Publications of Last five years (since 2021)
[1] V. Pennacchietti, L. Pagano, M. Di Felice, J. Toso, M. Bufano, A. Coluccia, R. Silvestri, R. Capelli, C. Camilloni, F. Malagrinò, A, Toto1, S. Gianni. Unveiling an unexpected redox regulation of the folding, function and inhibition in the PTB domain of FRS2. Int. J. Biol. Macromol. 2025, accepted.
[2] M. Puxeddu, L. Ling, S. Ripa, M. D’Ambrosio, M. Nalli, A. Parisi, P. Sciò, A. Coluccia, A. Granese, M. Santelli, D. Masci, P. Cuřínová, C. Naro, C. Sette, A. Pastore, M. Stornaiuolo, C. Bigogno, G. Dondio, L. Di Magno, G. Canettieri, T. Liu, R. Silvestri, G. La Regina. Development of N-(4-(1H-imidazol-1-yl)phenyl)-4-chlorobenzenesulfonamide, a novel potent inhibitor of β-catenin with enhanced antitumor activity and metabolic stability. J. Med. Chem. 2024, 67, 20298−20314 doi: 10.1021/acs.jmedchem.4c01708.
[3] D. Masci, M. Puxeddu, R. Silvestri, G. La Regina. CBP and p300 targets for Wnt/b-catenin emerging anticancer Agents. Molecules 2024, 28, 4524.
[4] M. Puxeddu, M. Donalisio, J.J. Bugert, A. Corona, P. Cocomazzi, M. Milani, F. Hucke, I. Arduino, F. Esposito, P. Moretti, M.G. Ortore, M. Nalli, S. Manetto, G. Mazzoccanti, C. Bigogno, G. Dondio, P. Sciò, A. Coluccia, D. Lembo, E. Tramontano, R. Silvestri, E. Mastrangelo, G. La Regina. 4-(3-Phenylsulfonylindol-2-yl)-1-(pyridin-2-yl)piperazinyl-methanones as Potent Inhibitors of both SARS-CoV-2 and HCoV-OC43 Viruses. ACS Infectious Diseases 2024, 10, 3158-3175. doi: 10.1021/acsinfecdis.4c00108
[5] H. Roux, F. Touret, A. Coluccia, O. Khoumeri, C. Majdi, P. Sciò, R. Silvestri, P.Vanelle, M. Roche, New potent EV-A71 antivirals targeting capsid. Eur. J. Med. Chem. 2024, 116658. https://doi.org/10.1016/j.ejmech.2024.116658.
[6] D. Masci, M. Puxeddu, R. Silvestri, G. La Regina. Metabolic rewiring in cancer: small molecule inhibitors in colorectal cancer therapy.Molecules 2024, 29, 2110. doi: https://doi.org/10.3390/molecules29092110.
[7] Ćurčić V, Olszewski M, Maciejewska N, Višnjevac A, Srdić-Rajić T, Dobričić V, García-Sosa AT, Kokanov SB, Araškov JB, Silvestri R, Schüle R, Jung M, Nikolić M, Filipović N.R. Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition. Arch Pharm (Weinheim) 2024, 357, e2300426. doi: 10.1002/ardp.202300426.
[8] D. Masci, C. Naro, M. Puxeddu, A. Urbani, C. Sette, G. La Regina, R. Silvestri. Recent advances in drug discovery for TNBC treatment. Molecules 2023, 28, 7513. Doi: https://doi.org/10.3390/molecules28227513.
[9] D. Masci, M. Puxeddu, L. Di Magno, M. D’Ambrosio, A. Parisi, M. Nalli, R. Bai, A. Coluccia, P. Sciò, V. Orlando, S. D’Angelo, S. Biagioni, A. Urbani, E. Hamel, A. Nocentini, S. Filiberti, M. Turati, R. Ronca, J. Kopecka, C. Riganti, C. Fionda, R. Bordone, G. Della Rocca, G. Canettieri, C. T. Supuran, R. Silvestri, G. La Regina. 4-(3-Phenyl-4-(3,4,5-trimethoxybenzoyl)-1H-pyrrol-1-yl)benzenesulfon-amide, a novel carbonic anhydrase and wnt/b-catenin signaling pathway dual targeting inhibitor with potent activity against multi-drug resistant cancer cells. J. Med. Chem. 2023, 66,14824-14842. Doi: 10.1021/acs.jmedchem.3c01424
[10] C. Mazzoccoli, F. Crispo, I. Laurenzana, M. Pietrafesa, L. Sisinni, R. Lerose, D. Telesca, M. R. Milella, T. Liu, J. Sebastiani, R. Silvestri, G. La Regina. Biological evaluation of (4-(4-Aminophenyl)-1-(4-fluorophenyl)-1H-pyrrol-3-yl)(3,4,5-trimethoxyphenyl)methanone as potential antineoplastic agent in 2D and 3D breast cancer models. Archiv der Pharmazie 2023, e2300354. https://doi.org/10.1002/ardp.202300354.
