gebhart/patrepeval huggingface dataset:
Design, synthesis, and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonists (2019)

Prostate cancer (PCa) is the second leading cause of death in men. Apart from androgen receptor, 5α-reductase has also been recognized as a potential target. In this study, a series of androst-17β-amide compounds have been designed and synthesized targeting both AR and 5α-reductase. Their anti-proliferation activities were evaluated in AR + cell line 22RV1 and AR - cell line PC-3. The results indicated that most of the synthesized compounds inhibited the testosterone-stimulated cell proliferation with good selectivity and safety. Among all the compounds, androst[3,2-c]pyrazole derivatives <b>(9a-9d)</b> displayed the best inhibition activity comparable with flutamide. Moreover, most of the synthesized compounds displayed good 5α-reductase inhibitory activities with IC<sub>50</sub> lower than 1 μM. The docking result of <b>9d</b>-AR indicated that AR was forced to expands its binding cavity and maintain an antagonistic conformation since the steric hindrance of <b>9d</b> impeded H12 transposition. Overall, compound <b>9d</b> can be identified as a potential dual 5α-reductase inhibitor and AR antagonist, which might be of therapeutic importance for PCa treatment.
Induction of benomyl-tolerant mutants from Trichoderma sp. SKT-1 and practicality of mutant SKT-3 in control of rice seedborne diseases. (2003)

Mutants of Trichoderma sp. SKT-1 with tolerance to benomyl were easily induced with UV irradiation or nitrosoguanidine. Strain SKT-3 induced by UV irradiation possesses high tolerance to benomyl (MIC 1000μg/ml). Because it could be re-isolated on benomyl-containing culture media, activity of the strain could be tested in the environment, including soil and water systems. SKT-3 had suppressive activities against “Bakanae” disease and bacterial seedling blight comparable to its parent strain, SKT-1 and was compatible with benomyl-containing fungicides.
Dynamic models of microring resonators (2013)

Quasi-static microring models assume the intracavity optical field adiabatically follows the modulated parameter(s). A non-quasi-static model shows the modulation of the microring coupling coefficient breaks the traditional tradeoffs between the modulation rate and resonator linewidth.
Tanshinone IIA Protects Against Folic Acid-Induced Acute Kidney Injury (2016)

Tanshinone IIA is a diterpene extracted from Salvia miltiorrhiza, a popular and safe herb medicine that has been widely used in China and other Asian countries. Previous studies have demonstrated the pleiotropic effects of Tanshinone IIA on many disease treatments via its antitoxicity, anti-inflammation, anti-oxidative stress, as well as antifibrosis activities. However, its effect on acute kidney injury (AKI) has not been fully investigated. Here, we show for the first time that systemic administration of Tanshinone IIA can lead to improved kidney function in folic acid-induced kidney injury mice. In the acute phase of AKI, Tanshinone IIA attenuated renal tubular epithelial injury, as determined by histologic changes and the detection of Neutrophil gelatinase-associated lipocalin (NGAL) in the kidney and urine. Additionally, Tanshinone IIA treatment resulted in elevated proliferating cell nuclear antigen (PCNA) expression and decreased inflammatory cells infiltration as well as chemokine expression, suggesting that Tanshinone IIA promoted renal repair following AKI and inhibited local inflammatory response in the injured kidney. This led to decreased long-term fibrosis in the injured kidney, characterized by less accumulation of fibronectin and collagen I in tubulointerstitium. Taken together, these results suggest that Tanshinone IIA may represent a potential approach for AKI treatment.
AnthOligo: automating the design of oligonucleotides for capture/enrichment technologies (2020)

Supplementary data are available at Bioinformatics online.
Minimum profile ultrahigh vacuum gate valve based on linear/rotary motion feedthrough (1996)

A simple, very low profile (&amp;lt;1 in.) ultrahigh vacuum gate valve for isolation of molecular beam sources is described. The radial gate drive is based upon a linear/rotary motion feedthrough. A novel coupling scheme is described where the linear motion is used to translate the gate while the rotary motion is used to independently raise and lower the gate. A molecular beam skimmer, mounted on the gate, may be accurately and reproducibly located.
Evidence Against the Presence of Tight Junctions in Normal Endocrine Pancreas (1984)

