Search Results - "Scarpelli, Rita"

Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection by Summa, Vincenzo, Petrocchi, Alessia, Bonelli, Fabio, Crescenzi, Benedetta, Donghi, Monica, Ferrara, Marco, Fiore, Fabrizio, Gardelli, Cristina, Gonzalez Paz, Odalys, Hazuda, Daria J, Jones, Philip, Kinzel, Olaf, Laufer, Ralph, Monteagudo, Edith, Muraglia, Ester, Nizi, Emanuela, Orvieto, Federica, Pace, Paola, Pescatore, Giovanna, Scarpelli, Rita, Stillmock, Kara, Witmer, Marc V, Rowley, Michael

“…Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded enzymes required for replication and therefore a rational target for…”
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Discovery of 2-{4-[(3S)-Piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A Novel Oral Poly(ADP-ribose)polymerase (PARP) Inhibitor Efficacious in BRCA-1 and -2 Mutant Tumors by Jones, Philip, Altamura, Sergio, Boueres, Julia, Ferrigno, Federica, Fonsi, Massimiliano, Giomini, Claudia, Lamartina, Stefania, Monteagudo, Edith, Ontoria, Jesus M, Orsale, Maria Vittoria, Palumbi, Maria Cecilia, Pesci, Silvia, Roscilli, Giuseppe, Scarpelli, Rita, Schultz-Fademrecht, Carsten, Toniatti, Carlo, Rowley, Michael

“…We disclose the development of a novel series of 2-phenyl-2H-indazole-7-carboxamides as poly(ADP-ribose)polymerase (PARP) 1 and 2 inhibitors. This series was…”
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Structural and Functional Analysis of the Human HDAC4 Catalytic Domain Reveals a Regulatory Structural Zinc-binding Domain by Bottomley, Matthew J., Lo Surdo, Paola, Di Giovine, Paolo, Cirillo, Agostino, Scarpelli, Rita, Ferrigno, Federica, Jones, Philip, Neddermann, Petra, De Francesco, Raffaele, Steinkühler, Christian, Gallinari, Paola, Carfí, Andrea

“…Histone deacetylases (HDACs) regulate chromatin status and gene expression, and their inhibition is of significant therapeutic interest. To date, no biological…”
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Potentiation of endocannabinoids and other lipid amides prevents hyperalgesia and inflammation in a pre-clinical model of migraine by Greco, Rosaria, Demartini, Chiara, Zanaboni, Anna Maria, Francavilla, Miriam, Reggiani, Angelo, Realini, Natalia, Scarpelli, Rita, Piomelli, Daniele, Tassorelli, Cristina

“…Targeting fatty acid amide hydrolase (FAAH) is a promising therapeutic strategy to combat certain forms of pain, including migraine headache. FAAH inhibitors,…”
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Peripheral FAAH inhibition causes profound antinociception and protects against indomethacin-induced gastric lesions by Sasso, Oscar, Bertorelli, Rosalia, Bandiera, Tiziano, Scarpelli, Rita, Colombano, Giampiero, Armirotti, Andrea, Moreno-Sanz, Guillermo, Reggiani, Angelo, Piomelli, Daniele

“…Fatty-acid amide hydrolase (FAAH) catalyzes the intracellular hydrolysis of the endocannabinoid anandamide and other bioactive lipid amides. In the present…”
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Identification and Characterization of Carprofen as a Multitarget Fatty Acid Amide Hydrolase/Cyclooxygenase Inhibitor by Favia, Angelo D, Habrant, Damien, Scarpelli, Rita, Migliore, Marco, Albani, Clara, Bertozzi, Sine Mandrup, Dionisi, Mauro, Tarozzo, Glauco, Piomelli, Daniele, Cavalli, Andrea, De Vivo, Marco

