- OXIDIZED GLUTATHIONE ASSAY
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The present invention provides an assay for detection of oxidized glutathione (GSSG).
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Paragraph 0103; 0107
(2016/03/14)
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- Novel Sulfonaminoquinoline Hepcidin Antagonists
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The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
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Page/Page column 126
(2012/09/05)
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- Preparation of arylsulfonyl chlorides by chlorosulfonylation of in situ generated diazonium salts using a continuous flow reactor
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A new flow procedure for the preparation of arylsulfonyl chlorides from aniline starting materials is described. The reaction conditions are mild, requiring no added acid and are amenable to continuous flow processing, in a safe, easily scalable and less labour intensive way than the corresponding batch method.
- Malet-Sanz, Laia,Madrzak, Julia,Ley, Steven V.,Baxendale, Ian R.
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experimental part
p. 5324 - 5332
(2011/01/12)
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- Design of a practical fluorescent probe for superoxide based on protection-deprotection chemistry of fluoresceins with benzenesulfonyl protecting groups
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A strategy for designing probes based on protection-deprotection chemistry involving fluoresceins and their benzenesulfonyl (BES) derivatives has led to the development of a much more practical superoxide (O2-.) probe than the previously reported bis(2,4-dinitro-BES) tetrafluorofluorescein (6a). Examination of various BES derivatives, developed from the starting point of the prototype probe 6a. yielded 4,5-dimethoxy-2-nitro-BES tetrafluorofluorescein (BESSo; 7j) as the optimal reagent. A microtiter plate assay with BESSo showed a tenfold improved detection limit for O 2-. compared with such an assay based on 6a. BESSo showed markedly better specificity for O2-. than for GSH or other reactive oxygen species, and this specificity was significantly higher than that of Fe2+ and some reducing enzymes. These features have resulted in the development of an assay based on BESSo that is capable of providing more unambiguous results for O2. release from neutrophils, with or without stimulation by phorbol myristate acetate, as compared with an assay based on 6a. Intracellular generation of O2. in human Jurkat T cells stimulated by butyric acid has been measured by using flow cytometry and fluorescence microscopy utilizing the acetoxymethyl derivative of BESSo.
- Maeda, Hatsuo,Yamamoto, Kayoko,Kohno, Iho,Hafsi, Leila,Itoh, Norio,Nakagawa, Shinsaku,Kanagawa, Naoko,Suzuki, Keiichiro,Uno, Tadayuki
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p. 1946 - 1954
(2008/02/03)
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- Electrophilic aromatic substituted luciferins as bioluminescent probes for glutathione S-transferase assays
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New highly sensitive latent bioluminescent luciferin substrates were designed and synthesized for monitoring mammalian glutathione S-transferase (GST) and Schistosoma japonicum enzyme activities. The Royal Society of Chemistry 2006.
- Zhou, Wenhui,Shultz, John W.,Murphy, Nancy,Hawkins, Erika M.,Bernad, Laurent,Good, Troy,Moothart, Leonard,Frackman, Susan,Klaubert, Dieter H.,Bulleit, Robert F.,Wood, Keith V.
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p. 4620 - 4622
(2007/10/03)
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- Novel benzopyridothiadiazepines as potential active antitumor agents
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The synthesis of novel thiadiazepine derivatives, that could be considered as constraint analogues of E-7010, are reported. These molecules were evaluated for their antiproliferative activity toward the murine L1210 leukemia cell line. Flow cytometric studies performed on L1210 cells with the most cytotoxic compounds showed an accumulation of the cells in the G2/M phases of the cell cycle with a significant percentage of tetraploid cells (8N DNA content). Submicromolar cytotoxicities were observed with compounds 2b, 4b, 4e, 4g, and 4i. Two of them, compounds 2b and 4b, were found to be potent inhibitors of tubulin polymerization with IC50 of respectively 3.8 and 2.4 μM compared to 2.4 μM for desoxypodophyllotoxin. A 4-methoxyphenylethyl substitution on the pyridinyl nitrogen of the benzopyridothiadiazepine was found to be essential for the antiproliferative activity. The in vitro activities of compounds 2b and 4b make benzopyridothiadiazepine dioxides a promising new class of tubulin binders which warrant further in vivo evaluation.
- Lebegue, Nicolas,Gallet, Sebastien,Flouquet, Nathalie,Carato, Pascal,Pfeiffer, Bruno,Renard, Pierre,Léonce, Stéphane,Pierré, Alain,Chavatte, Philippe,Berthelot, Pascal
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p. 7363 - 7373
(2007/10/03)
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