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Items: 1 to 50 of 51

1.

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
2.

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
3.

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
4.

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
5.

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
6.

Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.

Tong Y, Bouska JJ, Ellis PA, Johnson EF, Leverson J, Liu X, Marcotte PA, Olson AM, Osterling DJ, Przytulinska M, Rodriguez LE, Shi Y, Soni N, Stavropoulos J, Thomas S, Donawho CK, Frost DJ, Luo Y, Giranda VL, Penning TD.

J Med Chem. 2009 Nov 12;52(21):6803-13. doi: 10.1021/jm900697r.

PMID:
19888760
7.

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
8.

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
9.

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
10.

1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.

Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ.

J Med Chem. 2007 May 3;50(9):2011-29. Epub 2007 Apr 11.

PMID:
17425296
11.

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
12.

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.

13.

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
14.

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
15.

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.

16.

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.

17.

High-level bacterial expression and purification of human SirT2 protein for NMR studies.

Sun C, Song D, Marcotte PA, Richardson PL, Hajduk PJ.

Protein Expr Purif. 2006 Jul;48(1):56-60. Epub 2006 Jan 10.

PMID:
16442310
18.

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
19.

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
20.

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
21.

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
22.

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
23.

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
24.

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
25.

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
26.

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
27.

Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.

Wada CK, Holms JH, Curtin ML, Dai Y, Florjancic AS, Garland RB, Guo Y, Heyman HR, Stacey JR, Steinman DH, Albert DH, Bouska JJ, Elmore IN, Goodfellow CL, Marcotte PA, Tapang P, Morgan DW, Michaelides MR, Davidsen SK.

J Med Chem. 2002 Jan 3;45(1):219-32.

PMID:
11754593
28.

Characterization of matrix metalloproteinase inhibitors: enzymatic assays.

Marcotte PA, Davidsen SK.

Curr Protoc Pharmacol. 2001 Aug;Chapter 3:Unit3.7. doi: 10.1002/0471141755.ph0307s13.

PMID:
21959756
29.

Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.

Curtin ML, Florjancic AS, Heyman HR, Michaelides MR, Garland RB, Holms JH, Steinman DH, Dellaria JF, Gong J, Wada CK, Guo Y, Elmore IB, Tapang P, Albert DH, Magoc TJ, Marcotte PA, Bouska JJ, Goodfellow CL, Bauch JL, Marsh KC, Morgan DW, Davidsen SK.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1557-60.

PMID:
11412980
30.

Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.

Michaelides MR, Dellaria JF, Gong J, Holms JH, Bouska JJ, Stacey J, Wada CK, Heyman HR, Curtin ML, Guo Y, Goodfellow CL, Elmore IB, Albert DH, Magoc TJ, Marcotte PA, Morgan DW, Davidsen SK.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1553-6.

PMID:
11412979
31.

Evaluation of the inhibition of other metalloproteinases by matrix metalloproteinase inhibitors.

Marcotte PA, Elmore IN, Guan Z, Magoc TJ, Albert DH, Morgand DW, Curtin ML, Garland RB, Guo Y, Heyman HR, Holms JH, Sheppard GS, Steinman DH, Wada CK, Davidsen SK.

J Enzyme Inhib. 1999;14(6):425-35.

PMID:
10536876
32.

Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.

Sheppard GS, Florjancic AS, Giesler JR, Xu L, Guo Y, Davidsen SK, Marcotte PA, Elmore I, Albert DH, Magoc TJ, Bouska JJ, Goodfellow CL, Morgan DW, Summers JB.

Bioorg Med Chem Lett. 1998 Nov 17;8(22):3251-6.

PMID:
9873712
33.

The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.

Steinman DH, Curtin ML, Garland RB, Davidsen SK, Heyman HR, Holms JH, Albert DH, Magoc TJ, Nagy IB, Marcotte PA, Li J, Morgan DW, Hutchins C, Summers JB.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2087-92.

PMID:
9873491
34.

Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.

Curtin ML, Garland RB, Davidsen SK, Marcotte PA, Albert DH, Magoc TJ, Hutchins C.

Bioorg Med Chem Lett. 1998 Jun 16;8(12):1443-8.

PMID:
9873367
35.

