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Daniel Zaharevitz

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Chemicals & Drugs

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Grégoire Prévost; Marie O Lonchampt; Susan Holbeck; Samir Attoub; Daniel W Zaharevitz; Mike Alley; John Wright; Marie-Christine Brezak; Hélène Coulomb; Ann Savola; Marion Huchet; Sophie Chaumeron; Quang-Dé Nguyen; Patricia Forgez; Erik Bruyneel; Marc Bracke; Eric Ferrandis; Pierre Roubert; Danièle Demarquay; Christian Gespach; Philip G Kasprzyk
Anticancer activity of BIM-46174, a new inhibitor of the heterotrimeric Galpha/Gbetagamma protein complex.
Tam L Nguyen; Rick Gussio; jeffrey smith; Deborah A Lannigan; Sidney Hecht; Dominic A Scudiero; Robert H Shoemaker; Daniel W Zaharevitz
Homology model of RSK2 N-terminal kinase domain, structure-based identification of novel RSK2 inhibitors, and preliminary common pharmacophore.
Tam L Nguyen; Connor McGrath; Ann R Hermone; James C Burnett; Daniel W Zaharevitz; Billy W Day; Peter Wipf; Ernest Hamel; Rick Gussio
A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach.

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All Publications

2006: Grégoire Prévost; Marie O Lonchampt; Susan Holbeck; Samir Attoub; Daniel W Zaharevitz; Mike Alley; John Wright; Marie-Christine Brezak; Hélène Coulomb; Ann Savola; Marion Huchet; Sophie Chaumeron; Quang-Dé Nguyen; Patricia Forgez; Erik Bruyneel; Marc Bracke; Eric Ferrandis; Pierre Roubert; Danièle Demarquay; Christian Gespach; Philip G Kasprzyk
Anticancer activity of BIM-46174, a new inhibitor of the heterotrimeric Galpha/Gbetagamma protein complex.
Cancer research 2006;66(18):9227-34.
2006: Tam L Nguyen; Rick Gussio; jeffrey smith; Deborah A Lannigan; Sidney Hecht; Dominic A Scudiero; Robert H Shoemaker; Daniel W Zaharevitz
Homology model of RSK2 N-terminal kinase domain, structure-based identification of novel RSK2 inhibitors, and preliminary common pharmacophore.
Bioorganic & medicinal chemistry 2006;14(17):6097-105.
2005: Tam L Nguyen; Connor McGrath; Ann R Hermone; James C Burnett; Daniel W Zaharevitz; Billy W Day; Peter Wipf; Ernest Hamel; Rick Gussio
A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach.
Journal of medicinal chemistry 2005;48(19):6107-16.
2005: Xu Xie; Thomas Lemcke; Rick Gussio; Daniel W Zaharevitz; Maryse Leost; Laurent Meijer; Conrad Kunick
Epoxide-containing side chains enhance antiproliferative activity of paullones.
European journal of medicinal chemistry 2005;40(7):655-61.
2005: Tam L Nguyen; Guy Schoehn; Winfried Weissenhorn; Ann R Hermone; James C Burnett; Rekha G Panchal; Connor McGrath; Daniel W Zaharevitz; M Javad Aman; Rick Gussio; Sina Bavari
An all-atom model of the pore-like structure of hexameric VP40 from Ebola: structural insights into the monomer-hexamer transition.
Journal of structural biology 2005;151(1):30-40.
2005: Connor F McGrath; Nagarajan Pattabiraman; Glen E Kellogg; Thomas Lemcke; Conrad Kunick; Edward A Sausville; Daniel W Zaharevitz; Rick Gussio
Homology model of the CDK1/cyclin B complex.
Journal of biomolecular structure & dynamics 2005;22(5):493-502.
2005: Conrad Kunick; Zhihong Zeng; Rick Gussio; Daniel W Zaharevitz; Maryse Leost; Frank Totzke; Christoph Schächtele; Michael H G Kubbutat; Laurent Meijer; Thomas Lemcke
Structure-aided optimization of kinase inhibitors derived from alsterpaullone.
Chembiochem : a European journal of chemical biology 2005;6(3):541-9.
2005: James C Burnett; James J Schmidt; Connor F McGrath; Tam L Nguyen; Ann R Hermone; Rekha G Panchal; Jonathan L Vennerstrom; Krishna Kodukula; Daniel W Zaharevitz; Rick Gussio; Sina Bavari
Conformational sampling of the botulinum neurotoxin serotype A light chain: implications for inhibitor binding.
Bioorganic & medicinal chemistry 2005;13(2):333-41.
