Search results for "IPR"
showing 10 items of 1515 documents
ProteoPlex: stability optimization of macromolecular complexes by sparse-matrix screening of chemical space.
2015
Molecular machines or macromolecular complexes are supramolecular assemblies of biomolecules that ensure cellular homeostasis. Structure determination of those complexes in a purified state is often a tedious undertaking due to the compositional complexity and the related relative structural instability. To improve the stability of macromolecular complexes in vitro, we present here a generic method that optimizes the stability, homogeneity and solubility of macromolecular complexes by sparse-matrix screening of their thermal unfolding behaviour in the presence of various buffers and small molecules. The method includes the automated analysis of thermal unfolding curves based on a newly deve…
Indicaxanthin, a multi-target natural compound from Opuntia ficus-indica fruit: From its poly-pharmacological effects to biochemical mechanisms and m…
2019
Abstract Over the latest years phytochemical consumption has been associated to a decreased risk of both the onset and the development of a number of pathological conditions. In this context indicaxanthin, a betalain pigment from Opuntia ficus-indica fruit, has been the object of sound research. Explored, at first, for its mere antioxidant potential, Indicaxanthin is now regarded as a redox-active compound able to exert significant poly-pharmacological effects against several targets in a number of experimental conditions both in vivo and in vitro. This paper aims to provide an overview on the therapeutical effects of indicaxanthin, ranging from the anti-inflammatory to the neuro-modulatory…
Synthesis and antiproliferative activity of new derivatives containing the polycyclic system 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3’,4’:2,3]azep…
2013
The reaction under reflux between 1-phenyl-3-R-5-methylaminopyrazoles and 2,5-hexanedione lead to 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3′,4′:2,3]azepino[4,5-f]azocine derivatives 3b–g. These unusual molecules show the structural complexity of many biologically active natural products and are endowed with the chemical diversity that is required in drug discovery. The compounds 3b,e were reduced by hydrogen in the presence of Palladium on activated charcoal to give the dihydro derivatives 5b,e. Compounds 3b–f and 5b,e were selected by the NCI to evaluate their in vitro antiproliferative activity against 60 human cell lines derived from nine clinically isolated cancer types (leukaemia, lu…
β2 integrin phosphorylation on Thr758 acts as a molecular switch to regulate 14-3-3 and filamin binding
2008
AbstractLeukocyte integrins of the β2 family are essential for immune cell-cell adhesion. In activated cells, β2 integrins are phosphorylated on the cytoplasmic Thr758, leading to 14-3-3 protein recruitment to the β2 integrin. The mutation of this phosphorylation site impairs cell adhesion, actin reorganization, and cell spreading. Thr758 is contained in a Thr triplet of β2 that also mediates binding to filamin. Here, we investigated the binding of filamin, talin, and 14-3-3 proteins to phosphorylated and unphosphorylated β2 integrins by biochemical methods and x-ray crystallography. 14-3-3 proteins bound only to the phosphorylated integrin cytoplasmic peptide, with a high affinity (Kd, 261…
Root canal shaping of curved canals by Reciproc Blue system and Pro Taper Gold: A micro-computed tomographic study
2021
Background This study aimed to evaluate the centralization and transportation of ProTaper Gold (PTG) rotary system and Reciproc Blue (RB) reciprocating system in curved canals, by using micro-CT. Material and Methods Twenty extracted mandibular molars were previously scanned by using the SkyScan 1174 microtomograph to select the Vertucci IV anatomic type. The specimens were divided into two groups (n=10) according to the mechanized system used to prepare the root canals. The teeth were scanned by micro-CT to calculate the increase volume, percentage of dentin removed, remaining dentin thickness, structure model index (SMI), degree of transportation and centering ability of root canals. The …
Physics with Antiprotons at the Future GSI Facility
2003
Recently GSI presented the plans for a major new international research facility (http://www.gsi.de/GSI-future/). Highly luminous secondary beams with excellent quality encompassing the production of antiprotons will be delivered. In a High Energy Storage Ring (HESR) with a bending power of 50 Tm antiprotons will be cooled either stochastically or by electrons. The envisaged limits are a momentum range of 1.5 to 15 GeV/c and a luminosity of 2 × 1032 cm-2 s-1. Four major physical research goals can be addressed: high precision charmonium spectroscopy, medium effects of open and hidden charm, the search for glueballs and hybrids, and the production of hypernuclei.
Stereoselective Synthesis and Cytoselective Toxicity of Monoterpene-Fused 2-Imino-1,3-thiazines
2014
Starting from pinane-, apopinane- and carane-based 1,3-amino alcohols obtained from monoterpene-based β-amino acids, a library of monoterpene-fused 2-imino-1,3-thiazines as main products and 2-thioxo-1,3-oxazines as side-products were prepared via two- or three-step syntheses. When thiourea adducts prepared from 1,3-amino alcohols and aryl isothiocyanates were reacted with CDI under mild conditions, O-imidazolylcarbonyl intermediates were isolated which could be transformed to the desired 1,3-thiazines under microwave conditions. 1,3-Thiazines and 2-thioxo-1,3-oxazine side-products could also be prepared in one-step reactions through the application of CDI and microwave irradiation. The rin…
Fundamentos antropológicos en las relaciones interpersonales y de reciprocidad en el pensamiento de Emmanuel Mounier
2013
Uno puede preguntarse si el pensamiento de Emmanuel Mounier es actual o tiene capacidad de influir en el mundo contemporáneo. Sólo basta con echar un vistazo rápido a nuestra realidad actual y aquella que vivió nuestro autor para observar, sobre todo después de los acontecimientos del 11 de septiembre de 2001, las guerras en Irak y Afganistán, las distintas y variadas guerras menores a lo largo del mundo, tras el colapso las bolsas de valores y los mercados en 2008 y 2009, que el mundo nunca había estado tan cerca de una crisis de civilización como aquella crisis de económica del '29 que engendró a la Segunda Guerra Mundial y que parece poner en peligro la propia supervivencia de la cultura…
Drošības faktoru ietekme uz Armēnijas lēmumu pievienoties Muitas savienībai
2016
Darbā analizēta drošības faktoru ietekme uz Armēnijas lēmumu pievienoties Muitas savienībai. Darba mērķis ir noskaidrot, vai Armēnijas lēmums ir saistīts ar tās sarežģīto ģeopolitisko situāciju, vai arī šim lēmumam ir ekonomisks pamatojums. Galvenie darba uzdevumi ir: 1) izvērtēt Armēnijas, Azerbaidžānas un Krievijas varas potenciālu. 2) Analizēt Azerbaidžānas radīto apdraudējumu Armēnijai. 3) Novērtēt Armēnijas attiecības ar tuvākajiem kaimiņiem, ES un Krieviju. 4) Izvērtēt Armēnijas pievienošanās Muitas savienībai ekonomisko pamatotību. Darba teorētisko pieeju veido „pievienošanās stiprākajam” koncepts. Darbā izmantotas gan kvalitatīvās, gan kvantitatīvās pētījumu metodes. Darba rezultāti…
The Acts project: track reconstruction software for HL-LHC and beyond
2019
The reconstruction of trajectories of the charged particles in the tracking detectors of high energy physics experiments is one of the most difficult and complex tasks of event reconstruction at particle colliders. As pattern recognition algorithms exhibit combinatorial scaling to high track multiplicities, they become the largest contributor to the CPU consumption within event reconstruction, particularly at current and future hadron colliders such as the LHC, HL-LHC and FCC-hh. Current algorithms provide an extremely high standard of physics and computing performance and have been tested on billions of simulated and recorded data events. However, most algorithms were first written 20 year…