gebhart/patrepeval huggingface dataset:
Actions of vitamin D3, analogs on human prostate cancer cell lines: comparison with 1,25-dihydroxyvitamin D3 (1995)

Data from epidemiological studies has suggested that vitamin D deficiency may promote prostate cancer, although the mechanism is not understood. We have previously demonstrated the presence of vitamin D receptors (VDR) in three human prostate carcinoma cell lines (LNCaP, PC-3, and DU-145) as well as in primary cultures of stromal and epithelial cells derived from normal and malignant prostate tissues. We have also shown that 1,25-dihydroxyvitamin D3 [1,25-(OH)2D3] can elicit an antiproliferative action in these cells. In the present study we compared the biological actions of 1,25-(OH)2D3 to those of a series of natural vitamin D3 metabolites and several synthetic analogs of vitamin D3 known to exhibit less hypercalcemic activity in vivo. In ligand binding competition experiments, we demonstrated the following order of potency in displacing [3H]1,25-(OH)2D3 from VDR: EB-1089 > 1,25-(OH)2D3 > MC-903 > 1,24,25-(OH)3D3 > 22-oxacalcitriol (OCT) > 1 alpha,25-dihydroxy-16-enecholecalciferol (Ro24-2637) > 25-hydroxyvitamin D3, with EB-1089 being approximately 2-fold more potent than the native hormone. No competitive activity was found for 25-hydroxy-16,23-diene-cholecalciferol. When compared for ability to inhibit proliferation of LNCaP cells, MC-903, EB-1089, OCT, and Ro24-2637 exhibited 4-, 3-, and 2-fold greater inhibitory activity than 1,25-(OH)2D3. Interestingly, although OCT and Ro24-2637 exhibit, respectively, 10 and 14 times lower affinity for VDR than 1,25-(OH)2D3, both compounds inhibited the proliferation of LNCaP cells with a potency greater than that of the native hormone. The relative potency of vitamin D3 metabolites and analogs to inhibit cell proliferation correlated well with the ability of these compounds to stimulate prostate-specific antigen secretion by LNCaP cells as well as with their potency to induce the 25-hydroxyvitamin D3-24-hydroxylase messenger RNA transcript in PC-3 cells. In conclusion, these results demonstrate that synthetic analogs of vitamin D3, known to exhibit reduced calcemic activity, can elicit antiproliferative effects and other biological actions in LNCaP and PC-3 cell lines. It is noteworthy that although binding to VDR is critical for 1,25-(OH)2D3 action, the analog data indicate that additional factors significantly contribute to the magnitude of the biological response. Finally, the strong antiproliferative effects of several synthetic analogs known to exhibit less calcemic activity than 1,25-(OH)2D3 suggest that these compounds potentially may be useful as an additional therapeutic option for the treatment of prostate cancer.
Deep CNNs for HEp-2 Cells Classification : A Cross-specimen Analysis (2016)

Automatic classification of Human Epithelial Type-2 (HEp-2) cells staining patterns is an important and yet a challenging problem. Although both shallow and deep methods have been applied, the study of deep convolutional networks (CNNs) on this topic is shallow to date, thus failed to claim its top position for this problem. In this paper, we propose a novel study of using CNNs for HEp-2 cells classification focusing on cross-specimen analysis, a key evaluation for generalization. For the first time, our study reveals several key factors of using CNNs for HEp-2 cells classification. Our proposed system achieves state-of-the-art classification accuracy on public benchmark dataset. Comparative experiments on different training data reveals that adding different specimens,rather than increasing in numbers by affine transformations, helps to train a good deep model. This opens a new avenue for adopting deep CNNs to HEp-2 cells classification.
Targeted disruption of the glucocorticoid receptor gene blocks adrenergic chromaffin cell development and severely retards lung maturation. (1995)