2004: Helen B Stone; John E Moulder; C Norman Coleman; K. Kian Ang; Mitchell S. Anscher; Mary Helen Barcellos-Hoff; William S Dynan; John R Fike; David J Grdina; Joel S Greenberger; Martin Hauer-Jensen; Richard P Hill; Richard Kolesnick; Thomas J MacVittie; Cheryl Marks; william mcbride; Noelle Metting; Terry Pellmar; Mary Purucker; Mike E Robbins; Robert H Schiestl; Thomas M Seed; Joseph E Tomaszewski; Elizabeth L Travis; Paul E Wallner; Mary Wolpert; Daniel W Zaharevitz
Models for evaluating agents intended for the prophylaxis, mitigation and treatment of radiation injuries. Report of an NCI Workshop, December 3-4, 2003.
Radiation research 2004;162(6):711-28.
2004: Richard B Greenwald; Hong Zhao; Jing Xia; Dechun Wu; Stephen Nervi; Sherman F Stinson; Eva Majerova; Chris Bramhall; Daniel W Zaharevitz
Poly(ethylene glycol) prodrugs of the CDK inhibitor, alsterpaullone (NSC 705701): synthesis and pharmacokinetic studies.
Bioconjugate chemistry 2004;15(5):1076-83.
2004: Tanja Pies; Klaus-Jürgen Schaper; Maryse Leost; Daniel W Zaharevitz; Rick Gussio; Laurent Meijer; Conrad Kunicke
CDK1-inhibitory activity of paullones depends on electronic properties of 9-substituents.
Archiv der Pharmazie 2004;337(9):486-92.
2004: Rekha G Panchal; Ann R Hermone; Tam L Nguyen; Thiang Yian Wong; Robert Schwarzenbacher; James Schmidt; Douglas Lane; Connor McGrath; Benjamin E Turk; James Burnett; M Javad Aman; Stephen Little; Edward A Sausville; Daniel W Zaharevitz; Lewis C Cantley; Robert C Liddington; Rick Gussio; Sina Bavari
Identification of small molecule inhibitors of anthrax lethal factor.
Nature structural & molecular biology 2004;11(1):67-72.
2004: Conrad Kunick; Kathrin Lauenroth; Karen Wieking; Xu Xie; Christiane Schultz; Rick Gussio; Daniel W Zaharevitz; Maryse Leost; Laurent Meijer; Alexander Weber; Flemming Steen Jørgensen; Thomas Lemcke
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.
Journal of medicinal chemistry 2004;47(1):22-36.
2003: James C Burnett; James J Schmidt; Robert G Stafford; Rekha G Panchal; Tam L Nguyen; Ann R Hermone; Jonathan L Vennerstrom; Connor F McGrath; Douglas J Lane; Edward A Sausville; Daniel W Zaharevitz; Rick Gussio; Sina Bavari
Novel small molecule inhibitors of botulinum neurotoxin A metalloprotease activity.
Biochemical and biophysical research communications 2003;310(1):84-93.
2002: Xin Lu; Shimei Gong; Anne Monks; Daniel W Zaharevitz; Jeffrey A Moscow
Correlation of nucleoside and nucleobase transporter gene expression with antimetabolite drug cytotoxicity.
Journal of experimental therapeutics & oncology 2002;2(4):200-12.
2002: Karen Wieking; Marie Knockaert; Maryse Leost; Daniel W Zaharevitz; Laurent Meijer; Conrad Kunick
Synthesis of paullones with aminoalkyl side chains.
Archiv der Pharmazie 2002;335(7):311-7.
2002: John Lazo; Kaoru Nemoto; Katharine E Pestell; Kathleen A Cooley; Eileen C Southwick; Douglas Mitchell; William Furey; Rick Gussio; Daniel W Zaharevitz; Beomjun Joo; Peter Wipf
Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors.
Molecular pharmacology 2002;61(4):720-8.
2002: Daniel W Zaharevitz; Susan Holbeck; Christopher Bowerman; Penny A Svetlik
COMPARE: a web accessible tool for investigating mechanisms of cell growth inhibition.
Journal of molecular graphics & modelling 2002;20(4):297-303.
2001: John Irwin Johnson; S Decker; Daniel W Zaharevitz; Lawrence V Rubinstein; J M Venditti; S Schepartz; S Kalyandrug; Michaele Christian; Arbuck Susan; Melinda G Hollingshead; Edward A Sausville
Relationships between drug activity in NCI preclinical in vitro and in vivo models and early clinical trials.
British journal of cancer 2001;84(10):1424-31.
