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Items: 13


Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.

Parthasarathy S, Henry K, Pei H, Clayton J, Rempala M, Johns D, De Frutos O, Garcia P, Mateos C, Pleite S, Wang Y, Stout S, Condon B, Ashok S, Lu Z, Ehlhardt W, Raub T, Lai M, Geeganage S, Burkholder TP.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1887-1891. doi: 10.1016/j.bmcl.2018.03.092. Epub 2018 Apr 2.


Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration.

Zhao G, Green CF, Hui YH, Prieto L, Shepard R, Dong S, Wang T, Tan B, Gong X, Kays L, Johnson RL, Wu W, Bhattachar S, Del Prado M, Gillig JR, Fernandez MC, Roth KD, Buchanan S, Kuo MS, Geeganage S, Burkholder TP.

Mol Cancer Ther. 2017 Dec;16(12):2677-2688. doi: 10.1158/1535-7163.MCT-16-0674. Epub 2017 Oct 20.


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 TP, Cunningham BE, Clayton JR, Lander PA, Brown ML, Doti RA, Durst GL, Montrose-Rafizadeh C, King C, Osborne HE, Amos RM, Zink RW, Stramm LE, Burris TP, Cardona G, Konkol DL, Reidy C, Christe ME, Genin MJ.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1377-80. doi: 10.1016/j.bmcl.2015.02.062. Epub 2015 Mar 3.


Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F.

Ma L, Clayton JR, Walgren RA, Zhao B, Evans RJ, Smith MC, Heinz-Taheny KM, Kreklau EL, Bloem L, Pitou C, Shen W, Strelow JM, Halstead C, Rempala ME, Parthasarathy S, Gillig JR, Heinz LJ, Pei H, Wang Y, Stancato LF, Dowless MS, Iversen PW, Burkholder TP.

Blood Cancer J. 2013 Apr 12;3:e109. doi: 10.1038/bcj.2013.6.


Pharmacological inhibition of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme essential for NAD+ biosynthesis, in human cancer cells: metabolic basis and potential clinical implications.

Tan B, Young DA, Lu ZH, Wang T, Meier TI, Shepard RL, Roth K, Zhai Y, Huss K, Kuo MS, Gillig J, Parthasarathy S, Burkholder TP, Smith MC, Geeganage S, Zhao G.

J Biol Chem. 2013 Feb 1;288(5):3500-11. doi: 10.1074/jbc.M112.394510. Epub 2012 Dec 13.


Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics.

Wacheck V, Lahn M, Dickinson G, Füreder W, Meyer R, Herndlhofer S, Füreder T, Dorfner G, Pillay S, André V, Burkholder TP, Akunda JK, Flye-Blakemore L, Van Bockstaele D, Schlenk RF, Sperr WR, Valent P.

Cancer Manag Res. 2011;3:157-75. doi: 10.2147/CMR.S19341. Epub 2011 May 10.


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 TP, Clayton JR, Rempala ME, Henry JR, Knobeloch JM, Mendel D, McLean JA, Hao Y, Barda DA, Considine EL, Uhlik MT, Chen Y, Ma L, Bloem LJ, Akunda JK, McCann DJ, Sanchez-Felix M, Clawson DK, Lahn MM, Starling JJ.

Invest New Drugs. 2012 Jun;30(3):936-49. doi: 10.1007/s10637-011-9640-6. Epub 2011 Mar 1. Erratum in: Invest New Drugs. 2012 Jun;30(3):1270-1.


Developing and applying a gene functional association network for anti-angiogenic kinase inhibitor activity assessment in an angiogenesis co-culture model.

Chen Y, Wei T, Yan L, Lawrence F, Qian HR, Burkholder TP, Starling JJ, Yingling JM, Shou J.

BMC Genomics. 2008 Jun 2;9:264. doi: 10.1186/1471-2164-9-264.


The development of potent and selective bisarylmaleimide GSK3 inhibitors.

Engler TA, Malhotra S, Burkholder TP, Henry JR, Mendel D, Porter WJ, Furness K, Diefenbacher C, Marquart A, Reel JK, Li Y, Clayton J, Cunningham B, McLean J, O'toole JC, Brozinick J, Hawkins E, Misener E, Briere D, Brier RA, Wagner JR, Campbell RM, Anderson BD, Vaughn R, Bennett DB, Meier TI, Cook JA.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):899-903.


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 TA, Henry JR, Malhotra S, Cunningham B, Furness K, Brozinick J, Burkholder TP, Clay MP, Clayton J, Diefenbacher C, Hawkins E, Iversen PW, Li Y, Lindstrom TD, Marquart AL, McLean J, Mendel D, Misener E, Briere D, O'Toole JC, Porter WJ, Queener S, Reel JK, Owens RA, Brier RA, Eessalu TE, Wagner JR, Campbell RM, Vaughn R.

J Med Chem. 2004 Jul 29;47(16):3934-7.


The peripheral NK-1/NK-2 receptor antagonist MDL 105,172A inhibits tachykinin-mediated respiratory effects in guinea-pigs.

Kudlacz EM, Knippenberg RW, Shatzer SA, Kehne JH, McCloskey TC, Burkholder TP.

J Auton Pharmacol. 1997 Apr;17(2):109-19.


Effect of MDL 105,212, a nonpeptide NK-1/NK-2 receptor antagonist in an allergic guinea pig model.

Kudlacz EM, Knippenberg RW, Logan DE, Burkholder TP.

J Pharmacol Exp Ther. 1996 Nov;279(2):732-9.


In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist.

Kudlacz EM, Shatzer SA, Knippenberg RW, Logan DE, Poirot M, van Giersbergen PL, Burkholder TP.

J Pharmacol Exp Ther. 1996 May;277(2):840-51.


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