Search Results - "Dessanti, Paola"

Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent by 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

“…We report the stereoselective synthesis and biological activity of a novel series of tranylcypromine (TCPA) derivatives (14a–k, 15, 16), potent inhibitors of…”
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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 by 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

“…The balance of methylation levels at histone H3 lysine 4 (H3K4) is regulated by KDM1A (LSD1). KDM1A is overexpressed in several tumor types, thus representing…”
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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 by 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

“…Lysine specific demethylase 1 KDM1A (LSD1) regulates histone methylation and it is increasingly recognized as a potential therapeutic target in oncology. We…”
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Tranylcypromine‐Based LSD1 Inhibitors: Structure‐Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation by 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

“…: LSD1 is a lysine demethylase highly involved in initiation and development of cancer. To design highly effective covalent inhibitors, a strategy is to fill…”
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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 by 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

“…Histone demethylase KDM1A (also known as LSD1) has become an attractive therapeutic target for the treatment of cancer as well as other disorders such as viral…”
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Comprehensive in Vitro Characterization of the LSD1 Small Molecule Inhibitor Class in Oncology by Sacilotto, Natalia, Dessanti, Paola, Lufino, Michele M. P, Ortega, Alberto, Rodríguez-Gimeno, Alejandra, Salas, Jordi, Maes, Tamara, Buesa, Carlos, Mascaró, Cristina, Soliva, Robert

“…Lysine-specific demethylase 1 (LSD1 or KDM1A) is a chromatin modifying enzyme playing a key role in the cell cycle and cell differentiation and proliferation…”
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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 by 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

“…The pure enantiomers of the N-(2-, 3-, and 4-(2-aminocyclopropyl)phenyl)benzamides hydrochlorides 11a–j were prepared and tested against LSD1 and MAO enzymes…”
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Efficacy of Vafidemstat in Experimental Autoimmune Encephalomyelitis Highlights the KDM1A/RCOR1/HDAC Epigenetic Axis in Multiple Sclerosis by Cavalcanti, Fernando, Gonzalez-Rey, Elena, Delgado, Mario, Falo, Clara P., Mestre, Leyre, Guaza, Carmen, O’Valle, Francisco, Lufino, Michele M. P., Xaus, Jordi, Mascaró, Cristina, Lunardi, Serena, Sacilotto, Natalia, Dessanti, Paola, Rotllant, David, Navarro, Xavier, Herrando-Grabulosa, Mireia, Buesa, Carlos, Maes, Tamara

“…Lysine specific demethylase 1 (LSD1; also known as KDM1A), is an epigenetic modulator that modifies the histone methylation status. KDM1A forms a part of…”
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Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies by Valente, Sergio, Rodriguez, Veronica, Mercurio, Ciro, Vianello, Paola, Saponara, Bruna, Cirilli, Roberto, Ciossani, Giuseppe, Labella, Donatella, Marrocco, Biagina, Ruoppolo, Giovanni, Botrugno, Oronza A, Dessanti, Paola, Minucci, Saverio, Mattevi, Andrea, Varasi, Mario, Mai, Antonello

“…The pure four diastereomers (11a–d) of trans-benzyl (1-((4-(2-aminocyclopropyl)phenyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate hydrochloride 11, previously…”
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Further insights into the SAR of α-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A by Pieroni, Marco, Annunziato, Giannamaria, Azzali, Elisa, Dessanti, Paola, Mercurio, Ciro, Meroni, Giuseppe, Trifiró, Paolo, Vianello, Paola, Villa, Manuela, Beato, Claudia, Varasi, Mario, Costantino, Gabriele

“…Epigenetics alterations including histone methylation and acetylation, and DNA methylation, are thought to play important roles in the onset and progression of…”
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Abstract LB-003: Novel multi-functional chemoprobes for the characterization of the mechanism of action of histone lysine demethylases inhibitors in cancer by Lunardi, Serena, Ciceri, Filippo, Crusat, Cristina Mascaró, Ruiz, Raquel, Carceller, Elena, Ortega, Alberto, Sacilotto, Natalia, Dessanti, Paola, Salas, Jordi, Lufino, Michele, Maes, Tamara

“…Abstract Histone Lysine demethylases (KDMs) are emerging clinical targets in cancer. However, a characterization of the mechanism of action of KDMs small…”
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Tranylcypromine-based LSD1 Inhibitors: Structure-Activity Relationship, Antiproliferative Effect in Leukemias and Gene Target Modulation by 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

“…LSD1 is a lysine demethylase highly involved in initiation and development of cancer. To design highly effective covalent inhibitors, a strategy is to fill its…”
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Novel potent inhibitors of the histone demethylase KDM1A (LSD1), orally active in a murine promyelocitic leukemia model by Trifirò, Paolo, Cappa, Anna, Brambillasca, Silvia, Botrugno, Oronza A, Cera, Maria Rosaria, Zuffo, Roberto Dal, Dessanti, Paola, Meroni, Giuseppe, Thaler, Florian, Villa, Manuela, Minucci, Saverio, Mercurio, Ciro, Varasi, Mario, Vianello, Paola

“…Histone lysine demethylases (KDMs) are well-recognized targets in oncology drug discovery. They function at the post-translation level controlling chromatin…”
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Structural basis of the substrate specificity of Bacillus cereus adenosine phosphorylase by Dessanti, Paola, Zhang, Yang, Allegrini, Simone, Tozzi, Maria Grazia, Sgarrella, Francesco, Ealick, Steven E.

“…Purine nucleoside phosphorylases catalyze the phosphorolytic cleavage of the glycosidic bond of purine (2′‐deoxy)nucleosides, generating the corresponding free…”
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Structural basis of the substrate specificity of Bacillus cereus adenosine phosphorylase by Dessanti, Paola, Università di Sassari, Zhang, Yang, Allegrini, Simone, Tozzi, Maria Grazia, Sgarrella, Francesco, Ealick, Steven E.

“…Adenosine phosphorylase from B. cereus shows a strong preference for adenosine over other 6-oxopurine nucleosides. Mutation of Asp204 to asparagine reduces the…”
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