Publications

Last three years (2018-2020)

[1] Simona Daniele, Deborah Pietrobono, Barbara Costa, Mariateresa Giustiniano, Valeria La Pietra, Chiara Giacomelli, Giuseppe La Regina, Romano Silvestri,3 Maria Letizia Trincavelli, Ettore Novellino, Claudia Martini, Luciana Marinelli. Bax activation blocls self-renewal and induces apoptotis of human glioblastoma stem cells. ACS Chem. Neurosci. ACS Chem. Neurosci. 2018, 9, 85-99. (doi: 10.1021/acschemneuro.7b00023, IF 2016: 3883).


[2] Valeria Famiglini and Romano Silvestri. Indolylarylsulfones, a fascinating story of highly potent HIV type-1 non-nucleoside reverse transcriptase inhibitors. Antiviral Chem. and Chemoth. 2018, 26, 1-19. IF 2018 not yet available. AVCC is published by SAGE since 2017).


[3] Filipović, Nenad; Bjelogrlić, Snežana; Pelliccia, Sveva; Jovanović, Vesna ; Kojić, Milan; Senćanski, Milan; La Regina, Giuseppe; Silvestri, Romano; Muller, Christian; Todorović, Tamara. Selenotriapine – An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity, low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumors Arabian J. Chem. 2017, in press. (doi: 10.1016/j.arabjc.2017.11.017; 5-year IF 4.0).


[4] Riccio, Gennaro; Bottone, Sara; La Regina, Giuseppe; Badolati, Nadia; Passacantilli, Sara; Rossi, Giovanni; Accardo, Antonella; Dentice, Monica; Silvestri, Romano; Novellino, Ettore; Stornaiuolo, Mariano. A negative allosteric modulator of the WNT receptor Frizzled 4 switches into an allosteric. Biochemistry 2018, 57, 839-851. (doi: 10.1021/acs.biochem.7b01087, IF 2017 2.997).


[5] Concetta Saponaro, Sara Sergio, Antonio Coluccia, Maria De Luca, Luca Mologni, Daniele Vergar, Michel Salzet, Isabelle Fournier, Cecilia Bucci, Daniela Bonetti, Candice Gautier, Stefano Gianni, Romano Silvestri, Valeria Famiglini, Valentina Naccarato, Carlo Gambacorti Passerini, Michele Maffia, Addolorata M.L. Coluccia. β-Catenin knockdown promotes NHERF1-mediated survival of colorectal cancer cells: implications for a double-targeted therapy. Oncogene 2018, 37, 3301-3316. (doi: org/10.1038/s41388-018-0170-y, 5-year IF 6.993).


[6] F. Ricci, L. Carrassa, M. S. Christodoulou, D. Passarella, B. Michel, R. Benhida, N. Martinet, A. Hunyadi, E. Ioannou, V. Roussis, L. Musso, S. Dallavalle, R. Silvestri, N. Westwood, M. Mori, C. Ingallina, B. Botta, E. Kavetsou, A. Detsi, Z. Majer, F. Hudecz, S. Bosze, B. Kaminska, T.V. Hansen, P. Bertrand, C. M. Athanassopoulos, G. Damia. A high-throughput screening of a chemical compound library in ovarian cancer stem cells. Combinatorial Chemistry & High Throughput Screening 2018, 21, 50-56 (doi: 10.2174/1386207321666180124093406, IF 2017 1.205).


[7] R. Carnevale, R. Silvestri, L. Loffred, M. Novo, V. Cammisotto, V. Castellani, S. Bartimoccia, F. Violi. Oleuropein, a component of extra virgin olive oil, lowers post-prandial glycaemia in healthy subjects. British Journal of Clinical Pharmacology 2018, 84, 1566-1574. (doi:10.1111/bcp.13589, IF 2018: 3.838).


[8] G. La Regina, R. Bai, A. Coluccia, V. Naccarato, V. Famiglini, M. Nalli, D. Masci, A. Verrico, P. Rovella, C. Mazzoccoli, E. Da Pozzo, C. Cavallini, C. Martini, S. Vultaggio, G. Dondio, M. Varasi, C. Mercurio, E. Hamel, P. Lavia, R. Silvestri. New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors with potential to treat human liver carcinoma and glioblastoma. Eur. J. Med. Chem. 2018, 152, 283-297. (doi: 10.1016/j.ejmech.2018.04.042, IF 2018; IF 2017: 4.816).


