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An 19F NMR fragment-based approach for the discovery and development of BRCA2-RAD51 inhibitors to pursuit synthetic lethality in combination with PARP inhibition in pancreatic cancer.
Myers SH, Poppi L, Rinaldi F, Veronesi M, Ciamarone A, Previtali V, Bagnolini G, Schipani F, Ortega Martínez JA, Girotto S, Di Stefano G, Farabegoli F, Walsh N, De Franco F, Roberti M, Cavalli A. Myers SH, et al. Among authors: roberti m. Eur J Med Chem. 2024 Feb 5;265:116114. doi: 10.1016/j.ejmech.2023.116114. Epub 2023 Dec 31. Eur J Med Chem. 2024. PMID: 38194775 Free article.
Rad51/BRCA2 disruptors inhibit homologous recombination and synergize with olaparib in pancreatic cancer cells.
Roberti M, Schipani F, Bagnolini G, Milano D, Giacomini E, Falchi F, Balboni A, Manerba M, Farabegoli F, De Franco F, Robertson J, Minucci S, Pallavicini I, Di Stefano G, Girotto S, Pellicciari R, Cavalli A. Roberti M, et al. Eur J Med Chem. 2019 Mar 1;165:80-92. doi: 10.1016/j.ejmech.2019.01.008. Epub 2019 Jan 10. Eur J Med Chem. 2019. PMID: 30660828
Synthetic Lethality in Pancreatic Cancer: Discovery of a New RAD51-BRCA2 Small Molecule Disruptor That Inhibits Homologous Recombination and Synergizes with Olaparib.
Bagnolini G, Milano D, Manerba M, Schipani F, Ortega JA, Gioia D, Falchi F, Balboni A, Farabegoli F, De Franco F, Robertson J, Pellicciari R, Pallavicini I, Peri S, Minucci S, Girotto S, Di Stefano G, Roberti M, Cavalli A. Bagnolini G, et al. Among authors: roberti m. J Med Chem. 2020 Mar 12;63(5):2588-2619. doi: 10.1021/acs.jmedchem.9b01526. Epub 2020 Feb 24. J Med Chem. 2020. PMID: 32037829 Free PMC article.
Identification of RAD51-BRCA2 Inhibitors Using N-Acylhydrazone-Based Dynamic Combinatorial Chemistry.
Bagnolini G, Balboni B, Schipani F, Gioia D, Veronesi M, De Franco F, Kaya C, Jumde RP, Ortega JA, Girotto S, Hirsch AKH, Roberti M, Cavalli A. Bagnolini G, et al. Among authors: roberti m. ACS Med Chem Lett. 2022 Jul 28;13(8):1262-1269. doi: 10.1021/acsmedchemlett.2c00063. eCollection 2022 Aug 11. ACS Med Chem Lett. 2022. PMID: 35978685 Free PMC article.
Synthetic Lethality Triggered by Combining Olaparib with BRCA2-Rad51 Disruptors.
Falchi F, Giacomini E, Masini T, Boutard N, Di Ianni L, Manerba M, Farabegoli F, Rossini L, Robertson J, Minucci S, Pallavicini I, Di Stefano G, Roberti M, Pellicciari R, Cavalli A. Falchi F, et al. Among authors: roberti m. ACS Chem Biol. 2017 Oct 20;12(10):2491-2497. doi: 10.1021/acschembio.7b00707. Epub 2017 Sep 1. ACS Chem Biol. 2017. PMID: 28841282 Free article.
Innovative Strategy toward Mutant CFTR Rescue in Cystic Fibrosis: Design and Synthesis of Thiadiazole Inhibitors of the E3 Ligase RNF5.
Brusa I, Sondo E, Pesce E, Tomati V, Gioia D, Falchi F, Balboni B, Ortega Martínez JA, Veronesi M, Romeo E, Margaroli N, Recanatini M, Girotto S, Pedemonte N, Roberti M, Cavalli A. Brusa I, et al. Among authors: roberti m. J Med Chem. 2023 Jul 27;66(14):9797-9822. doi: 10.1021/acs.jmedchem.3c00608. Epub 2023 Jul 13. J Med Chem. 2023. PMID: 37440686 Free PMC article.
276 results