| Literature DB >> 28841282 |
Federico Falchi1, Elisa Giacomini1, Tiziana Masini1, Nicolas Boutard1, Lorenza Di Ianni2, Marcella Manerba2, Fulvia Farabegoli3, Lara Rossini4, Janet Robertson4, Saverio Minucci5,6, Isabella Pallavicini5, Giuseppina Di Stefano2, Marinella Roberti3, Roberto Pellicciari4, Andrea Cavalli1,3.
Abstract
In BRCA2-defective cells, poly(adenosine diphosphate [ADP]-ribose) polymerase inhibitors can trigger synthetic lethality, as two independent DNA-repairing mechanisms are simultaneously impaired. Here, we have pharmacologically induced synthetic lethality, which was triggered by combining two different small organic molecules. When administered with a BRCA2-Rad51 disruptor in nonmutant cells, Olaparib showed anticancer activity comparable to that shown when administered alone in BRCA2-defective cells. This strategy could represent an innovative approach to anticancer drug discovery and could be extended to other synthetic lethality pathways.Entities:
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Year: 2017 PMID： 28841282 DOI： 10.1021/acschembio.7b00707
Source DB: PubMed Journal: ACS Chem Biol ISSN： 1554-8929 Impact factor: 5.100