Search Results - "GIANELLINI, Laura"

NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies by Valsasina, Barbara, Beria, Italo, Alli, Cristina, Alzani, Rachele, Avanzi, Nilla, Ballinari, Dario, Cappella, Paolo, Caruso, Michele, Casolaro, Alessia, Ciavolella, Antonella, Cucchi, Ulisse, De Ponti, Anna, Felder, Eduard, Fiorentini, Francesco, Galvani, Arturo, Gianellini, Laura M, Giorgini, Maria L, Isacchi, Antonella, Lansen, Jaqueline, Pesenti, Enrico, Rizzi, Simona, Rocchetti, Maurizio, Sola, Francesco, Moll, Jürgen

“…Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase considered to be the master player of cell-cycle regulation during mitosis. It is indeed…”
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PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer by Carpinelli, Patrizia, Ceruti, Roberta, Giorgini, Maria Laura, Cappella, Paolo, Gianellini, Laura, Croci, Valter, Degrassi, Anna, Texido, Gemma, Rocchetti, Maurizio, Vianello, Paola, Rusconi, Luisa, Storici, Paola, Zugnoni, Paola, Arrigoni, Claudio, Soncini, Chiara, Alli, Cristina, Patton, Veronica, Marsiglio, Aurelio, Ballinari, Dario, Pesenti, Enrico, Fancelli, Daniele, Moll, Jürgen

“…PHA-739358 is a small-molecule 3-aminopyrazole derivative with strong activity against Aurora kinases and cross-reactivities with some receptor tyrosine…”
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PHA-680632, a Novel Aurora Kinase Inhibitor with Potent Antitumoral Activity by 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

“…Purpose: Aurora kinases play critical roles during mitosis in chromosome segregation and cell division. The aim of this study was to determine the preclinical…”
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Inhibition of protein-protein interactions: The discovery of druglike β-catenin inhibitors by combining virtual and biophysical screening by Trosset, Jean-Yves, Dalvit, Claudio, Knapp, Stefan, Fasolini, Marina, Veronesi, Marina, Mantegani, Sergio, Gianellini, Laura M., Catana, Cornel, Sundström, Michael, Stouten, Pieter F.W., Moll, Jürgen K.

“…The interaction between β‐catenin and Tcf family members is crucial for the Wnt signal transduction pathway, which is commonly mutated in cancer. This…”
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Phosphorylation of TCTP as a Marker for Polo-like Kinase-1 Activity In Vivo by CUCCHI, Ulisse, GIANELLINI, Laura M, GIORGINI, Maria L, CAPPELLA, Paolo, BERIA, Italo, VALSASINA, Barbara, DE PONTI, Anna, SOLA, Francesco, ALZANI, Rachele, PATTON, Veronica, PEZZONI, Alice, TROIANI, Sonia, SACCARDO, Maria B, RIZZI, Simona

“…Polo-like kinase 1 (PLK1) is the master regulator of mitosis and a target for anticancer therapy. To develop a marker of PLK1 activity in cells and tumour…”
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5-(2-Amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors by Caruso, Michele, Valsasina, Barbara, Ballinari, Dario, Bertrand, Jay, Brasca, Maria Gabriella, Caldarelli, Marina, Cappella, Paolo, Fiorentini, Francesco, Gianellini, Laura M., Scolaro, Alessandra, Beria, Italo

“…Synthesis of two new chemical classes of compounds with good PLK1 activity was reported. Crystal structure, enzymatic activity and in vitro cell proliferation…”
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4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors by Beria, Italo, Valsasina, Barbara, Brasca, Maria Gabriella, Ceccarelli, Walter, Colombo, Maristella, Cribioli, Sabrina, Fachin, Gabriele, Ferguson, Ronald D., Fiorentini, Francesco, Gianellini, Laura M., Giorgini, Maria L., Moll, Jurgen K., Posteri, Helena, Pezzetta, Daniele, Roletto, Fulvia, Sola, Francesco, Tesei, Dania, Caruso, Michele

“…A 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline series of Polo-like kinase inhibitors is reported and the SAR disclosed. The series led to low nanomolar PLK1…”
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Abstract 1324: NMS-P088, a novel FLT3, KIT and CSF1R inhibitor, is a promising clinical candidate for AML and CMML treatment by Ciomei, Marina, Ardini, Elena, Gianellini, Laura, Borleri, GianMaria, Romero, Gemma Texido, Ceruti, Roberta, Pastori, Wilma, Avanzi, Nilla, Casero, Daniele, Gnocchi, Paola, Borgia, Andrea Lombardi, Lussana, Federico, Rambaldi, Alessandro, Galvani, Arturo, Isacchi, Antonella

“…Abstract NMS-P088 is a potent and selective inhibitor of FLT3 and KIT kinases, including variants with both primary as well as secondary resistance mutations,…”
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Abstract 509: The MPS1/TTK inhibitor, NMS-01940153, synergizes with tisotumab vedotin in colorectal cancer by Texido, Gemma, Gasparri, Fabio, Ciavolella, Antonella, Gianellini, Laura, Pedersen, Anders E., Ocaña, Alberto, Colombo, Riccardo, Roberti, Domenico, Mahnke, Lisa, Perrera, Claudia

