Search Results - "BOSCHELLI, Frank"

Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants by Redaelli, Sara, Piazza, Rocco, Rostagno, Roberta, Magistroni, Vera, Perini, Pietro, Marega, Manuela, Gambacorti-Passerini, Carlo, Boschelli, Frank

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SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells by Vultur, Adina, Buettner, Ralf, Kowolik, Claudia, Liang, Wei, Smith, David, Boschelli, Frank, Jove, Richard

“…Src family kinase activity is elevated in many human tumors, including breast cancer, and is often associated with aggressive disease. We examined the effects…”
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In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells by Puttini, Miriam, Coluccia, Addolorata Maria Luce, Boschelli, Frank, Cleris, Loredana, Marchesi, Edoardo, Donella-Deana, Arianna, Ahmed, Shaheen, Redaelli, Sara, Piazza, Rocco, Magistroni, Vera, Andreoni, Federica, Scapozza, Leonardo, Formelli, Franca, Gambacorti-Passerini, Carlo

“…Resistance to imatinib represents an important scientific and clinical issue in chronic myelogenous leukemia. In the present study, the effects of the novel…”
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SKI-606 (Bosutinib) blocks prostate cancer invasion, growth, and metastasis in vitro and in vivo through regulation of genes involved in cancer growth and skeletal metastasis by Rabbani, Shafaat A, Valentino, Maria-Luisa, Arakelian, Ani, Ali, Suhad, Boschelli, Frank

“…In the current study, we have examined the efficacy of a Src/Abl kinase inhibitor SKI-606 (Bosutinib) for its effect on prostate cancer growth and skeletal…”
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Discovery of Benzisoxazoles as Potent Inhibitors of Chaperone Heat Shock Protein 90 by Gopalsamy, Ariamala, Shi, Mengxiao, Golas, Jennifer, Vogan, Erik, Jacob, Jaison, Johnson, Mark, Lee, Frederick, Nilakantan, Ramaswamy, Petersen, Roseann, Svenson, Kristin, Chopra, Rajiv, Tam, May S, Wen, Yingxia, Ellingboe, John, Arndt, Kim, Boschelli, Frank

“…Heat shock protein 90 (Hsp90) is a molecular chaperone that is responsible for activating many signaling proteins and is a promising target in tumor biology…”
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Efficacy and pharmacodynamic effects of bosutinib (SKI-606), a Src/Abl inhibitor, in freshly generated human pancreas cancer xenografts by Messersmith, Wells A, Rajeshkumar, N V, Tan, Aik Choon, Wang, Xiao Fei, Diesl, Veronica, Choe, Sung E, Follettie, Max, Coughlin, Christina, Boschelli, Frank, Garcia-Garcia, Elena, Lopez-Rios, Fernando, Jimeno, Antonio, Hidalgo, Manuel

“…Recently, Src tyrosine kinase has emerged as an attractive target for anticancer therapy, and Src is overexpressed in pancreatic cancer. The purpose of the…”
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Neuroprotective profile of novel SRC kinase inhibitors in rodent models of cerebral ischemia by Liang, Shi, Pong, Kevin, Gonzales, Cathleen, Chen, Yi, Ling, Huai-Ping, Mark, Robert J, Boschelli, Frank, Boschelli, Diane H, Ye, Fei, Barrios Sosa, Ana Carolina, Mansour, Tarek S, Frost, Philip, Wood, Andrew, Pangalos, Menelas N, Zaleska, Margaret M

“…Src kinase signaling has been implicated in multiple mechanisms of ischemic injury, including vascular endothelial growth factor (VEGF)-mediated vascular…”
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Optimization of 4-Phenylamino-3-quinolinecarbonitriles as Potent Inhibitors of Src Kinase Activity by Boschelli, Diane H, Ye, Fei, Wang, Yanong D, Dutia, Minu, Johnson, Steve L, Wu, Biqi, Miller, Karen, Powell, Dennis W, Yaczko, Deanna, Young, Mairead, Tischler, Mark, Arndt, Kim, Discafani, Carolyn, Etienne, Carlo, Gibbons, Jay, Grod, Janet, Lucas, Judy, Weber, Jennifer M, Boschelli, Frank

“…Subsequent to the discovery of 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile (1a) as an inhibitor of Src kinase activity (IC50 = 30 nM),…”
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Src family kinases promote AML cell survival through activation of signal transducers and activators of transcription (STAT) by Ozawa, Yukiyasu, Williams, Ann H, Estes, Myka L, Matsushita, Norimasa, Boschelli, Frank, Jove, Richard, List, Alan F

“…Abstract We investigated the role of Src family kinases (SFKs) in the regulation of STAT activation in myeloid leukemia cells. Two of 6 AML cell lines…”
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Synthesis and Src Kinase Inhibitory Activity of a Series of 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles by Boschelli, Diane H, Wu, Biqi, Ye, Fei, Wang, Yan, Golas, Jennifer M, Lucas, Judy, Boschelli, Frank

“…Compound 1 (SKI-606, bosutinib), a 7-alkoxy-4-[(2,4-dichloro-5-methoxyphenyl)amino]-3-quinolinecarbonitrile, is a potent inhibitor of Src kinase activity. We…”
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Identification of a Conserved Sequence Motif That Promotes Cdc37 and Cyclin D1 Binding to Cdk4 by Zhao, Qiang, Boschelli, Frank, Caplan, Avrom J., Arndt, Kim T.