Tight junctional fibrils were absent in freeze-fracture replicas of rat and human islets in situ, but were easily discerned in collagenase-isolated islets. Disruption of the pancreatic gland and its exposure to trypsin were each found to induce tight junction formation in rat islets. The amount of tight junctions between islet cells declined progressively during culture, but tight junctional structures remained detectable after 1 day of culture. It is suggested that rather than being involved in normal islet cell function tight junctions provide an adaptive mechanism intended to seal and hence to protect islet microdomains against sudden perturbations in local interstitial fluid.
EEG Findings in Chimeric Antigen Receptor T-Cell (CAR-T) Related Encephalopathy Syndrome (P1.6-004) (2019)

To describe the clinical and electrophysiologic characteristics of CRES (CAR-T related encephalopathy syndrome)
Tiotropium bromide suppresses smoke inhalation and burn injury-induced ERK 1/2 and SMAD 2/3 signaling in sheep bronchial submucosal glands (2014)

The effects of tiotropium bromide on ERK 1/2, SMAD 2/3 and NFκB signaling in bronchial submucosal gland (SMG) cells of sheep after smoke inhalation and burn injury (S + B) were studied. We hypothesized that tiotropium would modify intracellular signaling processes within SMG cells after injury. Bronchial tissues were obtained from uninjured (sham, n = 6), S + B injured sheep 48 h after injury (n = 6), and injured sheep nebulized with tiotropium (n = 6). The percentage (mean ± SD) of cells showing nuclear localization of phosphorylated ERK 1/2, pSMAD 2/3, and NFκB (p65) was determined by immunohistochemistry. Nuclear pERK 1/2 staining was increased in injured animals as compared to sham, (66 ± 20 versus 14 ± 9), p = 0.0022, as was nuclear pSMAD, 84 ± 10 versus 20 ± 10, p = 0.0022. There was a significant decrease in pERK 1/2 labeling in the tiotropium group compared to the injured group (31 ± 20 versus 66 ± 20, p = 0.013), and also a decrease in pSMAD labeling, 62 ± 17 versus 84 ± 10, p = 0.04. A significant increase for NFκB (p65) was noted in injured animals as compared to sham (73 ± 16 versus 7 ± 6, p = 0.0022). Tiotropium-treated animals showed decreased p65 labeling as compared to injured (35 ± 17 versus 74 ± 16, p = 0.02). The decrease in nuclear expression of pERK, pSMAD and NFκB molecules in SMG cells with tiotropium treatment is suggestive that their activation after injury is mediated in part through muscarinic receptors.
Uterine Cervical Distension Induces cFos Expression in Deep Dorsal Horn Neurons of the Rat Spinal Cord (2003)

The present study demonstrates that uterine cervical distension results in a similar pattern of spinal cord neuronal activation as seen with other noxious visceral stimuli. The inhibition of cFos expression by intrathecal ketorolac suggests that spinal cyclo-oxygenase plays a role in uterine cervical distension-induced nociception.
Case 21-2016 (2016)

A 32-year-old man was admitted to this hospital after being found in an unresponsive state in his jail cell. He had jaundice and encephalopathy; results of liver-function tests were abnormal, and CT revealed cerebral edema. Diagnostic tests were performed.
Palladium Nanoparticles Entrapped in Aluminum Hydroxide:  Dual Catalyst for Alkene Hydrogenation and Aerobic Alcohol Oxidation (2005)

[reaction: see text] A new aluminum hydroxide-supported palladium catalyst (1) made by a one-pot synthesis through nanoparticle generation and gelation shows a dual catalytic activity for olefinic hydrogenation and aerobic alcohol oxidation.
Validation of Carbon Monoxide Total Column Retrievals from SCIAMACHY Observations with NDACC/TCCON Ground-Based Measurements (2018)

