gebhart/patrepeval huggingface dataset:
Testosterone, dihydrotestosterone, trenbolone acetate, and zeranol alter the synthesis of cortisol in bovine adrenocortical cells (1993)

The objective of this study was to examine the effect of anabolic steroids (testosterone, T; dihydrotestosterone, D; trenbolone acetate, B; and zeranol, Z) on cortisol synthesis by cultured bovine adrenocortical cells. Adrenal glands were obtained from slaughter-aged steers (n = 4). Cortical cells were isolated and their steroidogenic capacity was examined. They were plated in multiwell culture plates. At confluence, cells were treated with T, D, B, or Z at 0, 10, 50, 125, or 500 ng/mL (eight wells per treatment). Twenty-four hours after treatment, one-half of each treatment concentration was stimulated with 10(-9) M ACTH. After 8 h of incubation, cortisol concentration in the media was measured using RIA. Cortical cells were removed from the plates using 1 mM EDTA and analyzed for DNA content. Data were subjected to rank transformation and analyzed by randomized complete block design. Adrenocorticotropic hormone stimulated (P < .01) the release of cortisol by more than threefold. Cortisol synthesis was lower (P < .05) in the presence of T, D, and B. Testosterone caused a greater (P < .05) suppression in cortisol production at 50 and 125 ng/mL than did D. The suppression of cortisol synthesis did not differ between B and T or between B and D. Cortisol synthesis was lowered (P < .05) by the presence of T, D, and B in both ACTH-stimulated and nonstimulated cells but was only suppressed in ACTH-stimulated cells of Z-treated cells.(ABSTRACT TRUNCATED AT 250 WORDS)
One-Handed Juggling: A Dynamical Approach to a Rhythmic Movement Task (1996)

The skill of rhythmically juggling a ball on a racket was investigated from the viewpoint of nonlinear dynamics. The difference equations that model the dynamical system were analyzed by means of local and nonlocal stability analyses. These analyses showed that the task dynamics offer an economical juggling pattern that is stable even for open-loop actuator motion. For this pattern, two types of predictions were extracted: (a) Stable periodic bouncing is sufficiently characterized by a negative acceleration of the racket at the moment of impact with the ball, and (b) a nonlinear scaling relation maps different juggling trajectories onto one topologically equivalent dynamical system. The relevance of these results for the human control of action was evaluated in an experiment in which subjects (N = 6) performed a comparable task of juggling a ball on a paddle. Task manipulations involved different juggling heights and gravity conditions of the ball. The following predictions were confirmed: (a) For stable rhythmic performance, the paddle's acceleration at impact is negative and fluctuations of the impact acceleration follow predictions from global stability analysis; and (b) for each subject, the realizations of juggling for the different experimental conditions are related by the scaling relation. These results permit one to conclude that humans reliably exploit the stable solutions inherent to the dynamics of the given task and do not overrule these dynamics by other control mechanisms. The dynamical scaling serves as an efficient principle for generating different movement realizations from only a few parameter changes and is discussed as a dynamical formalization of the principle of motor equivalence.
A Mechanism Design Approach for Coordination of Thermostatically Controlled Loads (2015)

This paper focuses on the coordination of a population of thermostatically controlled loads (TCLs) with unknown parameters to achieve group objectives. The problem involves designing the device bidding and market clearing strategies to motivate self-interested users to realize efficient energy allocation subject to a peak energy constraint. This coordination problem is formulated as a mechanism design problem, and we propose a mechanism to implement the social choice function in dominant strategy equilibrium. The proposed mechanism consists of a novel bidding and clearing strategy that incorporates the internal dynamics of TCLs in the market mechanism design, and we show it can realize the team optimal solution. A learning scheme is proposed to address the unknown load model parameters. Numerical simulations are performed to validate the effectiveness of the proposed coordination framework.
A Recombinant form of Pseudomonas Exotoxin a Containing Transforming Growth Factor Alpha Near its Carboxyl Terminus for the Treatment of Bladder Cancer (1993)