“…Pain and inflammation are major therapeutic areas for drug discovery. Current drugs for these pathologies have limited efficacy, however, and often cause a…”
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Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 1 by Malancona, Savina, Altamura, Sergio, Filocamo, Gessica, Kinzel, Olaf, Hernando, Jose Ignacio Martin, Rowley, Michael, Scarpelli, Rita, Steinkühler, Christian, Jones, Philip

“…The Hedgehog (Hh-) signaling pathway is a key developmental pathway which controls patterning, growth and cell migration in most tissues, but evidence has…”
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Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 2 by Kinzel, Olaf, Alfieri, Anna, Altamura, Sergio, Brunetti, Mirko, Bufali, Simone, Colaceci, Fabrizio, Ferrigno, Federica, Filocamo, Gessica, Fonsi, Massimiliano, Gallinari, Paola, Malancona, Savina, Hernando, Jose Ignacio Martin, Monteagudo, Edith, Orsale, Maria Vittoria, Palumbi, Maria Cecilia, Pucci, Vincenzo, Rowley, Michael, Sasso, Romina, Scarpelli, Rita, Steinkühler, Christian, Jones, Philip

“…The Hedgehog (Hh-) signaling pathway is a key developmental pathway which gets reactivated in many human tumors, and smoothened (Smo) antagonists are emerging…”
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Identification of a Dual Autophagy and REV-ERB Inhibitor with in Vivo Anticancer Efficacy by Palomba, Martina, Vecchio, Donatella, Allavena, Giulia, Capaccio, Vito, De Mei, Claudia, Scarpelli, Rita, Grimaldi, Benedetto

“…The autophagy process appears as a promising target for anticancer interventions. Chloroquine (CQ) and its derivative hydroxychloroquine (HCQ) are the only…”
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A Double Whammy: Targeting Both Fatty Acid Amide Hydrolase (FAAH) and Cyclooxygenase (COX) To Treat Pain and Inflammation by Scarpelli, Rita, Sasso, Oscar, Piomelli, Daniele

“…Pain states that arise from non‐resolving inflammation, such as inflammatory bowel disease or arthritis, pose an unusually difficult challenge for therapy…”
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Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy by Torrente, Esther, Parodi, Chiara, Ercolani, Luisa, De Mei, Claudia, Ferrari, Alessio, Scarpelli, Rita, Grimaldi, Benedetto

“…Autophagy inhibition is emerging as a promising anticancer strategy. We recently reported that the circadian nuclear receptor REV-ERBβ plays an unexpected role…”
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Multitarget fatty acid amide hydrolase/cyclooxygenase blockade suppresses intestinal inflammation and protects against nonsteroidal anti‐inflammatory drug‐dependent gastrointestinal damage by Sasso, Oscar, Migliore, Marco, Habrant, Damien, Armirotti, Andrea, Albani, Clara, Summa, Maria, Moreno‐Sanz, Guillermo, Scarpelli, Rita, Piomelli, Daniele

“…ABSTRACT The ability of nonsteroidal anti‐inflammatory drugs (NSAIDs) to inhibit cyclooxygenase (Cox)‐1 and Cox‐2 underlies the therapeutic efficacy of these…”
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Kernel-Based, Partial Least Squares Quantitative Structure-Retention Relationship Model for UPLC Retention Time Prediction: A Useful Tool for Metabolite Identification by Falchi, Federico, Bertozzi, Sine Mandrup, Ottonello, Giuliana, Ruda, Gian Filippo, Colombano, Giampiero, Fiorelli, Claudio, Martucci, Cataldo, Bertorelli, Rosalia, Scarpelli, Rita, Cavalli, Andrea, Bandiera, Tiziano, Armirotti, Andrea

