Search Results - "Schoonen, Willem G E J"

Pharmacologic profiling of human and rat cytochrome P450 1A1 and 1A2 induction and competition by Westerink, Walter M. A, Stevenson, Joe C. R, Schoonen, Willem G. E. J

“…Strong activation of the AhR can lead to various toxic effects such as (non-genotoxic) carcinogenicity. Moreover, drug-drug interactions by non- or competitive…”
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Screening of synthetic and plant-derived compounds for (anti)estrogenic and (anti)androgenic activities by Bovee, Toine F. H, Schoonen, Willem G. E. J, Hamers, Astrid R. M, Bento, Marta Jorge, Peijnenburg, Ad A. C. M

“…Recently we constructed yeast cells that either express the human estrogen receptor α or the human androgen receptor in combination with a consensus ERE or ARE…”
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Development and validation of a high-content screening in vitro micronucleus assay in CHO-k1 and HepG2 cells by Westerink, Walter M.A., Schirris, Tom J.J., Horbach, G. Jean, Schoonen, Willem G.E.J.

“…► In drug development assays for the early detection of genotoxicity are needed. ► Two high content screening (HCS) micronucleus assays were developed and…”
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Evaluation of the Vitotox™ and RadarScreen assays for the rapid assessment of genotoxicity in the early research phase of drug development by Westerink, Walter M.A., Stevenson, Joe C.R., Lauwers, Annick, Griffioen, Gerard, Horbach, G. Jean, Schoonen, Willem G.E.J.

“…The Vitotox™ and RadarScreen assays were evaluated as early screens for mutagenicity and clastogenicity, respectively. The Vitotox™ assay is a bacterial…”
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Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index by van Lierop, Marie-José C, Alkema, Wynand, Laskewitz, Anke J, Dijkema, Rein, van der Maaden, Hans M, Smit, Martin J, Plate, Ralf, Conti, Paolo G M, Jans, Christan G J M, Timmers, C Marco, van Boeckel, Constant A A, Lusher, Scott J, McGuire, Ross, van Schaik, Rene C, de Vlieg, Jacob, Smeets, Ruben L, Hofstra, Claudia L, Boots, Annemieke M H, van Duin, Marcel, Ingelse, Benno A, Schoonen, Willem G E J, Grefhorst, Aldo, van Dijk, Theo H, Kuipers, Folkert, Dokter, Wim H A

“…Glucocorticoids (GCs) such as prednisolone are potent immunosuppressive drugs but suffer from severe adverse effects, including the induction of insulin…”
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SERMs and SARMs: Detection of their activities with yeast based bioassays by Bovee, Toine F.H., Thevis, Mario, Hamers, Astrid R.M., Peijnenburg, Ad A.C.M., Nielen, Michel W.F., Schoonen, Willem G.E.J.

“…Selective estrogen receptor modulators (SERMs) and selective androgen receptor modulators (SARMs) are compounds that activate their cognate receptor in…”
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Cytochrome P450 enzyme levels in HepG2 cells and cryopreserved primary human hepatocytes and their induction in HepG2 cells by Westerink, Walter M.A., Schoonen, Willem G.E.J.

“…Early in vitro toxicity screening might improve the success rate of new chemical entities in pharmaceutical development. In previous studies, the advantage of…”
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Phase II enzyme levels in HepG2 cells and cryopreserved primary human hepatocytes and their induction in HepG2 cells by Westerink, Walter M.A., Schoonen, Willem G.E.J.

“…The HepG2 cell line is a valuable tool for screening for cytotoxicity in the early phase of pharmaceutical development. Some compounds which produce reactive…”
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Evaluation of Cytotoxic, Genotoxic and CYP450 Enzymatic Competition Effects of Tanzanian Plant Extracts Traditionally Used for Treatment of Fungal Infections by Van Den Bout‐van den Beukel, Carolien J. P., Hamza, Omar J. M., Moshi, Mainen J., Matee, Mecky I. N., Mikx, Frans, Burger, David M., Koopmans, Peter P., Verweij, Paul E., Schoonen, Willem G. E. J., Van Der Ven, André J. A. M.

“…:  HIV‐infected patients in sub‐Saharan countries highly depend on traditional medicines for the treatment of opportunistic oral infections as candidiasis…”
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Acute toxicity of CCl4 but not of paracetamol induces a transcriptomic signature of fibrosis in precision-cut liver slices by Vatakuti, Suresh, Schoonen, Willem G.E.J., Elferink, Marieke L.G., Groothuis, Geny M.M., Olinga, Peter

“…•PCLS is validated as a model to identify early gene expression changes related to fibrosis.•Early fibrosis related genes are regulated in CCl4, but not in…”
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The development of RAD51C, Cystatin A, p53 and Nrf2 luciferase-reporter assays in metabolically competent HepG2 cells for the assessment of mechanism-based genotoxicity and of oxidative stress in the early research phase of drug development by Westerink, Walter M.A., Stevenson, Joe C.R., Horbach, G. Jean, Schoonen, Willem G.E.J.

