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Items: 1 to 50 of 55

1.

Adventures in public data.

Zaharevitz DW.

J Cheminform. 2011 Oct 14;3:34. doi: 10.1186/1758-2946-3-34.

2.

Identification of small-molecule inhibitors of the colorectal cancer oncogene Krüppel-like factor 5 expression by ultrahigh-throughput screening.

Bialkowska AB, Crisp M, Bannister T, He Y, Chowdhury S, Schürer S, Chase P, Spicer T, Madoux F, Tian C, Hodder P, Zaharevitz D, Yang VW.

Mol Cancer Ther. 2011 Nov;10(11):2043-51. doi: 10.1158/1535-7163.MCT-11-0550. Epub 2011 Sep 1.

3.

RSK2 Binding Models Delineate Key Features for Activity.

Gussio R, Currens MJ, Scudiero DA, Smith JA, Lannigan DA, Shoemaker RH, Zaharevitz DW, Nguyen TL.

J Chem Pharm Res. 2010;2(5):587-598.

4.

Anticancer activity of BIM-46174, a new inhibitor of the heterotrimeric Galpha/Gbetagamma protein complex.

Prévost GP, Lonchampt MO, Holbeck S, Attoub S, Zaharevitz D, Alley M, Wright J, Brezak MC, Coulomb H, Savola A, Huchet M, Chaumeron S, Nguyen QD, Forgez P, Bruyneel E, Bracke M, Ferrandis E, Roubert P, Demarquay D, Gespach C, Kasprzyk PG.

Cancer Res. 2006 Sep 15;66(18):9227-34.

5.

Homology model of RSK2 N-terminal kinase domain, structure-based identification of novel RSK2 inhibitors, and preliminary common pharmacophore.

Nguyen TL, Gussio R, Smith JA, Lannigan DA, Hecht SM, Scudiero DA, Shoemaker RH, Zaharevitz DW.

Bioorg Med Chem. 2006 Sep 1;14(17):6097-105. Epub 2006 May 24.

PMID:
16723234
6.

A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach.

Nguyen TL, McGrath C, Hermone AR, Burnett JC, Zaharevitz DW, Day BW, Wipf P, Hamel E, Gussio R.

J Med Chem. 2005 Sep 22;48(19):6107-16. Erratum in: J Med Chem. 2005 Dec 1;48(24):7917.

PMID:
16162011
7.

Epoxide-containing side chains enhance antiproliferative activity of paullones.

Xie X, Lemcke T, Gussio R, Zaharevitz DW, Leost M, Meijer L, Kunick C.

Eur J Med Chem. 2005 Jul;40(7):655-61. Epub 2005 Apr 7.

PMID:
15935900
8.

An all-atom model of the pore-like structure of hexameric VP40 from Ebola: structural insights into the monomer-hexamer transition.

Nguyen TL, Schoehn G, Weissenhorn W, Hermone AR, Burnett JC, Panchal RG, McGrath C, Zaharevitz DW, Aman MJ, Gussio R, Bavari S.

J Struct Biol. 2005 Jul;151(1):30-40.

PMID:
15908231
9.

Homology model of the CDK1/cyclin B complex.

McGrath CF, Pattabiraman N, Kellogg GE, Lemcke T, Kunick C, Sausville EA, Zaharevitz DW, Gussio R.

J Biomol Struct Dyn. 2005 Apr;22(5):493-502.

PMID:
15702922
10.

Structure-aided optimization of kinase inhibitors derived from alsterpaullone.

Kunick C, Zeng Z, Gussio R, Zaharevitz D, Leost M, Totzke F, Schächtele C, Kubbutat MH, Meijer L, Lemcke T.

Chembiochem. 2005 Mar;6(3):541-9.

PMID:
15696597
11.

Conformational sampling of the botulinum neurotoxin serotype A light chain: implications for inhibitor binding.

Burnett JC, Schmidt JJ, McGrath CF, Nguyen TL, Hermone AR, Panchal RG, Vennerstrom JL, Kodukula K, Zaharevitz DW, Gussio R, Bavari S.

Bioorg Med Chem. 2005 Jan 17;13(2):333-41.

PMID:
15598556
12.

Models for evaluating agents intended for the prophylaxis, mitigation and treatment of radiation injuries. Report of an NCI Workshop, December 3-4, 2003.

