Tuning mTORC1 activity dictates the response of acute myeloid leukemia to LSD1 inhibition
Abdel-Aziz, Amal Kamal, Pallavicini, Isabella, Ceccacci, Elena, Meroni, Giuseppe, Saadeldin, Mona Kamal, Varasi, Mario, Minucci, Saverio
Published in Haematologica (Roma) (01.08.2020)
Published in Haematologica (Roma) (01.08.2020)
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LSD1-directed therapy affects glioblastoma tumorigenicity by deregulating the protective ATF4-dependent integrated stress response
Faletti, Stefania, Osti, Daniela, Ceccacci, Elena, Richichi, Cristina, Costanza, Brunella, Nicosia, Luciano, Noberini, Roberta, Marotta, Giulia, Furia, Laura, Faretta, Mario R, Brambillasca, Silvia, Quarto, Micaela, Bertero, Luca, Boldorini, Renzo, Pollo, Bianca, Gandini, Sara, Cora, Davide, Minucci, Saverio, Mercurio, Ciro, Varasi, Mario, Bonaldi, Tiziana, Pelicci, Giuliana
Published in Science translational medicine (08.12.2021)
Published in Science translational medicine (08.12.2021)
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Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent
Vianello, Paola, Botrugno, Oronza A, Cappa, Anna, Dal Zuffo, Roberto, Dessanti, Paola, Mai, Antonello, Marrocco, Biagina, Mattevi, Andrea, Meroni, Giuseppe, Minucci, Saverio, Stazi, Giulia, Thaler, Florian, Trifiró, Paolo, Valente, Sergio, Villa, Manuela, Varasi, Mario, Mercurio, Ciro
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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Journal Article
Thieno[3,2‑b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure–Activity Relationship
Vianello, Paola, Sartori, Luca, Amigoni, Federica, Cappa, Anna, Fagá, Giovanni, Fattori, Raimondo, Legnaghi, Elena, Ciossani, Giuseppe, Mattevi, Andrea, Meroni, Giuseppe, Moretti, Loris, Cecatiello, Valentina, Pasqualato, Sebastiano, Romussi, Alessia, Thaler, Florian, Trifiró, Paolo, Villa, Manuela, Botrugno, Oronza A, Dessanti, Paola, Minucci, Saverio, Vultaggio, Stefania, Zagarrí, Elisa, Varasi, Mario, Mercurio, Ciro
Published in Journal of medicinal chemistry (09.03.2017)
Published in Journal of medicinal chemistry (09.03.2017)
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Novel selective inhibitors of macropinocytosis-dependent growth in pancreatic ductal carcinoma
Brambillasca, Silvia, Cera, Maria Rosaria, Andronache, Adrian, Dey, Sumit Kumar, Fagá, Giovanni, Fancelli, Daniele, Frittoli, Emanuela, Pasi, Maurizio, Robusto, Michela, Varasi, Mario, Scita, Giorgio, Mercurio, Ciro
Published in Biomedicine & pharmacotherapy (01.08.2024)
Published in Biomedicine & pharmacotherapy (01.08.2024)
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Caloric restriction leads to druggable LSD1-dependent cancer stem cells expansion
Pallavi, Rani, Gatti, Elena, Durfort, Tiphanie, Stendardo, Massimo, Ravasio, Roberto, Leonardi, Tommaso, Falvo, Paolo, Duso, Bruno Achutti, Punzi, Simona, Xieraili, Aobuli, Polazzi, Andrea, Verrelli, Doriana, Trastulli, Deborah, Ronzoni, Simona, Frascolla, Simone, Perticari, Giulia, Elgendy, Mohamed, Varasi, Mario, Colombo, Emanuela, Giorgio, Marco, Lanfrancone, Luisa, Minucci, Saverio, Mazzarella, Luca, Pelicci, Pier Giuseppe
Published in Nature communications (27.01.2024)
Published in Nature communications (27.01.2024)
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Thieno[3,2‑b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration
Sartori, Luca, Mercurio, Ciro, Amigoni, Federica, Cappa, Anna, Fagá, Giovanni, Fattori, Raimondo, Legnaghi, Elena, Ciossani, Giuseppe, Mattevi, Andrea, Meroni, Giuseppe, Moretti, Loris, Cecatiello, Valentina, Pasqualato, Sebastiano, Romussi, Alessia, Thaler, Florian, Trifiró, Paolo, Villa, Manuela, Vultaggio, Stefania, Botrugno, Oronza A, Dessanti, Paola, Minucci, Saverio, Zagarrí, Elisa, Carettoni, Daniele, Iuzzolino, Lucia, Varasi, Mario, Vianello, Paola
Published in Journal of medicinal chemistry (09.03.2017)
Published in Journal of medicinal chemistry (09.03.2017)
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Toward Highly Potent Cancer Agents by Modulating the C‑2 Group of the Arylthioindole Class of Tubulin Polymerization Inhibitors
