- In silico design, synthesis, and assays of specific substrates for proteinase 3: Influence of fluorogenic and charged groups
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Neutrophil serine proteases are specific regulators of the immune response, and proteinase 3 is a major target antigen in antineutrophil cytoplasmic antibody-associated vasculitis. FRET peptides containing 2-aminobenzoic acid (Abz) and N-(2,4-dinitrophenyl)ethylenediamine (EDDnp) as fluorophore and quencher groups, respectively, have been widely used to probe proteases specificity. Using in silico design followed by enzymatic assays, we show that Abz and EDDnp significantly contribute to substrate hydrolysis by PR3. We also propose a new substrate specific for PR3.
- Narawane, Shailesh,Budnjo, Adnan,Grauffel, Cédric,Haug, Bengt Erik,Reuter, Nathalie
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supporting information
p. 1111 - 1115
(2014/03/21)
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- Nucleotides. Part LXXVIII: Double labeling of nucleosides and nucleotides
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Several N(-hydroxyalkyl)-2,4-dinitroanilines were transformed into their phosphoramidites (see 5 and 6 in Scheme 1) in view of their use as fluorescence quenchers, and modified 2-aminobenzamides (see 9, 10, 18, and 19 in Scheme 1) were applied in model re
- Maier, Thomas,Pfleiderer, Wolfgang
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experimental part
p. 2365 - 2392
(2011/02/18)
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- Synthesis of (alkylamino)nitroarenes by oxidative alkylamination of nitroarenes
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The viability of the oxidative alkylamination process for the derivatization of electron-deficient carboaromatics has been investigated. 1,3-Dinitrobenzene, 1-nitronaphthalene, and 1,5- and 1,8-dinitronaphthalenes have shown to react with a wide range of alkylamines in the presence of an oxidant (KMnO4, AgMnO4, AgPy2MnO4) to give access to the corre sponding N-alkyl-nitroarenamines in moderate to good yields. Nitroarenes are more reactive than azines towards alkylamines.
- Gulevskaya, Anna V.,Verbeeck, Stefan,Burov, Oleg N.,Meyers, Caroline,Korbukova, Inna N.,Herrebout, Wouter,Maes, Bert U. W.
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experimental part
p. 564 - 574
(2009/09/06)
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