Stone HB, Moulder JE, Coleman CN, Ang KK, Anscher MS, Barcellos-Hoff MH, Dynan WS, Fike JR, Grdina DJ, Greenberger JS, Hauer-Jensen M, Hill RP, Kolesnick RN, Macvittie TJ, Marks C, McBride WH, Metting N, Pellmar T, Purucker M, Robbins ME, Schiestl RH, Seed TM, Tomaszewski JE, Travis EL, Wallner PE, Wolpert M, Zaharevitz D.

Radiat Res. 2004 Dec;162(6):711-28.

PMID:
15548121
13.

Poly(ethylene glycol) prodrugs of the CDK inhibitor, alsterpaullone (NSC 705701): synthesis and pharmacokinetic studies.

Greenwald RB, Zhao H, Xia J, Wu D, Nervi S, Stinson SF, Majerova E, Bramhall C, Zaharevitz DW.

Bioconjug Chem. 2004 Sep-Oct;15(5):1076-83.

PMID:
15366962
14.

CDK1-inhibitory activity of paullones depends on electronic properties of 9-substituents.

Pies T, Schaper KJ, Leost M, Zaharevitz DW, Gussio R, Meijer L, Kunicke C.

Arch Pharm (Weinheim). 2004 Sep;337(9):486-92.

PMID:
15362121
15.

Identification of small molecule inhibitors of anthrax lethal factor.

Panchal RG, Hermone AR, Nguyen TL, Wong TY, Schwarzenbacher R, Schmidt J, Lane D, McGrath C, Turk BE, Burnett J, Aman MJ, Little S, Sausville EA, Zaharevitz DW, Cantley LC, Liddington RC, Gussio R, Bavari S.

Nat Struct Mol Biol. 2004 Jan;11(1):67-72. Epub 2003 Dec 29.

PMID:
14718925
16.

Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.

Kunick C, Lauenroth K, Wieking K, Xie X, Schultz C, Gussio R, Zaharevitz D, Leost M, Meijer L, Weber A, Jørgensen FS, Lemcke T.

J Med Chem. 2004 Jan 1;47(1):22-36.

PMID:
14695817
17.

Novel small molecule inhibitors of botulinum neurotoxin A metalloprotease activity.

Burnett JC, Schmidt JJ, Stafford RG, Panchal RG, Nguyen TL, Hermone AR, Vennerstrom JL, McGrath CF, Lane DJ, Sausville EA, Zaharevitz DW, Gussio R, Bavari S.

Biochem Biophys Res Commun. 2003 Oct 10;310(1):84-93.

PMID:
14511652
18.

Correlation of nucleoside and nucleobase transporter gene expression with antimetabolite drug cytotoxicity.

Lu X, Gong S, Monks A, Zaharevitz D, Moscow JA.

J Exp Ther Oncol. 2002 Jul-Aug;2(4):200-12.

PMID:
12416024
19.

Synthesis of paullones with aminoalkyl side chains.

Wieking K, Knockaert M, Leost M, Zaharevitz DW, Meijer L, Kunick C.

Arch Pharm (Weinheim). 2002 Jul;335(7):311-7.

PMID:
12207280
20.

Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors.

Lazo JS, Nemoto K, Pestell KE, Cooley K, Southwick EC, Mitchell DA, Furey W, Gussio R, Zaharevitz DW, Joo B, Wipf P.

Mol Pharmacol. 2002 Apr;61(4):720-8.

PMID:
11901209
21.

COMPARE: a web accessible tool for investigating mechanisms of cell growth inhibition.

Zaharevitz DW, Holbeck SL, Bowerman C, Svetlik PA.

J Mol Graph Model. 2002 Jan;20(4):297-303.

PMID:
11858638
22.

Synthesis and biological evaluation of 12,13-cyclopropyl and 12,13-cyclobutyl epothilones.

Nicolaou KC, Namoto K, Li J, Ritzén A, Ulven T, Shoji M, Zaharevitz D, Gussio R, Sackett DL, Ward RD, Hensler A, Fojo T, Giannakakou P.

Chembiochem. 2001 Jan 8;2(1):69-75. No abstract available.

PMID:
11828429
23.

Relationships between drug activity in NCI preclinical in vitro and in vivo models and early clinical trials.

