gebhart/patrepeval huggingface dataset:
Design, Synthesis, and Biological Activity of Novel, Potent, and Selective (Benzoylaminomethyl)thiophene Sulfonamide Inhibitors of c-Jun-N-Terminal Kinase (2004)

Several lines of evidence support the hypothesis that c-Jun N-terminal kinases (JNKs) play a critical role in a wide range of disease states including cell death (apoptosis)-related and inflammatory disorders (epilepsy, brain, heart and renal ischemia, neurodegenerative diseases, multiple sclerosis, rheumatoid arthritis, and inflammatory bowel syndrome). The screening of a compound collection led to the identification of a 2-(benzoylaminomethyl)thiophene sulfonamide (AS004509, compound I) as a potent and selective JNK inhibitor. Chemistry and structure--activity relationship (SAR) studies performed around this novel kinase-inhibiting motif indicated that the left and central parts of the molecule were instrumental to maintaining potency at the enzyme. Accordingly, we investigated the JNK-inhibiting properties of a number of variants of the right-hand moiety of the molecule, which led to the identification of 2-(benzoylaminomethyl)thiophene sulfonamide benzotriazole (AS600292, compound 50a), the first potent and selective JNK inhibitor of this class which demonstrates a protective action against neuronal cell death induced by growth factor and serum deprivation.
Peroxisome proliferator-activated receptor inhibits follicular and anaplastic thyroid carcinoma cells growth by upregulating p21Cip1/WAF1 gene in a Sp1-dependent manner (2008)

Peroxisome proliferator-activated receptor gamma (PPARgamma) has been demonstrated to be anti-neoplastic against various human tumors. The aim of this study was to delineate the molecular mechanism underlying PPARgamma ligand rosiglitazone (BRL) antiproliferative effects in follicular WRO and anaplastic FRO human thyroid carcinoma cells. BRL upregulated the p21Cip1/WAF1 levels in the two thyroid cancer cells, while did not modify the p53 protein content. Different evidences indicate that the p21Cip1/WAF1 upregulation by BRL requires a functional PPARgamma, since it was reversed by silencing PPARgamma and pretreatment with GW9662, an irreversible PPARgamma antagonist. Transient transfection assays showed that BRL triggered the transcriptional activity of p21Cip1/WAF1 promoter gene in a p53-independent way, being a p21Cip1/WAF1 promoter construct deleted in the p53 sites still activated by BRL. The Sp1 inhibitor mithramycin silenced the p21Cip1/WAF1 promoter activity suggesting an important role of Sp1 in mediating BRL activation. The electrophoretic mobility shift and chromatin immunoprecipitation (ChIP) assays evidenced a functional interaction between PPARgamma and Sp1 in regulating p21Cip1/WAF1. Intriguingly, ChIP analysis revealed in the p21Cip1/WAF1 gene promoter an increased recruitment of the RNA Pol II associated with an increased histone H3 acetylation and a reduced H3 methylation. The biological event, consistent with PPARgamma-induced WRO and FRO cell growth inhibition, was reversed by p21Cip1/WAF1 antisense oligonucleotides and was confirmed by increasing the PPARgamma expression, suggesting a crucial role exerted by p21Cip1/WAF1 in PPARgamma action. Our results further candidate BRL as a potential agent able to inhibit tumor progression of follicular and anaplastic thyroid carcinoma.
Metal Ion-Assisted Photochemical Vapor Generation for the Determination of Lead in Environmental Samples by Multicollector-ICPMS (2015)

A novel and sensitive approach for the accurate and precise determination of Pb in environmental samples is presented using transition metal ion-assisted photochemical vapor generation (PVG) for sample introduction with multicollector inductively coupled plasma mass spectrometry (MC-ICPMS) detection. A significant improvement in PVG efficiency of lead is achieved in the presence of transition metal ions (Co(2+) and Ni(2+)) in solutions of 5% (v/v) formic acid. The determination of Pb in digests of sediment or soil samples is readily achieved due to coexisting transition metal ions which facilitate the PVG reaction. The method detection limit of 0.005 ng g(-1) (3σ) using external calibration is comparable to that obtained using hydride generation (HG) ICPMS. However, PVG methodology is simpler, results in lower blanks, and avoids unstable reagents. The accuracy of the proposed method was demonstrated by analysis of several environmental certified reference materials (CRMs; SLRS-5 and SRM1640a river water CRMs and MESS-3, MESS-4, and SRM2702 sediments) with satisfying results. High precision of determination (<0.4% RSD) of Pb in river water and sediments was realized on the basis of isotope dilution calibration.
In vitro Invasion of Endothelial Cell Monolayer by Rat Ascites Hepatoma Cells (1989)