La Regina, Giuseppe, Bai, Ruoli, Rensen, Whilelmina Maria, Di Cesare, Erica, Coluccia, Antonio, Piscitelli, Francesco, Famiglini, Valeria, Reggio, Alessia, Nalli, Marianna, Pelliccia, Sveva, Da Pozzo, Eleonora, Costa, Barbara, Granata, Ilaria, Porta, Amalia, Maresca, Bruno, Soriani, Alessandra, Iannitto, Maria Luisa, Santoni, Angela, Li, Junjie, Miranda Cona, Marlein, Chen, Feng, Ni, Yicheng, Brancale, Andrea, Dondio, Giulio, Vultaggio, Stefania, Varasi, Mario, Mercurio, Ciro, Martini, Claudia, Hamel, Ernest, Lavia, Patrizia, Novellino, Ettore, Silvestri, Romano
Published in Journal of medicinal chemistry (10.01.2013)
Published in Journal of medicinal chemistry (10.01.2013)
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Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoic acid-induced differentiation
Ravasio, Roberto, Ceccacci, Elena, Nicosia, Luciano, Hosseini, Amir, Rossi, Pier Luigi, Barozzi, Iros, Fornasari, Lorenzo, Zuffo, Roberto Dal, Valente, Sergio, Fioravanti, Rossella, Mercurio, Ciro, Varasi, Mario, Mattevi, Andrea, Mai, Antonello, Pavesi, Giulio, Bonaldi, Tiziana, Minucci, Saverio
Published in Science advances (01.04.2020)
Published in Science advances (01.04.2020)
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New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer
La Regina, Giuseppe, Bai, Ruoli, Coluccia, Antonio, Famiglini, Valeria, Pelliccia, Sveva, Passacantilli, Sara, Mazzoccoli, Carmela, Ruggieri, Vitalba, Verrico, Annalisa, Miele, Andrea, Monti, Ludovica, Nalli, Marianna, Alfonsi, Romina, Di Marcotullio, Lucia, Gulino, Alberto, Ricci, Biancamaria, Soriani, Alessandra, Santoni, Angela, Caraglia, Michele, Porto, Stefania, Da Pozzo, Eleonora, Martini, Claudia, Brancale, Andrea, Marinelli, Luciana, Novellino, Ettore, Vultaggio, Stefania, Varasi, Mario, Mercurio, Ciro, Bigogno, Chiara, Dondio, Giulio, Hamel, Ernest, Lavia, Patrizia, Silvestri, Romano
Published in Journal of medicinal chemistry (13.08.2015)
Published in Journal of medicinal chemistry (13.08.2015)
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Tranylcypromine‐Based LSD1 Inhibitors: Structure‐Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation
Fioravanti, Rossella, Romanelli, Annalisa, Mautone, Nicola, Di Bello, Elisabetta, Rovere, Annarita, Corinti, Davide, Zwergel, Clemens, Valente, Sergio, Rotili, Dante, Botrugno, Oronza A., Dessanti, Paola, Vultaggio, Stefania, Vianello, Paola, Cappa, Anna, Binda, Claudia, Mattevi, Andrea, Minucci, Saverio, Mercurio, Ciro, Varasi, Mario, Mai, Antonello
Published in ChemMedChem (03.04.2020)
Published in ChemMedChem (03.04.2020)
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Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: A novel class of irreversible inhibitors of histone demethylase KDM1A
Vianello, Paola, Botrugno, Oronza A., Cappa, Anna, Ciossani, Giuseppe, Dessanti, Paola, Mai, Antonello, Mattevi, Andrea, Meroni, Giuseppe, Minucci, Saverio, Thaler, Florian, Tortorici, Marcello, Trifiró, Paolo, Valente, Sergio, Villa, Manuela, Varasi, Mario, Mercurio, Ciro
Published in European journal of medicinal chemistry (30.10.2014)
Published in European journal of medicinal chemistry (30.10.2014)
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Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models
Romussi, Alessia, Cappa, Anna, Vianello, Paola, Brambillasca, Silvia, Cera, Maria Rosaria, Dal Zuffo, Roberto, Fagà, Giovanni, Fattori, Raimondo, Moretti, Loris, Trifirò, Paolo, Villa, Manuela, Vultaggio, Stefania, Cecatiello, Valentina, Pasqualato, Sebastiano, Dondio, Giulio, So, Chi Wai Eric, Minucci, Saverio, Sartori, Luca, Varasi, Mario, Mercurio, Ciro
Published in ACS medicinal chemistry letters (14.05.2020)
Published in ACS medicinal chemistry letters (14.05.2020)
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High-throughput screening identifies histone deacetylase inhibitors that modulate GTF2I expression in 7q11.23 microduplication autism spectrum disorder patient-derived cortical neurons
