gebhart/patrepeval huggingface dataset:
Chiral Calcium VAPOL Phosphate Mediated Asymmetric Chlorination and Michael Reactions of 3-Substituted Oxindoles (2011)

We disclose a novel high yielding and highly enantioselective chiral calcium VAPOL phosphate-catalyzed chlorination of 3-substituted oxindoles with N-chlorosuccinimide (NCS). The reaction conditions are also shown to be effective for the catalytic enantioselective Michael addition of 3-aryloxindoles to methyl vinyl ketone.
Selective and Efficient Recognition of Thymidylylthymidine (TpT) by Bis(ZnII-cyclen) and Thymidylylthymidylylthymidine (TpTpT) by Tris(ZnII-cyclen) at Neutral pH in Aqueous Solution (1999)

As sequence-selective small molecules, bis(ZnII-cyclen) and tris(ZnII-cyclen) are excellent and novel host molecules for thymidylylthymidine (TpT) and thymidylylthymidylylthymidine (TpTpT), respectively. Bis(ZnII-cyclen) binds specifically with imide-deprotonated T−pT−(Kd=10−6 M), while the tris(ZnII-cyclen) binds more strongly with T−pT−pT− to form the 1:1 complex, [T−pT−pT−-tris(ZnII-cyclen)] (Kd=10−9 M) at pH 8 in aqueous solution (see equation).
A phase II study of vorinostat and rituximab for treatment of newly diagnosed and relapsed/refractory indolent non-Hodgkin lymphoma (2015)

This study examines the activity and tolerability of a regimen combining vorinostat and rituximab in patients with indolent B-cell non-Hodgkin lymphoma. A total of 28 patients with newly diagnosed or relapsed/refractory follicular, marginal zone, or mantle cell lymphoma, with 4 or less prior therapies were eligible for this open-label phase II study. Oral vorinostat 200 mg was administered twice daily on days 1-14 along with 375 mg/m(2) of intravenous rituximab on day 1 of a 21-day cycle, continuing until disease progression or unacceptable toxicity. Primary end point was objective response rate, with secondary end points of progression-free survival, time to progression, duration of response, safety, and tolerability. Median follow up was 25.6 months and median number of vorinostat cycles was 11.5. Overall response rate was 46% for all patients, 67% for previously untreated, and 41% for relapsed/refractory patients. Median progression-free survival was 29.2 months for all patients, 18.8 months for previously treated patients, and not reached for untreated patients. The regimen was well tolerated over long treatment periods with the most common grade 3/4 adverse events being asymptomatic thrombosis, neutropenia, thrombocytopenia, lymphopenia, and fatigue. The vorinostat/rituximab combination exhibits activity in indolent B-cell non-Hodgkin lymphoma with an acceptable safety profile and durable responses. Re-treatment was effective in 2 of 3 relapsing responders. This phase II clinical trial was registered at clinicaltrials.gov identifier: 00720876.
International Working Group (IWG) consensus criteria for treatment response in myelofibrosis with myeloid metaplasia, for the IWG for Myelofibrosis Research and Treatment (IWG-MRT) (2006)

Myelofibrosis with myeloid metaplasia (MMM) is a clinicopathologic entity characterized by stem cell-derived clonal myeloproliferation, ineffective erythropoiesis, extramedullary hematopoiesis, and bone marrow fibrosis and osteosclerosis. Patients with MMM have shortened survival and their quality of life is compromised by progressive anemia, marked hepatosplenomegaly, and severe constitutional symptoms including cachexia. After decades of frustration with ineffective therapy, patients are now being served by promising treatment approaches that include allogeneic hematopoietic stem cell transplantation and immunomodulatory drugs. Recent information regarding disease pathogenesis, including a contribution to the myeloproliferative disorder phenotype by a gain-of-function JAK2 mutation (JAK2(V617F)), has revived the prospect of targeted therapeutics as well as molecular monitoring of treatment response. Such progress calls for standardization of response criteria to accurately assess the value of new treatment modalities, to allow accurate comparison between studies, and to ensure that the definition of response reflects meaningful health outcome. Accordingly, an international panel of experts recently convened and delineated 3 response categories: complete remission (CR), partial remission (PR), and clinical improvement (CI). Bone marrow histologic and hematologic remissions characterize CR and CR/PR, respectively. The panel agreed that the CI response category is applicable only to patients with moderate to severe cytopenia or splenomegaly.
Thermal stability in oligomeric triphenylamine/tris(8-quinolinolato) aluminum electroluminescent devices (1997)

Thermal stability of the electroluminescent (EL) devices using various hole-transporting materials based on triphenylamine, and a typical emitting material, tris(8-quinolinolato) aluminum has been systematically studied. The thermal stability of the EL devices is clearly seen to depend on the glass transition temperature (Tg) of the hole-transporting material. The highest thermal stability up to 155 °C is obtained in the device using the pentamer of triphenylamine. It has been found that the linear linkage of triphenylamine is useful to attain high Tg rather than the branch linkage.
Peroxisome Proliferator-activated Receptor α (PPARα) Induces PPARγ Coactivator 1α (PGC-1α) Gene Expression and Contributes to Thermogenic Activation of Brown Fat (2011)