[9] Laurène Da Costa, Els Scheers, Antonio Coluccia, Adriano Casulli, Manon Roche, Carole Di Giorgio, Johan Neyts, Thierry Terme, Roberto Cirilli, Giuseppe La Regina, Romano Silvestri, Carmen Mirabelli, Patrice Vanelle. Structure-based drug design of potent pyrazolic derivatives against Rhinovirus replication. J. Med. Chem. 2018, 27, 8402-8416. (doi: 10.1021/acs.jmedchem.8b00931; IF 2018: 6.253).


[10] Antonio Coluccia, Giuseppe La Regina, Valentina Naccarato, Marianna Nalli, Viviana Orlando, Stefano Biagioni, Maria Laura De Angelis, Marta Baiocchi, Candice Gautier, Stefano Gianni, Fiorella Di Pastena, Laura Di Magno, Gianluca Canettieri, Addolorata Maria Luce Coluccia, Romano Silvestri. Drug Design and Synthesis of First in Class PDZ1 targeting NHERF1 Inhibitors as Anticancer Agents. ACS Med. Chem. Lett. 2019, 10, 499-503. article ASAP: doi: 10.1021/acsmedchemlett.8b00532; IF 2018: 3.794)


[11] Giuseppe La Regina, Antonio Coluccia, Valentina Naccarato, Romano Silvestri. New anti-cancer agents through an interaction with tubulin. European Journal of Pharmaceutical Sciences 2019, 131, 58-68. doi: 10.1021/acsmedchemlett.8b00532.


[12] Vittoria Cammisotto, Roberto Carnevale, Cristina Nocella, Lucia Stefanini, Simona Bartimoccia, Pasquale Pignatelli, Daniele Pastori, Antonio Coluccia, Romano Silvestri and Francesco Violi Nox2-mediated platelet activation by glycoprotein (GP) VI: effect of rivaroxaban alone and in combination with aspirin. Biochem. Pharmacol 2019, 163, 111-118. (doi: 10.1016/j.bcp.2019.02.016, IF 2018: 4.235).


[13] Marion Laudette, Antonio Coluccia, Yannis Sainte-Marie, Andrea Solari, Loubina Fazal, Pierre Sicard, Romano Silvestri, Sandrine Pons, Bijan Ghaleh, Jean-Paul Blondeau, Frank Lezoualc’h. Identification of a pharmacological inhibitor of Epac1 that protects the heart against acute and chronic models of cardiac stress. Cardiovascular Reserach 2019, 115, 1766-1777. doi: 10.1093/cvr/cvz076


[14] Simone Pippa, Cecilia Mannironi, Valerio Licursi, Luca Bombardi, Gianni Colotti, Enrico Cundari, Adriano Mollica, Antonio Coluccia, Valentina Naccarato, Giuseppe La Regina, Romano Silvestri, Rodolfo Negri. Small molecule inhibitors of KDM5 histone demethylases increase radio-sensitivity of breast cancer cells over-expressing JARID1B. Molecules 2019, 24, 1739-1758 (doi:10.3390/molecules24091739, IF 2017: 3098).


[15] Masci, Domiziana; Hind, Charlotte; Islam, Mohammad; Toscani, Anita; Clifford, Melanie; Coluccia, Antonio; Conforti, Irene; Touitou, Meir; Memdouh, Siham; Wei, Xumin; La Regina, Giuseppe; Silvestri, Romano; Sutton, J; Castagnolo, Daniele. Switching on the activity of 1,5-diaryl-pyrrole derivatives againstdrug-resistant ESKAPE bacteria: Structure-activity relationships and mode of action studies. Eur. J. Med. Chem. 2019, 178, 500-514. Doi: 10.1016/j.ejmech.2019.05.087.


[16] Caroline Capdevielle, Angélique Desplat, Justine Charpentier, Francis Saggliocco, Pierre Thiebaud, Nadine Thézé, Sandrine Fédou, Katarzyna B. Hooks, Romano Silvestri, Veronique Guyonnet-Duperat, Mélina Pretel, Anne-Aurélie Raymond, Jean-William Dupuy, Christophe F. Grosset, Martin Hagedorn. HDAC inhibition induces expression of scaffolding proteins critical for tumor progression in pediatric glioma: focus on EBP50 and IRSp53. Neuro-Oncology 2019, 20, 1-13 doi: org/10.1093/neuonc/noz215.


[17] Giuseppe La Regina, Michela Puxeddu, Marianna Nalli, Daniela Vullo, Paola Gratteri, Claudiu Trandafir Supuran Alessio Nocentini, Romano Silvestri. Discovery of new 1,1’-biphenyl-4-sulfonamides as selective sub-nanomolar human carbonic anhydrase II inhibitors. ACS Med. Chem. Lett. 2019, 11, 633-637. in press. 10.1021/acsmedchemlett.9b00437.