The epidermal growth factor receptor (EGFR) is overexpressed on the superficial layers of malignant urothelium and is suspected of playing a role in tumor progression. TP40 is a chimeric protein composed of transforming growth factor-alpha (TGF alpha) fused to a modified form of Pseudomonas exotoxin A (PE) that is selectively cytotoxic to EGFR-bearing cells and is currently undergoing clinical study for the intravesical therapy of bladder cancer. We constructed a recombinant toxin PE35/TGF alpha-KDEL as an improved agent for the local therapy of EGFR-bearing bladder cancer. PE35/TGF alpha-KDEL does not require intracellular proteolysis to generate a carboxyl-terminal fragment capable of reaching the target cell cytosol and contains a modified carboxyl-terminal sequence KDEL, that increases toxin activity. These features make PE35/TGF alpha-KDEL from 10- to 700-fold more potent than TP40 on four human bladder cancer cell lines. PE35/TGF alpha-KDEL may be a useful agent for treatment of EGFR-bearing cancers.
Synthesis and Pharmacological Properties of 11-Hydroxy-3-(1',1'-dimethylheptyl)hexahydrocannabinol: A High Affinity Cannabinoid Agonist (1994)

11-Hydroxy-3-(1',1'-dimethylheptyl)hexahydrocannabinol (1) was synthesized from the known cannabimimetic analog (+/-)-nabilone. Racemic 1 was resolved by HPLC on a semipreparative CHIRALCEL OD column (Daicel, Inc.), and pharmacological activities of the individual enantiomers were evaluated in the mouse model. The (-)-enantiomer was found to be much more potent than the (+)-enantiomer in all the four measures with the potency ratios in the production of catalepsy (RI), hypoactivity (SA), hypothermia (RT), and antinociception (TF) being 93, 143, 186, and 322, respectively. The racemic 11 alpha-OH diastereomer (2), a reaction side product, was also evaluated in the mouse model. Only small differences in the pharmacological activity of racemic 1 and 2 were found in the above four measures.
Synthesis and Reactions of Furo[3,2-b]pyrrole Type Aldehydes (1993)

The synthesis of ethyl 2-formyl-4-benzylfuro[3,2- b ]pyrrole-5-carboxylate ( I ) is described. A series of furo[3,2- b ]pyrrole-2-carbaldehyde 2,6-dialkylphenylhydrazones ( IIa - IIg ) and dimethylhydrazones ( IIIa - IIId ) were prepared. By reaction of title compounds with hydroxylammonium chloride in acetic anhydride in the presence of pyridine corresponding cyano-substituted compounds ( IVa - IVd ) were obtained. Alkaline hydrolysis of IVa - IVd gave Va - Vb and the reaction with sodium azide and ammonium chloride in dimethylformamide led to VIa - VId . the structure of the compounds have been proved by UV, IR, 1 H and 13 C NMR spectra.
Differential Regulation of Responsiveness to fMLP and C5a Upon Dendritic Cell Maturation: Correlation with Receptor Expression (2000)

The trafficking of immature and mature dendritic cells (DCs) to different anatomical sites in vivo is critical for fulfilling their roles in the induction of Ag-specific immune responses. Although this process is complex and regulated by many mediators, the capacity of DCs to migrate is predominantly dependent on the expression of particular chemotactic receptors on the surface of DCs that enable them to move along chemotactic gradients formed by the corresponding chemokines and/or classical chemoattractants. Here we show that immature DCs (iDCs) respond to both fMLP and C5a as determined by chemotaxis and Ca2+ mobilization, whereas mature DCs (mDCs) respond to C5a, but not fMLP. Additionally, iDCs express the receptors for both fMLP and C5a at mRNA and protein levels. Upon maturation of DCs, fMLP receptor expression is almost completely absent, whereas C5a receptor mRNA and protein expression is maintained. Concomitantly, mDCs migrate chemotactically and mobilize intracellular Ca2+ in response to C5a, but not fMLP. Thus the interaction between C5a and its receptor is likely involved in the regulation of trafficking of both iDCs and mDCs, whereas fMLP mobilizes only iDCs. The differential responsiveness to fMLP and C5a of iDCs and mDCs suggests that they play different roles in the initiation of immune responses.
MAP4K4 Gene Silencing in Human Skeletal Muscle Prevents Tumor Necrosis Factor-α-induced Insulin Resistance (2007)