[11] Nalli M., Di Magno L., Wen Y., Liu X. D’Ambrosio, M., Puxeddu, M., Parisi A., Sebastiani, J., Sorato A., Ripa S., Di Pastena F., Capelli D, Montanari R., Masci D., Urbani A., Naro C., Sette C., Orlando V, D’Angelo S., Biagioni S., Bigogno C., Dondio G., Pastore A., Stornaiuolo M., Canettieri G.. Liu, T., Silvestri R., La Regina G. Novel N-(heterocyclylphenyl)benzensulfonamide sharing an unreported binding site with t-cell factor 4 at the β-catenin armadillo repeats domain as anticancer agent. ACS Pharmacol. Transl. Sci. 2023, 6, 1087-1103.doi:10.1021/acsptsci.3c00092. PMCID# PMC10353061.
[12] Marianna Bufano, Michela Puxeddu, Marianna Nalli, Giuseppe La Regina, Angelo Toto, Francesca Romana Liberati, Alessio Paone, Francesca Cutruzzolà, Domiziana Masci, Chiara Bigogno, Giulio Dondio, Romano Silvestri, Stefano Gianni, Antonio Coluccia. Targeting the Grb2 cSH3 domain: design, synthesis and biological evaluation of the first series of modulators. Bioorganic Chemistry 2023, 138, 106607.
[13] Dvoracsko, Szabolcs; Dimmito, Marilisa Pia; Sebastiani, Jessica; La Regina, Giuseppe; Silvestri, Romano; Pieretti, Stefano; Tomboli, Csaba; Stefanucci, Azzurra; Mollica, Adriano. Rimonabant based compounds bearing hydrophobic amino acid derivatives as cannabinoid receptor subtype 1 ligand. ACS Med. Chem. Lett. 2023, 14, 479-486.
[14] K. R. Francisco, L. Monti, W. Wang, H. Park, L. J. Liu, D. Amarasinghe, M. Nalli, R. Silvestri, L. Guidi Magalhães, C. R. Caffreya. Structure-Activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei. Biorg Med. Chem. Lett. 2023, 81, 129123. https://doi.org/10.1016/j.bmcl.2023.129123
[15] R. Carnevale, V. Cammisotto, S. Bartimoccia, C. Nocella, M. Bufano, V. Castellani, L. Loffredo, S. Sciarretta, G. Frati, A. Coluccia, R. Silvestri, G. Ceccarelli, A. Oliva, M. Venditti, F. Pugliese, C. Mastroianni, O. Turriziani, M. Leopizzi, G. D’Amati, P. Pignatelli, F. Violi. Toll-Like Receptor 4-Dependent and Independent platelet-dependent thrombosis in SARS-CoV-2 Infection. Circulation Research 2023, 2023, 132, 290-305. doi: 10.1161/CIRCRESAHA.122.321541.
[16] F. R. Mammone, P. Rotundo, M. Puxeddu, R. Silvestri, R. Cirilli. Chemo- and enantio-selective reversed-phase HPLC analysis of rosuvastatin using a cellulose-based chiral stationary phase in gradient elution mode. Journal of Pharmaceutical and Biomedical Analysis 2023, 225, 115239.
[17] G. Giancotti, G. Nannetti, G. Padalino, M.Landini, N. Santos-Ferreira, J. Van Dycke, V. Naccarato, U. Patel, R. Silvestri, J. Neyts, R. Gozalbo-Rovira, J. Rodríguez-Díaz, J. Rocha-Pereira, A. Brancale, S. Ferla. Marcella Bassetto. Structural investigations on novel non-nucleoside inhibitors of human norovirus polymerase. Viruses 2022, 15, 74.
