Search Results - "Leopold, Wilbur"

Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts by Fry, David W, Harvey, Patricia J, Keller, Paul R, Elliott, William L, Meade, Maryanne, Trachet, Erin, Albassam, Mudher, Zheng, XianXian, Leopold, Wilbur R, Pryer, Nancy K, Toogood, Peter L

“…PD 0332991 is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) (IC 50 , 0.011 μmol/L) and Cdk6 (IC 50 , 0.016 μmol/L), having no activity…”
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The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901 by Barrett, Stephen D., Bridges, Alexander J., Dudley, David T., Saltiel, Alan R., Fergus, James H., Flamme, Cathlin M., Delaney, Amy M., Kaufman, Michael, LePage, Sophie, Leopold, Wilbur R., Przybranowski, Sally A., Sebolt-Leopold, Judith, Van Becelaere, Keri, Doherty, Annette M., Kennedy, Robert M., Marston, Dan, Howard, W. Allen, Smith, Yvonne, Warmus, Joseph S., Tecle, Haile

“…A novel series of benzhydroxamic esters were identified as potent MEK inhibitors. Optimization of these esters produced the two clinical candidates CI-1040 and…”
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Magnetic Resonance Imaging Determination of Tumor Grade and Early Response to Temozolomide in a Genetically Engineered Mouse Model of Glioma by MCCONVILLE, Patrick, HAMBARDZUMYAN, Dolores, MOODY, Jonathan B, LEOPOLD, Wilbur R, KREGER, Alicia R, WOOLLISCROFT, Michael J, REHEMTULLA, Alnawaz, ROSS, Brian D, HOLLAND, Eric C

“…Purpose: The median survival for patients diagnosed with glioblastoma multiforme, the most common type of brain tumor, is less than 1 year. Animal glioma…”
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Design and Synthesis of 2-Nitroimidazoles with Variable Alkylating and Acylating Functionality by Winters, Thomas, Sercel, Anthony, Suto, Carla, Elliott, William, Leopold, Wilbur, Leopold, Judith, Showalter, Hollis

“…The synthesis of a small series of 2-nitroimidazoles in which the β-amino alcohol side chain was amidated with a range of alkylating/acylating functionality is…”
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Radiosensitization by Pan ErbB Inhibitor CI-1033 in Vitro and in Vivo by NYATI, Mukesh K, MAHESHWARI, Divya, HANASOGE, Sheela, SREEKUMAR, Arun, RYNKIEWICZ, Susan D, CHINNAIYAN, Arul M, LEOPOLD, Wilbur R, ETHIER, Stephen P, LAWRENCE, Theodore S

“…Purpose: Overexpression of the ErbB family of receptor tyrosine kinases has been associated with uncontrolled growth of many tumor types and, therefore,…”
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A Specific Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase by Fry, David W., Kraker, Alan J., McMichael, Amy, Ambroso, Linda A., Nelson, James M., Leopold, Wilbur R., Conners, Richard W., Bridges, Alexander J.

“…A small molecule called PD 153035 inhibited the epidermal growth factor (EGF) receptor tyrosine kinase with a 5-pM inhibition constant. The inhibitor was…”
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Dynamic imaging of emerging resistance during cancer therapy by LEE, Kuei C, HALL, Daniel E, REHEMTULLA, Alnawaz, ROSS, Brian D, HOFF, Benjamin A, MOFFAT, Bradford A, SHARMA, Surabhi, CHENEVERT, Thomas L, MEYER, Charles R, LEOPOLD, Wilbur R, JOHNSON, Timothy D, MAZURCHUK, Richard V

“…One of the greatest challenges in developing therapeutic regimens is the inability to rapidly and objectively assess tumor response due to treatment. Moreover,…”
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The influence of tumor size and environment on gene expression in commonly used human tumor lines by Gieseg, Michael A, Man, Michael Z, Gorski, Nicholas A, Madore, Steven J, Kaldjian, Eric P, Leopold, Wilbur R

“…The expression profiles of solid tumor models in rodents have been only minimally studied despite their extensive use to develop anticancer agents. We have…”
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Design and Synthesis of 2-Nitroimidazoles with Variable Alkylating and Acylating Functionality by Thomas Winters, Anthony Sercel, Carla Suto, William Elliott, Wilbur Leopold, Judith Leopold, Hollis Showalter

“…The synthesis of a small series of 2-nitroimidazoles in which the β-amino alcohol side chain was amidated with a range of alkylating/acylating functionality is…”
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Specific, Irreversible Inactivation of the Epidermal Growth Factor Receptor and erbB2, by a New Class of Tyrosine Kinase Inhibitor by Fry, David W., Bridges, Alexander J., Denny, William A., Doherty, Annette, Greis, Kenneth D., Hicks, James L., Hook, Kenneth E., Keller, Paul R., Leopold, Wilbur R., Loo, Joseph A., McNamara, Dennis J., Nelson, James M., Sherwood, Veronika, Smaill, Jeff B., Trumpp-Kallmeyer, Susanne, Dobrusin, Ellen M.