To study the tissue preference of invasion, we developed an assay system for the invasion of endothelial cells as a modification of the previously established assay of tumor cell invasion of mesothelial cells. Rat ascites hepatoma cells (AH 130) that had been seeded on a monolayer of cultured endothelial cells penetrated and formed tumor cell colonies under the monolayer. The penetration was time-dependent and the number of penetrated tumor cells and colonies was proportional to the number of tumor cells seeded. Comparison of the in vitro tumor cell invasion of endothelial cell monolayer with that of cultured mesothelial cell layer showed that a clone from the tumor cells (Cl-30) which was highly penetrative into the mesothelial cell layer had only limited ability to penetrate the endothelial cell layer.
Thermal and rheological properties improvement of drilling fluids using functionalized carbon nanotubes (2014)

The application of functionalized/unfunctionalized (multi-walled) carbon nanotubes (CNT) was investigated in the context of formulating nano-based drilling fluids from water/oil-based fluid templates. CNT functionalization was attempted by applying hydrophilic functional groups onto the surface of the nanotubes via acid treatment. Experimental data were collected for thermal conductivity, viscosity/yield point, and filtrate amount in all samples. The time evolution of thermal conductivity was studied, as well as the effects of temperature and CNTs volume fraction on the parameter. Scanning electron microscopy (SEM) was used to monitor CNTs dispersion quality. The thermal conductivity results unveil considerable enhancements, by as much as 23.2 % (1 % vol. functionalized CNT) in CNT-water-based case at ambient temperature, with extended improvement of 31.8 % at an elevated temperature of 50 C. Corresponding results for the CNT-oil-based case exhibit an improvement in thermal conductivity by 40.3 % (unfunctionalized) and 43.1 % (functionalized) and 1 % volume fraction of CNT. The rheological results follow an analogous improvement trend. For the CNT-oil-based case, the filtration tests conducted at 138 C and 500 (psi) show a 16.67 % reduction in filtrate amount (1 % vol. CNT). The time evolution of thermal conductivity was found to nearly equalize (at an amount of 9.7 %) after 100 h of sample preparation in both functionalized and unfunctionalized CNT-oil-based cases.
Intra‐ and interreader reproducibility of PI‐RADSv2: A multireader study (2018)

2 Technical Efficacy: Stage 2.
A Randomized Clinical Trial of Greek High Phenolic Early Harvest Extra Virgin Olive Oil in Mild Cognitive Impairment: The MICOIL Pilot Study (2020)

Long-term intervention with HP-EH-EVOO or MP-EVOO was associated with significant improvement in cognitive function compared to MeDi, independent of the presence of APOEɛ4.
Wavelength-selective coupler and add-drop multiplexer using long-period fiber gratings (2002)

We demonstrate a low-insertion-loss wavelength-selective coupler that uses cladding-mode coupling between two identical fibers. The device is simple to manufacture, has >40 dB of channel isolation and no back-reflection.
Targeted therapy for HER2 driven colorectal cancer. (2017)