Peroxisome proliferator activated receptor α (PPARα) is a distinctive marker of the brown fat phenotype that has been proposed to coordinate the transcriptional activation of genes for lipid oxidation and for thermogenic uncoupling protein 1 in brown adipose tissue. Here, we investigated the involvement of PPARα in the transcriptional control of the PPARγ coactivator (PGC)-1α gene. Treatment with PPARα agonists induced PGC-1α mRNA expression in brown fat in vivo and in primary brown adipocytes. This enhancement of PGC-1α transcription was mediated by PPARα binding to a PPAR-responsive element in the distal PGC-1α gene promoter. PGC-1α gene expression was decreased in PPARα-null brown fat, both under basal conditions and in response to thermogenic activation. Moreover, PPARα- and cAMP-mediated pathways interacted to control PGC-1α transcription. PRDM16 (PRD1-BF1-RIZ1 homologous domain-containing 16) promoted PPARα induction of PGC-1α gene transcription, especially under conditions in which protein kinase A pathways were activated. This enhancement was associated with the interaction of PRDM16 with the PGC-1α promoter at the PPARα-binding site. In addition, PPARα promoted the expression of the PRDM16 gene in brown adipocytes, and activation of PPARα in human white adipocytes led to the appearance of a brown adipocyte pattern of gene expression, including induction of PGC-1α and PRDM16. Collectively, these results suggest that PPARα acts as a key component of brown fat thermogenesis by coordinately regulating lipid catabolism and thermogenic gene expression via induction of PGC-1α and PRDM16.
Histidine Suppresses Food Intake through Its Conversion into Neuronal Histamine (2002)

Hypothalamic neuronal histamine has been shown to regulate feeding behavior and energy metabolism as a target of leptin action in the brain. The present study aimed to examine the involvement of L-histidine, a precursor of neuronal histamine, in the regulation of feeding behavior in rats. Intraperitoneal (ip) injection of L-histidine at doses of 0.35 and 0.70 mmol/kg body weight significantly decreased the 24-hr cumulative food and water intakes compared to phosphate buffered saline injected controls (P < 0.05 for each). This suppression of feeding was mimicked dose-dependently by intracerebroventricular infusion of histidine at doses of 0.5, 1.0, and 2.0 micromol/rat (P < 0.05 for each). Pretreatment of the rats with an ip bolus injection of alpha-fluoromethylhistidine, a suicide inhibitor of a histidine decarboxylase (HDC), at a dosage of 224 micromol/kg blocked the conversion of histidine into histamine and attenuated the suppressive effect of histidine on food intake from 64.2% to 88.1% of the controls (P < 0.05). Administration of 0.35 mmol/kg histidine ip increased the concentration of hypothalamic neuronal histamine compared with the controls (P < 0.05). HDC activity was increased simultaneously by histidine administration compared with the controls (P < 0.05). The present findings indicate that L-histidine suppresses food intake through its conversion into histamine in the hypothalamus.
Legionnaires' Disease (1977)

An explosive, common-source outbreak of pneumonia caused by a previously unrecognized bacterium affected primarily persons attending an American Legion convention in Philadelphia in July, 1976. Twenty-nine of 182 cases were fatal. Spread of the bacterium appeared to be air borne. The source of the bacterium was not found, but epidemiologic analysis suggested that exposure may have occurred in the lobby of the headquarters hotel or in the area immediately surrounding the hotel. Person-to-person spread seemed not to have occurred. Many hotel employees appeared to be immune, suggesting that the agent may have been present in the vicinity, perhaps intermittently, for two or more years.
Preparation of Novel Metallic and Bimetallic Cross‐Linked Poly(vinyl alcohol) Nanocomposites under Microwave Irradiation (2007)

Abstract A facile method utilizing microwave irradiation is described that accomplishes the cross‐linking reaction of PVA with metallic and bimetallic systems. Nanocomposites of PVA‐cross‐linked metallic systems such as Pt, Cu, and In and bimetallic systems such as Pt‐In, Ag‐Pt, Pt‐Fe, Cu‐Pd, Pt‐Pd and Pd‐Fe were prepared expeditiously by reacting the respective metal salts with 3 wt.‐% PVA under microwave irradiation, maintaining the temperature at 100 °C, a radical improvement over the methods for preparing cross‐linked PVA described in the literature. The general preparative procedure is versatile and provides a simple route to manufacturing useful metallic and bimetallic nanocomposites with various shapes, such as nanospheres, nanodendrites and nanocubes. magnified image
Optimizing the pentetrazol infusion test for seizure threshold measurement (1986)

