Search Results - "Wishart, Neil"

In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494) by Parmentier, Julie M, Voss, Jeff, Graff, Candace, Schwartz, Annette, Argiriadi, Maria, Friedman, Michael, Camp, Heidi S, Padley, Robert J, George, Jonathan S, Hyland, Deborah, Rosebraugh, Matthew, Wishart, Neil, Olson, Lisa, Long, Andrew J

“…Anti-cytokine therapies such as adalimumab, tocilizumab, and the small molecule JAK inhibitor tofacitinib have proven that cytokines and their subsequent…”
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Preparation of enantiomerically pure protected 4-oxo .alpha.-amino acids and 3-aryl .alpha.-amino acids from serine by Jackson, Richard F. W, Wishart, Neil, Wood, Anthony, James, Keith, Wythes, Martin J

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Phase II Study of ABT‐122, a Tumor Necrosis Factor– and Interleukin‐17A–Targeted Dual Variable Domain Immunoglobulin, in Patients With Psoriatic Arthritis With an Inadequate Response to Methotrexate by Mease, Philip J., Genovese, Mark C., Weinblatt, Michael E., Peloso, Paul M., Chen, Kun, Othman, Ahmed A., Li, Yihan, Mansikka, Heikki T., Khatri, Amit, Wishart, Neil, Liu, John

“…Objective To investigate the safety and efficacy of ABT‐122, a tumor necrosis factor (TNF)– and interleukin‐17A (IL‐17A)–targeted dual variable domain…”
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Cell-Type and Stimulus Determine the Impact of the Serine/Threonine Kinase Cot/Tpl2 in Acute and Chronic Inflammation by Murtaza, Anwar, Senior Scientist, Abbott Bioresearch Center, Pharmacology, Worcester, MA, Bryant, Shaughn, Research Associate, Abbott Bioresearch Center, Pharmacology, Worcester, MA, Mathieu, Suzanne, Research Associate, Abbott Bioresearch Center, Pharmacology, Worcester, MA, Allen, Hamish, Director, Abbott Bioresearch Center, Molecular and Cellular Biology, Worcester, MA, Tripp, Catherine, Senior Director, Abbott Bioresearch Center, Worcester, MA, Wishart, Neil, Associate Director, Abbott Bioresearch Center, Chemistry, Worcester, MA

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Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors by Friedman, Michael, Frank, Kristine E., Aguirre, Ana, Argiriadi, Maria A., Davis, Heather, Edmunds, Jeremy J., George, Dawn M., George, Jonathan S., Goedken, Eric, Fiamengo, Bryan, Hyland, Deborah, Li, Bin, Murtaza, Anwar, Morytko, Michael, Somal, Gagandeep, Stewart, Kent, Tarcsa, Edit, Van Epps, Stacy, Voss, Jeffrey, Wang, Lu, Woller, Kevin, Wishart, Neil

“…[Display omitted] Previous work investigating tricyclic pyrrolopyrazines as kinase cores led to the discovery that…”
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Rotationally Constrained 2,4-Diamino-5,6-disubstituted Pyrimidines: A New Class of Histamine H 4 Receptor Antagonists with Improved Druglikeness and in Vivo Efficacy in Pain and Inflammation Models by Cowart, Marlon D., Altenbach, Robert J., Liu, Huaqing, Hsieh, Gin C., Drizin, Irene, Milicic, Ivan, Miller, Thomas R., Witte, David G., Wishart, Neil, Fix-Stenzel, Shannon R., McPherson, Michael J., Adair, Ronald M., Wetter, Jill M., Bettencourt, Brian M., Marsh, Kennan C., Sullivan, James P., Honore, Prisca, Esbenshade, Timothy A., Brioni, Jorge D.

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Design and synthesis of tricyclic cores for kinase inhibition by Van Epps, Stacy, Fiamengo, Bryan, Edmunds, Jeremy, Ericsson, Anna, Frank, Kristine, Friedman, Michael, George, Dawn, George, Jonathan, Goedken, Eric, Kotecki, Brian, Martinez, Gloria, Merta, Philip, Morytko, Michael, Shekhar, Shashank, Skinner, Barbara, Stewart, Kent, Voss, Jeffrey, Wallace, Grier, Wang, Lu, Wishart, Neil

