Search Results - "Luciani, Rosaria"

Structural Comparison of Enterococcus faecalis and Human Thymidylate Synthase Complexes with the Substrate dUMP and Its Analogue FdUMP Provides Hints about Enzyme Conformational Variabilities by Pozzi, Cecilia, Ferrari, Stefania, Luciani, Rosaria, Tassone, Giusy, Costi, Maria Paola, Mangani, Stefano

“…Thymidylate synthase (TS) is an enzyme of paramount importance as it provides the only de novo source of deoxy-thymidine monophosphate (dTMP). dTMP, essential…”
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Structural and Functional Characterization of the Human Thymidylate Synthase (hTS) Interface Variant R175C, New Perspectives for the Development of hTS Inhibitors by Pozzi, Cecilia, Ferrari, Stefania, Luciani, Rosaria, Costi, Maria Paola, Mangani, Stefano

“…Human thymidylate synthase (hTS) is pivotal for cell survival and proliferation, indeed it provides the only synthetic source of dTMP, required for DNA…”
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Cyclic Peptides Acting as Allosteric Inhibitors of Human Thymidylate Synthase and Cancer Cell Growth by Pacifico, Salvatore, Santucci, Matteo, Luciani, Rosaria, Saxena, Puneet, Linciano, Pasquale, Ponterini, Glauco, Lauriola, Angela, D'Arca, Domenico, Marverti, Gaetano, Guerrini, Remo, Costi, Maria Paola

“…Thymidylate synthase (TS) is a prominent drug target for different cancer types. However, the prolonged use of its classical inhibitors, substrate analogs that…”
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Protein–protein interface-binding peptides inhibit the cancer therapy target human thymidylate synthase by Cardinale, Daniela, Guaitoli, Giambattista, Tondi, Donatella, Luciani, Rosaria, Henrich, Stefan, Salo-Ahen, Outi M. H, Ferrari, Stefania, Marverti, Gaetano, Guerrieri, Davide, Ligabue, Alessio, Frassineti, Chiara, Pozzi, Cecilia, Mangani, Stefano, Fessas, Dimitrios, Guerrini, Remo, Ponterini, Glauco, Wade, Rebecca C, Costi, M. Paola

“…Human thymidylate synthase is a homodimeric enzyme that plays a key role in DNA synthesis and is a target for several clinically important anticancer drugs…”
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Repurposing the Trypanosomatidic GSK Kinetobox for the Inhibition of Parasitic Pteridine and Dihydrofolate Reductases by Santucci, Matteo, Luciani, Rosaria, Gianquinto, Eleonora, Pozzi, Cecilia, Pisa, Flavio di, Dello Iacono, Lucia, Landi, Giacomo, Tagliazucchi, Lorenzo, Mangani, Stefano, Spyrakis, Francesca, Costi, Maria Paola

“…Three open-source anti-kinetoplastid chemical boxes derived from a whole-cell phenotypic screening by GlaxoSmithKline (Tres Cantos Anti-Kinetoplastid…”
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Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth by Costantino, Luca, Ferrari, Stefania, Santucci, Matteo, Salo-Ahen, Outi M H, Carosati, Emanuele, Franchini, Silvia, Lauriola, Angela, Pozzi, Cecilia, Trande, Matteo, Gozzi, Gaia, Saxena, Puneet, Cannazza, Giuseppe, Losi, Lorena, Cardinale, Daniela, Venturelli, Alberto, Quotadamo, Antonio, Linciano, Pasquale, Tagliazucchi, Lorenzo, Moschella, Maria Gaetana, Guerrini, Remo, Pacifico, Salvatore, Luciani, Rosaria, Genovese, Filippo, Henrich, Stefan, Alboni, Silvia, Santarem, Nuno, da Silva Cordeiro, Anabela, Giovannetti, Elisa, Peters, Godefridus J, Pinton, Paolo, Rimessi, Alessandro, Cruciani, Gabriele, Stroud, Robert M, Wade, Rebecca C, Mangani, Stefano, Marverti, Gaetano, D'Arca, Domenico, Ponterini, Glauco, Costi, Maria Paola

“…Drugs that target human thymidylate synthase (hTS), a dimeric enzyme, are widely used in anticancer therapy. However, treatment with classical…”
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Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity by Realini, Natalia, Solorzano, Carlos, Pagliuca, Chiara, Pizzirani, Daniela, Armirotti, Andrea, Luciani, Rosaria, Costi, Maria Paola, Bandiera, Tiziano, Piomelli, Daniele

“…The expression of acid ceramidase (AC) – a cysteine amidase that hydrolyses the proapoptotic lipid ceramide – is abnormally high in several human tumors, which…”
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Microbiota of sliced cooked ham packaged in modified atmosphere throughout the shelf life: Microbiota of sliced cooked ham in MAP by Raimondi, Stefano, Luciani, Rosaria, Sirangelo, Tiziana Maria, Amaretti, Alberto, Leonardi, Alan, Ulrici, Alessandro, Foca, Giorgia, D'Auria, Giuseppe, Moya, Andrés, Zuliani, Véronique, Seibert, Tim Martin, Søltoft-Jensen, Jakob, Rossi, Maddalena

