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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: de franco f. 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. Among authors: de franco f. 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: de franco f. 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: de franco f. 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.
α-Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) Inhibitors as Novel Modulators of De Novo Nicotinamide Adenine Dinucleotide (NAD+) Biosynthesis.
Pellicciari R, Liscio P, Giacchè N, De Franco F, Carotti A, Robertson J, Cialabrini L, Katsyuba E, Raffaelli N, Auwerx J. Pellicciari R, et al. Among authors: de franco f. J Med Chem. 2018 Feb 8;61(3):745-759. doi: 10.1021/acs.jmedchem.7b01254. Epub 2018 Jan 26. J Med Chem. 2018. PMID: 29345930
Development of 3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites.
Cerra B, Venturoni F, Souma M, Ceccarelli G, Lozza AM, Passeri D, De Franco F, Baxendale IR, Pellicciari R, Macchiarulo A, Gioiello A. Cerra B, et al. Among authors: de franco f. Eur J Med Chem. 2022 Nov 15;242:114652. doi: 10.1016/j.ejmech.2022.114652. Epub 2022 Aug 20. Eur J Med Chem. 2022. PMID: 36049273
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
Bartolini D, De Franco F, Torquato P, Marinelli R, Cerra B, Ronchetti R, Schon A, Fallarino F, De Luca A, Bellezza G, Ferri I, Sidoni A, Walton WG, Pellock SJ, Redinbo MR, Mani S, Pellicciari R, Gioiello A, Galli F. Bartolini D, et al. Among authors: de franco f. J Med Chem. 2020 Apr 9;63(7):3701-3712. doi: 10.1021/acs.jmedchem.0c00012. Epub 2020 Mar 20. J Med Chem. 2020. PMID: 32160459 Free PMC article.
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Pellicciari R, Passeri D, De Franco F, Mostarda S, Filipponi P, Colliva C, Gadaleta RM, Franco P, Carotti A, Macchiarulo A, Roda A, Moschetta A, Gioiello A. Pellicciari R, et al. Among authors: de franco f, franco p. J Med Chem. 2016 Oct 13;59(19):9201-9214. doi: 10.1021/acs.jmedchem.6b01126. Epub 2016 Oct 4. J Med Chem. 2016. PMID: 27652492
Probing the Binding Site of Bile Acids in TGR5.
Macchiarulo A, Gioiello A, Thomas C, Pols TW, Nuti R, Ferrari C, Giacchè N, De Franco F, Pruzanski M, Auwerx J, Schoonjans K, Pellicciari R. Macchiarulo A, et al. Among authors: de franco f. ACS Med Chem Lett. 2013 Oct 15;4(12):1158-62. doi: 10.1021/ml400247k. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900622 Free PMC article.
46 results