Search results for " inhibition"
showing 10 items of 435 documents
Sugar specific cellular lectins of Phallusia mamillata hemocytes: Purification, characterization and evidence for cell surface localization
1989
Cellular lectins (CLs) of Phallusia mamillata were demonstrated in protein preparations obtained by salt fractionation from hemocytes sonicated in a suitable medium. Since the lectins from the precipitated fraction bind sugars containing D-galactosyl groups, they were purified by affinity chromatography on Sepharose. SDS-PAGE under reducing conditions showed that CLs are formed of two components of apparent MWs approximately 36,900 and 35,090 and thus differ from serum lectins (SLs) (MW about 62,200). The "shrinkage" observed when SLs were examined under nonreducing conditions suggest the presence of intrachain disulphide bonds which can affect the molecular structure of the SLs. CL-SL diff…
The action of iontophoretically applied acetylcholine and dopamine on single claustrum neurones in the cat.
1981
Abstract The effects of iontophoretically applied acetyl-choline (ACh) and dopamine (DA) on spontaneously active claustral neurones, in chloralose-anaesthetised cats, have been investigated. Acetylcholine had both facilitatory and inhibitory effects in almost the same proportions. The action of DA was prevalently inhibitory. Two types of inhibitory response to ACh and DA are described: short-lasting inhibition and long-lasting inhibition. The excitatory response always outlasted the period of drug application.
Single-digit nanomolar inhibitors lock the aromatase active site via a dualsteric targeting strategy
2022
The most frequently diagnosed breast cancer (BC) type in women expresses estrogen receptor (ER) , depends on estrogens for its growth, being classified as ER positive (ER+). The gold standard therapy for the treatment of this tumor relies on the inhibition of the aromatase enzyme, which catalyzes estrogen biosynthesis. Despite the clinical success of current aromatase inhibitors (AIs), after prolonged therapeutic regimens, BC ER + patients experience acquired resistance and disease relapse. This points up the urgent need for a newer generation of AIs able to overcome resistance issues, while mitigating toxicity and side effects of current therapies. Here we performed the synthesis, biologic…
2,3,7,8-Tetrachlorodibenzo-p-dioxin-Dependent Release from Contact Inhibition in WB-F344 Cells: Involvement of Cyclin A
2002
2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is the most potent tumor promoter ever tested in rodents. Although it is known that most of TCDD actions are mediated by binding to the aryl hydrocarbon receptor (AhR), the mechanisms leading to tumor promotion still remain to be elucidated. Loss of contact inhibition is one characteristic hallmark in tumorigenesis. In rat liver epithelial WB-F344 cells, TCDD induces a release from contact inhibition, which is manifested by a twofold increase in cell number when TCDD (1 nM for 48 h) is added to confluent cells in the presence of serum, but not when given to exponentially growing or subconfluent, serum-deprived WB-F344 cells. Loss of G1 arrest was a…
Manipulation of glycolysis in malignant tumors: fantasy or therapy?
2009
After Warburg stated his hypothesis on tumor cell metabolism about 80 years ago, the field of carbohydrate metabolism of cancer cells and solid tumors is experiencing a boom for the past few years. Numerous studies have been focused on the characteristics of cancer metabolism and its accessibility to novel therapeutic interventions. Malignant transformation is associated with an increase in glycolytic flux, mainly caused by an upregulation of numerous glycolysis-related genes in the majority of human cancers. As a consequence of these alterations, tumor cells are producing lactate at higher levels compared to non-malignant tissue, even in the presence of oxygen, a phenomenon termed “aerobic…
Left but not right temporal involvement in opaque idiom comprehension: a repetitive transcranial magnetic stimulation study
2004
Abstract It has been suggested that figurative language, which includes idioms, is controlled by the right hemisphere. We tested the right hemisphere hypothesis by using repetitive transcranial magnetic stimulation (rTMS) to transiently disrupt the function of the frontal and temporal areas of the right versus left hemisphere in a group of normal participants involved in a task of opaque idiom versus literal sentence comprehension. Forty opaque, nonambiguous idioms were selected. Fifteen young healthy participants underwent rTMS in two sessions. The experiment was run in five blocks, corresponding to the four stimulated scalp positions (left frontal and temporal and right frontal and tempor…
Effect of angular velocity on soleus and medial gastrocnemius H-reflex during maximal concentric and eccentric muscle contraction.
2009
At rest, the H-reflex is lower during lengthening than shortening actions. During passive lengthening, both soleus (SOL) and medial gastrocnemius (MG) H-reflex amplitudes decrease with increasing angular velocity. This study was designed to investigate whether H-reflex amplitude is affected by angular velocity during concentric and eccentric maximal voluntary contraction (MVC). Experiments were performed on nine healthy men. At a constant angular velocity of 60 degrees /s and 20 degrees /s, maximal H-reflex and M-wave potentials were evoked at rest (i.e., H(max) and M(max), respectively) and during concentric and eccentric MVC (i.e., H(sup) and M(sup), respectively). Regardless of the muscl…
Turing Patterns in Nonlinear Optics
2000
The phenomenon of pattern formation in nonlinear optical resonators is commonly related to an off-resonance excitation mechanism, where patterns occur due to mismatch between the excitation and resonance frequency. In this paper we show that the patterns in nonlinear optics can also occur due to the interplay between diffractions of coupled field components. The reported mechanism is analogous to that of local activation and lateral inhibition found in reaction-diffusion systems by Turing. We study concretely the degenerate optical parametric oscillators. A local activator-lateral inhibitor mechanism is responsible for generation of Turing patterns in form of hexagons.
l-Tyrosine β-naphthylamide is a potent competitive inhibitor of tyramine N-(hydroxycinnamoyl)transferase in vitro
2001
L-Tyrosine beta-naphthylamide, a synthetic substrate designed to measure tyrosine aminopeptidase activity, is a potent inhibitor of hydroxycinnamoyl-CoA:tyramine N-(hydroxycinnamoyl)transferase (THT) purified from elicited tobacco cell-suspension cultures. The inhibition is competitive, with the inhibitor binding reversibly to the tyramine binding site of the enzyme. Similar results were obtained with THT extracted from elicited potato cell-suspension cultures. Ki values were found to be 0.66 microM for the enzyme from tobacco and 0.3 microM for the enzyme from potato. L-Tyrosine 7-amido-4-methylcoumarin, a fluorogenic substrate for tyrosine aminopeptidases, the structure of which is close …
Platelet function testing in pigs using the Multiplate® Analyzer.
2019
PLOS ONE 14(8), e0222010 (2019). doi:10.1371/journal.pone.0222010