Johnson JI, Decker S, Zaharevitz D, Rubinstein LV, Venditti JM, Schepartz S, Kalyandrug S, Christian M, Arbuck S, Hollingshead M, Sausville EA.

Br J Cancer. 2001 May 18;84(10):1424-31.

24.

Chemical synthesis and biological properties of pyridine epothilones.

Nicolaou KC, Scarpelli R, Bollbuck B, Werschkun B, Pereira MM, Wartmann M, Altmann KH, Zaharevitz D, Gussio R, Giannakakou P.

Chem Biol. 2000 Aug;7(8):593-9.

25.

Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.

Leost M, Schultz C, Link A, Wu YZ, Biernat J, Mandelkow EM, Bibb JA, Snyder GL, Greengard P, Zaharevitz DW, Gussio R, Senderowicz AM, Sausville EA, Kunick C, Meijer L.

Eur J Biochem. 2000 Oct;267(19):5983-94.

26.

Inhibition of CDKs as a therapeutic modality.

Sausville EA, Johnson J, Alley M, Zaharevitz D, Senderowicz AM.

Ann N Y Acad Sci. 2000 Jun;910:207-21; discussion 221-2.

PMID:
10911915
27.

Structure-based design modifications of the paullone molecular scaffold for cyclin-dependent kinase inhibition.

Gussio R, Zaharevitz DW, McGrath CF, Pattabiraman N, Kellogg GE, Schultz C, Link A, Kunick C, Leost M, Meijer L, Sausville EA.

Anticancer Drug Des. 2000 Feb;15(1):53-66.

PMID:
10888036
28.

2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.

Kunick C, Schultz C, Lemcke T, Zaharevitz DW, Gussio R, Jalluri RK, Sausville EA, Leost M, Meijer L.

Bioorg Med Chem Lett. 2000 Mar 20;10(6):567-9.

PMID:
10741555
29.

A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells.

Giannakakou P, Gussio R, Nogales E, Downing KH, Zaharevitz D, Bollbuck B, Poy G, Sackett D, Nicolaou KC, Fojo T.

Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9.

30.

Cyclin-dependent kinases: initial approaches to exploit a novel therapeutic target.

Sausville EA, Zaharevitz D, Gussio R, Meijer L, Louarn-Leost M, Kunick C, Schultz R, Lahusen T, Headlee D, Stinson S, Arbuck SG, Senderowicz A.

Pharmacol Ther. 1999 May-Jun;82(2-3):285-92. Review.

PMID:
10454206
31.

Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.

Schultz C, Link A, Leost M, Zaharevitz DW, Gussio R, Sausville EA, Meijer L, Kunick C.

J Med Chem. 1999 Jul 29;42(15):2909-19.

PMID:
10425100
32.

Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases.

Zaharevitz DW, Gussio R, Leost M, Senderowicz AM, Lahusen T, Kunick C, Meijer L, Sausville EA.

Cancer Res. 1999 Jun 1;59(11):2566-9.

33.

Antitumor pyrido[3,2-d][1]benzazepines: synthesis and in vitro activity of thiophene analogs.

Link A, Zaharevitz DW, Kunick C.

Pharmazie. 1999 Mar;54(3):163-6.

PMID:
10192102
34.
35.

An information-intensive approach to the molecular pharmacology of cancer.

Weinstein JN, Myers TG, O'Connor PM, Friend SH, Fornace AJ Jr, Kohn KW, Fojo T, Bates SE, Rubinstein LV, Anderson NL, Buolamwini JK, van Osdol WW, Monks AP, Scudiero DA, Sausville EA, Zaharevitz DW, Bunow B, Viswanadhan VN, Johnson GS, Wittes RE, Paull KD.

Science. 1997 Jan 17;275(5298):343-9.

PMID:
8994024
36.

Evaluation of selected chemotypes in coupled cellular and molecular target-based screens identifies novel HIV-1 zinc finger inhibitors.

Rice WG, Turpin JA, Schaeffer CA, Graham L, Clanton D, Buckheit RW Jr, Zaharevitz D, Summers MF, Wallqvist A, Covell DG.

J Med Chem. 1996 Sep 13;39(19):3606-16.

PMID:
8809151
37.

