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Items: 1 to 50 of 79

1.

Identification of novel resistance mechanisms to NAMPT inhibition via the de novo NAD+ biosynthesis pathway and NAMPT mutation.

Guo J, Lam LT, Longenecker KL, Bui MH, Idler KB, Glaser KB, Wilsbacher JL, Tse C, Pappano WN, Huang TH.

Biochem Biophys Res Commun. 2017 Sep 23;491(3):681-686. doi: 10.1016/j.bbrc.2017.07.143. Epub 2017 Jul 26.

PMID:
28756225
2.

JAK2V617F drives Mcl-1 expression and sensitizes hematologic cell lines to dual inhibition of JAK2 and Bcl-xL.

Guo J, Roberts L, Chen Z, Merta PJ, Glaser KB, Shah OJ.

PLoS One. 2015 Mar 17;10(3):e0114363. doi: 10.1371/journal.pone.0114363. eCollection 2015.

3.

Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families.

Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH, Chen Z, Frey RR, Johnson EF, Osterling DJ, Olson AM, Bouska JJ, Luo Y, Curtin ML, Donawho CK, Michaelides MR, Tse C, Davidsen SK, Albert DH.

J Pharmacol Exp Ther. 2012 Dec;343(3):617-27. doi: 10.1124/jpet.112.197087. Epub 2012 Aug 30.

PMID:
22935731
4.

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

Ji Z, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Soni NB, Magoc TJ, Stewart KD, Wei RQ, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4528-31. doi: 10.1016/j.bmcl.2012.05.125. Epub 2012 Jun 7.

PMID:
22727637
5.

Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.

Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR, Bouska JJ, Montgomery DA, Palma JP, Donawho CK, Stewart KD, Tse C, Michaelides MR.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5. doi: 10.1016/j.bmcl.2012.05.067. Epub 2012 May 26.

PMID:
22695126
6.

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

Curtin ML, Frey RR, Heyman HR, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Magoc TJ, Tapang P, Albert DH, Osterling DJ, Olson AM, Bouska JJ, Guan Z, Preusser LC, Polakowski JS, Stewart KD, Tse C, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2012 May 1;22(9):3208-12. doi: 10.1016/j.bmcl.2012.03.035. Epub 2012 Mar 14.

PMID:
22465635
7.

1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): a cautionary note on the anticancer mechanism of an eEF2 kinase inhibitor.

Chen Z, Gopalakrishnan SM, Bui MH, Soni NB, Warrior U, Johnson EF, Donnelly JB, Glaser KB.

J Biol Chem. 2011 Dec 23;286(51):43951-8. doi: 10.1074/jbc.M111.301291. Epub 2011 Oct 21.

8.

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases.

McClellan WJ, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Magoc TJ, Marcotte PA, Osterling DJ, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5620-4. doi: 10.1016/j.bmcl.2011.06.041. Epub 2011 Jun 29.

PMID:
21778056
9.

The multitargeted receptor tyrosine kinase inhibitor linifanib (ABT-869) induces apoptosis through an Akt and glycogen synthase kinase 3β-dependent pathway.

Hernandez-Davies JE, Zape JP, Landaw EM, Tan X, Presnell A, Griffith D, Heinrich MC, Glaser KB, Sakamoto KM.

Mol Cancer Ther. 2011 Jun;10(6):949-59. doi: 10.1158/1535-7163.MCT-10-0904. Epub 2011 Apr 6.

10.

Cyanobacterial Microcystis aeruginosa lipopolysaccharide elicits release of superoxide anion, thromboxane B₂, cytokines, chemokines, and matrix metalloproteinase-9 by rat microglia.

Mayer AM, Clifford JA, Aldulescu M, Frenkel JA, Holland MA, Hall ML, Glaser KB, Berry J.

Toxicol Sci. 2011 May;121(1):63-72. doi: 10.1093/toxsci/kfr045. Epub 2011 Feb 28.

PMID:
21362633
11.

Bcl-XL represents a druggable molecular vulnerability during aurora B inhibitor-mediated polyploidization.

Shah OJ, Lin X, Li L, Huang X, Li J, Anderson MG, Tang H, Rodriguez LE, Warder SE, McLoughlin S, Chen J, Palma J, Glaser KB, Donawho CK, Fesik SW, Shen Y.