[18] F. R. Mammone, L. Zanitti, M. Puxeddu, G. La Regina, R. Silvestri, A. Borioni, R. Cirilli. A novel validated UHPLC method for the estimation of rosuvastatin and its complete impurity profile in tablet formulations. Molecules 2023, 28, 431.
[19] J. Sebastiani, M. Puxeddu, M. Nalli, R. Bai, L. Altieri, P. Rovella, E. Gaudio, D. Trisciuoglio, F. Spriano, P. Lavia, C. Fionda, D. Masci, A. Urbani, C. Bigogno, G. Dondio, E. Hamel, F. Bertoni, R. Silvestri, G. La Regina. RS6077 induces mitotic arrest and selectively activates cell death in human cancer cell lines and in a lymphoma tumor in vivo. Eur. J. Med. Chem. 2023, 246, 114997.
[20] M. Innocenti, R. Silvestri, M. Ceracchi, B. Silvestrini. Efficacy and safety of a novel food supplement in the treatment of functional dyspepsia: a pilot open study. Agro Food Industry Hi-Tech 2022 – ISSN 1722-6996
[21] M. Nalli, D. Masci, A. Urbani, G. La Regina, R. Silvestri. Emerging direct targeting β-catenin agents. Molecules 2022, 27, 7735-7747.
[22] M. Puxeddu, J. Wu, R.Bai, M. D’Ambrosio, M. Nalli, A. Coluccia, S. Manetto, A. Ciogli, D. Masci, A. Urbani, C. Fionda, S. Coni, R. Bordone, G. Canettieri, C. Bigogno, G. Dondio, E. Hamel, T. Liu, R. Silvestri, G. La Regina. Induction of ferroptosis in glioblastoma and ovarian cancers by a new pyrrole tubulin assembly inhibitor. J. Med. Chem. 2022, 65, 15805-15818 Doi: 10.1021/acs.jmedchem.2c01457. open access
[23] L. Jimenez, V. Mayoral-Varo, C. Amenábar, J. Ortega, M. Machuqueiro, R. Silvestri, A. Angeli, F. Carta, B. Ferreira, W. Link. Multiplexed cellular profiling using fluorescent fusion proteins identifies an inhibitor of CRM1-mediated nuclear export. Traffic 2022, 23, 587-599.
[24] L. Di Magno, A. Coluccia, Ma. Bufano, S. Ripa, G. La Regina, M. Nalli, G. Canettieri, R. Silvestri, L. Frati. Discovery of novel human lactate dehydrogenase inhibitors: structure-based virtual screening studies, in vitro and in vivo biological assessment. Eur. J. Med. Chem. 2022, 240, 114605. https://doi.org/10.1016/j.ejmech.2022.114605.
[25] M. Bufano, M. Laffranchi, S. Sozzani, D. Raimondo, R. Silvestri, A. Coluccia. Exploring CCRL2 Chemerin binding using Accelerated Molecular Dynamics. Proteins 2022, 1-7. Doi: 10.1002/prot.26348.
[26] A. Coluccia, M. Bufano, G. La Regina, M. Puxeddu, A. Toto, A. Paone, A. Bouzidi, G. Musto, N. Badolati, V. Orlando, S. Biagioni, Domiziana Masci, R. Cirilli, C. Cantatore, F. Cutruzzolà, S. Gianni, M. Stornaiuolo, R. Silvestri. (S)-5-Chloro-3-((3,5-dimethylphenyl)sulfonyl)-N-(1-oxo-1-((pyridin-4-ylmethyl)amino)propan-2-yl),1H-indole-2-carboxamide (RS4690) as a new Dishevelled 1 inhibitor. Cancers 2022, 14, 1358. https://doi.org/10.3390/cancers14051358.
[27] C. Cantatore, G. La Regina, R. Ferretti, R. Silvestri, R. Cirilli. Single-run chemo- and enantio-selective HPLC separation of tramadol and its principal metabolite, O-desmethyltramadol, using a chlorinated immobilized amylose-based chiral stationary phase under multimodal elution conditions. Sep. Sci. Plus 2022, 5, 99-104. https://doi.org/10.1002/sscp.202200009. IF 2020 = 3.645.