Identification of a novel inhibitor (NSC 665564) of dihydroorotate dehydrogenase with a potency equivalent to brequinar.

Cleaveland ES, Zaharevitz DW, Kelley JA, Paull K, Cooney DA, Ford H Jr.

Biochem Biophys Res Commun. 1996 Jun 25;223(3):654-9.

PMID:
8687451
38.

All-atom models for the non-nucleoside binding site of HIV-1 reverse transcriptase complexed with inhibitors: a 3D QSAR approach.

Gussio R, Pattabiraman N, Zaharevitz DW, Kellogg GE, Topol IA, Rice WG, Schaeffer CA, Erickson JW, Burt SK.

J Med Chem. 1996 Apr 12;39(8):1645-50.

PMID:
8648604
39.

Site of action of two novel pyrimidine biosynthesis inhibitors accurately predicted by the compare program.

Cleaveland ES, Monks A, Vaigro-Wolff A, Zaharevitz DW, Paull K, Ardalan K, Cooney DA, Ford H Jr.

Biochem Pharmacol. 1995 Mar 30;49(7):947-54.

PMID:
7741767
40.

Cyclopentenyl uracil: an effective inhibitor of uridine salvage in vivo.

Cysyk RL, Malinowski N, Marquez V, Zaharevitz D, August EM, Moyer JD.

Biochem Pharmacol. 1995 Jan 18;49(2):203-7.

PMID:
7840797
41.

The discovery of novel, structurally diverse protein kinase C agonists through computer 3D-database pharmacophore search. Molecular modeling studies.

Wang S, Zaharevitz DW, Sharma R, Marquez VE, Lewin NE, Du L, Blumberg PM, Milne GW.

J Med Chem. 1994 Dec 23;37(26):4479-89.

PMID:
7799398
42.

National Cancer Institute Drug Information System 3D database.

Milne GW, Nicklaus MC, Driscoll JS, Wang S, Zaharevitz D.

J Chem Inf Comput Sci. 1994 Sep-Oct;34(5):1219-24.

PMID:
7962217
43.

Vanadate inhibition of hyaluronic acid synthesis in Swiss 3T3 fibroblasts.

Zaharevitz DW, Chisena CA, Duncan KL, August EM, Cysyk RL.

Biochem Mol Biol Int. 1993 Nov;31(4):627-33.

PMID:
7507761
44.

Chem-X and CAMBRIDGE. Comparison of computer generated chemical structures with X-ray crystallographic data.

Nicklaus MC, Milne GW, Zaharevitz D.

J Chem Inf Comput Sci. 1993 Jul-Aug;33(4):639-46.

PMID:
8366147
45.

Effect of high-protein diet on pyrimidine synthesis and response to PALA in mouse tissues.

Zaharevitz DW, Grubb MF, Hyman R, Chisena C, Cysyk RL.

J Natl Cancer Inst. 1993 Apr 21;85(8):662-6.

PMID:
8468725
46.

Contribution of de-novo and salvage synthesis to the uracil nucleotide pool in mouse tissues and tumors in vivo.

Zaharevitz DW, Anderson LW, Malinowski NM, Hyman R, Strong JM, Cysyk RL.

Eur J Biochem. 1992 Nov 15;210(1):293-6.

47.

De novo synthesis of uracil nucleotides in mouse liver and intestine studied using [15N]alanine.

Zaharevitz DW, Anderson LW, Strong JM, Hyman R, Cysyk RL.

Eur J Biochem. 1990 Apr 30;189(2):437-40.

48.

Rapid increase of cellular UDP-glucuronide after mitogen stimulation of quiescent 3T3 mouse fibroblasts.

Zaharevitz DW, Chisena CA, Cysyk RL.

Biochem Int. 1990;20(6):1067-76.

PMID:
2196057
49.

Stimulation of uracil nucleotide synthesis in mouse liver, intestine and kidney by ammonium chloride infusion.

Zaharevitz DW, Napier EA, Anderson LW, Strong JM, Cysyk RL.

Eur J Biochem. 1988 Jul 15;175(1):193-8.

50.

Glutamine and glutamate: automated quantification and isotopic enrichments by gas chromatography/mass spectrometry.

Anderson LW, Zaharevitz DW, Strong JM.

Anal Biochem. 1987 Jun;163(2):358-68.

PMID:
2889398

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