Search results for "AAS"
showing 10 items of 1173 documents
Structure-Activity Relationship Analysis of 3-Phenylcoumarin-Based Monoamine Oxidase B Inhibitors
2018
Monoamine oxidase B (MAO-B) catalyzes deamination of monoamines such as neurotransmitters dopamine and norepinephrine. Accordingly, small-molecule MAO-B inhibitors potentially alleviate the symptoms of dopamine-linked neuropathologies such as depression or Parkinson's disease. Coumarin with a functionalized 3-phenyl ring system is a promising scaffold for building potent MAO-B inhibitors. Here, a vast set of 3-phenylcoumarin derivatives was designed using virtual combinatorial chemistry or rationally de novo and synthesized using microwave chemistry. The derivatives inhibited the MAO-B at 100 nM−1 μM. The IC50 value of the most potent derivative 1 was 56 nM. A docking-based structure-activi…
Identification and structural characterization of LytU, a unique peptidoglycan endopeptidase from the lysostaphin family
2017
AbstractWe introduce LytU, a short member of the lysostaphin family of zinc-dependent pentaglycine endopeptidases. It is a potential antimicrobial agent for S. aureus infections and its gene transcription is highly upregulated upon antibiotic treatments along with other genes involved in cell wall synthesis. We found this enzyme to be responsible for the opening of the cell wall peptidoglycan layer during cell divisions in S. aureus. LytU is anchored in the plasma membrane with the active part residing in the periplasmic space. It has a unique Ile/Lys insertion at position 151 that resides in the catalytic site-neighbouring loop and is vital for the enzymatic activity but not affecting the …
Real life experiences in HCV management in 2018
2019
Introduction: Hepatitis C virus (HCV) infection is a major cause of chronic liver disease, with approximately 71 million chronically infected individuals worldwide. Treatment of chronic hepatitis C has considerably improved in the last few years thanks to the introduction of direct-acting antivirals able to achieve sustained virological response in more than 95% of patients. Successful anti-HCV treatment can halt liver disease progression and solve the HCV-related extra-hepatic manifestations, eventually reducing liver-related and overall mortality. Areas covered: With the aim to respond to unmet needs in patient’s identification, universal access to antiviral therapy and treatment optimiza…
Phosphorylated immunoreceptor tyrosine-based activation motifs and integrin cytoplasmic domains activate spleen tyrosine kinase via distinct mechanis…
2018
Spleen tyrosine kinase (Syk) is involved in cellular adhesion and also in the activation and development of hematopoietic cells. Syk activation induced by genomic rearrangement has been linked to certain T-cell lymphomas, and Syk inhibitors have been shown to prolong survival of patients with B-cell lineage malignancies. Syk is activated either by its interaction with a double-phosphorylated immunoreceptor tyrosine-based activation motif (pITAM), which induces rearrangements in the Syk structure, or by the phosphorylation of specific tyrosine residues. In addition to its immunoreceptor function, Syk is activated downstream of integrin pathways, and integrins bind to the same region in Syk a…
Toxicity of biomining effluents to Daphnia magna: Acute toxicity and transcriptomic biomarkers
2018
Increasing metal consumption is driving the introduction of new techniques such as biomining to exploit low grade ores. The biomining impacts notably aquatic ecosystems, yet, the applicability of ecotoxicological tests to study the complex mixture effects of mining waters is insufficiently understood. The aim of the present work was to test if transcriptomic biomarkers are suitable and sensitive for the ecotoxicity assessment of biomining affected waters. The study site had been affected by a multimetal biomine, and the studied water samples formed a concentration gradient of contamination downstream from the biomining site. Cadmium and nickel were used as positive controls in the toxicity …
Trend of Drug Abuse in 2011– 2014 in Italy
2017
Doping, although was born as a medication and not with the purpose of enhancing performance, is a widespread practice in all sports, between amateur and gym-goers. The Italian sports federations were in second place worldwide for positive doping-test, after Russia. This review focuses on the analysis of data collected by Italian National Olympic Committee (CONI) in the 2012–2014 period, showing that the most commonly used substances were anabolic androgenic agents, glucocorticoids, diuretics and stimulants. Prevention in doping could be a key to limit the damage caused by this harmful practice both, for the physical health and the athlete’s moral integrity and anti-doping campai…
Narratives of Burnout and Recovery from an Agency Perspective : A Two-Year Longitudinal Study
2017
Abstract Purpose To provide knowledge about the recovery process during rehabilitation and two years later by exploring the manifestation of agency and spheres of meaning in the narratives of participants in a national rehabilitation course. Material and methods The subjects of the study were four participants in a national rehabilitation course, whose burnout levels had decreased between the initial and follow-up periods of the course. Semi-structured interviews on two occasions and an electronic questionnaire 1.5 years post rehabilitation comprised the main material. In addition, the BBI -15 (Bergen Burnout Indicator) and DEPS-screen were used. Results Thematic narrative analysis revealed…
‘It has given me this kind of courage…’: the significance of CLIL in forming a positive target language self-concept
2019
This article sets out to broaden the understanding of foreign language self-concept in CLIL context. The few existing studies on self-concept in CLIL have been quantitative and provided somewhat discrepant results, highlighting the need for approaching the topic qualitatively. The data of the present study are in-depth interviews with 24 former Finnish CLIL pupils who retrospectively reflected on their CLIL experiences. The participants had received English-medium CLIL for nine years during their comprehensive school in the 1990s. The data were analyzed qualitatively using thematic analysis. The participants generally felt that CLIL had had a significant role in contributing to their very p…