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排序方式: 共有94条查询结果,搜索用时 31 毫秒
1.
Phosphono Bisbenzguanidines as Irreversible Dipeptidomimetic Inhibitors and Activity‐Based Probes of Matriptase‐2 下载免费PDF全文
Daniela Häußler Martin Mangold Norbert Furtmann Dr. Annett Braune Prof. Dr. Michael Blaut Prof. Dr. Jürgen Bajorath Dr. Marit Stirnberg Prof. Dr. Michael Gütschow 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(25):8525-8535
Matriptase‐2, a type II transmembrane serine protease, plays a key role in human iron homeostasis. Inhibition of matriptase‐2 is considered as an attractive strategy for the treatment of iron‐overload diseases, such as hemochromatosis and β‐thalassemia. In the present study, synthetic routes to nine dipeptidomimetic inactivators were developed. Five active compounds ( 41 – 45 ) were identified and characterized kinetically as irreversible inhibitors of matriptase‐2. In addition to a phosphonate warhead, these dipeptides possess two benzguanidine moieties as arginine mimetics to provide affinity for matriptase‐2 by binding to the S1 and S3/S4 subpockets, respectively. This binding mode was strongly supported by covalent docking analysis. Compounds 41 – 45 were obtained as mixtures of two diastereomers and were therefore separated into the single epimers. Compound 45 A , with S configuration at the N‐terminal amino acid and R configuration at the phosphonate carbon atom, was the most potent matriptase‐2 inactivator with a rate constant of inactivation of 2790 m ?1 s?1 and abolished the activity of membrane‐bound matriptase‐2 on the surface of intact cells. Based on the chemotyp of phosphono bisbenzguanidines, the design and synthesis of a fluorescent probe ( 51 A ) by insertion of a coumarin label is described. The in‐gel fluorescence detection of matriptase‐2 was demonstrated by applying 51 A as the first activity‐based probe for this enzyme. 相似文献
2.
Cíntia Salomão Pinto Zarth Andreas Koschella Annett Pfeifer Susann Dorn Thomas Heinze 《Cellulose (London, England)》2011,18(5):1315-1325
The homogeneous conversion of cellulose dissolved in N-methyl-2-pyrrolidone/LiCl and 1-N-butyl-3-methylimidazolium chloride with N-methyl-2-pyrrolidone, ε-caprolactam, N-methyl-ε-caprolactam, and N-methyl-2-piperidone in the presence of p-toluenesulphonic acid chloride was studied. Depending on the reaction conditions, novel cellulose esters with degree of substitution
(DS) values ranging from 0.12 to 1.17 could be prepared. The structure of the amino group containing cellulose esters was
elucidated by elemental analysis, FTIR- and NMR spectroscopy. NMR spectroscopy revealed an almost complete esterification
of position 6 of the anhydroglucose unit at DS of 1. The conversion can be conducted between room temperature and 40 °C, while
side-reactions became predominant at 60 °C. Starting with DS of 0.24, the samples were soluble both in water and dimethyl
sulphoxide. The derivatives described are capable of forming polyelectrolyte complexes. The samples were stable at room temperature
in aqueous solution at pH 2 and 7. Lower viscosities were found for samples with higher DS in aqueous solution at comparable
molar mass. 相似文献
3.
We present an analysis of the Hall conductivity σ(xy)(ω,T) in time reversal symmetry breaking states of exotic superconductors. We find that the dichroic signal is nonzero in systems with interband order parameters. This new intrinsic mechanism may explain the Kerr effect observed in strontium ruthenate and possibly other superconductors. We predict coherence factor effects in the temperature dependence of the imaginary part of the ac Hall conductivity Imσ(xy)(ω,T), which can be tested experimentally. 相似文献
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Alonso JM Reichel A Piehler J del Campo A 《Langmuir : the ACS journal of surfaces and colloids》2008,24(2):448-457
Photosensitive silanes containing nitroveratryl (Nvoc)-caged amine groups and protein repellent tetraethylene glycol units were synthesized and used for modification of silica surfaces. Functional surface layers containing different densities of caged amine groups were prepared and activated by UV-irradiation of the surface. The performance of these layers for functional and site-selective immobilization of proteins was tested. For this purpose, biotin and tris-nitrilotriacetic acid (tris-NTA) were fist coupled to the activated surface, and the interaction of streptavidin and His-tagged proteins with the functionalized surfaces was monitored by real-time label-free detection. After optimizing the coupling protocols, highly selective functionalization of the deprotected amine groups was possible. Furthermore, the degree of functionalization (and therefore the amount of immobilized protein) was controlled by diluting the surface concentration of the amine-functionalized silane with a nonreactive (OMe-terminated) tetraethylene glycol silane. Immobilized proteins were highly functional on these surfaces, as demonstrated by protein-protein interaction assays with the type I interferon receptor. Protein micropatterns were successfully generated after masked irradiation and functionalization of the caged surface following the optimized coupling protocols. 相似文献
7.
[reaction: see text] Nuclear amination of p-hydroquinones with primary aromatic amines was catalyzed by fungal laccases (EC 1.10.3.2) from Trametes spec. and Myceliophthora thermophila. This is the first report of laccase-catalyzed synthesis of aminoquinones. Incubation of two compounds with laccase in the presence of oxygen resulted in the formation of the corresponding monoaminated or diaminated quinones. No hydroquinonoids were formed. Observed differences in the reaction courses for different p-hydroquinones and aromatic amines with different laccases are discussed. 相似文献
8.
Jakub Koza Margitta Uhlemann Annett Gebert Ludwig Schultz 《Journal of Solid State Electrochemistry》2008,12(2):181-192
The effect of a uniform magnetic field with flux density up to 1 T on the electrodeposition of Fe from sulphate electrolyte
has been investigated under different field configurations relative to the electrode surface. Voltammetric and chronoamperometric
experiments have been carried out coupled with an electrochemical quartz crystal microbalance for in situ mass change measurements.
The structure and morphology of the deposited films were determined by scanning electron microscopy, atomic force microscopy
and X-ray diffraction measurements. Results show that, when the magnetic field is applied parallel to the electrode surface,
the limiting current density and the deposition rate are increased due to the magnetohydrodynamic effect. The nucleation process
is also affected in parallel configuration; the current density of the maximum on the chronoamperograms is decreased, and
an additional nucleation step might be observed. This effect is attributed to the hydrodynamic response of the electrochemical
system. No significant influence on the electrochemical reaction was observed when a magnetic field was applied perpendicular
to the electrode. But in this configuration, the morphology of deposited layers is changed by the magnetic field. The morphology
changes are discussed. No effect of the magnetic field on the crystallographic structure was observed. 相似文献
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10.
The total synthesis of an alkylcitrate secondary metabolite from the fungi Trichoderma viride is described. An ester dienolate [2,3]-Wittig rearrangement and a S. Julia-Kocienski olefination served as key C/C-connecting transformations. The highly convergent synthesis consists of a longest linear sequence of 17 steps. 相似文献