectivity profiles. Concurrent inhibition of BAZ2 and BRD9 did not reproduce t
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Cazzanelli, G., Dalle Vedove, A., Parolin, E., D’Agostino, V. G., Unzue, A., Nevado, C., Caflisch, A., & Lolli, G. (2023). Reevaluation of bromodomain ligands targeting BAZ2A. Protein Science, 32(9), e4752. https://doi.org/10.1002/pro.4752