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Digitale Medien

A rapid luciferase transfection assay for transcription activation effects and stability control of estrogenic drugs in cell cultures (1994)

Meyer, Thomas ; Koop, Ronald ; Angerer, Erwin ; [weitere]

Springer

Journal of cancer research and clinical oncology 120 (1994), S. 359-364

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ISSN: 1432-1335

Schlagwort(e): Estrogen receptor ; Estrogenic plantinum(II) complex ; Luciferase ; Transfection ; Drug stability

Quelle: Springer Online Journal Archives 1860-2000

Thema: Medizin

Notizen: Abstract A rapid assay system for measuring the potential of estrogenic drugs is introduced. Luciferase induction could be measured in estrogen-receptor-positive human MCF-7 breast cancer cells, which had been transfected with a novel luciferase reporter plasmid ERE luc. The minimal requirement was 1 h exposure to the inducing drug and 3.5 h of incubation after removal of the drug. The assay system was used to measure the stability of the drug diaqua-[1,2-bis (2,6-dichloro-4-hydroxyphenyl) ethylenediamine] platinum(II) sulfate, containing an estrogenic ligand and reactive platinum. Luciferase activity was observed only when the drug was in the culture medium and cells for short times, whereas the estrogenic ligand alone remained active. It is assumed that binding of the platinum moiety to macromolecular constituents of the culture or cells renders the drug inaccessible for binding to the estrogen receptor.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1007/BF01247461

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Digitale Medien

Structure-based design of potent CDK1 inhibitors derived from olomoucine (2000)

Furet, Pascal ; Zimmermann, Juerg ; Capraro, Hans-Georg ; [weitere]

Springer

Journal of computer aided molecular design 14 (2000), S. 403-409

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ISSN: 1573-4951

Schlagwort(e): cyclin-dependent kinase ; CDK1 ; inhibitor ; olomoucine ; structure-based design

Quelle: Springer Online Journal Archives 1860-2000

Thema: Chemie und Pharmazie

Notizen: Abstract Cyclin-dependent kinase 1 (CDK1), an enzyme participating in the regulation of the cell cycle, constitutes a possible target in the search for new antitumor agents. Starting from the purine derivative olomoucine and following a structure-based approach, potent inhibitors of this enzyme were rapidly identified. The molecular modeling aspects of this work are described.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1023/A:1008115004986

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Digitale Medien

The secretion pathway of IgA protease-type proteins in gram-negative bacteria (1993)

Klauser, Thomas ; Pohlner, Johannes ; Meyer, Thomas F.

New York, NY : Wiley-Blackwell

BioEssays 15 (1993), S. 799-805

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ISSN: 0265-9247

Schlagwort(e): Life and Medical Sciences ; Cell & Developmental Biology

Quelle: Wiley InterScience Backfile Collection 1832-2000

Thema: Biologie , Medizin

Notizen: The pathogenic, Gram-negative bacteria, Neisseria gon-orrhoeae, Neisseria meningitidis and Haemophilus influenzae, secrete immunoglobulin A1 proteases into their extracellular surroundings. An extraordinary feature in the secretory pathway of these putative virulence factors is a self-directed outer membrane transport step allowing the proteins to be secreted autonomously, even from foreign Gram-negative host cells like Escherichia coli. Here we summarize recent achievements in the understanding of IgA protease outer membrane translocation.

Zusätzliches Material: 3 Ill.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1002/bies.950151205

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