“…A class of high-affinity inhibitors is disclosed that selectively target and irreversibly inactivate the epidermal growth factor receptor tyrosine kinase…”
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Plasma vascular endothelial growth factor and interleukin-8 as biomarkers of antitumor efficacy of a prototypical erbB family tyrosine kinase inhibitor by Christensen, James G, Vincent, Patrick W, Klohs, Wayne D, Fry, David W, Leopold, Wilbur R, Elliott, William L

“…CI-1033 ( N -[4-[ N -(3-chloro-4-fluorophenyl)amino-7-[3-(4-morpholynyl)propoxy]quinazolin-6-yl]acrylamide, PD 0183805-mesylate salt) was identified as a…”
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Abstract 5194: Focal radiation enhances paclitaxel therapy in a mouse model of triple negative breast cancer by Franklin, Maryland, Dailey, Thomas, Leopold, Wilbur

“…Abstract Triple negative breast cancer (TNBC) accounts for 15-20% of all breast cancers in the US. In general, patients have poorer prognosis and therapeutic…”
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Tyrosine Kinase Inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(Phenylamino)pyrido[d]pyrimidine Acrylamides as Irreversible Inhibitors of the ATP Binding Site of the Epidermal Growth Factor Receptor by Smaill, Jeff B, Palmer, Brian D, Rewcastle, Gordon W, Denny, William A, McNamara, Dennis J, Dobrusin, Ellen M, Bridges, Alexander J, Zhou, Hairong, Showalter, H. D. Hollis, Winters, R. Thomas, Leopold, Wilbur R, Fry, David W, Nelson, James M, Slintak, Veronika, Elliot, William L, Roberts, Billy J, Vincent, Patrick W, Patmore, Sandra J

“…A series of 6- and 7-acrylamide derivatives of the 4-(phenylamino)quinazoline and -pyridopyrimidine classes of epidermal growth factor receptor (EGFR)…”
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3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and Related 2-Urea Derivatives Are Potent and Selective Inhibitors of the FGF Receptor-1 Tyrosine Kinase by Thompson, Andrew M, Connolly, Cleo J. C, Hamby, James M, Boushelle, Stacey, Hartl, Brian G, Amar, Aneesa M, Kraker, Alan J, Driscoll, Denise L, Steinkampf, Randall W, Patmore, Sandra J, Vincent, Patrick W, Roberts, Bill J, Elliott, William L, Klohs, Wayne, Leopold, Wilbur R, Showalter, H. D. Hollis, Denny, William A

“…A series of 3-aryl-1,6-naphthyridine-2,7-diamines and related 2-ureas were prepared and evaluated as inhibitors of the FGF receptor-1 tyrosine kinase…”
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Differential Utilization and Localization of ErbB Receptor Tyrosine Kinases in Skin Compared to Normal and Malignant Keratinocytes by Stoll, Stefan W., Kansra, Sanjay, Peshick, Scott, Fry, David W., Leopold, Wilbur R., Wiesen, Jane F., Sibilia, Maria, Zhang, Tong, Werb, Zena, Derynck, Rik, Wagner, Erwin F., Elder, James T.

“…Induction of heparin-binding epidermal growth factorlike growth factor (HB-EGF) mRNA in mouse skin organ culture was blocked by two pan-ErbB receptor tyrosine…”
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C-Terminal Modifications of Histidyl-N-benzylglycinamides To Give Improved Inhibition of Ras Farnesyltransferase, Cellular Activity, and Anticancer Activity in Mice by McNamara, Dennis J, Dobrusin, Ellen, Leonard, Daniele M, Shuler, Kevon R, Kaltenbronn, James S, Quin, John, Bur, Scott, Thomas, Charles E, Doherty, Annette M, Scholten, Jeffrey D, Zimmerman, Karen K, Gibbs, Barbara S, Gowan, Richard C, Latash, Michael P, Leopold, Wilbur R, Przybranowski, Sally A, Sebolt-Leopold, Judith S

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Abstract B15: Increased clinical relevance of orthotopic glioma models through bioluminescence and MR imaging by Lister, Deanne, Meade, Mary Anne, Woolliscroft, Tracey, Balagurunathan, Deepa, Trachet, Erin, Leopold, Wilbur, McConville, Patrick

“…Abstract Glioblastoma multiforme (GBM) is the most common and most aggressive form of malignant primary brain tumors, affecting nearly 35,000 people in the…”
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Abstract 3929: Orthotopic human choroidal melanoma model characterization with bioluminescence and magnetic resonance imaging for therapeutic efficacy evaluation by Chunta, John L., Baugher, Meridith, Lister, Deanne, Trachet, Erin, Guley, Kevin P., Bull, Chris, Wise, Scott, Leopold, Wilbur R., McConville, Patrick

“…Abstract BACKGROUND: Intraocular melanomas in the West represents 70% of all primary eye cancers with a mortality rate greater than 50%. Current treatment…”
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Amino-terminal sequence determinants for substrate recognition by platelet-derived growth factor receptor tyrosine kinase by Chan, Perry M., Keller, Paul R., Connors, Richard W., Leopold, Wilbur R., Miller, W.Todd

“…The specificity of protein kinases has been shown to be influenced by residues near the phosphoaccepting amino acid. To examine the determinants for…”
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Anthrapyrazoles, a new class of intercalating agents with high-level, broad spectrum activity against murine tumors by LEOPOLD, W. R, NELSON, J. M, PLOWMAN, J, JACKSON, R. C

“…A series of 5-[(aminoalkyl)amino]-substituted anthra[1,9-cd] pyrazol-6(2H)ones (anthrapyrazoles) were synthesized. These compounds, which differ from the…”
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