Characterization of the activation of pro-urokinase by thermolysin.

Marcotte PA, Henkin J.

Biochim Biophys Acta. 1993 Jan 15;1161(1):105-12.

PMID:
8422417
36.
37.

Synthesis of 2,2-dimethyl-4-hydroxy-4-androstene-3,17-dione as an inhibitor of aromatase.

Furth PS, Rosenberger J, Marcotte PA, Robinson CH.

J Enzyme Inhib. 1990;4(2):131-5.

PMID:
2098519
38.

Pure human inactive renin. Evidence that native inactive renin is prorenin.

Higashimori K, Mizuno K, Nakajo S, Boehm FH, Marcotte PA, Egan DA, Holleman WH, Heusser C, Poisner AM, Inagami T.

J Biol Chem. 1989 Sep 5;264(25):14662-7.

39.

Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.

Plattner JJ, Marcotte PA, Kleinert HD, Stein HH, Greer J, Bolis G, Fung AK, Bopp BA, Luly JR, Sham HL, et al.

J Med Chem. 1988 Dec;31(12):2277-88.

PMID:
3143010
40.

Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency.

Luly JR, BaMaung N, Soderquist J, Fung AK, Stein H, Kleinert HD, Marcotte PA, Egan DA, Bopp B, Merits I, et al.

J Med Chem. 1988 Dec;31(12):2264-76.

PMID:
3143009
41.

Human placental chorionic renin: production, purification and characterization.

Egan DA, Grzegorczyk V, Tricarico KA, Rueter A, Holleman WH, Marcotte PA.

Biochim Biophys Acta. 1988 Apr 14;965(1):68-75.

PMID:
3280035
42.

Renin inhibitors. Improvements in the stability and biological activity of small peptides containing novel Leu-Val replacements.

Kleinert HD, Luly JR, Marcotte PA, Perun TJ, Plattner JJ, Stein H.

FEBS Lett. 1988 Mar 28;230(1-2):38-42.

43.

Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.

Sham HL, Bolis G, Stein HH, Fesik SW, Marcotte PA, Plattner JJ, Rempel CA, Greer J.

J Med Chem. 1988 Feb;31(2):284-95.

PMID:
3276890
44.

Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.

Bolis G, Fung AK, Greer J, Kleinert HD, Marcotte PA, Perun TJ, Plattner JJ, Stein HH.

J Med Chem. 1987 Oct;30(10):1729-37.

PMID:
3309313
45.

Novel renin inhibitors containing analogues of statine retro-inverted at the C-termini: specificity at the P2 histidine site.

Rosenberg SH, Plattner JJ, Woods KW, Stein HH, Marcotte PA, Cohen J, Perun TJ.

J Med Chem. 1987 Jul;30(7):1224-8.

PMID:
3298652
46.

Modified peptides which display potent and specific inhibition of human renin.

Luly JR, Plattner JJ, Stein H, Yi N, Soderquist J, Marcotte PA, Kleinert HD, Perun TJ.

Biochem Biophys Res Commun. 1987 Feb 27;143(1):44-51.

PMID:
3548726
47.

Design of mechanism-based inactivators of human placental aromatase.

Marcotte PA, Robinson CH.

Cancer Res. 1982 Aug;42(8 Suppl):3322s-3326s.

48.

Inhibition and inactivation of estrogen synthetase (aromatase) by fluorinated substrate analogues.

Marcotte PA, Robinson CH.

Biochemistry. 1982 May 25;21(11):2773-8.

PMID:
7093221
49.

Synthesis and evaluation of 10 beta-substituted 4-estrene-3, 17-diones as inhibitors of human placental microsomal aromatase.

Marcotte PA, Robinson CH.

Steroids. 1982 Mar;39(3):325-44. No abstract available.

PMID:
7090028
50.

Inactivation of aromatase in vitro by 4-hydroxy-4-androstene-3,17-dione and 4-acetoxy-4-androstene-3,17-dione and sustained effects in vivo.

Brodie AM, Garrett WM, Hendrickson JR, Tsai-Morris CH, Marcotte PA, Robinson CH.

Steroids. 1981 Dec;38(6):693-702.

PMID:
7336466

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