@article{e620cd75d1cd4ac9ae7058abdc7fbf90,
title = "New rad51 inhibitors to target homologous recombination in human cells",
abstract = "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.",
keywords = "DNA repair, Homologous recombination, Small-molecule inhibitors, Triple-negative breast cancer",
author = "Shkundina, {Irina S.} and Gall, {Alexander A.} and Alexej Dick and Simon Cocklin and Mazin, {Alexander V.}",
note = "Funding Information: Funding: This research was funded by NCI: National Institutes of Health, Grants R01 CA188347 and P30CA056036 (to AVM), NIH/NIAID grant R01AI150491 (to SC). Funding Information: This research was funded by NCI: National Institutes of Health, Grants R01 CA188347 and P30CA056036 (to AVM), NIH/NIAID grant R01AI150491 (to SC).MDA-MB-231 and MCF 10A cells were a gift from M. Reginato, and the U-2 OS DR-GFP cell line was a gift from R. Pomerantz. ddSceGR plasmid was a gift from S. Powell. We thank C. Sell for help with U-2 OS IndDR-GFP cell line construction, and for guidance in cell proliferation and cell cycle analysis assays. We thank J. Shumsky for help with statistical analysis. Publisher Copyright: {\textcopyright} 2021 by the authors. Licensee MDPI, Basel, Switzerland.",
year = "2021",
month = jun,
doi = "10.3390/genes12060920",
language = "English (US)",
volume = "12",
journal = "Genes",
issn = "2073-4425",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "6",
}