Search results for "PIP"

CCDC 1420811: Experimental Crystal Structure Determination

2018

Related Article: Inese Sarceviča, IlzeGrante, Sergey Belyakov, Toms Rekis, Kārlis Bērziņš, Andris Actiņš, Liāna Orola|2016|J.Pharm.Sci.|105|1489|doi:10.1016/j.xphs.2016.01.024

CCDC 1891128: Experimental Crystal Structure Determination

2020

Related Article: Marcos Escolano, Marta Guerola, Javier Torres, Daniel Gaviña, Gloria Alzuet-Piña, María Sánchez-Rosello, Carlos del Pozo|2020|Chem.Commun.|56|1425|doi:10.1039/C9CC09113K

2019

Glycogen synthase kinase-3β (GSK-3β) represents a relevant drug target for the treatment of neurodegenerative pathologies including Alzheimer’s disease. We herein report on the optimization of a novel class of GSK-3β inhibitors based on the tofacitinib-derived screen hit 3-((3R,4R)-3-((7-chloro-9H-pyrimido[4,5-b]indol-4-yl)(methyl)amino)-4-methylpiperidin-1-yl)-3-oxopropanenitrile (1). We synthesized a series of 19 novel 7-chloro-9H-pyrimido[4,5-b]indole-based derivatives and studied their structure–activity relationships with focus on the cyanoacetyl piperidine moiety. We unveiled the crucial role of the nitrile group and its importance for the activity of this compound series. A successfu…

Stochastic response of offshore structures by a new approach to statistical cubicization

2001

This study presents a new statistical cubicization approach for predicting the stochastic response of offshore platforms subjected to a Morison-type nonlinear drag loading. Statistics of the original system are obtained from an equivalent nonlinear system, which is constructed by replacing the Morison drag force by a cubic polynomial function of the relative fluid-structure velocity, up to cubic order. A Volterra series expansion with a finite Fourier series representation is used to approximate the response of the equivalent system. Exact solutions are developed to express the Fourier coefficients of the second and third-order response as functions of the Fourier coefficients of the first-…

Data-independent acquisition strategies for quantitative proteomics

2013

In shotgun proteomics, data-dependent precursor acquisition (DDA) is widely used to profile protein components in complex samples. Although very popular, there are some inherent limitations to the DDA approach, such as irreproducible precursor ion selection, under-sampling and long instrument cycle times. Unbiased ‘data-independent acquisition’ (DIA) strategies try to overcome those limitations. In MSE, which is supported by Waters Q-TOF instrument platforms, such as the Synapt G2-S, a wide band pass filter is used for precursor selection. During acquisition, alternating MS scans are collected at low and high collision energy (CE), providing precursor and fragment ion information, respectiv…

Analyses of single- and two-phase flow pressure drops in helical pipes using a modified RELAP5 code

2012

Abstract Thermal fluid dynamics analyses on single- and two-phase flows in helical pipes of steam generators to be used in Generation III and IV nuclear reactors have been performed. The study concerned with experimental activities as well code simulations carried out in the framework of a collaboration between the Department of Energetics of the Polytechnic of Torino and the Department of Energy of the University of Palermo. The goal was the validation of models implemented in Relap5/Mod3.2β thermal–hydraulic advanced code to simulate the hydrodynamic behaviour of helical pipe components in spite of the one-dimensional nature of the code. It is shown that much of the experimental data obta…

Proton Direct Ionization in Sub-Micron Technologies: Numerical Method for RPP Parameter Extraction

2022

This work introduces a numerical method to iteratively extract parameters of a rectangular parallelepiped (RPP) sensitive volume (SV) from experimental proton direct ionization SEU data. The method combines two separate numerical models. The first model estimates the average LET values for energetic ions, including protons and also heavy ions, in elemental solid targets. The second model describes the statistical variance in the energy deposition events of projectile-induced primary ionization within a RPP shaped target volume. To benchmark the method, simulated cross-section values based on RPP parameters derived with this method are compared with literature data from four SRAM devices. Th…

Effects of the MDM2 inhibitor Nutlin-3a on sensitivity of pancreatic cancer cells to berberine and modified berberines in the presence and absence of…

2021

Abstract Approaches to improve pancreatic cancer therapy are essential as this disease has a very bleak outcome. Approximately 80% of pancreatic cancers are pancreatic ductal adenocarcinomas (PDAC). A key regulatory gene frequently mutated (∼75%) in PDAC is the TP53 tumor suppressor gene which controls the transcription of multiple genes involved in cell cycle progression, apoptosis, cancer progression and other growth regulatory processes. The mouse double minute 2 homolog (MDM2) gene product is a nuclear-localized E3 ubiquitin ligase and negatively regulates the TP53 protein which results in its proteasomal degradation. Various MDM2 inhibitors have been isolated and examined in clinical t…

Phenology of Migratory Bat Activity Across the Baltic Sea and the South-Eastern North Sea

2014

We compiled the available information on the occurrence and timing of migratory bat activity across the Baltic Sea and south-eastern North Sea coasts and islands, based on ultrasonic monitoring projects at 19 localities in 2007–2009. The data refer to three species; Nathusius' pipistrelle Pipistrellus nathusii, soprano pipistrelle P. pygmaeus and common noctule Nyctalus noctula. Pipistrellus nathusii occurred at all sites (north to 61°N in Finland), while the other species were scarcer, particularly at the northernmost sites. The status of the recorded individuals is unknown. However, the activity most likely was of migrating individuals or individuals on migration stopover, because very fe…

Iconography and monumental art in "feodal space" from the 10th to the 12th century : the depiction of the Three Kings and its spread

2012

This dissertation deals with the iconography of the Three Kings from the Xth to the XIIth century, by means of a study of its adaptation on monumental decoration in Latin Europe, so as to unravel how it was adapted by feudal society. In order to do so, the first question is that of the new royal status acquired in the Xth century by the Magi from the Gospel of Matthew, analyzed thanks to the concept of “ruler figure” that emerged at the time and was depicted by Marc Bloch in Les Rois thaumaturges (1924) and Ernst Kantorowicz in the The King’s Two Bodies (1957). The aim is to define where the newly defined Three Kings stand in the intricate network of “ties between man and man” theorized by …