The role of the glucocorticoid receptor (GR) in glucocorticoid physiology and during development was investigated by generation of GR-deficient mice by gene targeting. GR -/- mice die within a few hours after birth because of respiratory failure. The lungs at birth are severely atelectatic, and development is impaired from day 15.5 p.c. Newborn livers have a reduced capacity to activate genes for key gluconeogenic enzymes. Feedback regulation via the hypothalamic-pituitary-adrenal axis is severely impaired resulting in elevated levels of plasma adrenocorticotrophic hormone (15-fold) and plasma corticosterone (2.5-fold). Accordingly, adrenal glands are enlarged because of hypertrophy of the cortex, resulting in increased expression of key cortical steroid biosynthetic enzymes, such as side-chain cleavage enzyme, steroid 11 beta-hydroxylase, and aldosterone synthase. Adrenal glands lack a central medulla and synthesize no adrenaline. They contain no adrenergic chromaffin cells and only scattered noradrenergic chromaffin cells even when analyzed from the earliest stages of medulla development. These results suggest that the adrenal medulla may be formed from two different cell populations: adrenergic-specific cells that require glucocorticoids for proliferation and/or survival, and a smaller noradrenergic population that differentiates normally in the absence of glucocorticoid signaling.
Stereoselective Synthesis of Conjugated Trienols from Allylic Alcohols and 1-Iodo-1,3-dienes (2012)

The stereoselective synthesis of conjugated trienes has been achieved from allylic alcohols and 1-iodo-1,3-dienes using Pd(OAc)(2)/AgOAc.
Songaricalarins A–E, Cytotoxic Oplopane Sesquiterpenes from Ligularia songarica (2020)

Five new highly oxygenated oplopane sesquiterpenes, songaricalarins A–E (1–5), and two known analogues (6 and 7) were isolated from the roots and rhizomes of Ligularia songarica. Their structures and configurations were elucidated by spectroscopic methods, including 2D-NMR techniques, and the structure of 1 was confirmed by single-crystal X-ray diffraction. All compounds were evaluated for in vitro cytotoxic activity against cultured A-549, MCF-7, KB, and KBVIN cells, and 4 exhibited cytotoxicity with EC50 values of 4.9, 0.8, 3.4, and 3.2 µg/mL, respectively.
Control of Exhaust Emissions from Copper Coated Gasohol Run Two Stroke Spark Ignition Engine with Catalytic Converter (2011)

The major pollutants emitted from spark ignition (SI) engine are carbon mono oxide (CO) and un-burnt hydrocarbons (UBHC). If the engine is run with alcohol, aldehydes have to be checked also. These are hazardous and cause health problems to human beings but also have impact on environment. Hence control of these pollutants call for immediate attention. Copper of thickness 300 microns is coated over piston crown, and indie portion of cylinder liner and cylinder head of the spark ignition engine. Investigations have been carried out for controlling pollutants from two strokes, 2.2 kW brake power at the rated speed of 3000 rpm, copper coated spark ignition engine fitted with catalytic converter with different catalysts such as sponge iron and manganese ore run with gasohol (blend of 20% ethanol and 80% gasoline by volume). The influence of parameters of catalytic converter (such as void ratio, mass of catalyst, airflow rate, temperature of injected air) and parameters of engine (such as brake power and equivalence ratio) on these emissions are studied. A microprocessor-based analyzer is used for the measurement of CO/UBHC in the exhaust of the engine. Aldehydes are measured by DNPH (dinitrophenyl hydrazine) method. Catalytic parameters are found to show strong influence on reduction of the pollutants in the exhaust. Copper coated spark ignition engine (CCE) with gasohol operation reduced the exhaust emissions considerably when compared to conventional engine (CE) with pure gasoline operation.
The evolution of natural killer cell receptors (2015)

Natural killer (NK) cells are immune cells that play a crucial role against viral infections and tumors. To be tolerant against healthy tissue and simultaneously attack infected cells, the activity of NK cells is tightly regulated by a sophisticated array of germline-encoded activating and inhibiting receptors. The best characterized mechanism of NK cell activation is "missing self" detection, i.e., the recognition of virally infected or transformed cells that reduce their MHC expression to evade cytotoxic T cells. To monitor the expression of MHC-I on target cells, NK cells have monomorphic inhibitory receptors which interact with conserved MHC molecules. However, there are other NK cell receptors (NKRs) encoded by gene families showing a remarkable genetic diversity. Thus, NKR haplotypes contain several genes encoding for receptors with activating and inhibiting signaling, and that vary in gene content and allelic polymorphism. But if missing-self detection can be achieved by a monomorphic NKR system why have these polygenic and polymorphic receptors evolved? Here, we review the expansion of NKR receptor families in different mammal species, and we discuss several hypotheses that possibly underlie the diversification of the NK cell receptor complex, including the evolution of viral decoys, peptide sensitivity, and selective MHC-downregulation.
Chloride transport in rabbit esophageal epithelial cells (2002)