[28] M. Nalli, M. Puxeddu, G. La Regina, S. Gianni, R. Silvestri. Emerging therapeutic agents for colorectal cancer. Molecules 2021, 26, 7463. https://doi.org/10.3390/molecules26247463. IF = 4.41
[29] C. Passirani, A. Vessières, G. La Regina, W. Link, R. Silvestri. Modulating undruggable targets to overcome cancer therapy resistance. Drug Resistance Updates 2022, 60, 100788. https://doi.org/10.1016/j.drup.2021.100788. IF = 18.50
[30] Bruno Silvestrini, Romano Silvestri, C.Y. Cheng, Maurizio Ceracchi, Matteo Innocenti. A method to measure the barrier effect of drugs and its application in the study of hydrolyzed collagen. Journal Agro Food Industry Hi-Tech 2021, 32 (3). ISSN 1722-6996
[31] Jana Van Dycke, Michela Puxeddu, Giuseppe La Regina, Eloise Mastrangelo, Delia Tarantino, Jasper Rymenants, Jessica Sebastiani, Marianna Nalli, Jelle Matthijnssens, Johan Neyts, Romano Silvestri, Joana Rocha-Pereira. Discovery of a novel class of Norovirus inhibitors with high barrier of resistance. Pharmaceuticals 2021, 14, 1006-1021 (IF 5.863, doi: 10.3390/ph14101006).
[32] Caterina Nardella, Lorenzo Visconti, Francesca Malagrinò, Livia Pagano, Marianna Bufano, Marianna Nalli, Antonio Coluccia, Giuseppe La Regina, Romano Silvestri, Stefano Gianni, Angelo Toto. Targeting PDZ domains as potential treatment for viral infections, neurodegeneration and cancer. Biology Direct 2021, 16, 15, 1-21. https://doi.org/10.1186/s13062-021-00303-9. IF = 4.78.
[33] Te Liu, Jianchao Wu, Changpeng Han, Zhangbin Gong Giuseppe La Regina, Jiulin Chen, Fangfang Dou, Romano Silvestri, Chuan Chen, Zhihua Yu. RS-5645 attenuates inflammatory cytokine storm induced by SARS-CoV-2 spike protein and LPS by modulating pulmonary microbiota. International Journal of Biological Sciences 2021, 17, 3305-3319. doi:10.7150/ijbs.63329. IF = 6.8.
[34] Shirong Li, Anjian Xu, Yanmeng Li, Chunting Tan, Giuseppe La Regina, Romano Silvestri, Haoyan Wang, Wenjie Qi. RS4651 suppresses lung fibroblast activation via the TGF-β1/SMAD signalling pathway. Eur. J. Pharmacology 2021, 903, 174135. https://doi.org/10.1016/j.ejphar.2021.174135. IF = 4.43.
[35] Michela Puxeddu, Hongliang Shen, Ruoli Bai, Antonio Coluccia, Marianna Bufano, Marianna Nalli, Jessica Sebastiani, Diego Brancaccio, Eleonora Da Pozzo, Chiara Tremolanti, Claudia Martini, Viviana Orlando, Stefano Biagioni, Maria Stefania Sinicropi, Jessica Ceramella, Domenico Iacopetta, Addolorata Maria Luce Coluccia, Ernest Hamel, Te Liu, Romano Silvestri and Giuseppe La Regina. Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia. Eur. J. Med. Chem. 2021, 221, 113532.doi: https://doi.org/10.1016/j.ejmech.2021.113532
[36] Simona Daniele, Valeria La Pietra, Rebecca Piccarducci, Debora Pietrobono, Chiara Cavallini, Vincenzo Maria D’Amore, Stefano Tomassi, Linda Cerofolini, Stefano Giuntini, Pasquale Russomanno, Michela Puxeddu, Marco Fragai,Claudio Luchinat,Ettore Novellino, Sabrina Taliani, Giuseppe La Regina, Romano Silvestri, Claudia Martini,Luciana Marinelli. The CXCR4 antagonism sensitizes cancer cells to novel indole-based MDM2/4 inhibitors in glioblastoma multiforme. European Journal of Pharmacology 2021, 897, e173936
DDSC
Department of Drug Chemistry and Technologies
Sapienza University of Rome
Laboratory affiliated to Istituto Pasteur Italia
Fondazione Cenci Bolognetti
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