“…Four different mechanism-based high-throughput luciferase-reporter assays were developed in human HepG2 cells, which contain phase I and II metabolic activity…”
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Cytotoxic effects of 109 reference compounds on rat H4IIE and human HepG2 hepatocytes. III: Mechanistic assays on oxygen consumption with MitoXpress and NAD(P)H production with Alamar Blue by Schoonen, Willem G.E.J., Stevenson, Joe C.R., Westerink, Walter M.A., Horbach, G. Jean

“…► MitoXpress oxygen consumption assays have additive value for cytotoxicity. ► One hundred and nine drugs had similar toxic effects in rat H4IIE and human…”
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Receptor profiling and endocrine interactions of tibolone by de Gooyer, Marcel E, Deckers, Godefrides H, Schoonen, Willem G.E.J, Verheul, Herman A.M, Kloosterboer, Helenius J

“…The receptor profiles and in vivo activity of tibolone, and its primary metabolites, Δ 4-isomer, and 3α- and 3β-hydroxytibolone, were studied and compared to…”
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A portrait of cisplatin-induced transcriptional changes in mouse embryonic stem cells reveals a dominant p53-like response by Kruse, Jacqueline J C M, Svensson, J Peter, Huigsloot, Merei, Giphart-Gassler, Micheline, Schoonen, Willem G E J, Polman, Jan E M, Jean Horbach, G, van de Water, Bob, Vrieling, Harry

“…Accumulation of damage in undifferentiated cells may threaten homeostasis and regenerative capacity. Remarkably, p53 has been suggested to be transcriptionally…”
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High-throughput screening for analysis of in vitro toxicity by Schoonen, Willem G E J, Westerink, Walter M A, Horbach, G Jean

“…The influence of combinatorial chemistry and high-throughput screening (HTS) technologies in the pharmaceutical industry during the last 10 years has been…”
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Cytotoxic effects of 110 reference compounds on HepG2 cells and for 60 compounds on HeLa, ECC-1 and CHO cells. II mechanistic assays on NAD(P)H, ATP and DNA contents by Schoonen, Willem G E J, de Roos, Jeroen A D M, Westerink, Walter M A, Débiton, Eric

“…In this study the focus is on the comparison of fluorometric assays, using Alamar Blue (AB) and Hoechst 33342 coloration, and luminometric assays, using…”
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Cytotoxic effects of 100 reference compounds on Hep G2 and HeLa cells and of 60 compounds on ECC-1 and CHO cells. I Mechanistic assays on ROS, glutathione depletion and calcein uptake by Schoonen, Willem G.E.J., Westerink, Walter M.A., de Roos, Jeroen A.D.M., Débiton, Eric

“…In this study fluorometric assays have been used for medium throughput screening on toxicity. Dichlorofluorescein diacetate, monochlorobimane and calcein-AM…”
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Uniform procedure of (1)H NMR analysis of rat urine and toxicometabonomics Part II: comparison of NMR profiles for classification of hepatotoxicity by Schoonen, Willem G E J, Kloks, Cathelijne P A M, Ploemen, Jan-Peter H T M, Smit, Martin J, Zandberg, Pieter, Horbach, G Jean, Mellema, Jan-Remt, Thijssen-Vanzuylen, Carol, Tas, Albert C, van Nesselrooij, Joop H J, Vogels, Jack T W E

“…A procedure of nuclear magnetic resonance (NMR) urinalysis using pattern recognition is proposed for early detection of toxicity of investigational compounds…”
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Sensitivity of (1)H NMR analysis of rat urine in relation to toxicometabonomics. Part I: dose-dependent toxic effects of bromobenzene and paracetamol by Schoonen, Willem G E J, Kloks, Cathelijne P A M, Ploemen, Jan-Peter H T M, Horbach, G Jean, Smit, Martin J, Zandberg, Pieter, Mellema, Jan-Remt, Zuylen, Carol Thijssen-van, Tas, Albert C, van Nesselrooij, Joop H J, Vogels, Jack T W E

“…(1)H nuclear magnetic resonance (NMR) spectroscopy of rat urine in combination with pattern recognition analysis was evaluated for early noninvasive detection…”
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Uniform Procedure of 1H NMR Analysis of Rat Urine and Toxicometabonomics Part II: Comparison of NMR Profiles for Classification of Hepatotoxicity by Schoonen, Willem G. E. J., Kloks, Cathelijne P. A. M., Ploemen, Jan-Peter H. T. M., Smit, Martin J., Zandberg, Pieter, Horbach, G. Jean, Mellema, Jan-Remt, Thijssen-vanZuylen, Carol, Tas, Albert C., van Nesselrooij, Joop H. J., Vogels, Jack T. W. E.

“…A procedure of nuclear magnetic resonance (NMR) urinalysis using pattern recognition is proposed for early detection of toxicity of investigational compounds…”
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