New rad51 inhibitors to target homologous recombination in human cells

Irina S. Shkundina, Alexander A. Gall, Alexej Dick, Simon Cocklin, Alexander V. Mazin

Producción científica: Articlerevisión exhaustiva

21 Citas (Scopus)

Resumen

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.

Idioma originalEnglish (US)
Número de artículo920
PublicaciónGenes
Volumen12
N.º6
DOI
EstadoPublished - jun 2021

ASJC Scopus subject areas

  • Genetics(clinical)
  • Genetics

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