The objective was to validate the carbon monoxide (CO) total column product inferred from Scanning Imaging Absorption Spectrometer for Atmospheric Chartography (SCIAMACHY) full-mission (2003–2011) short-wave infrared (SWIR) nadir observations using the Beer InfraRed Retrieval Algorithm (BIRRA). Globally distributed Network for the Detection of Atmospheric Composition Change (NDACC) and Total Carbon Column Observing Network (TCCON) ground-based (g-b) measurements were used as a true reference. Weighted averages of SCIAMACHY CO observations within a circle around the g-b observing system were utilized to minimize effects due to spatial mismatch of space-based (s-b) and g-b observations, i.e., disagreements due to representation errors rather than instrument and/or algorithm deficiencies. In addition, temporal weighted averages were examined and then the unweighted (classical) approach was compared to the weighted (non-classical) method. The delivered distance-based filtered SCIAMACHY data were in better agreement with respect to CO averages as compared to square-shaped sampling areas throughout the year. Errors in individual SCIAMACHY retrievals have increased substantially since 2005. The global bias was determined to be in the order of − 10 parts per billion in volume (ppbv) depending on the reference network and validation strategy used. The largest negative bias was found to occur in the northern mid-latitudes in Europe and North America, and was partly caused by insufficient a priori estimates of CO and cloud shielding. Furthermore, no significant trend was identified in the global bias throughout the mission. The global analysis of the CO columns retrieved by the BIRRA shows results that are largely consistent with similar investigations in previous works.
Clinical Course and Significance of the Clear Zone Around the Pedicle Screws in the Lumbar Degenerative Disease (2008)

As approximately two thirds of the clear zones disappeared over time, the presence of clear zones did not necessarily mean pseudarthrosis. However, clear zones persisting for 2 years or longer after surgery are a great risk of pseudarthrosis. Therefore, careful observation of clear zones around pedicle screws is of great significance as an evaluation of bone union.
Texture fluctuations and emergent dynamics in coupled nanomagnets (2022)

We analyse the thermal fluctuations of magnetization textures in two stray field coupled elements, forming mesospins. To this end, the energy landscape associated with the thermal dynamics of the textures is mapped out and asymmetric energy barriers are identified. These barriers are modified by changing the gap that separates the mesospins. Moreover, the coupling between the edges leads to an anisotropy in the curvature of the energy surface at the metastable minima. This yields a dynamic mode splitting of the edge modes and affects the attempt switching frequencies. Thus, we elucidate the mechanism with which the magnons in the thermal bath generate the stochastic fluctuations of the magnetization at the edges.
Granulation of silicone production dust waste for recycling (2019)

The purpose of the work is to propose a granulation technology for dust waste of metallurgical silicon production for its recycling in the process of ore-thermal reduction of silica. The technology includes the stages of magnetic separation, granulation and drying. Experimental works on iron oxide separation from cyclone dust were performed using a magnetic analyzer of the AMR type (Ukraine). Granulation was carried out using a drum granulator R-020 (Russia). The chemical composition was analyzed with the help of an optical emission spectrometer Varian 730-ES (USA). It has been determined that up to 37% of iron oxide is separated by the method of magnetic separation of silicon production cyclone dust. In the laboratory pelletization in a drum granulator the granules of 10-70 mm in size with the porosity of 40-45% were obtained. The carried out experiments have showed that there is a possibility in principle to use production wastes in the production technology of silicon of metallurgical grades as a pelletized additive to the main (lump) charge. Based on the results obtained, a line for granulating dust waste was proposed.
Redox-Induced Conformational Change in Mercaptoalkanoic Acid Multilayer Films (2012)

We discuss the assembly, structure, and stability of multilayer molecular films formed from multiple mercaptoalkanoic acid monolayers ligated via carboxyl and thiol interactions with divalent copper ions. Using dual-polarization interferometry to study the assembly of multilayer films in real time, we observe a clear linear relationship between the number of layers within a film and the overall average film thickness. Unexpectedly, however, we find a restructuring of the lower monolayer upon association of the Cu(2+) ions to form the Cu carboxylate surface. In particular, the thickness of the lower monolayer was found to decrease significantly, accompanied by an increase in the film density. The conformation of the monolayer subsequently recovered to that observed originally following the reduction of the Cu ion to Cu(+) upon chemisorption of the adlayer. Comparable restructuring was also observed in molecular dynamics simulations of a bilayer film assembled on a gold surface. Our combined experimental and theoretical study suggests that the observed restructuring is a result of charge-charge interactions between adjacent Cu ions that exist in the +2 oxidation state in the copper carboxylate surface and in the +1 oxidation state following chemisorption of the adlayer.
Electrically tunable delay line using an optical single-side-band modulator (2002)