3583 Background: ERBB2 ( HER2) genomic alterations (GA) are evolving therapy taregets in metastatc coorectal cancer (mCRC). Methods: Hybrid capture based comprehensive genomic profiling (CGP) was performed on 8874 (9.6%) mCRC including both colonic adenocarcinomas (7587 cases; 85%) and rectal adenocarcinomas (1287 cases, 15%) Tumor mutational burden (TMB) was calculated from a minimum of 1.2 Mb of sequenced DNA. Results: ERBB2 amplifications or a short variant (SV) alterations or both were found in 433 (4.9%) of the total mCRC. 195 (45%) of the ERBB2 positive mCRC were female and 238 (55%) were male. Median age was 54 years (range 22 to 88 years). The most frequently co-altered genes were SV GA in TP53 (82%), APC (70%), KRAS (26%), SMAD4 (15%) and PIK3CA (13%). Clinically relevant GA significantly under-represented in ERBB2-altered CRC included significantly reduced GA in KRAS at 26% (p = 0.001) and BRAF at 4% (p = 0.003) as well as other kinases at 1% including EGFR, KIT, MET and RET. The frequency of TMB at &gt; 10 mut/Mb (p &lt; 0.0001), but at &gt; 20 mut/Mb mCRC cases demonstrated virtually the same results regardless to ERBB2 status at a frequency of x%. The overall ERBB2 GA frequency at 5.3% in rectal mCRC is slightly higher than that seen in colonic mCRC at 4.9%, (p = 0.36). The frequency of TMB &gt; 10 mut/Mb in ERBB2 WT mCRC is greater in the colonic mCRC than the rectal mCRC (p &lt; 0.0001 for both comparisons). When &gt; 20 mut/Mb is used as the cut-off, the greater frequency of TMB in colonic mCRC versus rectal mCRC remains significant (p &lt; 0.0001). When the ERBB2altered mCRC cases are evaluated, the greater frequency of TMB &gt; 10 mu/Mb in colonic mCRC versus rectal mCRC remains significant (p = 0.009), but the greater frequency in colonic verses rectal mCRC at the &gt; 20 mut/Mb is not significant (p = 0.37). Conclusions: Although lower than observed in breast and upper gastrointestinal carcinomas where anti-HER2 therapies are approved indications, the frequency of ERBB2 GA in CRC at 4.9% is significant. Importantly, nearly half of CRC ERBB2 alterations are SVs, not detectable by routine IHC and FISH testing. However, the success of anti-HER2 therapies shown here and progress in on-going clinical trials indicates that targeting ERBB2 has potential to become an approved advance in precision therapy for mCRC patients.
One Bad Apple Spoils the Barrel: Understanding the Security Risks Introduced by Third-Party Components in IoT Firmware (2022)

Currently, the development of IoT firmware heavily depends on third-party components (TPCs) to improve development efficiency. Nevertheless, TPCs are not secure, and the vulnerabilities in TPCs will influence the security of IoT firmware. Existing works pay less attention to the vulnerabilities caused by TPCs, and we still lack a comprehensive understanding of the security impact of TPC vulnerability against firmware. To fill in the knowledge gap, we design and implement FirmSec, which leverages syntactical features and control-flow graph features to detect the TPCs in firmware, and then recognizes the corresponding vulnerabilities. Based on FirmSec, we present the first large-scale analysis of the security risks raised by TPCs on $34,136$ firmware images. We successfully detect 584 TPCs and identify 128,757 vulnerabilities caused by 429 CVEs. Our in-depth analysis reveals the diversity of security risks in firmware and discovers some well-known vulnerabilities are still rooted in firmware. Besides, we explore the geographical distribution of vulnerable devices and confirm that the security situation of devices in different regions varies. Our analysis also indicates that vulnerabilities caused by TPCs in firmware keep growing with the boom of the IoT ecosystem. Further analysis shows 2,478 commercial firmware images have potentially violated GPL/AGPL licensing terms.
Human autologous mixed lymphocyte reactivity is primarily specific for xenoprotein determinants adsorbed to antigen-presenting cells during rosette formation with sheep erythrocytes. (1982)

We present evidence that most T cells proliferating in response to autologous sheep erythrocyte (SRBC)-separated non-T cells (NT) cells are not specific for autoantigens but for antigens derived from xenogeneic sources. The conclusion was based on the following three observations. First, we found that NT cells isolated in the absence of xenoproteins by means of density gradient centrifugation on Percoll only weakly stimulated autologous T cells. Because this weak proliferation could not be expanded in restimulation experiments, its significance as an immune recognitive event remains questionable. NT cells isolated by the above method in the absence of xenogeneic determinants readily acquired stimulatory capacity after brief exposure to either SRBC or fetal calf serum. Second, restimulation of T memory cells generated in 1 degree autologous mixed lymphocyte reaction (AMLR) against SRBC-separated autologous NT cells was exclusively seen when NT cells exposed to or separated with xenoproteins were used for restimulation. Third, T memory cells generated against SRBC-separated autologous NT cells were specifically restimulated by autologous Percoll-separated NT cells that had been pulsed with a variety of xenogeneic mammalian sera. These xenogeneic determinants were preferentially recognized in context with autologous HLA-DR+ cells. From these findings and from our previous results that indicated an absolute requirement of HLA-DR+-adherent NT cells (8), we conclude that human AMLR primarily does not represent an autoantigen but a xenoantigen response that is genetically restricted by the HLA-DR type of the antigen-presenting cell.
Speciated Hydrocarbon Emissions from the Combustion of Single Component Fuels. I. Effect of Fuel Structure (1992)