“…Interest in therapeutic kinase inhibitors continues to grow beyond success in oncology. To date, ATP-mimetic kinase inhibitors have focused primarily on…”
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Syk Inhibition Induces Platelet Dependent Peri-islet Hemorrhage in the Rat Pancreas by Long, Andrew J., Sampson, Erik, McCarthy, Richard W., Harris, Christopher M., Barnard, Marc, Shi, Dan, Conlon, Donna, Caldwell, Robert, Honor, David, Wishart, Neil, Hoemann, Michael, Duggan, Lori, Fritz, Douglas, Stedman, Christopher, O’Connor, Elizabeth, Mikaelian, Igor, Schwartz, Annette

“…Spleen tyrosine kinase (Syk) is a nonreceptor tyrosine kinase that is an important signaling enzyme downstream of immunoreceptors containing an intracellular…”
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Structure−Activity Studies on a Series of a 2-Aminopyrimidine-Containing Histamine H 4 Receptor Ligands by Altenbach, Robert J., Adair, Ronald M., Bettencourt, Brian M., Black, Lawrence A., Fix-Stenzel, Shannon R., Gopalakrishnan, Sujatha M., Hsieh, Gin C., Liu, Huaqing, Marsh, Kennan C., McPherson, Michael J., Milicic, Ivan, Miller, Thomas R., Vortherms, Timothy A., Warrior, Usha, Wetter, Jill M., Wishart, Neil, Witte, David G., Honore, Prisca, Esbenshade, Timothy A., Hancock, Arthur A., Brioni, Jorge D., Cowart, Marlon D.

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Rotationally Constrained 2,4-Diamino-5,6-disubstituted Pyrimidines: A New Class of Histamine H4 Receptor Antagonists with Improved Druglikeness and in Vivo Efficacy in Pain and Inflammation Models by Cowart, Marlon D, Altenbach, Robert J, Liu, Huaqing, Hsieh, Gin C, Drizin, Irene, Milicic, Ivan, Miller, Thomas R, Witte, David G, Wishart, Neil, Fix-Stenzel, Shannon R, McPherson, Michael J, Adair, Ronald M, Wetter, Jill M, Bettencourt, Brian M, Marsh, Kennan C, Sullivan, James P, Honore, Prisca, Esbenshade, Timothy A, Brioni, Jorge D

“…A new structural class of histamine H4 receptor antagonists (6−14) was designed based on rotationally restricted 2,4-diaminopyrimidines. Series compounds…”
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Thienopyrimidine Ureas as Novel and Potent Multitargeted Receptor Tyrosine Kinase Inhibitors by Dai, Yujia, Guo, Yan, Frey, Robin R, Ji, Zhiqin, Curtin, Michael L, Ahmed, Asma A, Albert, Daniel H, Arnold, Lee, Arries, Shannon S, Barlozzari, Teresa, Bauch, Joy L, Bouska, Jennifer J, Bousquet, Peter F, Cunha, George A, Glaser, Keith B, Guo, Jun, Li, Junling, Marcotte, Patrick A, Marsh, Kennan C, Moskey, Maria D, Pease, Lori J, Stewart, Kent D, Stoll, Vincent S, Tapang, Paul, Wishart, Neil, Davidsen, Steven K, Michaelides, Michael R

“…A series of novel thienopyrimidine-based receptor tyrosine kinase inhibitors has been discovered. Investigation of structure−activity relationships at the 5-…”
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Structure−Activity Studies on a Series of a 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands by Altenbach, Robert J, Adair, Ronald M, Bettencourt, Brian M, Black, Lawrence A, Fix-Stenzel, Shannon R, Gopalakrishnan, Sujatha M, Hsieh, Gin C, Liu, Huaqing, Marsh, Kennan C, McPherson, Michael J, Milicic, Ivan, Miller, Thomas R, Vortherms, Timothy A, Warrior, Usha, Wetter, Jill M, Wishart, Neil, Witte, David G, Honore, Prisca, Esbenshade, Timothy A, Hancock, Arthur A, Brioni, Jorge D, Cowart, Marlon D

“…A series of 2-aminopyrimidines was synthesized as ligands of the histamine H4 receptor (H4R). Working in part from a pyrimidine hit that was identified in an…”
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Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production by Cusack, Kevin, Allen, Hamish, Bischoff, Agnieszka, Clabbers, Anca, Dixon, Richard, Fix-Stenzel, Shannon, Friedman, Michael, Gaumont, Yvette, George, Dawn, Gordon, Thomas, Grongsaard, Pintipa, Janssen, Bernd, Jia, Yong, Moskey, Maria, Quinn, Christopher, Salmeron, Andres, Thomas, Christine, Wallace, Grier, Wishart, Neil, Yu, Zhengtian