“…Cdc37 is a molecular chaperone that is important for the stability and activity of several protein kinases, including Cdk4 and Raf1. We first determined, using…”
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Synthesis and Src Kinase Inhibitory Activity of a Series of 4-Phenylamino-3-quinolinecarbonitriles by Boschelli, Diane H, Wang, Yanong D, Ye, Fei, Wu, Biqi, Zhang, Nan, Dutia, Minu, Powell, Dennis W, Wissner, Allan, Arndt, Kim, Weber, Jennifer M, Boschelli, Frank

“…Screening of a directed compound library in a yeast-based assay identified 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile (2a) as a Src…”
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Bosutinib: A review of preclinical studies in chronic myelogenous leukaemia by Boschelli, Frank, Arndt, Kim, Gambacorti-Passerini, Carlo

“…Abstract Bosutinib (SKI-606) is an orally active Src and Abl kinase inhibitor presently in Phase III trials for treatment of chronic myelogenous leukaemia…”
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A Src/Abl kinase inhibitor, SKI-606, blocks breast cancer invasion, growth, and metastasis in vitro and in vivo by JALLAL, Houda, VALENTINE, Maria-Luisa, GAOPING CHEN, BOSCHELLI, Frank, ALI, Suhad, RABBANI, Shafaat A

“…The central role of Src in the development of several malignancies, including breast cancer, and the accumulating evidence of its interaction with receptor…”
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In vitro and in vivo identification of ABCB1 as an efflux transporter of bosutinib by Redaelli, Sara, Perini, Pietro, Ceccon, Monica, Piazza, Rocco, Rigolio, Roberta, Mauri, Mario, Boschelli, Frank, Giannoudis, Athina, Gambacorti-Passerini, Carlo

“…Bosutinib is a recently approved ABL inhibitor. In spite of the well-documented effectiveness of BCR-ABL inhibitors in treating chronic myeloid leukemia,…”
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SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice by GOLAS, Jennifer M, ARNDT, Kim, ETIENNE, Carlo, LUCAS, Judy, NARDIN, Danielle, GIBBONS, James, FROST, Philip, FEI YE, BOSCHELLI, Diane H, BOSCHELLI, Frank

“…Constitutive tyrosine kinase activity of Bcr-Abl promotes proliferation and survival of chronic myelogenous leukemia (CML) cells. Inhibition of Bcr-Abl…”
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SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models by GALAS, Jennifer M, LUCAS, Judy, FANGBIAO LI, TITSCH, Craig, HUSELTON, Christine, CHAUDHARY, Inder, BOSCHELLI, Frank, ETIENNE, Carlo, GOLAS, Jonathan, DISCAFANI, Carolyn, SRIDHARAN, Latha, BOGHAERT, Erwin, ARNDT, Kim, FEI YE, BOSCHELLI, Diane H

“…Src up-regulation is a common event in human cancers. In colorectal cancer, increased Src levels are an indicator of poor prognosis, and progression to…”
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Valproic acid enhances bosutinib cytotoxicity in colon cancer cells by Mologni, Luca, Cleris, Loredana, Magistroni, Vera, Piazza, Rocco, Boschelli, Frank, Formelli, Franca, Gambacorti‐Passerini, Carlo

“…Unbalanced histone deacetylase (HDAC) hyperactivity is a common feature of tumor cells. Inhibition of HDAC activity is often associated with cancer cell growth…”
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Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment by Mayer, Scott C., Banker, Annette L., Boschelli, Frank, Di, Li, Johnson, Mark, Kenny, Cynthia Hess, Krishnamurthy, Girija, Kutterer, Kristina, Moy, Franklin, Petusky, Susan, Ravi, Malini, Tkach, Diane, Tsou, Hwei-Ru, Xu, Weixin

“…The strategies, synthesis, and SAR behind novel isoquinolinedione IGFR inhibitors ( 1) are reported. Insulin-like growth factor receptor (IGF-1R) is a growth…”
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Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model by Zapf, Christoph W., Bloom, Jonathan D., Li, Zhong, Dushin, Russell G., Nittoli, Thomas, Otteng, Mercy, Nikitenko, Antonia, Golas, Jennifer M., Liu, Hao, Lucas, Judy, Boschelli, Frank, Vogan, Erik, Olland, Andrea, Johnson, Mark, Levin, Jeremy I.

“…An extension of our previously reported series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. Addition of a second methyl group to the…”
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