“…Fourteen lots of cooked ham in modified atmosphere packaging (CH) were analyzed within a few days from packaging (S) and at the end of the shelf-life (E),…”
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Multitarget, Selective Compound Design Yields Potent Inhibitors of a Kinetoplastid Pteridine Reductase 1 by Pöhner, Ina, Quotadamo, Antonio, Panecka-Hofman, Joanna, Luciani, Rosaria, Santucci, Matteo, Linciano, Pasquale, Landi, Giacomo, Di Pisa, Flavio, Dello Iacono, Lucia, Pozzi, Cecilia, Mangani, Stefano, Gul, Sheraz, Witt, Gesa, Ellinger, Bernhard, Kuzikov, Maria, Santarem, Nuno, Cordeiro-da-Silva, Anabela, Costi, Maria P., Venturelli, Alberto, Wade, Rebecca C.

“…The optimization of compounds with multiple targets is a difficult multidimensional problem in the drug discovery cycle. Here, we present a systematic,…”
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X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors by Catalano, Alessia, Luciani, Rosaria, Carocci, Alessia, Cortesi, Debora, Pozzi, Cecilia, Borsari, Chiara, Ferrari, Stefania, Mangani, Stefano

“…Infections caused by Enterococcus faecalis (Ef) represent nowadays a relevant health problem. We selected Thymidylate synthase (TS) from this organism as a…”
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The discovery of aryl-2-nitroethyl triamino pyrimidines as anti-Trypanosoma brucei agents by Linciano, Pasquale, Pozzi, Cecilia, Tassone, Giusy, Landi, Giacomo, Mangani, Stefano, Santucci, Matteo, Luciani, Rosaria, Ferrari, Stefania, Santarem, Nuno, Tagliazucchi, Lorenzo, Cordeiro-da-Silva, Anabela, Tonelli, Michele, Tondi, Donatella, Bertarini, Laura, Gul, Sheraz, Witt, Gesa, Moraes, Carolina B, Costantino, Luca, Costi, Maria Paola

“…Pteridine reductase 1 (PTR1) is a catalytic protein belonging to the folate metabolic pathway in Trypanosmatidic parasites. PTR1 is a known target for the…”
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High-Throughput Phenotypic Screening and Machine Learning Methods Enabled the Selection of Broad-Spectrum Low-Toxicity Antitrypanosomatidic Agents by Linciano, Pasquale, Quotadamo, Antonio, Luciani, Rosaria, Santucci, Matteo, Zorn, Kimberley M, Foil, Daniel H, Lane, Thomas R, Cordeiro da Silva, Anabela, Santarem, Nuno, B Moraes, Carolina, Freitas-Junior, Lucio, Wittig, Ulrike, Mueller, Wolfgang, Tonelli, Michele, Ferrari, Stefania, Venturelli, Alberto, Gul, Sheraz, Kuzikov, Maria, Ellinger, Bernhard, Reinshagen, Jeanette, Ekins, Sean, Costi, Maria Paola

“…Broad-spectrum anti-infective chemotherapy agents with activity against , and species were identified from a high-throughput phenotypic screening program of…”
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Comparing Drug Images and Repurposing Drugs with BioGPS and FLAPdock: The Thymidylate Synthase Case by Siragusa, Lydia, Luciani, Rosaria, Borsari, Chiara, Ferrari, Stefania, Costi, Maria Paola, Cruciani, Gabriele, Spyrakis, Francesca

“…Repurposing and repositioning drugs has become a frequently pursued and successful strategy in the current era, as new chemical entities are increasingly…”
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Virtual Screening and X‑ray Crystallography Identify Non-Substrate Analog Inhibitors of Flavin-Dependent Thymidylate Synthase by Luciani, Rosaria, Saxena, Puneet, Surade, Sachin, Santucci, Matteo, Venturelli, Alberto, Borsari, Chiara, Marverti, Gaetano, Ponterini, Glauco, Ferrari, Stefania, Blundell, Tom L, Costi, Maria Paola

“…Thymidylate synthase X (ThyX) represents an attractive target for tuberculosis drug discovery. Herein, we selected 16 compounds through a virtual screening…”
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2‑Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1 by Neres, João, Hartkoorn, Ruben C, Chiarelli, Laurent R, Gadupudi, Ramakrishna, Pasca, Maria Rosalia, Mori, Giorgia, Venturelli, Alberto, Savina, Svetlana, Makarov, Vadim, Kolly, Gaelle S, Molteni, Elisabetta, Binda, Claudia, Dhar, Neeraj, Ferrari, Stefania, Brodin, Priscille, Delorme, Vincent, Landry, Valérie, de Jesus Lopes Ribeiro, Ana Luisa, Farina, Davide, Saxena, Puneet, Pojer, Florence, Carta, Antonio, Luciani, Rosaria, Porta, Alessio, Zanoni, Giuseppe, De Rossi, Edda, Costi, Maria Paola, Riccardi, Giovanna, Cole, Stewart T