“…COT (Tpl2 in mice) is a serine/threonine MAP3 kinase that regulates production of TNF-alpha and other pro-inflammatory cytokines such as IL-1beta via the…”
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Minimum significant ratio of selectivity ratios (MSRSR) and confidence in ratio of selectivity ratios (CRSR): quantitative measures for selectivity ratios obtained by screening assays by Goedken, Eric R, Devanarayan, Viswanath, Harris, Christopher M, Dowding, Lori A, Jakway, James P, Voss, Jeffrey W, Wishart, Neil, Jordan, David C, Talanian, Robert V

“…Development of inhibitor compounds selective against undesirable targets is critical in drug discovery. Selectivity ratios for candidate compounds are…”
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Discovery of thieno[2,3- c]pyridines as potent COT inhibitors by George, Dawn, Friedman, Michael, Allen, Hamish, Argiriadi, Maria, Barberis, Claude, Bischoff, Agnieszka, Clabbers, Anca, Cusack, Kevin, Dixon, Richard, Fix-Stenzel, Shannon, Gordon, Thomas, Janssen, Bernd, Jia, Yong, Moskey, Maria, Quinn, Christopher, Salmeron, Jose-Andres, Wishart, Neil, Woller, Kevin, Yu, Zhengtian

“…A series of thieno[2,3- c]pyridines were identified as potent inhibitors of COT kinase activity. Structural modifications exploring SAR resulted in the…”
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2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization by Harris, Christopher M., Ericsson, Anna M., Argiriadi, Maria A., Barberis, Claude, Borhani, David W., Burchat, Andrew, Calderwood, David J., Cunha, George A., Dixon, Richard W., Frank, Kristine E., Johnson, Eric F., Kamens, Joanne, Kwak, Silvia, Li, Biqin, Mullen, Kelly D., Perron, Denise C., Wang, Lu, Wishart, Neil, Wu, Xiaoyun, Zhang, Xiaolei, Zmetra, Tami R., Talanian, Robert V.

“…We describe structure-based optimization of a series of novel 2,4-diaminopyrimidine MK2 inhibitors. Co-crystal structures (see accompanying Letter)…”
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Enabling structure-based drug design of Tyk2 through co-crystallization with a stabilizing aminoindazole inhibitor by Argiriadi, Maria A, Goedken, Eric R, Banach, David, Borhani, David W, Burchat, Andrew, Dixon, Richard W, Marcotte, Doug, Overmeyer, Gary, Pivorunas, Valerie, Sadhukhan, Ramkrishna, Sousa, Silvino, Moore, Nigel St John, Tomlinson, Medha, Voss, Jeffrey, Wang, Lu, Wishart, Neil, Woller, Kevin, Talanian, Robert V

“…Structure-based drug design (SBDD) can accelerate inhibitor lead design and optimization, and efficient methods including protein purification,…”
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Comparative analysis of various in vitro COT kinase assay formats and their applications in inhibitor identification and characterization by Jia, Yong, Quinn, Christopher M., Clabbers, Anca, Talanian, Robert, Xu, Yajun, Wishart, Neil, Allen, Hamish

“…Cancer osaka thyroid (COT) is a member of the mitogen-activated protein kinase kinase kinase family of enzymes and plays a pivotal role in tumor necrosis…”
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Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-a production by CUSACK, Kevin, ALLEN, Hamish, GRONGSAARD, Pintipa, JANSSEN, Bernd, YONG JIA, MOSKEY, Maria, QUINN, Christopher, SALMERON, Andres, THOMAS, Christine, WALLACE, Grier, WISHART, Neil, ZHENGTIAN YU, BISCHOFF, Agnieszka, CLABBERS, Anca, DIXON, Richard, FIX-STENZEL, Shannon, FRIEDMAN, Michael, GAUMONT, Yvette, GEORGE, Dawn, GORDON, Thomas

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Purification and kinetic characterization of recombinant human mitogen-activated protein kinase kinase kinase COT and the complexes with its cellular partner NF-κB1 p105 by Jia, Yong, Quinn, Christopher M., Bump, Nancy J., Clark, Kevin M., Clabbers, Anca, Hardman, Jennifer, Gagnon, Andrew, Kamens, Joanne, Tomlinson, Medha J., Wishart, Neil, Allen, Hamish

“…Cancer osaka thyroid (COT), a human MAP3K, is essential for lipopolysaccharide activation of the Erk MAPK cascade in macrophages. COT30-467 is insoluble,…”
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