Speciated hydrocarbon emissions data have been collected for six single-component fuels run in a laboratory pulse flame combustor (PFC). The six fuels include n-heptane, isooctane (2, 2, 4-trimethylpentane), cyclohexane, 1-hexene, toluene, and methyl-t-butyl ether (MTBE: an oxygenated fuel extender). Combustion of non-aromatic fuels in the PFC (at a fuel/air equivalence ratio of Φ = 1.02) produced low levels of unburned fuel and high yields of methane and olefins (> 75 percent combined) irrespective of the molecular structure of the fuel. In contrast, hydrocarbon emissions from toluene combustion in the PFC were comprised predominantly of unburned fuel (72 percent). With the PFC, low levels of 1, 3-butadiene (0.3-1.8 percent) were observed from all the fuels except MTBE, for which no measurable level (<0.2 percent) was detected; low levels of benzene were observed from isooctane, heptane, and 1-hexene, but significant levels (9 percent) from cyclohexane and toluene. No measurable amount of benzene (< 0.2 percent) was observed in the MTBE exhaust. For isooctane and toluene the speciated hydrocarbon emissions from a spark-ignited (SI) single-cylinder engine were also determined. HC emissions from the SI engine contained the same species as observed from the PFC, although the relative composition was different. For the non-aromatic fuel isooctane, unburned fuel represented a larger fraction (50 percent) of the HC emissions when run in the engine. HC emissions from toluene combustion in the engine were similar to those from the PFC.
A role for matrix remodelling proteins in invasive and malignant meningiomas (2014)

Overall, the results support a role for MMP16 in promoting invasive properties of the meningioma tumours. Further studies to explore the potential value for clinical use of matrix metalloproteinases inhibitors are warranted.
Figure S2 from Multikinase Inhibitors Induce Cutaneous Toxicity through OAT6-Mediated Uptake and MAP3K7-Driven Cell Death (2023)

&lt;p&gt;Identification of OAT-dependent sorafenib transport in human primary keratinocytes&lt;/p&gt;
Selecting a Computer for your Needs (1982)

Realistic goals and adequate information about equipment and program capabilities are essential prerequisites when selecting a computer system. Problems of equipment selection are dealt with by discussing a range of microcomputers emphasising the need to consider expansion and compatibility with standards such as the S. 100 bus. The importance of ready availability of word processing and management programs is emphasised.
Biological functions of haptoglobin--new pieces to an old puzzle. (1997)

Haptoglobin, an "acute phase" protein, has different functions, which display genetic polymorphism. The complex of haptoglobin with haemoglobin is metabolized in the heptic reticuloendothelial system. Biosynthesis of haptoglobin occurs not only in the liver, but also in adipose tissue and in lung; providing antioxidant and antimicrobial activity. Changes in the measured concentrations of haptoglobin in serum may help to assess the disease status of patients with inflammations, infections, malignancy etc. (increases) as well as in haemolytic conditions (decreases). Haptoglobin plays a role in stimulation of angiogenesis and has highly potent cholesterolcrystallization-promoting activity. Probably the most important biological function of haptoglobin consists in the host defence responses to infection and inflammation, acting as a natural antagonist for receptor-ligand activation of the immune system.
A method for measuring the anisotropy ratio of the thermal conductivity of anisotropy solids (1983)

Using the modern methods of radiative temperature measurements a refined De Senarmont method (1848) is developed. It allows the measurement of the anisotropy ratio k1/k2 of the thermal conductivity in different directions 1,2 of an anisotropic solid at room temperature and above. This transient method is especially suited for poor thermal conductors like polymers and does also provide an estimate of the absolute thermal diffusivity.
Evidence for the involvement of metalloendoproteases in the acrosome reaction in sea urchin sperm. (1987)

An essential initial step in fertilization in the sea urchin Strongylocentrotus purpuratus is an intracellular membrane fusion event in the sperm known as the acrosome reaction. This Ca2+-dependent, exocytotic process involves fusion of the membrane of the acrosomal vesicle and the plasma membrane. Recently, metalloendoproteases requiring divalent metals have been implicated in several Ca2+-dependent membrane fusion events in other biological systems. In view of the suggested involvement of Zn2+ in the sea urchin sperm acrosome reaction (Clapper, D.L., Davis, J.A., Lamothe, P.J., Patton, C., and Epel, D. (1985) J. Cell Biol. 100, 1817-1824) and the fact that Zn2+ is a metal cofactor for metalloendoproteases, we investigated the potential role of this protease in the acrosome reaction. A soluble metalloendoprotease was demonstrated and characterized in sperm homogenates using the fluorogenic protease substrate succinyl-alanine-alanine-phenylalanine-4-aminomethylcoumarin. The protease was inhibited by the metal chelators EDTA and 1,10-phenanthroline, and activity of the inactive apoenzyme could be reconstituted with Zn2+. The metalloendoprotease substrate and inhibitors blocked the acrosome reaction induced either by egg jelly coat or by ionophore, but had no effect on the influx of Ca2+. These observations suggest that inhibition occurs at a step independent of Ca2+ entry. Overall, the results of this study provide strong indirect evidence that the acrosome reaction requires the action of metalloendoprotease.
Performance characterization of STAP algorithms with mismatched steering and clutter statistics (2002)