“…Phenotypic screening of a quinoxaline library against replicating Mycobacterium tuberculosis led to the identification of lead compound Ty38c…”
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Enhancement of Benzothiazoles as Pteridine Reductase‑1 Inhibitors for the Treatment of Trypanosomatidic Infections by Linciano, Pasquale, Pozzi, Cecilia, Iacono, Lucia dello, di Pisa, Flavio, Landi, Giacomo, Bonucci, Alessio, Gul, Sheraz, Kuzikov, Maria, Ellinger, Bernhard, Witt, Gesa, Santarem, Nuno, Baptista, Catarina, Franco, Caio, Moraes, Carolina B, Müller, Wolfgang, Wittig, Ulrike, Luciani, Rosaria, Sesenna, Antony, Quotadamo, Antonio, Ferrari, Stefania, Pöhner, Ina, Cordeiro-da-Silva, Anabela, Mangani, Stefano, Costantino, Luca, Costi, Maria Paola

“…2-Amino-benzo­[d]­thiazole was identified as a new scaffold for the development of improved pteridine reductase-1 (PTR1) inhibitors and anti-trypanosomatidic…”
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Aryl thiosemicarbazones for the treatment of trypanosomatidic infections by Linciano, Pasquale, Moraes, Carolina B., Alcantara, Laura M., Franco, Caio H., Pascoalino, Bruno, Freitas-Junior, Lucio H., Macedo, Sara, Santarem, Nuno, Cordeiro-da-Silva, Anabela, Gul, Sheraz, Witt, Gesa, Kuzikov, Maria, Ellinger, Bernhard, Ferrari, Stefania, Luciani, Rosaria, Quotadamo, Antonio, Costantino, Luca, Costi, Maria Paola

“…Basing on a library of thiadiazole derivatives showing anti-trypanosomatidic activity, we have considered the thiadiazoles opened forms and reaction…”
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Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics by Borsari, Chiara, Jiménez-Antón, María Dolores, Eick, Julia, Bifeld, Eugenia, Torrado, Juan José, Olías-Molero, Ana Isabel, Corral, María Jesús, Santarem, Nuno, Baptista, Catarina, Severi, Leda, Gul, Sheraz, Wolf, Markus, Kuzikov, Maria, Ellinger, Bernhard, Reinshagen, Jeanette, Witt, Gesa, Linciano, Pasquale, Tait, Annalisa, Costantino, Luca, Luciani, Rosaria, Tejera Nevado, Paloma, Zander-Dinse, Dorothea, Franco, Caio H., Ferrari, Stefania, Moraes, Carolina B., Cordeiro-da-Silva, Anabela, Ponterini, Glauco, Clos, Joachim, Alunda, José María, Costi, Maria Paola

“…Leishmaniasis, a major health problem worldwide, has a limited arsenal of drugs for its control. The appearance of resistance to first- and second-line…”
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Conformational Propensity and Biological Studies of Proline Mutated LR Peptides Inhibiting Human Thymidylate Synthase and Ovarian Cancer Cell Growth by Saxena, Puneet, Severi, Leda, Santucci, Matteo, Taddia, Laura, Ferrari, Stefania, Luciani, Rosaria, Marverti, Gaetano, Marraccini, Chiara, Tondi, Donatella, Mor, Marco, Scalvini, Laura, Vitiello, Simone, Losi, Lorena, Fonda, Sergio, Pacifico, Salvatore, Guerrini, Remo, D’Arca, Domenico, Ponterini, Glauco, Costi, Maria Paola

“…LR and [d-Gln 4 ]­LR peptides bind the monomer–monomer interface of human thymidylate synthase and inhibit cancer cell growth. Here, proline-mutated LR…”
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Profiling of Flavonol Derivatives for the Development of Antitrypanosomatidic Drugs by Borsari, Chiara, Luciani, Rosaria, Pozzi, Cecilia, Poehner, Ina, Henrich, Stefan, Trande, Matteo, Cordeiro-da-Silva, Anabela, Santarem, Nuno, Baptista, Catarina, Tait, Annalisa, Di Pisa, Flavio, Dello Iacono, Lucia, Landi, Giacomo, Gul, Sheraz, Wolf, Markus, Kuzikov, Maria, Ellinger, Bernhard, Reinshagen, Jeanette, Witt, Gesa, Gribbon, Philip, Kohler, Manfred, Keminer, Oliver, Behrens, Birte, Costantino, Luca, Tejera Nevado, Paloma, Bifeld, Eugenia, Eick, Julia, Clos, Joachim, Torrado, Juan, Jiménez-Antón, María D, Corral, María J, Alunda, José Ma, Pellati, Federica, Wade, Rebecca C, Ferrari, Stefania, Mangani, Stefano, Costi, Maria Paola

“…Flavonoids represent a potential source of new antitrypanosomatidic leads. Starting from a library of natural products, we combined target-based screening on…”
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