Search results for " inhibition"
showing 10 items of 435 documents
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
2014
Given our interest in finding potential antitumor agents and in view of the multifactorial mechanistic nature of cancer, in the present work, taking advantage of the multifunctional ligands approach, new chimeric molecules were designed and synthesized by combining in single chemical entities structural features of SAHA, targeting histone deacetylases (HDACs), with substituted stilbene or terphenyl derivatives previously obtained by us and endowed with antiproliferative and pro-apoptotic activity. The new chimeric derivatives were characterized with respect to their cytotoxic activity and their effects on cell cycle progression on different tumor cell lines, as well as their HDACs inhibitio…
Combined Targeting of the Menin-MLL1 Chromatin Complex and FLT3 As a Novel Therapeutic Concept Against NPM1 Mutant or MLL-Rearranged AML with Mutated…
2019
NPM1mutant (NPM1mut) and MLL1-rearranged (MLL-r) acute myeloid leukemias (AMLs) exhibit aberrant expression of HOX and MEIS1 transcription factors and commonly harbor an activating mutation in the receptor tyrosine kinase FLT3. Pharmacologic inhibition of the menin-MLL1 complex reverses leukemogenic gene expression including MEIS1 and FLT3 and represents a therapeutic opportunity for the treatment of these leukemias. Here, we investigate the contribution of the menin-MLL1 complex to leukemic FLT3 signaling and assess the therapeutic potential of dual menin-MLL1 and FLT3 targeting. First, we performed RNA sequencing to delineate transcriptional changes associated with menin-MLL1 inhibition (…
Biogenic iron-silver nanoparticles inhibit bacterial biofilm formation due to Ag+ release as determined by a novel phycoerythrin-based assay
2020
Silver nanoparticles (Ag-NPs) can be considered as a cost-effective alternative to antibiotics. In the presence of Fe(III)-citrate and Ag+, Klebsiella oxytoca DSM 29614 produces biogenic Ag-NPs embedded in its peculiar exopolysaccharide (EPS). K. oxytoca DSM 29614 was cultivated in a defined growth medium–containing citrate (as sole carbon source) and supplemented with Ag+ and either low or high Fe(III) concentration. As inferred from elemental analysis, transmission and scanning electron microscopy, Fourier transform infrared spectrometry and dynamic light scattering, Ag-EPS NPs were produced in both conditions and contained also Fe. The production yield of high-Fe/Ag-EPS NPs was 12 times …
Disruption of Slc4a10 augments neuronal excitability and modulates synaptic short-term plasticity
2015
Slc4a10 is a Na(+)-coupled Cl(-)-HCO3 (-) exchanger, which is expressed in principal and inhibitory neurons as well as in choroid plexus epithelial cells of the brain. Slc4a10 knockout (KO) mice have collapsed brain ventricles and display an increased seizure threshold, while heterozygous deletions in man have been associated with idiopathic epilepsy and other neurological symptoms. To further characterize the role of Slc4a10 for network excitability, we compared input-output relations as well as short and long term changes of evoked field potentials in Slc4a10 KO and wildtype (WT) mice. While responses of CA1 pyramidal neurons to stimulation of Schaffer collaterals were increased in Slc4a1…
Mechanism underlying the inhibitory sidebands in the receptive field of simple striate cells of the cat: pure on/off antagonism only or true inhibiti…
1985
The intrinsic organization of the receptive fields of simple striate cells revealed by moving stimuli is much more complex than could have been suspected from the use of stationary ones. There is, in fact, a small excitatory region centrally located in these receptive fields and an inhibitory region encompassing the whole excitatory component. These inhibitory regions or “inhibitory sidebands”, were identified by stimulating the cells with bars of light against anartificial background discharge produced by repeated asynchronous stimulation of the excitatory component of the cell's receptive field. For a long time' these inhibitory sidebands have been accounted for on the basis of the recept…
Study on the transient characteristic in the human visual system using masking experiments
1979
In this paper the visual masking effect is interpreted on the basic of the transient characteristic in two dimensional neuronal networks. The study investigates the suitability of the effect for use as a measurement method. It is shown that the stimulus distribution in space can be scanned at different points in time and that various dynamic characteristic values of the system can be measured.
Neuronal network characteristics in the cat superior colliculus
1977
The system theoretical description of the superficial layers of neurons in the cat's superior colliculus is based on homogeneous linear space-time filters. The most important neurophysiological findings on the superior colliculus are simulated on the digital computer by generating suitable coupling functions and matching the space and time parameters. It is shown that the neurophysiological measurements can be interpreted by varying a few system parameters. The curves of velocity dependent responses, direction specificity and the effects of the colliculus specific surround are examined in particular. Computer simulation shows that such a surround can evaluate small moving stimuli differentl…
Coupling of electrochemical, electrogravimetric and surface analysis techniques to study dithiocarbamate/bronze interactions in chloride media
2018
International audience; Interaction between ammonium pyrrolidinedithiocarbamate (PDTC) and bronze in 30 g L-1 NaCl was investigated at several concentrations between 0.1 and 10 mM by means of various electrochemical and spectroscopic techniques. Electrochemical measurements revealed a fast adsorption process of PDTC on Cu and Pb and the formation of a thick insulating and protective film with a high surface coverage. At high concentrations, PDTC prevents oxides formation. Surface analyses confirm PDTC adsorption on bronze mainly via interaction between sulphur atoms and Cu sites to form Cu I-PDTC complex.
ChemInform Abstract: Synthesis and Antineoplastic Activity of New 4-Diazopyrazole Derivatives.
2010
Several new 4-diazopyrazole derivatives were synthesized by reaction of 1-(R-substituted)phenyl-3-methyl-5-benzamidopyrazoles with a sevenfold excess of nitrous acid in acetic media. The compounds were tested at 20 microM concentration for their antineoplastic activity in vitro against Raji (human Burkitt lymphoma), K562 (human chronic myelogenous leukemia) and U937 (human histiocytic lymphoma) cell lines. They showed a percent of growth inhibition in the range 23.4-100%.
Phytosterols: to be or not to be toxic; that is the question
2008
Plant sterols (phytosterols) are membrane constituents of all plants with a structure analogous to that of cholesterol. Thus, phytosterols have either an additional methyl or ethyl group on the carbon-24 position or an additional double bond in the side chain (1) . Noteworthy, in patients with the rare inherited disease of phytosterolaemia characterized by a hyperabsorption and diminished biliary secretion of cholesterol and phytosterols as well as by tendon and tuberous xanthoma, elevated plasma concentrations of phytosterols (campesterol, sitosterol) have been shown to constitute a risk factor for premature atherosclerosis (2) . However, whether plasma concentrations of campesterol and si…