Substituted 3-Imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino- [6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as Highly Selective and Potent Inhibitors of Glycogen Synthase Kinase-3
Engler, Thomas A, Henry, James R, Malhotra, Sushant, Cunningham, Brian, Furness, Kelly, Brozinick, Joseph, Burkholder, Timothy P, Clay, Michael P, Clayton, Joshua, Diefenbacher, Clive, Hawkins, Eric, Iversen, Philip W, Li, Yihong, Lindstrom, Terry D, Marquart, Angela L, McLean, Johnathan, Mendel, David, Misener, Elizabeth, Briere, Daniel, O'Toole, John C, Porter, Warren J, Queener, Steven, Reel, Jon K, Owens, Rebecca A, Brier, Richard A, Eessalu, Thomas E, Wagner, Jill R, Campbell, Robert M, Vaughn, Renee
Published in Journal of medicinal chemistry (29.07.2004)
Published in Journal of medicinal chemistry (29.07.2004)
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Pharmacological inhibition of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme essential for NAD+ biosynthesis, in human cancer cells: metabolic basis and potential clinical implications
Tan, Bo, Young, Debra A, Lu, Zhao-Hai, Wang, Tao, Meier, Timothy I, Shepard, Robert L, Roth, Kenneth, Zhai, Yan, Huss, Karen, Kuo, Ming-Shang, Gillig, James, Parthasarathy, Saravanan, Burkholder, Timothy P, Smith, Michele C, Geeganage, Sandaruwan, Zhao, Genshi
Published in The Journal of biological chemistry (01.02.2013)
Published in The Journal of biological chemistry (01.02.2013)
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Developing and applying a gene functional association network for anti-angiogenic kinase inhibitor activity assessment in an angiogenesis co-culture model
Chen, Yuefeng, Wei, Tao, Yan, Lei, Lawrence, Frank, Qian, Hui-Rong, Burkholder, Timothy P, Starling, James J, Yingling, Jonathan M, Shou, Jianyong
Published in BMC genomics (02.06.2008)
Published in BMC genomics (02.06.2008)
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Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration
Zhao, Genshi, Green, Colin F, Hui, Yu-Hua, Prieto, Lourdes, Shepard, Robert, Dong, Sucai, Wang, Tao, Tan, Bo, Gong, Xueqian, Kays, Lisa, Johnson, Robert L, Wu, Wenjuan, Bhattachar, Shobha, Del Prado, Miriam, Gillig, James R, Fernandez, Maria-Carmen, Roth, Ken D, Buchanan, Sean, Kuo, Ming-Shang, Geeganage, Sandaruwan, Burkholder, Timothy P
Published in Molecular cancer therapeutics (01.12.2017)
Published in Molecular cancer therapeutics (01.12.2017)
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The development of potent and selective bisarylmaleimide GSK3 inhibitors
Engler, Thomas A., Malhotra, Sushant, Burkholder, Timothy P., Henry, James R., Mendel, David, Porter, Warren J., Furness, Kelly, Diefenbacher, Clive, Marquart, Angela, Reel, Jon K., Li, Yihong, Clayton, Joshua, Cunningham, Brian, McLean, Johnathan, O’Toole, John C., Brozinick, Joseph, Hawkins, Eric, Misener, Elizabeth, Briere, Daniel, Brier, Richard A., Wagner, Jill R., Campbell, Robert M., Anderson, Bryan D., Vaughn, Renee, Bennett, Donald B., Meier, Timothy I., Cook, James A.
Published in Bioorganic & medicinal chemistry letters (15.02.2005)
Published in Bioorganic & medicinal chemistry letters (15.02.2005)
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Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT
Parthasarathy, Saravanan, Henry, Kenneth, Pei, Huaxing, Clayton, Josh, Rempala, Mark, Johns, Deidre, De Frutos, Oscar, Garcia, Pablo, Mateos, Carlos, Pleite, Sehila, Wang, Yong, Stout, Stephanie, Condon, Bradley, Ashok, Sheela, Lu, Zhohai, Ehlhardt, William, Raub, Tom, Lai, Mei, Geeganage, Sandaruwan, Burkholder, Timothy P.
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
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Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists
Burkholder, Timothy P., Cunningham, Brian E., Clayton, Joshua R., Lander, Peter A., Brown, Matthew L., Doti, Robert A., Durst, Gregory L., Montrose-Rafizadeh, Chahrzad, King, Constance, Osborne, Harold E., Amos, Robert M., Zink, Richard W., Stramm, Lawrence E., Burris, Thomas P., Cardona, Guemalli, Konkol, Debra L., Reidy, Charles, Christe, Michael E., Genin, Michael J.