The authors propose a tunable delay line using an optical single-side-band modulator, a fiber Bragg grating and an optical fiber loop. The number of times light circulates in the loop can be controlled by the electric signal fed to the modulator. Packets of any lengths can go through the proposed delay line without any collisions, even if the length of the packet is larger than that of the delay loop.
Analysis of Phosphorescence Decay in Heterogeneous Systems: Consequences of Finite Excitation Flash Duration (1999)

Analysis of phosphorescence lifetimes using the Stern-Volmer equation is a reliable means of determining quencher concentration for a uniform sample. Methods of analysis for heterogeneous systems are based on the assumption that the excitation is produced by a momentary flash. This condition is an idealization because a real flash has a finite duration and a complex time profile. In the case of a heterogeneous quencher concentration, an excitation flash produces different initial intensities and different times of peak intensity from compartments having different concentrations of quencher. We formulated a model to explore the effects of flash duration on the shape of the emission curve obtained from systems in which the heterogeneity is continuous. We developed mathematical models that can be used to recover fitting parameters of continuous distributions of reciprocal lifetimes approximated as rectangular or Gaussian distributions, or an arbitrary histogram. We also formulated a procedure to convert the distribution of reciprocal lifetimes into a volume distribution of quencher concentration. We found that (1) the Stern-Volmer ratio of phosphorescence intensities cannot be employed for interpretation of pulse phosphorometric data in terms of a volume distribution of quencher; (2) shortening the flash duration decreases the difference of initial intensities between compartments having high and low quencher concentration; (3) the parameters of the volume distribution of quencher concentration can be recovered correctly only after taking account of the difference in initial intensities; and (4) calibration of the initial intensities for a given fitting delay and flash function is necessary.
Flame Propagation : The Random Walk of Chemical Energy (1956)

A new approach to the theory of burning velocity is presented in which a flame front moves forward at a rate determined by the random walk of chemical (potential) energy. The flame velocity is determined by the value of n which is a collision rate divided by a reaction rate, both determined at the point of maximum reaction velocity. The comparison between theoretical and experimental flame velocities is given for cases in which the chemical kinetics are quite well understood. Empirical activation energies for reaction are given for certain hydrocarbon flames. It is hoped that these may be useful in determining the important chemical processes in hydrocarbon flame propagation.
An algorithm for constrained one-step inversion of spectral CT data (2016)

We develop a primal-dual algorithm that allows for one-step inversion of spectral CT transmission photon counts data to a basis map decomposition. The algorithm allows for image constraints to be enforced on the basis maps during the inversion. The derivation of the algorithm makes use of a local upper bounding quadratic approximation to generate descent steps for non-convex spectral CT data discrepancy terms, combined with a new convex-concave optimization algorithm. Convergence of the algorithm is demonstrated on simulated spectral CT data. Simulations with noise and anthropomorphic phantoms show examples of how to employ the constrained one-step algorithm for spectral CT data.
Processing of CFTR: Traversing the cellular maze—How much CFTR needs to go through to avoid cystic fibrosis? (2005)

Biosynthesis of the cystic fibrosis transmembrane conductance regulator (CFTR), like other proteins aimed at the cell surface, involves transport through a series of membranous compartments, the first of which is the endoplasmic reticulum (ER), where CFTR encounters the appropriate environment for folding, oligomerization, maturation, and export from the ER. After exiting the ER, CFTR has to traffic through complex pathways until it reaches the cell surface. Although not yet fully understood, the fine details of these pathways are starting to emerge, partially through identification of an increasing number of CFTR-interacting proteins (CIPs) and the clarification of their roles in CFTR trafficking and function. These aspects of CFTR biogenesis/degradation and by membrane traffic and CIPs are discussed in this review. Following this description of complex pathways and multiple checkpoints to which CFTR is subjected in the cell, the basic question remains of how much CFTR has to overcome these barriers and be functionally expressed at the plasma membrane to avoid CF. This question is also discussed here.
Abnormal lipoprotein metabolism and reversible female infertility in HDL receptor (SR-BI)–deficient mice (2001)