“…Abstract Background: MPS1 kinase plays a crucial role in maintaining genomic integrity by controlling the spindle assembly checkpoint (SAC). MPS1 is highly…”
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Abstract 4790: Identification and characterization of ATP-mimetic choline kinase inhibitors by Gnocchi, Paola, Quartieri, Francesca, Badari, Alessandra, Bosotti, Roberta, Casale, Elena, Corti, Emiliana, Cristiani, Cinzia G., Cucchi, Ulisse, Gasparri, Fabio, Gianellini, Laura M., Giorgini, Laura M., Montemartini, Marisa, Mion, Giuliana, Nesi, Marcella, Orrenius, Christian, Re, Claudia E., Donati, Daniele, Felder, Eduard R., Galvani, Arturo, Isacchi, Antonella

“…Abstract Introduction: Choline kinase alpha (ChoKα), the first enzyme in the Kennedy pathway that catalyzes the phosphorylation of free choline to…”
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Abstract 1615: NMS-812, a novel potent PERK inhibitor that also inhibits GCN2, exhibits strong anti-tumor activity as single agent and in combination in preclinical models by Perrera, Claudia, Pulici, Maurizio, Banfi, Patrizia, Avanzi, Nilla, Carenzi, Davide, Casero, Daniele, Ciavolella, Antonella, Gianellini, Laura, Gasparri, Fabio, Saturno, Grazia, Valsasina, Barbara, Ardini, Elena, Montagnoli, Alessia, Galvani, Arturo P., Isacchi, Antonella

“…Abstract PERK and GCN2 are eIF-2α serine-threonine kinases activated by endoplasmic reticulum (ER) stress and amino acid deprivation respectively. These…”
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NMS-E973, a Novel Synthetic Inhibitor of Hsp90 with Activity against Multiple Models of Drug Resistance to Targeted Agents, Including Intracranial Metastases by FOGLIATTO, Gianpaolo, GIANELLINI, Laura, PAOLUCCI, Mauro, POLUCCI, Paolo, RUSSO, Micaela, SOLA, Francesco, VALSASINA, Barbara, VISCO, Carlo, ZUCCOTTO, Fabio, DONATI, Daniele, FELDER, Eduard, PESENTI, Enrico, BRASCA, Maria G, GALVANI, Arturo, MANTEGANI, Sergio, ISACCHI, Antonella, CASALE, Elena, BALLINARI, Dario, CIOMEI, Marina, DEGRASSI, Anna, DE PONTI, Anna, GERMANI, Massimiliano, GUANCI, Marco

“…Recent developments of second generation Hsp90 inhibitors suggested a potential for development of this class of molecules also in tumors that have become…”
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Identification of Myb-binding Protein 1A (MYBBP1A) as a Novel Substrate for Aurora B Kinase by Perrera, Claudia, Colombo, Riccardo, Valsasina, Barbara, Carpinelli, Patrizia, Troiani, Sonia, Modugno, Michele, Gianellini, Laura, Cappella, Paolo, Isacchi, Antonella, Moll, Jurgen, Rusconi, Luisa

“…Aurora kinases are mitotic enzymes involved in centrosome maturation and separation, spindle assembly and stability, and chromosome condensation, segregation,…”
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5-(2-Amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridi n -4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors by Caruso, Michele, Valsasina, Barbara, Ballinari, Dario, Bertrand, Jay, Brasca, Maria Gabriella, Caldarelli, Marina, Cappella, Paolo, Fiorentini, Francesco, Gianellini, Laura M, Scolaro, Alessandra, Beria, Italo

“…The discovery and characterization of two new chemical classes of potent and selective Polo-like kinase 1 (PLK1) inhibitors is reported. For the most…”
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Abstract 691: In vitro and in vivo characterization of selective orally available Parp-1 inhibitors with demonstrated antitumor efficacy in BRCA negative cancer models by Papeo, Gianluca, Rainoldi, Sonia, Gianellini, Laura, Ciavolella, Antonella, Leone, Antonella, Lupi, Rosita, Sola, Francesco, Caprera, Francesco, Paolucci, Mauro, Thieffine, Sandrine, Perego, Rita, Albanese, Clara, Casale, Elena, Forte, Barbara, Guanci, Marco, Orsini, Paolo, Posteri, Helena, Scolaro, Alessandra, Riccardi-Sirtori, Federico, Zuccotto, Fabio, Donati, Daniele, Moll, Jurgen, Montagnoli, Alessia

“…Abstract Poly (ADP-ribose) polymerase 1 and 2 (Parp-1 and Parp-2) are nuclear enzymes responsible for signaling the presence of DNA damages by catalyzing the…”
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Inhibition of protein-protein interactions: The discovery of druglike [beta]-catenin inhibitors by combining virtual and biophysical screening by Trosset, Jean-Yves, Dalvit, Claudio, Knapp, Stefan, Fasolini, Marina, Veronesi, Marina, Mantegani, Sergio, Gianellini, Laura M, Catana, Cornel, Sundstroem, Michael, Stouten, Pieter FW, Moll, Juergen K

“…The interaction between [beta]-catenin and Tcf family members is crucial for the Wnt signal transduction pathway, which is commonly mutated in cancer. This…”
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