Tumor necrosis factor-alpha (TNF-alpha) induces skeletal muscle insulin resistance by impairing insulin signaling events involved in GLUT4 translocation. We tested whether mitogenic-activated protein kinase kinase kinase kinase isoform 4 (MAP4K4) causes the TNF-alpha-induced negative regulation of extracellular signal-regulated kinase-1/2 (ERK-1/2), c-Jun NH2-terminal kinase (JNK), and the insulin receptor substrate-1 (IRS-1) on the insulin signaling pathway governing glucose metabolism. Using small interfering RNA (siRNA) to suppress the expression of MAP4K4 protein 85% in primary human skeletal muscle cells, we provide evidence that TNF-alpha-induced insulin resistance on glucose uptake was completely prevented. MAP4K4 silencing inhibited TNF-alpha-induced negative signaling inputs by preventing excessive JNK and ERK-1/2 phosphorylation, as well as IRS-1 serine phosphorylation. These results highlight the MAPK4K4/JNK/ERK/IRS module in the negative regulation of insulin signaling to glucose transport in response to TNF-alpha. Depletion of MAP4K4 also prevented TNF-alpha-induced insulin resistance on Akt and the Akt substrate 160 (AS160), providing evidence that appropriate insulin signaling inputs for glucose metabolism were rescued. Silencing of MAP2K1 and MAP2K4, signaling proteins downstream of MAP4K4, recapitulated the effect of MAP4K4 siRNA in TNF-alpha-treated cells. Thus, strategies to inhibit MAP4K4 may be efficacious in the prevention of TNF-alpha-induced inhibitory signals that cause skeletal muscle insulin resistance on glucose metabolism in humans. Moreover, in myotubes from insulin-resistant type II diabetic patients, siRNA against MAP4K4, MAP2K4, or MAP2K1 restored insulin action on glucose uptake to levels observed in healthy subjects. Collectively, our results demonstrate that MAP4K4 silencing prevents insulin resistance in human skeletal muscle and restores appropriate signaling inputs to enhance glucose uptake.
Isolation and characterization of β-act in gene of carp ( Cyprinus carpio ) (1990)

A beta-actin gene of carp (Cyprinus carpio) was isolated from a genomic EMBL3 library. The nucleotide sequence of the gene indicates six exons spanning 3.6 kb. Southern blot hybridization of restriction endonuclease digests of carp genomic DNA indicate that there are two copies of the beta-actin isotype and several other species of actin genes. The transcriptional start site is 85 bp and 24 bp downstream respectively from consensus CCAAT and TATA promoter elements. The organization of the carp beta-actin gene is identical to that of chicken, human, and rat genes in terms of size, exon/intron locations and junctions and in having a translationally silent first exon. The fish gene is 90% and 99% conserved at the nucleotide and amino acid levels, respectively, with land vertebrate beta-actin genes. Northern blot analysis of beta-actin gene expression indicated that the gene is highly expressed in brain, less so in muscle, and much less so in liver cells. The putative beta-actin proximal promoter of carp, identified by the conservation of known actin regulatory sequences, is transcriptionally active in both mammalian and piscine cells.
From image parsing to painterly rendering (2009)

We present a semantics-driven approach for stroke-based painterly rendering, based on recent image parsing techniques [Tu et al. 2005; Tu and Zhu 2006] in computer vision. Image parsing integrates segmentation for regions, sketching for curves, and recognition for object categories. In an interactive manner, we decompose an input image into a hierarchy of its constituent components in a parse tree representation with occlusion relations among the nodes in the tree. To paint the image, we build a brush dictionary containing a large set (760) of brush examples of four shape/appearance categories, which are collected from professional artists, then we select appropriate brushes from the dictionary and place them on the canvas guided by the image semantics included in the parse tree, with each image component and layer painted in various styles. During this process, the scene and object categories also determine the color blending and shading strategies for inhomogeneous synthesis of image details. Compared with previous methods, this approach benefits from richer meaningful image semantic information, which leads to better simulation of painting techniques of artists using the high-quality brush dictionary. We have tested our approach on a large number (hundreds) of images and it produced satisfactory painterly effects.
Clinical diagnosis of Alzheimer's disease (1984)

Clinical criteria for the diagnosis of Alzheimer's disease include insidious onset and progressive impairment of memory and other cognitive functions. There are no motor, sensory, or coordination deficits early in the disease. The diagnosis cannot be determined by laboratory tests. These tests are important primarily in identifying other possible causes of dementia that must be excluded before the diagnosis of Alzheimer's disease may be made with confidence. Neuropsychological tests provide confirmatory evidence of the diagnosis of dementia and help to assess the course and response to therapy. The criteria proposed are intended to serve as a guide for the diagnosis of probable, possible, and definite Alzheimer's disease; these criteria will be revised as more definitive information become available.
Case 13-2013 (2013)

A 6-year-old girl was admitted to this hospital because of bone and joint pain for 1 year and recent onset of fever and abdominal distention. Imaging revealed a mass in the abdominal and pelvic region and lesions in the liver, kidneys, and multiple bones.
Production Options for Psilocybin: Making of the Magic (2018)

