Search results for "TYR"

Age-related differences of γ-aminobutyric acid (GABA)ergic transmission in human colonic smooth muscle.

2021

Background: Enteric neurons undergo to functional changes during aging. We investigated the possible age-associated differences in enteric γ-aminobutyric acid (GABA)ergic transmission evaluating function and distribution of GABAergic receptors in human colon. Methods: Mechanical responses to GABA and GABA receptor agonists on slow phasic contractions were examined in vitro as changes in isometric tension in colonic muscle strips from young (<65 years old) and aged patients (>65 years old). GABAergic receptor expression was assessed by quantitative RT-PCR. Key Results: In both preparations GABA induced an excitatory effect, consisting in an increase in the basal tone, antagonized by th…

Synthesis and Pharmacological Evaluation of [11C]4-Methoxy-N-[2-(thiophen-2-yl)imidazo[1,2-a]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand S…

2019

The α4/6βδ-containing GABAA receptors are involved in a number of brain diseases. Despite the potential of a δ-selective imaging agent, no PET radioligand is currently available for in vivo imaging...

Design of antitumor drugs targeting c-kit receptor by a new mixed ligand-structure based method

2020

An important challenge, in the medicinal chemistry field, is the research of novel forceful drugs to overcome tumor-acquired resistance. The c-Kit tyrosine kinase receptor (TKR) represents a suitable target for the carcinogenesis control of gastro-intestinal stromal (GIST), leukemia, and mastocytosis tumors; nevertheless, several hotspot mutations of the protein limit the efficacy of a few clinical administered TKRs inhibitors. In this study, a new in silico protocol based on ligand and structure-based combined method is proposed, with the aim to identify a set of new c-Kit inhibitors able to complex c-Kit mutated proteins. A recent and freely available web-server DRUDIT is used for the lig…

Solution properties of polyelectrolytes. III. Effect of sodium polystyrene sulfonate concentration on viscometric and size exclusion chromatographic …

1988

The effect of sodium polystyrene sulfonate concentration on the shape of its molecules in aqueous solution at different NaNO3 ionic strengths has been analyzed by viscometry and size-exclusion chromatography (s.e.c). An equation has been developed which predicts the intrinsic viscosity, [η] p.cp.cs, at finite concentration of both polyion (cp) and electrolyte (cs). The experimental results obtained by both techniques can be accounted for in terms of the theory. Several factors involved in the elution mechanism have been considered and the variation of the slopes of s.e.c. calibration curves with cp and cs has been discussed in terms of polyion conformation changes.

Solution properties of polyelectrolytes. I. Exclusion chromatography of sodium polystyrene sulphonate in salt-free water as eluent

1987

The effect of concentration of sodium polystyrene sulphonate on the elution volume in exclusion chromatography has been investigated using salt-free water as eluent. A non-linear increase in the elution volume has been observed with increasing injected sample concentration. Concentration-dependent calibrations have been obtained which approach the universal calibration for uncharged polymers (dextrans) as polyelectrolyte concentration increases. The separation mechanisms are interpreted in terms of electrostatic and hydrodynamic interactions. A semi-empirical model is proposed to predict concentration effects of linear polyions in exclusion chromatography and good agreement has been found b…

Zur Gelpermeationschromatographie in organischen Lösungsmitteln

1965

Die Gelpermeationschromatographie hat sich vor allem mittels der Sephadexgele fur die Trennung polymerhomologer wasserloslicher Makromolekule als sehr erfolgreich erwiesen. Die Trennung nur in organischen Losungsmitteln loslicher Polymerer ist erst in jungster Zeit gelungen, wobei vernetzte Polystyrol-, Polymethacrylat- und Dextranderivatgele benutzt werden. Der Mechanismus dieses chromatographischen Prozesses wird untersucht. Ein Vergleich dieses Vorganges, bei dem das Polymere nur in einer Phase vorliegt, mit den klassischen Methoden, die mit Auftrennung in zwei Phasen arbeiten, wird durchgefuhrt. Insbesondere werden die Methoden der Dreiecks-Fallungsfraktionierung, der Kolonnentechnik mi…

Disproportionierung und Kombination als Abbruchsmechanismen bei der radikalischen Polymerisation von Styrol, 2. Analyse der temperaturabhängigkeiten

1975

Styrol wurde in Substanz mit 14C-markiertem 2,2′-Azoisobutyronitril im Temperatur-bereich von 30 bis 80°C polymerisiert. Aus der Polymerisationsgeschwindigkeit und der Anzahl der radioaktiven Endgruppen im Polymeren wurden die Effektivitat des Starters f und die Verhaltnisse der Geschwindigkeitskonstanten fur Wachstum, Abbruch und Start k/ka und ka, PR/(kwkst) berechnet. Die Bestimmung der Molekulargewichtsverteilungen mit Hilfe der Gelpermeationschromatographie ermoglichte es, die Ubertragungskonstante CM und das Verhaltnis ka, disp/ka, comb zu berechnen. Die Temperaturabhangigkeiten der Geschwindigkeitskonstanten erwiesen sich als physikalisch sinnvoll. Styrene was bulk polymerised by ini…

Disproportionierung und kombination als abbruchmechanismen bei der radikalischen polymerisation von styrol, 1.Versuche mit 14C-markierten 2,2′-azoiso…

1975

Die Substanzpolymerisation von Styrol mit 14C-markiertem 2,2′-Azoisobutyronitril (AIBN) wurde bei 52°C experimentell untersucht. Die Polymerisation wurde dilatometrisch verfolgt, die Molekulargewichte der entstandenen Polymeren viskosimetrisch ermit-telt, der Gewichtsbruch der einkettigen Molekule gelchromatographisch bestimmt und die Anzahl der markierten Endgruppen ausgezahlt. Die eingehende kinetische Analyse erhartet die neueren Erkenntnisse uber den Abbruchmechanismus. Danach liegt bei der Polymerisation von Styrol neben der Kombination auch Disproportionierung vor. Bulk polymerisation of styrene initiated by 14C-labelled 2,2′-azoisobutyronitrile (AIBN) was studied at 52°C. The polymer…

Anaplastic lymphoma kinase expression in neuroblastomas and its relationship with genetic, prognostic, and predictive factors

2011

Oxidative stress inhibits IFN-α-induced antiviral gene expression by blocking the JAK–STAT pathway

2006

Abstract BACKGROUND/AIMS: Unresponsiveness to IFN-alpha is common in chronic hepatitis C. Since conditions associated with an increased oxidative stress (advanced age, steatosis, fibrosis, iron overload, and alcohol consumption) reduce the likelihood of response, we hypothesized that oxidative stress may affect the antiviral actions of IFN-alpha. METHODS: We examined in a human hepatocellular carcinoma cell line (Huh-7) the effect of hydrogen peroxide (H2O2), as a generator of oxidative stress, on the IFN-alpha signaling pathway. RESULTS: Pretreatment of Huh-7 cells with 0.5-1 mM H2O2 resulted in the suppression of the IFN-alpha-induced antiviral protein MxA and of IRF-9 mRNA expression. Th…