Mammalian female fertility depends on complex interactions between the ovary and the extraovarian environment (e.g., the hypothalamic-hypophyseal ovarian axis). The role of plasma lipoproteins in fertility was examined using HDL-receptor SR-BI knockout (KO) mice. SR-BI KO females have abnormal HDLs, ovulate dysfunctional oocytes, and are infertile. Fertility was restored when the structure and/or quantity of abnormal HDL was altered by inactivating the apoAI gene or administering the cholesterol-lowering drug probucol. This suggests that abnormal lipoprotein metabolism can cause murine infertility — implying a functional hepatic-ovarian axis — and may contribute to some forms of human female infertility.
Gold-black coatings for freestanding pyroelectric detectors (2003)

We describe the process of depositing gold-black on thin, freestanding pyroelectric detector substrates and compare this with previous work documented in the literature. We have evaluated gold-black coatings on thin, freestanding pyroelectric detector substrates by means of scanning electron microscope, Fourier transform infrared spectrophotometer reflectance, and spectral responsivity measurements. Spectrophotometric measurements indicate that reflectance at normal incidence varies by less than 1% at wavelengths shorter than 2.5 µm and by less than 10% at 10 µm. These results are correlated with the spectral responsivity of the detector and demonstrate that radiation not reflected by the gold-black is absorbed by the detector element. We have evaluated gold-black coatings as a function of position at two wavelengths and found variations of less than 1% at 1.25 µm and less than 5% at 10.3 µm, which demonstrates that spatial uniformity can be coating dependent. Gold-black coatings exposed to a 193 nm wavelength excimer laser were evaluated by visual inspection for damage and determined to have a damage threshold of approximately 38 mJ cm−2.
Synthesis of malononitriles of potential cytostatic and pesticidal activity by reaction of Grignard reagents with ylidenemalononitriles (1974)

The preparation of various α-substituted malononitriles, for biological evaluation, by the action of organomagnesium halides on ylidenemalononitriles is described. The nature of the products is dependent on the nature of the Grignard reagent as well as the substrate, in particular their stereochemical requirements. Reaction mechanisms are suggested, and the cytostatic activity of malononitriles is discussed.
Tangential AC breakdown strength of solid-solid interfaces considering surface roughness (2017)

The following topics are dealt with: filled polymers; permittivity; electric breakdown; space charge; resins; power cable insulation; ageing; nanocomposites; partial discharges; XLPE insulation.
Inside Cover: Porous and Water Stable 2D Hybrid Metal Halide with Broad Light Emission and Selective H2O Vapor Sorption (Angew. Chem. Int. Ed. 12/2023) (2023)

Porous and water-stable hybrid semiconductors as multifunctional materials display traits that are essential for demanding commercial applications. In their Research Article (e202218429), Ioannis Spanopoulos and co-workers report a strategy for generating porosity in hybrid metal halide semiconductors by using molecular cages as both structure-directing agents and counter-cations. This strategy gave rise to a direct bandgap semiconductor with record water stability and selective vapor sorption.
Regulation of Ventricular Contraction (1960)

At constant heart rates, efferent stimulation of the vagus nerve and of the left stellate ganglion revealed the following: 1. Vagal stimulation exerts a profound depressant effect on the strength of the atrial contraction and can thereby influence ventricular filling and ventricular stroke work; it elevates mean atrial pressure at any given level of ventricular stroke work. This occurs under experimental conditions wherein the vagal stimulation used does not produce an alteration in the performance characteristics of the ventricle. The effects of vagal stimulation are blocked by atropine. 2. Stellate ganglion stimulation or norepinephrine infusion augments the strength of atrial contraction and thus the atrial contribution to ventricular filling. The augmented atrial contraction takes place in a shorter period of time. 3. Stellate ganglion stimulation or norepinephrine infusion increases the external stroke work and power produced by the ventricle from any given mean atrial pressure and from any given end-diastolic pressure or fiber length.4. There is a family of curves representing the relation between end-diastolic fiber length and stroke work, as well as a family of curves representing the relation between mean atrial or end-diastolic pressure and stroke work.5. When taken together with the well-known sympathetic and parasympathetic effects on heart rate, the above data are believed to comprise a reasonably comprehensive description of the means available to the central nervous system for directly inducing acute changes in the activity of the heart.