Adaptive algorithms for receivers employing antenna arrays have received significant attention for radar systems applications. We present exact expressions for the space-time adaptive processing (STAP) algorithm performance when the covariance matrix of the test cell is different from the average covariance matrix of the surrounding range cells. Numerical evaluation of these expressions illustrates the probability of detection and the probability of false alarm for various cases of interest. The equations are utilized to determine an upper bound on the performance of a class of STAP algorithms.
Poly(2-ethyl-2-oxazoline)–Doxorubicin Conjugate-Based Dual Endosomal pH-Sensitive Micelles with Enhanced Antitumor Efficacy (2014)

Dual endosomal pH-sensitive micelles were designed and fabricated to deliver doxorubicin (DOX) for treating breast cancer based on a poly(2-ethyl-2-oxazoline) (PEOz)-DOX (PEOz-hyd-DOX) conjugate. PEOz-hyd-DOX was successfully synthesized by connecting DOX to PEOz via an acid cleavable hydrazone linker and self-assembled into nanosized micelles, which further physically encapsulated DOX. The conjugate and DOX-loaded conjugate micelles displayed faster release of DOX at pH 5.0 than at pH 7.4. This pH-dependent release behavior might assist the quick diffusion of DOX from acidic endosomes or lysosomes and the intracellular transfer into the nucleus after internalization, which was confirmed by confocal laser scanning microscopy images. As expected, PEOz-hyd-DOX conjugate and DOX-loaded conjugate micelles maintained cytotoxicity of DOX. In addition, the dual endosomal pH-sensitive micelles were found to substantially enhance antitumor efficacy and reduce side effects compared with free DOX. Therefore, PEOz-hyd-DOX conjugate-based micelles might be potential drug delivery vehicles of DOX for safe and effective breast cancer therapy.
Das Politische (in) der Politischen Theorie (2021)

Flügel-Martinsen O, Martinsen F, Saar M, eds. &lt;em&gt;Das Politische (in) der Politischen Theorie&lt;/em&gt;. Baden-Baden: Nomos; 2021.
An evaluation scheme of adaptive configuration techniques (2007)

In this paper, we present a set of metrics (scalability, adaptability, overhead, latency, complexity, and effectiveness) to evaluate dynamic configuration techniques. We have applied these metrics to two real systems: remote management system and dynamic security configuration of networked systems. The evaluation results show that our approach can efficiently and dynamically manage system resources and network security with little overhead.
Bioavailability of two ibuprofen oral paste formulations in fed or nonfed ponies (1992)

The bioavailability and pharmacokinetics of ibuprofen, a nonsteroidal antiinflammatory drug, was studied in healthy Shetland ponies. Ibuprofen was administered IV, as a suspension, and as a solid solution oral paste to ponies from which food was withheld. The suspension paste was also administered to ponies that received hay and water ad libitum. Both formulations had an absolute bioavailability of about 80%. Bioavailability was not influenced by feeding.
Populisme, immigratie en Europa (2018)

Populisme kan onder andere worden gezien als een negatieve houding van kiezers ten aanzien van de nationale politieke elite. Deze negatieve houding is in meer of mindere mate aanwezig bij alle burgers. Het heeft dus geen zin onderscheid te maken tussen populisten en de rest van de bevolking. Populisme hangt vooral sterk samen met opleiding en veel minder met geslacht en leeftijd. Verder hangt populisme sterk samen met negatieve opvattingen over Europese samenwerking en immigratie, een roep om kleinere inkomensverschillen en met ontevredenheid over de Nederlandse democratie. Populistische sentimenten leven sterker onder niet-stemmers en aanhangers van de PVV, SP, 50PLUS, DENK en FvD dan onder aanhangers van andere partijen.