Proc Natl Acad Sci U S A. 2010 Jul 13;107(28):12634-9. doi: 10.1073/pnas.0913615107. Epub 2010 Jun 28.

12.

The odyssey of marine pharmaceuticals: a current pipeline perspective.

Mayer AM, Glaser KB, Cuevas C, Jacobs RS, Kem W, Little RD, McIntosh JM, Newman DJ, Potts BC, Shuster DE.

Trends Pharmacol Sci. 2010 Jun;31(6):255-65. doi: 10.1016/j.tips.2010.02.005. Epub 2010 Apr 2. Review.

PMID:
20363514
13.

ABT-869 inhibits the proliferation of Ewing Sarcoma cells and suppresses platelet-derived growth factor receptor beta and c-KIT signaling pathways.

Ikeda AK, Judelson DR, Federman N, Glaser KB, Landaw EM, Denny CT, Sakamoto KM.

Mol Cancer Ther. 2010 Mar;9(3):653-60. doi: 10.1158/1535-7163.MCT-09-0812. Epub 2010 Mar 2.

14.

A renaissance in marine pharmacology: from preclinical curiosity to clinical reality.

Glaser KB, Mayer AM.

Biochem Pharmacol. 2009 Sep 1;78(5):440-8. doi: 10.1016/j.bcp.2009.04.015. Epub 2009 Apr 22.

PMID:
19393227
15.

Identification of genes that confer tumor cell resistance to the aurora B kinase inhibitor, AZD1152.

Guo J, Anderson MG, Tapang P, Palma JP, Rodriguez LE, Niquette A, Li J, Bouska JJ, Wang G, Semizarov D, Albert DH, Donawho CK, Glaser KB, Shah OJ.

Pharmacogenomics J. 2009 Apr;9(2):90-102. doi: 10.1038/tpj.2008.20. Epub 2009 Feb 3.

PMID:
19188929
16.

Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML.

Zhou J, Bi C, Janakakumara JV, Liu SC, Chng WJ, Tay KG, Poon LF, Xie Z, Palaniyandi S, Yu H, Glaser KB, Albert DH, Davidsen SK, Chen CS.

Blood. 2009 Apr 23;113(17):4052-62. doi: 10.1182/blood-2008-05-156422. Epub 2009 Jan 14.

PMID:
19144991
17.

Inhibition of Aurora B kinase sensitizes a subset of human glioma cells to TRAIL concomitant with induction of TRAIL-R2.

Li J, Anderson MG, Tucker LA, Shen Y, Glaser KB, Shah OJ.

Cell Death Differ. 2009 Mar;16(3):498-511. doi: 10.1038/cdd.2008.174. Epub 2008 Dec 12.

18.

ABT-869, a multi-targeted tyrosine kinase inhibitor, in combination with rapamycin is effective for subcutaneous hepatocellular carcinoma xenograft.

Jasinghe VJ, Xie Z, Zhou J, Khng J, Poon LF, Senthilnathan P, Glaser KB, Albert DH, Davidsen SK, Chen CS.

J Hepatol. 2008 Dec;49(6):985-97. doi: 10.1016/j.jhep.2008.08.010. Epub 2008 Oct 1.

PMID:
18930332
19.

7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.

Frey RR, Curtin ML, Albert DH, Glaser KB, Pease LJ, Soni NB, Bouska JJ, Reuter D, Stewart KD, Marcotte P, Bukofzer G, Li J, Davidsen SK, Michaelides MR.

J Med Chem. 2008 Jul 10;51(13):3777-87. doi: 10.1021/jm701397k. Epub 2008 Jun 17.

PMID:
18557606
20.

Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.

Gracias V, Ji Z, Akritopoulou-Zanze I, Abad-Zapatero C, Huth JR, Song D, Hajduk PJ, Johnson EF, Glaser KB, Marcotte PA, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR, Djuric SW.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2691-5. doi: 10.1016/j.bmcl.2008.03.021. Epub 2008 Mar 10.

PMID:
18362070
21.

3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.

Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Diaz G, Glaser KB, Guo J, Harris CM, Li J, Marcotte PA, Moskey MD, Oie T, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR.

J Med Chem. 2008 Mar 13;51(5):1231-41. doi: 10.1021/jm701096v. Epub 2008 Feb 9.