2001: Kyriacos C Nicolaou; Kenji Namoto; Jian Li; Andreas Ritzén; T Ulven; M Shoji; Daniel W Zaharevitz; Rick Gussio; D L Sackett; R D Ward; A Hensler; T Fojo; Paraskevi Giannakakou
Synthesis and biological evaluation of 12,13-cyclopropyl and 12,13-cyclobutyl epothilones.
Chembiochem : a European journal of chemical biology 2001;2(1):69-75.
2000: Maryse Leost; Christiane Schultz; Andreas Link; Y Z Wu; J Biernat; Eva-Maria Mandelkow; James A Bibb; Gretchen L Snyder; Paul Greengard; Daniel W Zaharevitz; Rick Gussio; Adrian M Senderowicz; Edward A Sausville; Conrad Kunick; Laurent Meijer
Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.
European journal of biochemistry / FEBS 2000;267(19):5983-94.
2000: Kyriacos C Nicolaou; R Scarpelli; B Bollbuck; B Werschkun; M M Pereira; Markus Wartmann; Karl-Heinz Altmann; Daniel W Zaharevitz; Rick Gussio; Paraskevi Giannakakou
Chemical synthesis and biological properties of pyridine epothilones.
Chemistry & biology 2000;7(8):593-9.
2000: Edward A Sausville; J Johnson; M Alley; Daniel W Zaharevitz; Adrian M Senderowicz
Inhibition of CDKs as a therapeutic modality.
Annals of the New York Academy of Sciences 2000;910():207-21; discussion 221-2.
2000: Conrad Kunick; Christiane Schultz; Thomas Lemcke; Daniel W Zaharevitz; Rick Gussio; R K Jalluri; Edward A Sausville; Maryse Leost; Laurent Meijer
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.
Bioorganic & medicinal chemistry letters 2000;10(6):567-9.
2000: Paraskevi Giannakakou; Rick Gussio; Eva Nogales; K H Downing; Daniel W Zaharevitz; B Bollbuck; G Poy; Dan L Sackett; Kyriacos C Nicolaou; Tito Fojo
A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells.
Proceedings of the National Academy of Sciences of the United States of America 2000;97(6):2904-9.
2000: Rick Gussio; Daniel W Zaharevitz; Connor F McGrath; Nagarajan Pattabiraman; Glen E Kellogg; C Schultz; A Link; Conrad Kunick; Maryse Leost; Laurent Meijer; Edward A Sausville
Structure-based design modifications of the paullone molecular scaffold for cyclin-dependent kinase inhibition.
Anti-cancer drug design 2000;15(1):53-66.
1999: Christiane Schultz; Andreas Link; Maryse Leost; Daniel W Zaharevitz; Rick Gussio; Edward A Sausville; Laurent Meijer; Conrad Kunick
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.
Journal of medicinal chemistry 1999;42(15):2909-19.
1999: Daniel W Zaharevitz; Rick Gussio; Maryse Leost; Adrian M Senderowicz; Tyler Lahusen; Conrad Kunick; Laurent Meijer; Edward A Sausville
Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases.
Cancer research 1999;59(11):2566-9.
1999: Edward A Sausville; Daniel W Zaharevitz; Rick Gussio; Laurent Meijer; M Louarn-Leost; Conrad Kunick; R Schultz; Tyler Lahusen; Donna Headlee; Sherman F Stinson; Arbuck Susan; Adrian M Senderowicz
Cyclin-dependent kinases: initial approaches to exploit a novel therapeutic target.
Pharmacology & therapeutics 1999;82(2-3):285-92.
1999: Andreas Link; Daniel W Zaharevitz; Conrad Kunick
Antitumor pyrido[3,2-d][1]benzazepines: synthesis and in vitro activity of thiophene analogs.
Die Pharmazie 1999;54(3):163-6.
1998: Rick Gussio; Nagarajan Pattabiraman; Glen E Kellogg; Daniel W Zaharevitz
Use of 3D QSAR methodology for data mining the National Cancer Institute Repository of Small Molecules: application to HIV-1 reverse transcriptase inhibition.
Methods (San Diego, Calif.) 1998;14(3):255-63.
1997: J N Weinstein; Timothy G Myers; P M O'Connor; S H Friend; Albert J Fornace; K W Kohn; T Fojo; S E Bates; L V Rubinstein; N L Anderson; JK Buolamwini; W W van Osdol; Anne Monks; Dominic A Scudiero; Edward A Sausville; Daniel W Zaharevitz; B Bunow; Vellarkad Viswanadhan; G S Johnson; R E Wittes; KD Paull
An information-intensive approach to the molecular pharmacology of cancer.