The fungal genus Psilocybe and other genera comprise numerous mushroom species that biosynthesize psilocybin (4-phosphoryloxy-N,N-dimethyltryptamine). It represents the prodrug to its dephosphorylated psychotropic analogue, psilocin. The colloquial term "magic mushrooms" for these fungi alludes to their hallucinogenic effects and to their use as recreational drugs. However, clinical trials have recognized psilocybin as a valuable candidate to be developed into a medication against depression and anxiety. We here highlight its recently elucidated biosynthesis, the concurrently developed concept of enzymatic in vitro and heterologous in vivo production, along with previous synthetic routes. The prospect of psilocybin as a promising therapeutic may entail an increased demand, which can be met by biotechnological production. Therefore, we also briefly touch on psilocybin's therapeutic relevance and pharmacology.
Inhibition of angiogenesis and growth of human nerve-sheath tumors by AGM-1470 (1993)

The effectiveness of AGM-1470, a potent, fungal-derived inhibitor of angiogenesis, in suppressing the neovascularization and growth of human Schwann cell tumors was tested in six schwannomas, seven neurofibromas, and one neurofibrosarcoma. Tumor fragments from surgical specimens were implanted into the subrenal capsule of 348 nude mice (nu/nu). Seven days after implantation, the tumors were measured and vascularity was graded. The animals were then randomly assigned to one of two groups, to receive either saline (control group) or systemic AGM-1470 treatment. After 2 to 6 weeks of treatment, tumor size and degree of vascularity were recorded. In the six different schwannomas implanted into 138 mice, the average vascular grade in the control group after 2 weeks of treatment increased from 2.2 to 3.2 (+1.0), while in the AGM-1470-treated group it decreased from 2.2 to 1.7 (-0.5) (p < 0.01). In the seven different neurofibromas implanted into 158 mice, the change in the average vascular grade in control and AGM-1470-treated animals was +0.5 and -1.0, respectively (p < 0.01). In the one neurofibrosarcoma implanted into 52 mice, the change in average vascular grade in each group during the 6-week treatment period was +1.9 and -1.0, respectively (p < 0.01). Neurofibrosarcoma growth after 6 weeks of AGM-1470 treatment was only 8.5% of the growth found in the control animals (p < 0.01). This study determined that AGM-1470 is effective in inhibiting angiogenesis and the growth of human nerve-sheath tumors.
Prevalence and Serovars of Leptospira Involved in Equine Abortions in Central Kentucky during the 1991–1993 Foaling Seasons (1995)

In this study, the prevalence of leptospira-induced abortions/stillbirths for the past 3 foaling seasons (1991–1993) was determined, and fetal tissues and/or the mare's urine from positive cases were cultured in an attempt to isolate and identify the leptospira serovars responsible for the abortions. The sensitivity and specificity of the primary diagnostic tests, the fluorescent antibody test (FAT) and the microscopic agglutination test (MAT), used for the diagnosis of leptospirosis were also determined. For the 3 years, 74 (3.3%) of 2,264 abortion/ stillborn submissions were diagnosed as leptospirosis. Twelve cases occurred in the 1991, 19 in the 1992, and 43 in the 1993 foaling seasons. Leptospires were isolated from 45 (60.8%) of the 74 cases, and they were identified as serovar kennewicki (43 cases), serovar grippotyphosa (1 case), and a serovar similar to pomona (1 case). Of the 29 culture-negative cases, serologic results indicated that leptospires in the Pomona serogroup (kennewicki is a member of this serogroup) were responsible for 25 abortions, leptospires in the Grippotyphosa serogroup for 1 abortion, and leptospires in the Sejroe serogroup for 1 abortion. The specificities of the FAT on fetal tissues and mare's placenta and of the MAT on fetal fluid were 100%. The sensitivity of the FAT was 98.7%, and that of the MAT was 81.3%.
Graphene-P(VDF-TrFE) Multilayer Film for Flexible Applications (2013)

A flexible, transparent acoustic actuator and nanogenerator based on graphene/P(VDF-TrFE)/graphene multilayer film is demonstrated. P(VDF-TrFE) is used as an effective doping layer for graphene and contributes significantly to decreasing the sheet resistance of graphene to 188 ohm/sq. The potentiality of graphene/P(VDF-TrFE)/graphene multilayer film is realized in fabricating transparent, flexible acoustic devices and nanogenerators to represent its functionality. The acoustic actuator shows good performance and sensitivity over a broad range of frequency. The output voltage and the current density of the nanogenerator are estimated to be ∼3 V and ∼0.37 μAcm(-2), respectively, upon the application of pressure. These values are comparable to those reported earlier for ZnO- and PZT-based nanogenerators. Finally, the possibility of rollable devices based on graphene/P(VDF-TrFE)/graphene structure is also demonstrated under a dynamic mechanical loading condition.
A Mild Stereo‐ and Enantiospecific Conversion of 2,3‐Diaryl‐Substituted Oxiranes into 2,2‐Dimethyl‐1,3‐Dioxolanes by an Acetone/Amberlyst 15 System (2006)