PMID:
18260617
22.

In vivo activity of ABT-869, a multi-target kinase inhibitor, against acute myeloid leukemia with wild-type FLT3 receptor.

Zhou J, Khng J, Jasinghe VJ, Bi C, Neo CH, Pan M, Poon LF, Xie Z, Yu H, Yeoh AE, Lu Y, Glaser KB, Albert DH, Davidsen SK, Chen CS.

Leuk Res. 2008 Jul;32(7):1091-100. Epub 2007 Dec 26.

PMID:
18160102
23.

Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.

Dai Y, Hartandi K, Soni NB, Pease LJ, Reuter DR, Olson AM, Osterling DJ, Doktor SZ, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):386-90. Epub 2007 Oct 17.

PMID:
18023347
24.

Differential response of p53 and p21 on HDAC inhibitor-mediated apoptosis in HCT116 colon cancer cells in vitro and in vivo.

Zopf S, Neureiter D, Bouralexis S, Abt T, Glaser KB, Okamoto K, Ganslmayer M, Hahn EG, Herold C, Ocker M.

Int J Oncol. 2007 Dec;31(6):1391-402.

PMID:
17982666
25.

Synergistic antileukemic effects between ABT-869 and chemotherapy involve downregulation of cell cycle-regulated genes and c-Mos-mediated MAPK pathway.

Zhou J, Pan M, Xie Z, Loh SL, Bi C, Tai YC, Lilly M, Lim YP, Han JH, Glaser KB, Albert DH, Davidsen SK, Chen CS.

Leukemia. 2008 Jan;22(1):138-46. Epub 2007 Oct 18.

PMID:
17943175
26.

G1P3, an IFN-induced survival factor, antagonizes TRAIL-induced apoptosis in human myeloma cells.

Cheriyath V, Glaser KB, Waring JF, Baz R, Hussein MA, Borden EC.

J Clin Invest. 2007 Oct;117(10):3107-17.

27.

HDAC inhibitors: clinical update and mechanism-based potential.

Glaser KB.

Biochem Pharmacol. 2007 Sep 1;74(5):659-71. Epub 2007 Apr 7.

PMID:
17498667
28.

Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

Dai Y, Hartandi K, Ji Z, Ahmed AA, Albert DH, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Harris CM, Hickman D, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Martin RL, Olson AM, Osterling DJ, Pease LJ, Soni NB, Stewart KD, Stoll VS, Tapang P, Reuter DR, Davidsen SK, Michaelides MR.

J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.

PMID:
17343372
29.

ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia.

Shankar DB, Li J, Tapang P, Owen McCall J, Pease LJ, Dai Y, Wei RQ, Albert DH, Bouska JJ, Osterling DJ, Guo J, Marcotte PA, Johnson EF, Soni N, Hartandi K, Michaelides MR, Davidsen SK, Priceman SJ, Chang JC, Rhodes K, Shah N, Moore TB, Sakamoto KM, Glaser KB.

Blood. 2007 Apr 15;109(8):3400-8. Epub 2007 Jan 5.

30.

Thienopyridine urea inhibitors of KDR kinase.

Heyman HR, Frey RR, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Yates M, Bouska JJ, Albert DH, Black-Schaefer CL, Dandliker PJ, Stewart KD, Rafferty P, Davidsen SK, Michaelides MR, Curtin ML.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1246-9. Epub 2006 Dec 9.

PMID:
17188869
31.

Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.

Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Moskey MD, Pease LJ, Stewart KD, Yates M, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4326-30. Epub 2006 Jun 2.

PMID:
16735117
32.

Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors.

Guo J, Marcotte PA, McCall JO, Dai Y, Pease LJ, Michaelides MR, Davidsen SK, Glaser KB.

Mol Cancer Ther. 2006 Apr;5(4):1007-13.

33.

Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor.

Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS, Wang B, Bukofzer GT, Wang YC, Stavropoulos JA, Hartandi K, Niquette AL, Soni N, Johnson EF, McCall JO, Bouska JJ, Luo Y, Donawho CK, Dai Y, Marcotte PA, Glaser KB, Michaelides MR, Davidsen SK.

Mol Cancer Ther. 2006 Apr;5(4):995-1006.

34.
35.

Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.

