New rad51 inhibitors to target homologous recombination in human cells

25Citations
Citations of this article
46Readers
Mendeley users who have this article in their library.

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.

Cite

CITATION STYLE

APA

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

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Save time finding and organizing research with Mendeley

Sign up for free