Luisa
Baracaldo

Colombian Research Scholars Program Evaluation of BRD7 inhibitors in prostate and breast cancer cell models

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Authors:

Luisa Baracaldo

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Bromodomain-containing protein 7 (BRD7) has been reported to be involved in the advancemen of several types of cancer. However, little is known about the role of BRD7 in prostate cancer (PCa). Previous efforts in our research group BRD7 knockdown results demonstrated that reduced expression of BRD7 decreased cell proliferation in androgen receptor(AR)-positive PCa cells, while having little to no effect on normal epithelial prostate cells or AR-negative PCa cells. To further study the role of BRD7 in PCa and demonstrate its value as potential therapeutic target, we developed two BRD7-selective inhibitors, 1-78 and 2-77, which are cellular active and inhibit proliferation in PCa cells at 1 µM. However, an IC50 for the compounds in different PCa cell lines had not been reported. Additionally, the compounds had not been tested in other models of disease. In the present study, we determined IC50 values of the inibitors in PCa cell-based models representing the different stages of the disease, and observed higher sensibility in AR-positive cells. Moreover, we tested the compounds in a triple-negative breast cancer cell model and observed BRD7 knockdown as well as treatment with 2-77 inhibit cell growth and migration.

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Purdue University / 2023

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Luisa Baracaldo

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