Dai Y, Guo Y, Frey RR, Ji Z, Curtin ML, Ahmed AA, Albert DH, Arnold L, Arries SS, Barlozzari T, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Pease LJ, Stewart KD, Stoll VS, Tapang P, Wishart N, Davidsen SK, Michaelides MR.

J Med Chem. 2005 Sep 22;48(19):6066-83.

PMID:
16162008
36.

Differential protein acetylation induced by novel histone deacetylase inhibitors.

Glaser KB, Li J, Pease LJ, Staver MJ, Marcotte PA, Guo J, Frey RR, Garland RB, Heyman HR, Wada CK, Vasudevan A, Michaelides MR, Davidsen SK, Curtin ML.

Biochem Biophys Res Commun. 2004 Dec 17;325(3):683-90.

PMID:
15541343
37.

Isoindolinone ureas: a novel class of KDR kinase inhibitors.

Curtin ML, Frey RR, Heyman HR, Sarris KA, Steinman DH, Holmes JH, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Pease LJ, Glaser KB, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4505-9.

PMID:
15357981
38.

Fluorescence assay of SIRT protein deacetylases using an acetylated peptide substrate and a secondary trypsin reaction.

Marcotte PA, Richardson PL, Guo J, Barrett LW, Xu N, Gunasekera A, Glaser KB.

Anal Biochem. 2004 Sep 1;332(1):90-9. Erratum in: Anal Biochem. 2006 Mar 15;350(2):316. Richardson, Paul R [corrected to Richardson, Paul L].

PMID:
15301953
39.

Expression and functional characterization of recombinant human HDAC1 and HDAC3.

Li J, Staver MJ, Curtin ML, Holms JH, Frey RR, Edalji R, Smith R, Michaelides MR, Davidsen SK, Glaser KB.

Life Sci. 2004 Apr 16;74(22):2693-705.

PMID:
15043985
40.

Heterocyclic ketones as inhibitors of histone deacetylase.

Vasudevan A, Ji Z, Frey RR, Wada CK, Steinman D, Heyman HR, Guo Y, Curtin ML, Guo J, Li J, Pease L, Glaser KB, Marcotte PA, Bouska JJ, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.

PMID:
14592473
41.

A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.

Dai Y, Guo Y, Curtin ML, Li J, Pease LJ, Guo J, Marcotte PA, Glaser KB, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Nov 3;13(21):3817-20.

PMID:
14552787
42.

Role of class I and class II histone deacetylases in carcinoma cells using siRNA.

Glaser KB, Li J, Staver MJ, Wei RQ, Albert DH, Davidsen SK.

Biochem Biophys Res Commun. 2003 Oct 17;310(2):529-36.

PMID:
14521942
43.

Alpha-keto amides as inhibitors of histone deacetylase.

Wada CK, Frey RR, Ji Z, Curtin ML, Garland RB, Holms JH, Li J, Pease LJ, Guo J, Glaser KB, Marcotte PA, Richardson PL, Murphy SS, Bouska JJ, Tapang P, Magoc TJ, Albert DH, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.

PMID:
12951120
44.

Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.

Dai Y, Guo Y, Guo J, Pease LJ, Li J, Marcotte PA, Glaser KB, Tapang P, Albert DH, Richardson PL, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1897-901.

PMID:
12749893
45.
46.

Transforming growth factor beta mimetics: discovery of 7-[4-(4-cyanophenyl)phenoxy]-heptanohydroxamic acid, a biaryl hydroxamate inhibitor of histone deacetylase.

Glaser KB, Li J, Aakre ME, Morgan DW, Sheppard G, Stewart KD, Pollock J, Lee P, O'Connor CZ, Anderson SN, Mussatto DJ, Wegner CW, Moses HL.

Mol Cancer Ther. 2002 Aug;1(10):759-68.

47.

Trifluoromethyl ketones as inhibitors of histone deacetylase.

Frey RR, Wada CK, Garland RB, Curtin ML, Michaelides MR, Li J, Pease LJ, Glaser KB, Marcotte PA, Bouska JJ, Murphy SS, Davidsen SK.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.

PMID:
12419380
48.

Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).

Curtin ML, Garland RB, Heyman HR, Frey RR, Michaelides MR, Li J, Pease LJ, Glaser KB, Marcotte PA, Davidsen SK.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2919-23.

PMID:
12270175

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