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.
New RAD51 Inhibitors to Target Homologous Recombination in Human Cells
Creators
Irina S. Shkundina - Drexel University
Alexander A. Gall - IDbyDNA, Bothell, WA 89011, USA.
Alexej Dick - Drexel University
Simon Cocklin - Drexel University
Alexander Mazin - Drexel University
Publication Details
Genes, v 12(6), p920
Publisher
Mdpi
Number of pages
21
Grant note
R01 CA188347; P30CA056036 / NCI: National Institutes of Health; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Cancer Institute (NCI)
R01AI150491 / NIH/NIAID; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Institute of Allergy & Infectious Diseases (NIAID)
Resource Type
Journal article
Language
English
Academic Unit
Biochemistry and Molecular Biology
Web of Science ID
WOS:000666312800001
Scopus ID
2-s2.0-85108870253
Other Identifier
991019168544604721
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Collaboration types
Domestic collaboration
Web of Science research areas
Genetics & Heredity
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