New RAD51 Inhibitors to Target Homologous Recombination in Human Cells.
Genes (Basel)
; 12(6)2021 06 16.
Article
en En
| MEDLINE
| ID: mdl-34208492
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.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores Enzimáticos
/
Recombinasa Rad51
/
Quinazolinonas
/
Recombinación Homóloga
/
Antineoplásicos
Límite:
Humans
Idioma:
En
Revista:
Genes (Basel)
Año:
2021
Tipo del documento:
Article
País de afiliación:
Estados Unidos
Pais de publicación:
CH
/
SUIZA
/
SUÍÇA
/
SWITZERLAND