“…We propose a new QSRR model based on a Kernel-based partial least-squares method for predicting UPLC retention times in reversed phase mode. The model was…”
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Multitarget Drug Discovery for Alzheimer's Disease: Triazinones as BACE-1 and GSK-3β Inhibitors by Prati, Federica, De Simone, Angela, Bisignano, Paola, Armirotti, Andrea, Summa, Maria, Pizzirani, Daniela, Scarpelli, Rita, Perez, Daniel I., Andrisano, Vincenza, Perez-Castillo, Ana, Monti, Barbara, Massenzio, Francesca, Polito, Letizia, Racchi, Marco, Favia, Angelo D., Bottegoni, Giovanni, Martinez, Ana, Bolognesi, Maria Laura, Cavalli, Andrea

“…Cumulative evidence strongly supports that the amyloid and tau hypotheses are not mutually exclusive, but concomitantly contribute to neurodegeneration in…”
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Benzoxazolone Carboxamides as Potent Acid Ceramidase Inhibitors: Synthesis and Structure–Activity Relationship (SAR) Studies by Bach, Anders, Pizzirani, Daniela, Realini, Natalia, Vozella, Valentina, Russo, Debora, Penna, Ilaria, Melzig, Laurin, Scarpelli, Rita, Piomelli, Daniele

“…Ceramides are lipid-derived intracellular messengers involved in the control of senescence, inflammation, and apoptosis. The cysteine amidase, acid ceramidase…”
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Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies by Migliore, Marco, Habrant, Damien, Sasso, Oscar, Albani, Clara, Bertozzi, Sine Mandrup, Armirotti, Andrea, Piomelli, Daniele, Scarpelli, Rita

“…Non-steroidal anti-inflammatory drugs (NSAIDs) exert their pharmacological effects by inhibiting cyclooxygenase (COX)-1 and COX-2. Though widely prescribed for…”
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Fluorine nuclear magnetic resonance-based assay in living mammalian cells by Veronesi, Marina, Giacomina, Francesca, Romeo, Elisa, Castellani, Beatrice, Ottonello, Giuliana, Lambruschini, Chiara, Garau, Gianpiero, Scarpelli, Rita, Bandiera, Tiziano, Piomelli, Daniele, Dalvit, Claudio

“…Nuclear magnetic resonance (NMR)-based screening has been recognized as a powerful approach for the identification and characterization of molecules…”
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Discovery of a New Class of Highly Potent Inhibitors of Acid Ceramidase: Synthesis and Structure–Activity Relationship (SAR) by Pizzirani, Daniela, Pagliuca, Chiara, Realini, Natalia, Branduardi, Davide, Bottegoni, Giovanni, Mor, Marco, Bertozzi, Fabio, Scarpelli, Rita, Piomelli, Daniele, Bandiera, Tiziano

“…Acid ceramidase (AC) is an intracellular cysteine amidase that catalyzes the hydrolysis of the lipid messenger ceramide. By regulating ceramide levels in…”
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Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors by Caputo, Samantha, Di Martino, Simona, Cilibrasi, Vincenzo, Tardia, Piero, Mazzonna, Marco, Russo, Debora, Penna, Ilaria, Summa, Maria, Bertozzi, Sine Mandrup, Realini, Natalia, Margaroli, Natasha, Migliore, Marco, Ottonello, Giuliana, Liu, Min, Lansbury, Peter, Armirotti, Andrea, Bertorelli, Rosalia, Ray, Soumya S, Skerlj, Renato, Scarpelli, Rita

“…Acid ceramidase (AC) is a cysteine hydrolase that plays a crucial role in the metabolism of lysosomal ceramides, important members of the sphingolipid family,…”
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A Binding Site for Nonsteroidal Anti-inflammatory Drugs in Fatty Acid Amide Hydrolase by Bertolacci, Laura, Romeo, Elisa, Veronesi, Marina, Magotti, Paola, Albani, Clara, Dionisi, Mauro, Lambruschini, Chiara, Scarpelli, Rita, Cavalli, Andrea, De Vivo, Marco, Piomelli, Daniele, Garau, Gianpiero

“…In addition to inhibiting the cyclooxygenase (COX)-mediated biosynthesis of prostanoids, various widely used nonsteroidal anti-inflammatory drugs (NSAIDs)…”
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