Targeting DNA repair proteins with small-molecule inhibitors became a proven anti-cancer strategy. Previously, we identified an inhibitor of a major protein of homologous recombination (HR) RAD51, named B02. B02 inhibited HR in human cells and sensitized them to chemotherapeutic drugs in vitro and in vivo. Here, using a medicinal chemistry approach, we aimed to improve the potency of B02. We identified the B02 analog, B02-isomer, which inhibits HR in human cells with significantly higher efficiency. We also show that B02-iso sensitizes triple-negative breast cancer MDA-MB-231 cells to the PARP inhibitor (PARPi) olaparib.
CITATION STYLE
Shkundina, I. S., Gall, A. A., Dick, A., Cocklin, S., & Mazin, A. V. (2021). New rad51 inhibitors to target homologous recombination in human cells. Genes, 12(6). https://doi.org/10.3390/genes12060920
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