Research Topics
| Roy M GolsteynSummaryAffiliation: Institut de Recherches Servier Country: France Publications
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Detail Information
Publications
Recent advances in cancer researchRoy M Golsteyn
Cancer Research Division, Institut de Recherches Servier, Croissy sur Seine, France
Drug News Perspect 17:405-16. 2004..A selection from the many excellent presentations and posters are described with an emphasis on new compounds, new methods to identify cancers, and recent discoveries that may change how we treat cancer...- Cdk1 and Cdk2 complexes (cyclin dependent kinases) in apoptosis: a role beyond the cell cycleRoy M Golsteyn
Cancer Research Division, Institut de Recherches Servier, 125 ch de Ronde, Croissy sur Seine, Paris F 78290, France
Cancer Lett 217:129-38. 2005..By understanding how Cdks function during apoptosis it may be possible to optimise the use of these inhibitors in treating human tumours by blocking proliferation but permitting apoptosis... - An unusual DNA binding compound, S23906, induces mitotic catastrophe in cultured human cellsNathalie Cahuzac
Institut de Recherches Servier, Cancer Research Division, Croissy sur Seine, France
Cancer Lett 289:178-87. 2010..These results suggest that mitotic catastrophe is one of the cellular responses to S23906 and that mitotic catastrophe may be a common cellular response to many different types of DNA damage... - Characterization of novel checkpoint kinase 1 inhibitors by in vitro assays and in human cancer cells treated with topoisomerase inhibitorsGilles Ferry
Institut de Recherches Servier, Molecular and Cellular Pharmacology, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
Life Sci 89:259-68. 2011..We have developed biochemical and cell based assays to characterize small therapeutic molecules that inhibit the DNA damage checkpoint enzyme, Chk1 (Checkpoint kinase 1)... - The role of cyclin-dependent kinases in apoptosisAnnie Borgne
, Institut de Recherches Servier, 125, Chemin de Ronde, 78290 Croissy-sur-Seine, France
Prog Cell Cycle Res 5:453-9. 2003..Protein kinase complexes known as cyclin-dependent kinases (Cdks) are the first example of such enzymes. In this review, we focus on the role of the subunits of different Cdks in both apoptosis and the cell cycle... - Generation of replication-dependent double-strand breaks by the novel N2-G-alkylator S23906-1Stephane Leonce
Institut de Recherches Servier, Cancer Drug Discovery, Croissy sur Seine, France
Cancer Res 66:7203-10. 2006..These results suggest that secondary DNA lesions play an important role in the cytotoxicity of this compound and make histone H2AX phosphorylation an attractive marker for monitoring the efficacy of S23906-1... - Novel 5-azaindolocarbazoles as cytotoxic agents and Chk1 inhibitorsMyriam Lefoix
Institut de Chimie Organique et Analytique, Universite d Orleans, UMR CNRS 6005, rue de Chartres, BP 6759, 45067 Orleans Cedex 2, France
Bioorg Med Chem 16:5303-21. 2008..This is the case of compounds 45-47 with IC(50) of, respectively, 72, 27, and 14nM toward Chk1. Compound 46, which exhibits moderate cytotoxicity, appears to be a good candidate for development in a multi-drug anticancer therapy... - The story of gefitinib, an EGFR kinase that works in lung cancerRoy M Golsteyn
Drug Discov Today 9:587. 2004 - Pyrrolocarbazoles as checkpoint 1 kinase inhibitorsHélène Hénon
Laboratoire SEESIB, Universite Blaise Pascal, UMR 6504 du CNRS, 24 avenue des Landais, 63177 Aubiere, France
Anticancer Agents Med Chem 8:577-97. 2008..This review reports the synthesis and Chk1 inhibitory activities of pyrrolocarbazole compounds bearing four or five fused rings... - Synthesis, checkpoint kinase 1 inhibitory properties and in vitro antiproliferative activities of new pyrrolocarbazolesElisabeth Conchon
Laboratoire SEESIB, Universite Blaise Pascal, UMR 6504 du CNRS, 63177 Aubiere, France
Bioorg Med Chem 16:4419-30. 2008.... - Inhibition of Chk1 kills tetraploid tumor cells through a p53-dependent pathwayIlio Vitale
INSERM, U848, Cancer and Immunity, Villejuif, France
PLoS ONE 2:e1337. 2007..Altogether, our results demonstrate that, in tetraploid tumor cells, the inhibition of Chk1 sequentially triggers aberrant mitosis, p53 activation and Puma/BBC3-dependent mitochondrial apoptosis... - Phosphorylation of CDC25C at S263 controls its intracellular localisationCharlotte Esmenjaud Mailhat
LBCMCP CNRS, IFR109 Institut d Exploration Fonctionnelle des Génomes, University of Toulouse, 118 route de Narbonne, 31062 Toulouse, France
FEBS Lett 581:3979-85. 2007..We propose that phosphorylation at S263 is part of the regulatory mechanism that modulates nuclear import of CDC25C, thus preventing cytoplasm to nucleus shuttling... - Synthesis and biological activities of isogranulatimide analoguesBernadette Hugon
Laboratoire SEESIB, Universite Blaise Pascal, UMR 6504 du CNRS, Aubiere, France
Bioorg Med Chem 15:5965-80. 2007..The selectivity of two potent Chk1 inhibitors 24 and 26 has been evaluated using various kinases. The strongest inhibitory properties are found toward Chk1... - Synthesis, in vitro antiproliferative activities, and Chk1 inhibitory properties of pyrrolo[3,4-a]carbazole-1,3-diones, pyrrolo[3,4-c]carbazole-1,3-diones, and 2-aminopyridazino[3,4-a]pyrrolo[3,4-c]carbazole-1,3,4,7-tetraoneElisabeth Conchon
Laboratoire SEESIB, Universite Blaise Pascal, UMR 6504 du CNRS, 24, avenue des Landais, 63177 Aubiere, France
Eur J Med Chem 43:282-92. 2008..The ATP binding pocket of Chk1 seems to be adaptable to substitution of the nitrogen of the imide E heterocycle with a hydroxymethyl group, allowing the fundamental hydrogen bond with the Glu(85) residue of the enzyme... - Gefitinib does not increase survival in lung cancer patientsRoy M Golsteyn
Drug Discov Today 10:381. 2005 - Synthesis, in vitro antiproliferative activities, and Chk1 inhibitory properties of indolylpyrazolones and indolylpyridazinedioneElisabeth Conchon
Laboratoire SEESIB, , UMR 6504 du CNRS, , France
Eur J Med Chem 41:1470-7. 2006..To get an insight into the kinase selectivity of these compounds, their inhibitory activities toward Src kinase were evaluated... - Synthesis and biological activities of 7-aza rebeccamycin analogues bearing the sugar moiety on the nitrogen of the pyridine ringSamir Messaoudi
, , UMR 6504 du CNRS, , France
Bioorg Med Chem 14:7551-62. 2006..Their abilities to inhibit the checkpoint kinase Chk1 have been evaluated... - Bis-imide granulatimide analogues as potent Checkpoint 1 kinase inhibitorsHélène Hénon
Laboratoire SEESIB, Universite Blaise Pascal, UMR 6504 du CNRS, 63177 Aubiere, France
Eur J Pharmacol 554:106-12. 2007..The inhibitory activities of compounds A, 5 and 11 toward Src tyrosine kinase and the cytotoxicity of various tumor cell lines were also evaluated...