Search Results - "MINUTOLO, Filippo"

Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy by Rossari, Federico, Minutolo, Filippo, Orciuolo, Enrico

“…Bcr-Abl inhibitors paved the way of targeted therapy epoch. Imatinib was the first tyrosine kinase inhibitor to be discovered with high specificity for Bcr-Abl…”
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Activators of Sirtuin-1 and their Involvement in Cardioprotection by Granchi, Carlotta, Minutolo, Filippo

“…SIRT1 is a nicotinamide adenosine dinucleotide (NAD+)-dependent deacetylase, which removes acetyl groups from many target proteins, such as histone proteins,…”
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Increased Lactate Secretion by Cancer Cells Sustains Non-cell-autonomous Adaptive Resistance to MET and EGFR Targeted Therapies by Apicella, Maria, Giannoni, Elisa, Fiore, Stephany, Ferrari, Karin Johanna, Fernández-Pérez, Daniel, Isella, Claudio, Granchi, Carlotta, Minutolo, Filippo, Sottile, Antonino, Comoglio, Paolo Maria, Medico, Enzo, Pietrantonio, Filippo, Volante, Marco, Pasini, Diego, Chiarugi, Paola, Giordano, Silvia, Corso, Simona

“…The microenvironment influences cancer drug response and sustains resistance to therapies targeting receptor-tyrosine kinases. However, if and how the tumor…”
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An update on therapeutic opportunities offered by cancer glycolytic metabolism by Granchi, Carlotta, Fancelli, Daniele, Minutolo, Filippo

“…[Display omitted] Almost all invasive cancers, regardless of tissue origin, are characterized by specific modifications of their cellular energy metabolism. In…”
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The Benzoylpiperidine Fragment as a Privileged Structure in Medicinal Chemistry: A Comprehensive Review by Bononi, Giulia, Lonzi, Chiara, Tuccinardi, Tiziano, Minutolo, Filippo, Granchi, Carlotta

“…The phenyl(piperidin-4-yl)methanone fragment (here referred to as the benzoylpiperidine fragment) is a privileged structure in the development of new drugs…”
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Structural Optimization of 4‑Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors by Granchi, Carlotta, Rizzolio, Flavio, Palazzolo, Stefano, Carmignani, Sara, Macchia, Marco, Saccomanni, Giuseppe, Manera, Clementina, Martinelli, Adriano, Minutolo, Filippo, Tuccinardi, Tiziano

“…Monoacylglycerol lipase (MAGL) inhibitors are considered potential therapeutic agents for a variety of pathological conditions, including several types of…”
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Lactate dehydrogenase-A inhibition induces human glioblastoma multiforme stem cell differentiation and death by Daniele, Simona, Giacomelli, Chiara, Zappelli, Elisa, Granchi, Carlotta, Trincavelli, Maria Letizia, Minutolo, Filippo, Martini, Claudia

“…Therapies that target the signal transduction and metabolic pathways of cancer stem cells (CSCs) are innovative strategies to effectively reduce the recurrence…”
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Sirtuin 1-Activating Compounds: Discovery of a Class of Thiazole-Based Derivatives by Bononi, Giulia, Citi, Valentina, Lapillo, Margherita, Martelli, Alma, Poli, Giulio, Tuccinardi, Tiziano, Granchi, Carlotta, Testai, Lara, Calderone, Vincenzo, Minutolo, Filippo

“…Sirtuin 1 (SIRT1) is a NAD+-dependent deacetylase implicated in various biological and pathological processes, including cancer, diabetes, and cardiovascular…”
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SMS121, a new inhibitor of CD36, impairs fatty acid uptake and viability of acute myeloid leukemia by Åbacka, Hannah, Masoni, Samuele, Poli, Giulio, Huang, Peng, Gusso, Francesco, Granchi, Carlotta, Minutolo, Filippo, Tuccinardi, Tiziano, Hagström-Andersson, Anna K., Lindkvist-Petersson, Karin

“…Acute myeloid leukemia (AML) is the most common form of acute leukemia in adults and the second most common among children. AML is characterized by aberrant…”
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Metabolic Effects of New Glucose Transporter (GLUT-1) and Lactate Dehydrogenase-A (LDH-A) Inhibitors against Chemoresistant Malignant Mesothelioma by Franczak, Marika A, Krol, Oliwia, Harasim, Gabriela, Jedrzejewska, Agata, Zaffaroni, Nadia, Granchi, Carlotta, Minutolo, Filippo, Avan, Amir, Giovannetti, Elisa, Smolenski, Ryszard T, Peters, Godefridus J

“…Malignant mesothelioma (MM) is a highly aggressive and resistant tumor. The prognostic role of key effectors of glycolytic metabolism in MM prompted our…”
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Targeting GLUT1 in acute myeloid leukemia to overcome cytarabine resistance by Åbacka, Hannah, Hansen, Jesper S, Huang, Peng, Venskutonytė, Raminta, Hyrenius-Wittsten, Axel, Poli, Giulio, Tuccinardi, Tiziano, Granchi, Carlotta, Minutolo, Filippo, Hagström-Andersson, Anna K, Lindkvist-Petersson, Karin

