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New RAD51 Inhibitors to Target Homologous Recombination in Human Cells
Journal article   Open access   Peer reviewed

New RAD51 Inhibitors to Target Homologous Recombination in Human Cells

Irina S. Shkundina, Alexander A. Gall, Alexej Dick, Simon Cocklin and Alexander Mazin
Genes, v 12(6), p920
01 Jun 2021
PMID: 34208492
url
https://doi.org/10.3390/genes12060920View
Published, Version of Record (VoR)CC BY V4.0 Open

Abstract

Genetics & Heredity Life Sciences & Biomedicine Science & Technology
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.

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32 citations in Scopus

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Collaboration types
Domestic collaboration
Web of Science research areas
Genetics & Heredity
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