We investigated Cl(-) transport pathways in the apical and basolateral membranes of rabbit esophageal epithelial cells (EEC) using conventional and ion-selective microelectrodes. Intact sections of esophageal epithelium were mounted serosal or luminal side up in a modified Ussing chamber, where transepithelial potential difference and transepithelial resistance could be determined. Microelectrodes were used to measure intracellular Cl(-) activity (a), basolateral or apical membrane potentials (V(mBL) or V(mC)), and the voltage divider ratio. When a basal cell was impaled, V(mBL) was -73 +/- 4.3 mV and a(i)(Cl) was 16.4 +/- 2.1 mM, which were similar in presence or absence of bicarbonate. Removal of serosal Cl(-) caused a transient depolarization of V(mBL) and a decrease in a(i)(Cl) of 6.5 +/- 0.9 mM. The depolarization and the rate of decrease of a(i)(Cl) were inhibited by approximately 60% in the presence of the Cl(-)-channel blocker flufenamate. Serosal bumetanide significantly decreased the rate of change of a(i)(Cl) on removal and readdition of serosal Cl(-). When a luminal cell was impaled, V(mC) was -65 +/- 3.6 mV and a was 16.3 +/- 2.2 mM. Removal of luminal Cl(-) depolarized V(mC) and decreased a by only 2.5 +/- 0.9 mM. Subsequent removal of Cl(-) from the serosal bath decreased a(i)(Cl) in the luminal cell by an additional 6.4 +/- 1.0 mM. A plot of V(mBL) measurements vs. log a(i)(Cl)/log a(o)(Cl) (a(o)(Cl) is the activity of Cl(-) in a luminal or serosal bath) yielded a straight line [slope (S) = 67.8 mV/decade of change in a(i)(Cl)/a(o)(Cl)]. In contrast, V(mC) correlated very poorly with log a/a (S = 18.9 mV/decade of change in a/a). These results indicate that 1) in rabbit EEC, a(i)(Cl) is higher than equilibrium across apical and basolateral membranes, and this process is independent of bicarbonate; 2) the basolateral cell membrane possesses a conductive Cl(-) pathway sensitive to flufenamate; and 3) the apical membrane has limited permeability to Cl(-), which is consistent with the limited capacity for transepithelial Cl(-) transport. Transport of Cl(-) at the basolateral membrane is likely the dominant pathway for regulation of intracellular Cl(-).
Treatment of Herpesvirus Infections (1983)

Guidelines for the prophylaxis or therapy of herpesvirus infections are shown in Table 1. Progress is so rapid in this area that frequent revisions of such guidelines will be necessary. Newer drugs or new formulations of older agents are constantly being developed. Combination therapies--e.g., interferon plus acyclovir--appear promising in laboratory models of herpesvirus infections and will undoubtedly receive clinical investigation in the years ahead. The problem of dealing with latent virus infections still eludes us, and major breakthroughs will be necessary before we can discuss cure of recurrent infections. Nevertheless, important strides have been made in the past few years, and further progress is predictable in the years ahead.
Decomposition of the Height Function of Scherk's First Surface (2000)

We show that Scherk's first surface, a one-parameter family of solutions to the minimal surface equation, may be written as a linear superposition of other solutions with specific parametric values.
ChemInform Abstract: Novel Triethylsilane Mediated Reductive N‐Alkylation of Amines: Improved Synthesis of 1‐(4‐Imidazolyl)methyl‐4‐sulfonylbenzodiazepines, New Farnesyltransferase Inhibitors. (2001)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Enhancement of Abiotic Stress Tolerance in Plants by Probiotic Bacteria (2019)