Cavallo, Francesca, Troglio, Flavia, Fagà, Giovanni, Fancelli, Daniele, Shyti, Reinald, Trattaro, Sebastiano, Zanella, Matteo, D'Agostino, Giuseppe, Hughes, James M, Cera, Maria Rosaria, Pasi, Maurizio, Gabriele, Michele, Lazzarin, Maddalena, Mihailovich, Marija, Kooy, Frank, Rosa, Alessandro, Mercurio, Ciro, Varasi, Mario, Testa, Giuseppe
Published in Molecular autism (19.11.2020)
Published in Molecular autism (19.11.2020)
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Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts
Valente, Sergio, Rodriguez, Veronica, Mercurio, Ciro, Vianello, Paola, Saponara, Bruna, Cirilli, Roberto, Ciossani, Giuseppe, Labella, Donatella, Marrocco, Biagina, Monaldi, Daria, Ruoppolo, Giovanni, Tilset, Mats, Botrugno, Oronza A., Dessanti, Paola, Minucci, Saverio, Mattevi, Andrea, Varasi, Mario, Mai, Antonello
Published in European journal of medicinal chemistry (13.04.2015)
Published in European journal of medicinal chemistry (13.04.2015)
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PHA-680632, a Novel Aurora Kinase Inhibitor with Potent Antitumoral Activity
Soncini, Chiara, Carpinelli, Patrizia, Gianellini, Laura, Fancelli, Daniele, Vianello, Paola, Rusconi, Luisa, Storici, Paola, Zugnoni, Paola, Pesenti, Enrico, Croci, Valter, Ceruti, Roberta, Giorgini, Maria Laura, Cappella, Paolo, Ballinari, Dario, Sola, Francesco, Varasi, Mario, Bravo, Rodrigo, Moll, Jürgen
Published in Clinical cancer research (01.07.2006)
Published in Clinical cancer research (01.07.2006)
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A high-throughput screening identifies MCM chromatin loading inhibitors targeting cells with increased replication origins
Falbo, Lucia, Técher, Hervé, Sannino, Vincenzo, Robusto, Michela, Fagà, Giovanni, Pezzimenti, Federica, Romeo, Francesco, Colombo, Luca Gabriele, Vultaggio, Stefania, Fancelli, Daniele, Monzani, Silvia, Cecatiello, Valentina, Pasqualato, Sebastiano, Varasi, Mario, Mercurio, Ciro, Costanzo, Vincenzo
Published in iScience (16.08.2024)
Published in iScience (16.08.2024)
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Quantitative Chemical Proteomics Identifies Novel Targets of the Anti-cancer Multi-kinase Inhibitor E-3810
Colzani, Mara, Noberini, Roberta, Romanenghi, Mauro, Colella, Gennaro, Pasi, Maurizio, Fancelli, Daniele, Varasi, Mario, Minucci, Saverio, Bonaldi, Tiziana
Published in Molecular & cellular proteomics (01.06.2014)
Published in Molecular & cellular proteomics (01.06.2014)
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Cdc7 Kinase Inhibitors: 5-Heteroaryl-3-Carboxamido-2-Aryl Pyrroles as Potential Antitumor Agents. 1. Lead Finding
Menichincheri, Maria, Albanese, Clara, Alli, Cristina, Ballinari, Dario, Bargiotti, Alberto, Caldarelli, Marina, Ciavolella, Antonella, Cirla, Alessandra, Colombo, Maristella, Colotta, Francesco, Croci, Valter, D’Alessio, Roberto, D’Anello, Matteo, Ermoli, Antonella, Fiorentini, Francesco, Forte, Barbara, Galvani, Arturo, Giordano, Patrizia, Isacchi, Antonella, Martina, Katia, Molinari, Antonio, Moll, Jürgen K, Montagnoli, Alessia, Orsini, Paolo, Orzi, Fabrizio, Pesenti, Enrico, Pillan, Antonio, Roletto, Fulvia, Scolaro, Alessandra, Tatò, Marco, Tibolla, Marcellino, Valsasina, Barbara, Varasi, Mario, Vianello, Paola, Volpi, Daniele, Santocanale, Corrado, Vanotti, Ermes
Published in Journal of medicinal chemistry (28.10.2010)
Published in Journal of medicinal chemistry (28.10.2010)
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Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potential Antitumor Agents. 1. Synthesis and Structure–Activity Relationships
Vanotti, Ermes, Amici, Raffaella, Bargiotti, Alberto, Berthelsen, Jens, Bosotti, Roberta, Ciavolella, Antonella, Cirla, Alessandra, Cristiani, Cinzia, D’Alessio, Roberto, Forte, Barbara, Isacchi, Antonella, Martina, Katia, Menichincheri, Maria, Molinari, Antonio, Montagnoli, Alessia, Orsini, Paolo, Pillan, Antonio, Roletto, Fulvia, Scolaro, Alessandra, Tibolla, Marcellino, Valsasina, Barbara, Varasi, Mario, Volpi, Daniele, Santocanale, Corrado
Published in Journal of medicinal chemistry (14.02.2008)
Published in Journal of medicinal chemistry (14.02.2008)
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