Search results for "ISM [Radio continuum]"
showing 10 items of 703 documents
Apoptotic activities of Mediterranean plants
2020
Medicinal plants from the Mediterranean region show great potential in the improvement of health and in the prevention of disease. Epidemiological studies indicate that some of these plants reduce the incidence of inflammatory diseases and cancer by inducing programmed cell death, thus arresting proliferation. These medicinal properties are related to the presence of compounds such as phenolics with antioxidant properties or nonphenolic compounds, including essential oils, terpenoids, or saponins. Our aim is to review role of different medicinal plants and phytochemicals in apoptosis and disease prevention and the mechanism of action implicated in these beneficial effects. Sin financiación …
Development of a second generation of inhibitors of microsomal prostaglandin E synthase 1 expression bearing the γ-hydroxybutenolide scaffold
2008
Petrosaspongiolide M (PM), a marine sesterterpene metabolite bearing the gamma-hydroxybutenolide scaffold and displaying a potent inhibitory activity toward PLA(2) enzyme, was selected by us as an attractive target in order to explore its mechanism of action at molecular level. In the course of our investigations we decided to synthetically modify the parent compound to clarify the structural determinants responsible for the activity; in fact, very recently, our research group reported the synthesis and the pharmacological properties of a first collection of PM analogues generated by Ludi approach. The synthesized compounds showed a poor or moderate activity toward PLA(2) enzymes, neverthel…
Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
2002
Crystal structure and co-regulator interaction studies have led to a general mechanistic view of the initial steps of nuclear receptor (NR) action. Agonist-induced transconformation of the ligand-binding domain (holo-LBD) leads to the formation of co-activator complexes, and destabilizes the co-repressor complexes bound to the ligand-free (apo) LBD. However, the molecular basis of retinoid-X receptor (RXR) 'subordination' in heterodimers, an essential mechanism to avoid signalling pathway promiscuity, has remained elusive. RXR, in contrast to its heterodimer partner, cannot autonomously induce transcription on binding of cognate agonists. Here we show that RXR can bind ligand and recruit co…
An overview on chemical structures as ΔF508-CFTR correctors
2019
Deletion of phenylalanine at position 508 (F508del) in the CFTR protein, is the most common mutation causing cystic fibrosis (CF). F508del causes misfolding and rapid degradation of CFTR protein a defect that can be targeted with pharmacological agents termed “correctors”. Correctors belong to various chemical classes but are generally small molecules based on nitrogen sulfur or oxygen heterocycles. The mechanism of action of correctors is generally unknown but there is experimental evidence that some of them can directly act on mutant CFTR improving folding and stability. Here we overview the characteristics of the various F508del correctors described so far to obtain indications on key ch…
Heat shock protein 27 is involved in SUMO-2/3 modification of heat shock factor 1 and thereby modulates the transcription factor activity
2009
Heat shock protein 27 (HSP27) accumulates in stressed cells and helps them to survive adverse conditions. We have already shown that HSP27 has a function in the ubiquitination process that is modulated by its oligomerization/phosphorylation status. Here, we show that HSP27 is also involved in protein sumoylation, a ubiquitination-related process. HSP27 increases the number of cell proteins modified by small ubiquitin-like modifier (SUMO)-2/3 but this effect shows some selectivity as it neither affects all proteins nor concerns SUMO-1. Moreover, no such alteration in SUMO-2/3 conjugation is achievable by another HSP, such as HSP70. Heat shock factor 1 (HSF1), a transcription factor responsib…
Longitudinal CSF proteome profiling in mice to uncover the acute and sustained mechanisms of action of rapid acting antidepressant (2R,6R)-hydroxynor…
2021
Delayed onset of antidepressant action is a shortcoming in depression treatment. Ketamine and its metabolite (2R,6R)-hydroxynorketamine (HNK) have emerged as promising rapid-acting antidepressants. However, their mechanism of action remains unknown. In this study, we first described the anxious and depression-prone inbred mouse strain, DBA/2J, as an animal model to assess the antidepressant-like effects of ketamine and HNK in vivo. To decode the molecular mechanisms mediating HNK's rapid antidepressant effects, a longitudinal cerebrospinal fluid (CSF) proteome profiling of its acute and sustained effects was conducted using an unbiased, hypothesis-free mass spectrometry-based proteomics app…
The role of gut micorbiome in obesity and diabetes
2019
Background Obesity and diabetes became a grooving problem in both adults and children. Many hypotheses concerned agents involved in the excessive weight gain process and it’s consequences. Not only genetic or environmental factors, but also intestinal microbiome seems to play a role in the pathophysiology of this phenomenon. Data sources A systematic review was conducted using Pubmed as the medical database source. Studies concerning connection between microbiome and metabolic disorders such as obesity and diabetes from last 10 years were analyzed. Results Intestinal bacteria may be involved both in the development of obesity, and its further complications. The pro-infammatory and immunomod…
Measuring Seasonality: Performance of Accommodation Establishments in Sicily through the analysis of Occupancy Rates
2011
Tourism, more than other fields, needs to be managed. As such, the provision of reliable information and adequate tools is one of the major challenges to monitor and to manage tourism destinations. Sicily (Italy) seems to have a great potential coming from its tourism resources, and most of the recent development programs have been focused on tourism. In line with the world’s trend, tourism in Sicily faced a growth in terms of overnight stays, from about 9 millions in 1994, to more than 14 millions in 2007. The regional expenditure in tourism from 1996 to 2006 was of euro 785 millions (Federalberghi, 2007), which ranks Sicily as the second region in Italy for tourism expenditure, in the yea…
Sobolev Extension on Lp-quasidisks
2021
AbstractIn this paper, we study the Sobolev extension property of Lp-quasidisks which are the generalizations of classical quasidisks. After that, we also find some applications of this property.
Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[2E]-3-phenylprop-2-enoylamino}benzamides
2011
Several new 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides 12a–s and 17t–v were synthesized by stirring in pyridine the (E)-3-(2-R1-3-R2-4-R3-phenyl)acrylic acid chlorides 11c–k and 11t–v with the appropriate anthranilamide derivatives 10a–c or the 5-iodoanthranilic acid 13. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). COMPARE analysis, effects on tubulin polymerization in cells and with purified tubulin, and effects on cell cycle distribution for 17t, the mo…