As sessile organisms, plants are constantly subjected to numerous environmental stresses that may seriously impair growth, development and productivity. Probiotic bacteria that colonize plant roots and/or internal tissues can augment plant tolerance to abiotic stresses such as as salinity, drought, flooding, extreme temperatures, and heavy metals through a variety of mechanisms. Therefore, the use of probiotic bacteria as bioinoculants to increase crop productivity in marginal agricultural lands has a promising future. This chapter reviews recent findings on bacteria-mediated plant tolerance to the effects of diverse abiotic stresses. The mechanisms through which probiotic bacteria enhance abiotic stress tolerance in plants are also discussed.
Detection of beta-glucuronidase in lactose-fermenting members of the family Enterobacteriaceae and its presence in bacterial urine cultures (1984)

Four hundred strains of lactose-fermenting Enterobacteriaceae were tested for hydrolysis of p-nitrophenyl-beta-D-glucopyranosiduronic acid, the chromogenic enzyme substrate of beta-glucuronidase. Escherichia coli was found to be homogeneous with respect to beta-glucuronidase: more than 94% of the examined E. coli strains were positive, whereas none of the other lactose-fermenting strains possessed beta-glucuronidase activity. The qualitative beta-glucuronidase test, as rapid and simple as the o-nitrophenyl-beta-D-galactopyranosidase test, proved to be of diagnostic value, especially in the identification of E. coli in primary urine cultures. No significant differences were observed in the results of experiments in which either substrate-impregnated disks prepared in the laboratory or commercially available tablets were used.
Adversarial Regression for Detecting Attacks in Cyber-Physical Systems (2018)

Attacks in cyber-physical systems (CPS) which manipulate sensor readings can cause enormous physical damage if undetected. Detection of attacks on sensors is crucial to mitigate this issue. We study supervised regression as a means to detect anomalous sensor readings, where each sensor's measurement is predicted as a function of other sensors. We show that several common learning approaches in this context are still vulnerable to stealthy attacks, which carefully modify readings of compromised sensors to cause desired damage while remaining undetected. Next, we model the interaction between the CPS defender and attacker as a Stackelberg game in which the defender chooses detection thresholds, while the attacker deploys a stealthy attack in response. We present a heuristic algorithm for finding an approximately optimal threshold for the defender in this game, and show that it increases system resilience to attacks without significantly increasing the false alarm rate.
Integrated system for preparation of bone cement and effects on cement quality and environment (1997)

We developed a prepacked mixing system for the preparation of bone cement. The system is based on mixing and collection of bone cement under a vacuum and serves as both the storage and mixing device for the cement components, thereby minimizing the exposure of the operating staff to the monomer and the risk for contamination of the cement during preparation. We evaluated the system using Palacos R and Simplex P. The cement produced was compared with cement obtained from a commercially available mixing system. Temperature evolution during curing, handling characteristics, density, and porosity of the cement obtained were analyzed. The results showed that the experimental system produces cement with physical properties (i.e., setting times and temperature, porosity, and density) equal to or better than those obtained with commercially available systems. Reducing the amount of monomer in the experimental system led to a reduction of the curing temperature without compromising the physical properties of the cements.
Hydrosilylation catalysed by activated nickel (1991)

Activated nickel, prepared by lithium reduction of nickel iodide under sonication, efficiently catalyses the hydrosilylation of hexene, styrene, vinyl butyl ether and acrylonitrile under mild conditions.
Synthesis and properties of Fe3O4-activated carbon magnetic nanoparticles for removal of aniline from aqueous solution: equilibrium, kinetic and thermodynamic studies (2013)