Abstract Amberlyst 15 is an efficient catalyst for the reaction of aryl‐substituted oxiranes with acetone to prepare 2,2‐dimethyl‐1,3‐dioxolanes in high yields. trans ‐2,3‐Diaryloxiranes afford trans ‐acetonides enantiospecifically at room temperature, and the use of enantiopure 2,3‐diaryloxiranes results in no loss of stereochemical integrity in the resulting trans ‐acetonides. (© Wiley‐VCH Verlag GmbH &amp; Co. KGaA, 69451 Weinheim, Germany, 2006)
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists (2019)

While the melanocortin receptors (MCRs) are known to be involved in numerous biological pathways, the potential roles of the MC5R have not been clearly elucidated in humans. Agouti-related protein (AgRP), an MC3R/MC4R antagonist and MC4R inverse agonist, contains an exposed β-hairpin loop composed of six residues (Arg-Phe-Phe-Asn-Ala-Phe) that is imperative for binding and function. Within this active loop of AgRP, four human missense polymorphisms were deposited into the NIH Variation Viewer database. These polymorphisms, Arg111Cys, Arg111His, Phe112Tyr, and Ala115Val (AgRP full-length numbering), were incorporated into the peptide macrocycles c[Pro<sup>1</sup>-Arg<sup>2</sup>-Phe<sup>3</sup>-Phe<sup>4</sup>-Xaa<sup>5</sup>-Ala<sup>6</sup>-Phe<sup>7</sup>-dPro<sup>8</sup>], where Xaa was Dap<sup>5</sup> or Asn<sup>5</sup>, to explore the functional effects of these naturally occurring substitutions in a simplified AgRP scaffold. All peptides lowered potency at least 10-fold in a cAMP accumulation assay compared to the parent sequences at the MC4Rs. Compounds MDE 6-82-3c, ZMK 2-82, MDE 6-82-1c, ZMK 2-85, and ZMK 2-112 are also the first AgRP-based chemotypes that antagonize the MC5R.
Non-destructive characterization of thermal ageing of the Cu-rich WB36 steel 15 NiCuMoNb 5 (1.6368) (2006)

The phenomenon of precipitation hardening in steels is usually associated with carbon and nitrogen additions which precipitate out under heat treatment or specific service conditions as carbides or carbo-nitrides. In some alloys, however, for instance in Western nuclear pressure vessel steels, small additions of copper can be the driving force for embrittlement and hardening. In the case of the steel grade WB36 (15 NiCuMoNb 5, 1.6368), which is in service in fossil power plants and German nuclear power plants, the effects of copper precipitation are even larger. The progress of precipitation can be characterized by Vickers hardness measurements which, however, cannot be applied in an area-wide manner under practical circumstances. A demand for the development of equivalent NDT techniques, therefore, arises.To this end, Fraunhofer IZFP has adapted and developed the so-called 3MA approach which combines several micro-magnetic testing quantities for the characterization of mechanical properties. This paper presents and discusses recent results obtained using the 3MA approach applied to characterizing the ageing response of steel WB36.
A Colorimetric Sensor Array for Organics in Water (2005)

Molecular recognition of organic compounds in aqueous solutions is inherently challenging due to the potential interference from the very high concentration of water. Here we present a simple colorimetric sensor array that probes a wide range of chemical properties. By printing hydrophobic dyes on a hydrophobic membrane, sensor arrays are easily prepared that provide substantial chemical selectivity for the identification and quantification of various organics (both single compounds and complex mixtures) dissolved in water. It is possible to differentiate easily even among closely related organic compounds. Upon immersion in aqueous solutions, digital imaging of the dye array before and after exposure to an analyte provide a color change profile that is a fingerprint for the organic components of the solution. Facile identification of a wide variety of aqueous organic solutions is possible over a concentration range of 0.1 M to 1 muM. Complex mixtures present no inherent difficulty; for example, a series of commercial soft drinks were easily distinguished using the colorimetric sensor array approach.