Science (New York, N.Y.) 1997;275(5298):343-9.
1996: William G Rice; Jim A Turpin; CA Schaeffer; L Graham; D Clanton; Robert W Buckheit; Daniel W Zaharevitz; Michael F Summers; Anders Wallqvist; David G Covell
Evaluation of selected chemotypes in coupled cellular and molecular target-based screens identifies novel HIV-1 zinc finger inhibitors.
Journal of medicinal chemistry 1996;39(19):3606-16.
1996: E S Cleaveland; Daniel W Zaharevitz; James A Kelley; KD Paull; D A Cooney; Harry Ford
Identification of a novel inhibitor (NSC 665564) of dihydroorotate dehydrogenase with a potency equivalent to brequinar.
Biochemical and biophysical research communications 1996;223(3):654-9.
1996: Rick Gussio; Nagarajan Pattabiraman; Daniel W Zaharevitz; G E Kellogg; Igor A Topol; William G Rice; CA Schaeffer; John W Erickson; Stanley K Burt
All-atom models for the non-nucleoside binding site of HIV-1 reverse transcriptase complexed with inhibitors: a 3D QSAR approach.
Journal of medicinal chemistry 1996;39(8):1645-50.
1995: E S Cleaveland; Anne Monks; A Vaigro-Wolff; Daniel W Zaharevitz; KD Paull; K Ardalan; D A Cooney; Harry Ford
Site of action of two novel pyrimidine biosynthesis inhibitors accurately predicted by the compare program.
Biochemical pharmacology 1995;49(7):947-54.
1995: R L Cysyk; N Malinowski; Victor E Marquez; Daniel W Zaharevitz; E M August; J D Moyer
Cyclopentenyl uracil: an effective inhibitor of uridine salvage in vivo.
Biochemical pharmacology 1995;49(2):203-7.
1994: Shulin Wang; Daniel W Zaharevitz; R Sharma; Victor E Marquez; Nancy E Lewin; L Du; Peter M Blumberg; GW Milne
The discovery of novel, structurally diverse protein kinase C agonists through computer 3D-database pharmacophore search. Molecular modeling studies.
Journal of medicinal chemistry 1994;37(26):4479-89.
1994: GW Milne; Marc C Nicklaus; J S Driscoll; Shaomeng Wang; Daniel W Zaharevitz
National Cancer Institute Drug Information System 3D database.
Journal of chemical information and computer sciences 1994;34(5):1219-24.
1993: Daniel W Zaharevitz; C A Chisena; KIMBERLY DUNCAN; E M August; R L Cysyk
Vanadate inhibition of hyaluronic acid synthesis in Swiss 3T3 fibroblasts.
Biochemistry and molecular biology international 1993;31(4):627-33.
1993: Marc C Nicklaus; GW Milne; Daniel W Zaharevitz
Chem-X and CAMBRIDGE. Comparison of computer generated chemical structures with X-ray crystallographic data.
Journal of chemical information and computer sciences 1993;33(4):639-46.
1993: Daniel W Zaharevitz; M F Grubb; R Hyman; C Chisena; R L Cysyk
Effect of high-protein diet on pyrimidine synthesis and response to PALA in mouse tissues.
Journal of the National Cancer Institute 1993;85(8):662-6.
1992: Daniel W Zaharevitz; L W Anderson; N M Malinowski; R Hyman; John M Strong; R L Cysyk
Contribution of de-novo and salvage synthesis to the uracil nucleotide pool in mouse tissues and tumors in vivo.
European journal of biochemistry / FEBS 1992;210(1):293-6.
1990: Daniel W Zaharevitz; L W Anderson; John M Strong; R Hyman; R L Cysyk
De novo synthesis of uracil nucleotides in mouse liver and intestine studied using [15N]alanine.
European journal of biochemistry / FEBS 1990;189(2):437-40.
1990: Daniel W Zaharevitz; C A Chisena; R L Cysyk
Rapid increase of cellular UDP-glucuronide after mitogen stimulation of quiescent 3T3 mouse fibroblasts.
Biochemistry international 1990;20(6):1067-76.
1988: Daniel W Zaharevitz; E A Napier; L W Anderson; John M Strong; R L Cysyk
Stimulation of uracil nucleotide synthesis in mouse liver, intestine and kidney by ammonium chloride infusion.
European journal of biochemistry / FEBS 1988;175(1):193-8.
1987: L W Anderson; Daniel W Zaharevitz; John M Strong
Glutamine and glutamate: automated quantification and isotopic enrichments by gas chromatography/mass spectrometry.
Analytical biochemistry 1987;163(2):358-68.