In this study, powder activated carbon (PAC) and magnetic nanoparticles of iron (III) oxide were used for synthesis of Fe3O4-activated carbon magnetic nanoparticles (AC-Fe3O4 MNPs) as an adsorbent for the removal of aniline. The characteristics of adsorbent were evaluated by SEM, TEM, XRD and BET. Also, the impact of different parameters such as pH, contact time, adsorbent dosage, aniline initials concentration and solution temperature were studied. The experimental data investigated by Langmuir and Freundlich adsorption isotherms and two models kinetically of pseudo first-order and pseudo second-order. The results indicated that the adsorption followed Langmuir and pseudo second-order models with correlation r(2) > 0.98 and r(2) > 0.99, respectively. The equilibrium time was obtained after 5 h. According to Langmuir model, the maximum adsorption capacity was 90.91 mg/g at pH = 6, and 20°C. The thermodynamic parameters indicated that adsorption of aniline on magnetic activated carbon was exothermic and spontaneous. This synthesized AC-Fe3O4 MNPs due to have advantages such as easy and rapid separation from solution could be applied as an adsorbent effective for removal of pollutants such as aniline from water and wastewater.
Homocysteine, heat shock proteins, genistein and vitamins in ischemic stroke--pathogenic and therapeutic implications. (2012)

Stroke is one of the most devastating neurological conditions, with an approximate worldwide mortality of 5.5 million annually and loss of 44 million disability-adjusted life-years. The etiology of stroke is often unknown; it has been estimated that the etiology and pathophysiology remains unexplained in more than 40% of stroke cases. The conventional stroke risk factors, including hypertension, diabetes mellitus, smoking, and cardiac diseases, do not fully account for the risk of stroke, and stroke victims, especially young subjects, often do not have any of these factors. It is very likely that inflammation, specific genetic predispositions and traditional risk factors interact with each other and may together increase the risk of stroke. Inflammatory and immune responses play important roles in the course of ischemic stroke. Hyperhomocysteinemia (hcy) is considered a modifiable risk factor for stroke, possibly through an atherogenic and prothrombotic mechanism. Both genetic and environmental factors (e.g., dietary intake of folic acid and B vitamins) affect homocysteine level. Identification of the role of hcy as a modifiable risk factor for stroke and of HSPs as regulators of the immune response may lead to more effective prevention and treatment of stroke through dietary and pharmacological intervention. Dietary modification may also include supplementation with novel preventive compounds, such as the antioxidative isoflavones--genistein or daidzein.
Contextual relevance feedback in web information retrieval (2006)

In this paper, we present an alternative approach to the problem of contextual relevance feedback in web-based information retrieval. Our approach utilises a rich contextual model that exploits a user's implicit and explicit data. Each user's implicit data are gathered from their Internet search histories on their local machine. The user's explicit data are captured from a lexical database, a shared contextual knowledge base and domain-specific concepts using data mining techniques and a relevance feedback approach. This data is later used by our approach to modify queries to more accurately reflect the user's interests as well as to continually build the user's contextual profile and a shared contextual knowledge base. Finally, the approach retrieves personalised or contextual search results from the search engine using the modified/expanded query. Preliminary experiments indicate that our approach has the potential to not only aid in the contextual relevance feedback but also contribute towards the long term goal of intelligent relevance feedback in web-based information retrieval.
A functional CRISPR/Cas9 screen identifies kinases that modulate FGFR inhibitor response in gastric cancer (2019)

Some gastric cancers have FGFR2 amplifications, making them sensitive to FGFR inhibitors. However, cancer cells inevitably develop resistance despite initial response. The underlying resistance mechanism to FGFR inhibition is unclear. In this study, we applied a kinome-wide CRISPR/Cas9 screen to systematically identify kinases that are determinants of sensitivity to a potent FGFR inhibitor AZD4547 in KatoIII cells, a gastric cancer cell line with FGFR2 amplification. In total, we identified 20 kinases, involved in ILK, SRC, and EGFR signaling pathways, as determinants that alter cell sensitivity to FGFR inhibition. We functionally validated the top negatively selected and positively selected kinases, ILK and CSK, from the CRISPR/Cas9 screen using RNA interference. We observed synergistic effects on KatoIII cells as well as three additional gastric cancer cell lines with FGFR2 amplification when AZD4547 was combined with small molecular inhibitors Cpd22 and lapatinib targeting ILK and EGFR/HER2, respectively. Furthermore, we demonstrated that GSK3b is one of the downstream effectors of ILK upon FGFR inhibition. In summary, our study systematically evaluated the kinases and associated signaling pathways modulating cell response to FGFR inhibition, and for the first time, demonstrated that targeting ILK would enhance the effectiveness of AZD4547 treatment of gastric tumors with amplifications of FGFR2.