[18] Michela Puxeddu, Hongliang Shen, Ruoli Bai, Antonio Coluccia, Marianna Nalli, Carmela Mazzoccoli, Eleonora Da Pozzo, Chiara Cavallini, Claudia Martini, Viviana Orlando, Stefano Biagioni, Cristina Mazzoni, Addolorata Maria Luce Coluccia, Ernest Hamel, Te Liu, Romano Silvestri, Giuseppe La Regina. Structure-activity relationship studies and in vitro and in vivo anticancer activity of novel 3‑aroyl-1,4-diarylpyrroles against solid tumors and hematological malignancies. Eur. J. Med. Chem 2020, 185, 111828 Article 111828. /doi.org/10.1016/j.ejmech.2019.111828.


[19] Sharon Spizzichino, Giulio Mattedi, Kate Lauder, Coralie Valle, Wahiba Aouadi, Bruno Canard, Etienne Decroly, Suzanne J.F. Kaptein, Johan Neyts, Carl Graham, Zakary Sule, David J. Barlow, Romano Silvestri, Daniele Castagnolo. Design, synthesis and discovery of novel N,N’-carbazoyl-aryl-urea inhibitors of Zika NS5 methyltransferase and virus replication. ChemMedChem 2020, 15, 1-7. doi: 10.1002/cmdc.201900533.


[20] Antonio Coluccia, Michela Puxeddu, Marianna Nalli, Chih-Ku Wei, Yu-Hsuan Wu, Eloise Mastrangelo, Tasneem Mohmmed, Delia Tarantino, Joachim Jakob Bugert, Benno Schreiner, Juliane Nolte, Frank Schwarze, Giuseppe La Regina, Jin-Ching Lee, Romano Silvestri. Discovery of new Zika Virus NS2B/NS3 inhibitors that prevent mice from life-threatening infection and brain damage. ACS Med. Chem. Lett. 2020, 11, 10, 1869-1874. doi: org/10.1021/acsmedchemlett.9b00405. Special issue in memory of Maurizio Botta.


[21] Romina Scala, Adele Di Matteo, Antonio Coluccia, Alessandra Lo Sciuto, Luca Federici, Carlo Travaglini-Allocatelli, Paolo Visca, Romano Silvestri, Francesco Imperi. Mutational analysis of the essential lipopolysaccharide-transport protein LptH of Pseudomonas aeruginosa to uncover critical oligomerization sites. Sci. Reports 2020, accepted.


[22] Marianna Bufano, Marion Laudette, Jean-Paul Blondeau, Frank Lezoualc’h, Marianna Nalli, Romano Silvestri, Andrea Brancale, Antonio Coluccia. Modeling Epac1 Interactions with the allosteric inhibitor AM-001 by co-solvent molecular dynamics. J. Comp.-Aid. Mol. Des. 2020, accepted


[23] Nalli, Marianna; Armijos Rivera, Jorge; Masci, Domiziana; Crespan, Emmanuele; Coluccia, Antonio; Badia, Roger; Riveira Muñoz, Eva; Brambilla, Alessandro; Cinquina, Elisabetta; Turriziani, Ombretta; Falasca, Francesca; Catalano, Myriam; Limatola, cristina; Este, Jose; Maga, Giovanni; Silvestri, Romano; La Regina, Giuseppe. New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. Eur. J. Med. Chem. 2020, 208, 112696


[24] Laura Di Magno, Fiorella Di Pastena, Michela Puxeddu, Giuseppe La Regina, Antonio Coluccia, Alessia Ciogli, Simone Manetto, Marella Maroder, Gianluca Canettieri, Romano Silvestri, Marianna Nalli. Sulfonamide inhibitors of b-catenin signaling with different output on c-MYC as anticancer agents. ChemMedChem 2020, 15, 2264-2268.


[25] Francesca Malagrinò, Antonio Coluccia, Marianna Bufano, Giuseppe La Regina, Michela Puxeddu, Angelo Toto, Lorenzo Visconti, Alessio Paone, Maria Chiara Magnifico, Francesca Troilo, Francesca Cutruzzolà, Romano Silvestri and Stefano Gianni. Targeting the interaction between the SH3 domain of Grb2 and Gab2. Cells 2020, 9, 2435. Doi: doi.org/10.3390/cells9112435.