Search results for "TYR"
showing 10 items of 2017 documents
Conformation-specific blockade of the integrin GPIIb/IIIa: a novel antiplatelet strategy that selectively targets activated platelets.
2006
Platelet activation causes conformational changes of integrin GPIIb/IIIa (α IIb β 3 ), resulting in the exposure of its ligand-binding pocket. This provides the unique possibility to design agents that specifically block activated platelets only. We used phage display of single-chain antibody (scFv) libraries in combination with several rounds of depletion/selection to obtain human scFvs that bind specifically to the activated conformation of GPIIb/IIIa. Functional evaluation of these scFv clones revealed that fibrinogen binding to human platelets and platelet aggregation can be effectively inhibited by activation-specific scFvs. In contrast to clinically used GPIIb/IIIa blockers, which ar…
Anti-inflammatory and analgesic activity of a novel inhibitor of microsomal prostaglandin E synthase-1 expression
2009
Abstract In a previous study, we reported a new γ-hydroxybutenolide derivative, 4-benzo[ b ]thiophen-2-yl-3-bromo-5-hydroxy-5 H -furan-2-one (BTH), as inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) expression in lypopolysaccharide (LPS) stimulated RAW 264.7 and TPH-1 cells, without affecting cyclooxygenase-2 (COX-2). In this study, we evaluated the in vivo effect of BTH on some acute and chronic inflammatory animal models in relation to its inhibitory profile on mPGES-1 expression. In the zymosan-induced mouse air pouch model, BTH produced a dose-dependent inhibition of prostaglandin E 2 (PGE 2 ) production and mPGES-1 protein expression in pouch exudates without any effect on…
Deciphering of ADP-induced, phosphotyrosine-dependent signaling networks in human platelets by Src-homology 2 region (SH2)-profiling.
2012
Tyrosine phosphorylation plays a central role in signal transduction controlling many important biological processes. In platelets, the activity of several signaling proteins is controlled by tyrosine phosphorylation ensuring proper platelet activation and aggregation essential for regulation of the delicate balance between bleeding and hemostasis. Here, we applied Src-homology 2 region (SH2)-profiling for deciphering of the phosphotyrosine state of human platelets activated by adenosine diphosphate (ADP). Applying a panel of 31 SH2-domains, rapid and complex regulation of the phosphotyrosine state of platelets was observed after ADP stimulation. Specific inhibition of platelet P2Y receptor…
Rapid formation of plasma protein corona critically affects nanoparticle pathophysiology
2013
In biological fluids, proteins bind to the surface of nanoparticles to form a coating known as the protein corona, which can critically affect the interaction of the nanoparticles with living systems. As physiological systems are highly dynamic, it is important to obtain a time-resolved knowledge of protein-corona formation, development and biological relevancy. Here we show that label-free snapshot proteomics can be used to obtain quantitative time-resolved profiles of human plasma coronas formed on silica and polystyrene nanoparticles of various size and surface functionalization. Complex time- and nanoparticle-specific coronas, which comprise almost 300 different proteins, were found to …
New Insights into the Provenance of the Obsidian Fragments of the Island of Ustica (Palermo, Sicily)
2017
In this study we applied a multidisciplinary approach, coupling geophysical and geochemical measurements, to unveil the provenance of 170 obsidian flakes, collected on the volcanic island of Ustica (Sicily). On this island there are some prehistoric settlements dated from the Neolithic to the Middle Bronze Age. Despite not having geological outcrops of obsidian rocks, the countryside of Ustica is rich in fragments of this volcanic glass, imported from other source areas. The study of obsidian findings was carried out first through visual observations and density measurements. At least two different obsidian families have been distinguished, probably imported from Lipari and Pantelleria isla…
Insect-associated bacteria assemble the antifungal butenolide gladiofungin by non-canonical polyketide chain termination
2020
Abstract Genome mining of one of the protective symbionts (Burkholderia gladioli) of the invasive beetle Lagria villosa revealed a cryptic gene cluster that codes for the biosynthesis of a novel antifungal polyketide with a glutarimide pharmacophore. Targeted gene inactivation, metabolic profiling, and bioassays led to the discovery of the gladiofungins as previously‐overlooked components of the antimicrobial armory of the beetle symbiont, which are highly active against the entomopathogenic fungus Purpureocillium lilacinum. By mutational analyses, isotope labeling, and computational analyses of the modular polyketide synthase, we found that the rare butenolide moiety of gladiofungins deriv…
Cationic and Zwitterionic Polymerizable Surfactants: Quaternary Ammonium Dialkyl Maleates. 1. Synthesis and Characterization
1999
Cationic and zwitterionic reactive dialkyl maleates with different hydrophobic chain lengths (R = C10H21, C12H25, C16H33, and C18H37), and some similar surfactants without double bonds were synthesized with an aim to use them as stabilizers in the batch and seeded emulsion copolymerization of styrene and butyl acrylate (part 2 of this series). Surfactants are obtained in a three-step synthesis, starting from ring opening of maleic anhydride, followed by O alkylation with an aminoalkyl compound, and finishing with quaternization of the amino group in the hydrophilic part of the molecule. The chemical structure of surfactants was confirmed by 1H NMR. Melting points and critical micelle concen…
Gelchromatographie. 6. Mitt. trennungen im präparativen maßstab mit hoher auflösung
1968
Zur gelchromatographischen Trennung im Grammengen-Bereich wurde ein Recycling-Verfahren mit kontinuierlicher Einengung des Eluates entwickelt. Die Trennung von Oligomeren des Styrols, des Butylmethacrylates und des Athylenoxids unter Anwendung dieser Methode wire beschrieben. Vorteile und Grenzen des Verfahrens werden diskutiert. A recycling technic with continuous concentration of the eluate has been developed for gel chromatographic separation in the gram-scale. The separation of oligomers of styrene, butyl methacrylate and ethylene oxide by use of this method is described. Advantages and limitation of this procedure are discussed.
Concept Matching Technique for Assessing importance of Volatile Compounds for Cheddar Cheese Aroma
1994
Many volatile compounds have been identified in Cheddar cheese, but the importance of each compound for the characteristic Cheddar aroma is unknown. We screened 15 compounds for importance for Cheddar cheese aroma using a factorial design. The resulting mixtures were judged by a concept matching technique. The most important compounds for Cheddar cheese aroma were butyric acid, diacetyl and methional. A three-way factorial experiment was used to find their optimum concentrations. The optimum mixtures were compared to several Cheddar and non-Cheddar cheeses. Partial agreement was found between the mixtures and the Cheddar cheese concept. They were as Cheddar-like as some true Cheddar cheeses.
Investigation of Diketopiperazines Containing a Guanidino-Functionalized Sidechain as Potential Catalysts of Enantioselective Strecker Reactions
2005
Diketopiperazine 1 consisting of L-(γ-guanidino-α-amino)butyric acid and L-phenylalanine was synthesized as the hydroacetate and as the hydronitrate. Its structure was confirmed by X-ray analysis. In contrast to reports in the literature (Lipton et al.), compound 1 does not induce enantioselevtive catalysis of Strecker reactions. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005)