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Impact of hypoxia on chemoresistance of mesothelioma mediated by the proton-coupled folate transporter, and preclinical activity of new anti-LDH-A compounds by Li Petri, Giovanna, El Hassouni, Btissame, Sciarrillo, Rocco, Funel, Niccola, Mantini, Giulia, Zeeuw van der Laan, Eveline A., Cascioferro, Stella, Avan, Amir, Zucali, Paolo Andrea, Zaffaroni, Nadia, Lagerweij, Tonny, Parrino, Barbara, Smid, Kees, Deraco, Marcello, Granchi, Carlotta, Braczko, Alicja, Smolenski, Ryszard T., Matherly, Larry H., Jansen, Gerrit, Assaraf, Yehuda G., Diana, Patrizia, Cloos, Jacqueline, Peters, Godefridus J., Minutolo, Filippo, Giovannetti, Elisa

“…Background Expression of proton-coupled folate transporter (PCFT) is associated with survival of mesothelioma patients treated with pemetrexed, and is reduced…”
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Discovery of N-Hydroxyindole-Based Inhibitors of Human Lactate Dehydrogenase Isoform A (LDH-A) as Starvation Agents against Cancer Cells by Granchi, Carlotta, Roy, Sarabindu, Giacomelli, Chiara, Macchia, Marco, Tuccinardi, Tiziano, Martinelli, Adriano, Lanza, Mario, Betti, Laura, Giannaccini, Gino, Lucacchini, Antonio, Funel, Nicola, León, Leticia G, Giovannetti, Elisa, Peters, Godefridus J, Palchaudhuri, Rahul, Calvaresi, Emilia C, Hergenrother, Paul J, Minutolo, Filippo

“…Highly invasive tumor cells are characterized by a metabolic switch, known as the Warburg effect, from “normal” oxidative phosphorylation to increased…”
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Computationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors by Poli, Giulio, Lapillo, Margherita, Jha, Vibhu, Mouawad, Nayla, Caligiuri, Isabella, Macchia, Marco, Minutolo, Filippo, Rizzolio, Flavio, Tuccinardi, Tiziano, Granchi, Carlotta

“…Monoacylglycerol lipase (MAGL) is an attractive therapeutic target for many pathologies, including neurodegenerative diseases, cancer as well as chronic pain…”
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Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer by Granchi, Carlotta, Fortunato, Serena, Meini, Serena, Rizzolio, Flavio, Caligiuri, Isabella, Tuccinardi, Tiziano, Lee, Hyang Yeon, Hergenrother, Paul J, Minutolo, Filippo

“…Inhibition of lactate dehydrogenase (LDH) represents an innovative approach to tackle cancer because this peculiar glycolytic metabolism is characteristic of…”
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New PIN1 inhibitors identified through a pharmacophore-driven, hierarchical consensus docking strategy by Poli, Giulio, Di Stefano, Miriana, Estevez, Joan Arias, Minutolo, Filippo, Granchi, Carlotta, Giordano, Antonio, Parisi, Salvatore, Mauceri, Matteo, Canzonieri, Vincenzo, Macchia, Marco, Caligiuri, Isabella, Tuccinardi, Tiziano, Rizzolio, Flavio

“…PIN1 is considered as a therapeutic target for a wide variety of tumours. However, most of known inhibitors are devoid of cellular activity despite their good…”
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Three-Dimensional Analysis of the Interactions between hLDH5 and Its Inhibitors by Poli, Giulio, Granchi, Carlotta, Aissaoui, Mohamed, Minutolo, Filippo, Tuccinardi, Tiziano

“…Inhibitors of human lactate dehydrogenase ( LDH5)-the enzyme responsible for the conversion of pyruvate to lactate coupled with oxidation of NADH to NAD⁺-are…”
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Phospho-Akt overexpression is prognostic and can be used to tailor the synergistic interaction of Akt inhibitors with gemcitabine in pancreatic cancer by Massihnia, Daniela, Avan, Amir, Funel, Niccola, Maftouh, Mina, van Krieken, Anne, Granchi, Carlotta, Raktoe, Rajiv, Boggi, Ugo, Aicher, Babette, Minutolo, Filippo, Russo, Antonio, Leon, Leticia G, Peters, Godefridus J, Giovannetti, Elisa

“…There is increasing evidence of a constitutive activation of Akt in pancreatic ductal adenocarcinoma (PDAC), associated with poor prognosis and…”
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Discovery of Monoacylglycerol Lipase (MAGL) Inhibitors Based on a Pharmacophore-Guided Virtual Screening Study by Jha, Vibhu, Biagi, Marzia, Spinelli, Valeria, Di Stefano, Miriana, Macchia, Marco, Minutolo, Filippo, Granchi, Carlotta, Poli, Giulio, Tuccinardi, Tiziano

“…Monoacylglycerol lipase (MAGL) is an important enzyme of the endocannabinoid system that catalyzes the degradation of the major endocannabinoid…”
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Binding investigation and preliminary optimisation of the 3-amino-1,2,4-triazin-5(2H)-one core for the development of new Fyn inhibitors by Poli, Giulio, Lapillo, Margherita, Granchi, Carlotta, Caciolla, Jessica, Mouawad, Nayla, Caligiuri, Isabella, Rizzolio, Flavio, Langer, Thierry, Minutolo, Filippo, Tuccinardi, Tiziano

“…Fyn tyrosine kinase inhibitors are considered potential therapeutic agents for a variety of human cancers. Furthermore, the involvement of Fyn kinase in…”
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