Search results for "taas"
showing 10 items of 18 documents
Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives
2018
A comprehensive set of 3-phenylcoumarin analogues with polar substituents was synthesised for blocking oestradiol synthesis by 17-b-hydroxysteroid dehydrogenase 1 (HSD1) in the latter part of the sulphatase pathway. Five analogues produced 62% HSD1 inhibition at 5 mM and, furthermore, three of them produced 68% inhibition at 1 mM. A docking-based structure-activity relationship analysis was done to determine the molecular basis of the inhibition and the cross-reactivity of the analogues was tested against oestrogen receptor, aromatase, cytochrome P450 1A2, and monoamine oxidases. Most of the analogues are only modestly active with 17-b-hydroxysteroid dehydrogenase 2 – a requirement for lowe…
Characterization of sulfhydryl oxidase from Aspergillus tubingensis
2017
Background Despite of the presence of sulfhydryl oxidases (SOXs) in the secretomes of industrially relevant organisms and their many potential applications, only few of these enzymes have been biochemically characterized. In addition, basic functions of most of the SOX enzymes reported so far are not fully understood. In particular, the physiological role of secreted fungal SOXs is unclear. Results The recently identified SOX from Aspergillus tubingensis (AtSOX) was produced, purified and characterized in the present work. AtSOX had a pH optimum of 6.5, and showed a good pH stability retaining more than 80% of the initial activity in a pH range 4-8.5 within 20 h. More than 70% of the initia…
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…
Creating stable Floquet–Weyl semimetals by laser-driving of 3D Dirac materials
2017
Nature Communications 8, 13940 (2017). doi:10.1038/ncomms13940
Elizabeth Strout: Olive, taas
2021
Kirja-arvostelu teoksesta Elizabeth Strout, Olive, taas, Tammi, s.354, suom. Kristiina Rikman nonPeerReviewed
Coin repas, intérieur nuit : analyse pragmatique et cinématographique d'une scène de Conte de printemps d'Eric Rohmer: les actes de discours et le…
2003
Svina noteikšanas iespējas asinīs ar instrumentālajām analīzes metodēm, izmantojot dažādus paraugu sagatavošanas veidus
2017
Svina noteikšanas iespējas asinīs ar instrumentālajām analīzes metodēm, izmantojot dažādus paraugu sagatavošanas veidus. Ribkinska L., darba vadītājas Dr. med. Inese Mārtiņsone un Dr. Chem. Agnese Osīte. Maģistra darbs, 45 lappuses, 18 attēli, 12 tabulas, 45 literatūras avoti, 18 pielikumi. Latviešu valodā. Maģistra darbā ir apkopota literatūra par instrumentālajām analīzes metodēm (ETAAS un ICP-MS), paraugu sagatavošanas metodēm un svina toksisko iedarbību uz cilvēka veselību. Eksperimentālajā daļā veikta svina masas koncentrācijas noteikšana asinīs, izmantojot dažādus paraugu sagatavošanas veidus. Paraugu sagatavošanas metodēm veikta to salīdzināšana, kā arī rezultātu pareizības kontrolei…
Short films : dispersive effects of clip thinking
2013
The New Media have a vast influence on human mind and its cognitive functions. Clip thinking is a state of perception, knowledge and, therefore, consciousness that is formed by the perceptual patterns based on deconstruction of narratives. Practically, the main symptoms of clip thinking are the following: the lack of concentration while dealing with narratives, the incline to multitask work and random access to the information as well as an urge for immediate answers and the frustration if such an answer is impossible to get. Clip thinking is based on the database logic as an opposite to narrative. The present thesis discusses the clip thinking in terms of New Media theory of Lev Manovich a…
Small molecule modulators of amine oxidation, nuclear receptor signaling and glucuronidation : 3-phenylcoumarin as a scaffold of interest
2018
The costs of the drug development process are moderated as computer-aided drug design methods are able to expedite the steps required for lead identification. In fact, computational tools are nowadays virtually indispensable from target identification and validation to preclinical tests due to exponential growth of available information regarding both potential targets and small molecules. One such small molecule with growing number of variations is coumarin. Coumarin scaffold and its various derivatives continue to interest researchers for their vast application potential. Since naturally occurring coumarins are known for example for their antioxidant and anti-inflammatory properties, thos…