Published in Bioorganic & medicinal chemistry letters (01.04.2015)
Published in Bioorganic & medicinal chemistry letters (01.04.2015)
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Pharmacological Inhibition of Nicotinamide Phosphoribosyltransferase (NAMPT), an Enzyme Essential for NAD+ Biosynthesis, in Human Cancer Cells
Tan, Bo, Young, Debra A., Lu, Zhao-Hai, Wang, Tao, Meier, Timothy I., Shepard, Robert L., Roth, Kenneth, Zhai, Yan, Huss, Karen, Kuo, Ming-Shang, Gillig, James, Parthasarathy, Saravanan, Burkholder, Timothy P., Smith, Michele C., Geeganage, Sandaruwan, Zhao, Genshi
Published in The Journal of biological chemistry (01.02.2013)
Published in The Journal of biological chemistry (01.02.2013)
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Discovery of LY2457546: a multi-targeted anti-angiogenic kinase inhibitor with a novel spectrum of activity and exquisite potency in the acute myelogenous leukemia-Flt-3-internal tandem duplication mutant human tumor xenograft model
Burkholder, Timothy P., Clayton, Joshua R., Rempala, Mark E., Henry, James R., Knobeloch, John M., Mendel, David, McLean, Johnathan A., Hao, Yan, Barda, David A., Considine, Eileen L., Uhlik, Mark T., Chen, Yuefeng, Ma, Liandong, Bloem, Laura J., Akunda, Jacqueline K., McCann, Denis J., Sanchez-Felix, Manuel, Clawson, David K., Lahn, Michael M., Starling, James J.
Published in Investigational new drugs (01.06.2012)
Published in Investigational new drugs (01.06.2012)
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Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics
Wacheck, Volker, Lahn, Michael, Dickinson, Gemma, Füreder, Wolfgang, Meyer, Renata, Herndlhofer, Susanne, Füreder, Thorsten, Dorfner, Georg, Pillay, Sada, André, Valérie, Burkholder, Timothy P, Akunda, Jacqueline K, Flye-Blakemore, Leann, Van Bockstaele, Dirk, Schlenk, Richard F, Sperr, Wolfgang R, Valent, Peter
Published in Cancer management and research (2011)
Published in Cancer management and research (2011)
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Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics
Wacheck, Volker, Lahn, Michael, Dickinson, Gemma, Füreder, Wolfgang, Meyer, Renata, Herndlhofer, Susanne, Füreder, Thorsten, Dorfner, Georg, Pillay, Sada, André, Valérie, Burkholder, Timothy P, Akunda, Jacqueline K, Flye-Blakemore, Leann, Van Bockstaele, Dirk, Schlenk, Richard F, Sperr, Wolfgang R, Valent, Peter
Published in Cancer management and research (01.05.2011)
Published in Cancer management and research (01.05.2011)
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Synthesis and SAR of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/Tachykinin NK1 receptor antagonist activity
MAYNARD, G. D, BRATTON, L. D, LOGAN, D. E, KANE, J. M, BURKHOLDER, T. P, SANTIAGO, B, STEWART, K. T, KUDLACZ, E. M, SHATZER, S. A, KNIPPENBERG, R. W, FARRELL, A. M
Published in Bioorganic & medicinal chemistry letters (18.11.1997)
Published in Bioorganic & medicinal chemistry letters (18.11.1997)
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Abstract 3042: LY2801653: An orally bioavailable MET kinase inhibitor with inhibitory activity against the oncoproteins ROS1 and MKNK1/2
Yan, Sau-Chi B., Thobe, Megan N., Konicek, Bruce W., Peek, Victoria L., Um, Suzane L., Walgren, Richard A., Pei, Huaxing, Burkholder, Timothy P., Graff, Jeremy R.
Published in Cancer research (Chicago, Ill.) (15.04.2013)
Published in Cancer research (Chicago, Ill.) (15.04.2013)
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Abstract 2820: LY2784544, a small molecule JAK2 inhibitor, induces apoptosis in inflammatory breast cancer spheres through targeting IL-6-JAK-STAT3 pathway
Ma, Liandong, Zhao, Baohui, Walgren, Richard A., Clayton, Joshua R., Burkholder, Timothy P.
Published in Cancer research (Chicago, Ill.) (15.04.2011)
Published in Cancer research (Chicago, Ill.) (15.04.2011)
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Efficacy of LY2784544, a Small Molecule Inhibitor Selective for Mutant JAK2 Kinase, In JAK2 V617F-Induced Hematologic Malignancy Models
Ma, Liandong, Zhao, Baohui, Walgren, Richard, Clayton, Joshua A, Blosser, Wayne D, Burkholder, Timothy P, Smith, Michele C
Published in Blood (19.11.2010)
Published in Blood (19.11.2010)
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Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors
Burkholder, Timothy P., Kudlacz, Elizabeth M., Tieu-Binh Le, Knippenberg, Robert W., Shatzer, Scott A., Maynard, George D., Webster, Mark E., Horgan, Stephen W.
Published in Bioorganic & medicinal chemistry letters (23.04.1996)
Published in Bioorganic & medicinal chemistry letters (23.04.1996)
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In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist
Kudlacz, E M, Shatzer, S A, Knippenberg, R W, Logan, D E, Poirot, M, van Giersbergen, P L, Burkholder, T P
Published in The Journal of pharmacology and experimental therapeutics (01.05.1996)
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Published in The Journal of pharmacology and experimental therapeutics (01.05.1996)
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