Seizure thresholds in mice were determined using the pentetrazol infusion method. Concentration of infusate and rate of infusion were varied to assess the optimal parameters for seizure threshold detection. Seizure threshold elevations were produced by flurazepam and threshold decreases by FG 7142. An infusion rate of 1.1 ml min-1 was best for detecting both increases and decreases in threshold. However a concentration of 2.5 mg ml-1 gave optimal measurement of elevations in threshold whereas decreased thresholds were best detected with a concentration of 10 mg ml-1.
Inhibitors of proline-specific dipeptidyl peptidases: DPP IV inhibitors as a novel approach for the treatment of Type 2 diabetes (2005)

Dipeptidyl peptidase IV (DPP IV) is a validated target for the treatment of Type 2 diabetes, with several inhibitors currently in Phase III clinical trials. This review will mainly focus on DPP IV inhibitors that were published in scientific literature and patents after 2002. Medicinal chemistry aspects of several classes of inhibitors are described with respect to inhibitory potency, selectivity over DPP8, DPP9, FAPα and DPP II, stability and ADME/Tox issues. Although the main part of this review is on potent and selective DPP IV inhibitors, selective inhibitors for the related proline-specific dipeptidyl peptidases will be described.
Using ecological diversity measures with bacterial communities (2003)

Abstract There are many ecological diversity measures, but their suitability for use with highly diverse bacterial communities is unclear and seldom considered. We assessed a range of species richness and evenness/dominance indices, and the use of species abundance models using samples of bacteria from zinc-contaminated and control soils. Bacteria were assigned to operational taxonomic units (OTUs) using amplified ribosomal DNA restriction analysis of 236 clones from each soil. The reduced diversity apparent in the contaminated soil was reflected by the diversity indices to varying degrees. The number of clones analysed and the weighting given to rare vs. abundant OTUs are the most important considerations when selecting measures. Our preferences, arrived at using theory and practical experience, include: the log series index alpha; the Q statistic (but only if coverage is 50% or more); the Berger-Parker and Simpson's indices, although their ecological relevance may be limited; and, unexpectedly, the Shannon-Wiener and Shannon evenness indices, even though their meanings may not be clear and their values inaccurate when coverage is low. For extrapolation, the equation for the log series distribution seems the best for extrapolating from OTU accumulation curves while non-parametric methods, such as Chao 1, show promise for estimating total OTU richness. Due to a preponderance of single-occurrence OTUs, none of the five species abundance models fit the OTU abundance distribution of the control soil, but both the log and log normal models fit the less diverse contaminated soil. Species abundance models are useful, irrespective of coverage, because they address the whole distribution of a sample, aiding comparison by revealing overall trends as well as specific changes in particular abundance classes.
Simplified lysed-blood culture technique (1986)

A blood culture system was developed in which a lysing agent (either Tween 20, one of several other polyoxyethylene adducts, digitonin, or Triton X-100) is added to the blood culture medium. Of 33 Triton compounds, 9 lysed human blood, as did 7 of 21 polyoxyethylene compounds and digitonin, all at a concentration of 0.05%. Under the specific test conditions, three of the hemolytic polyoxyethylene compounds and digitonin had no inhibitory effect. All of the Triton compounds had at least some inhibitory effect on the most sensitive of the pathogenic bacteria that were tested, Streptococcus pneumoniae and Neisseria meningitidis. Because of results from previous studies, Triton X-100 was tested further, despite evidence in this study of its inhibition of bacteria. Of the 55 lysing agents tested, digitonin, Triton X-100, Brij 96, and Tween 20 were selected for further testing as additions to conventional culture broth. Comparative culture studies with bacteremic blood from infected rabbits were performed with the conventional blood culture, the Isolator system (Du Pont Co., Wilmington, Del.), and the new lysing medium. The new system has the advantages of lysis filtration and lysis centrifugation without the associated added cost and processing complexity.
Survey, Approach and Examples of Modeling Variants in Industrial Automation (2011)

In order to meet requirements of different stakeholders, product lines for industrial automation systems have a high degree of variability. Despite the remarkable effort made by researchers and practitioners, modeling variants remains a challenge. It is often difficult to decide what does vary, how it varies and which interdependencies have to be considered between variants of an industrial automation system. This paper discusses the state of the art in modeling variants and proposes a new approach based on SysML for modeling variants of an industrial automation system within a product line.
Electrical Characteristics of Nonpolar InGaN-Based Light-Emitting Diodes Evaluated at Low Temperature (2007)

The present article is a follow-up of our previous article [Jpn. J. Appl. Phys. 45 (2006) 7661]. InGaN-based light-emitting diodes of nonpolar orientation were grown on high-quality commercial GaN substrates. Results of low-temperature characterization showed that they were electrically conductive at temperature as low as 5 K. This experimental confirmation of electrical conduction at low temperature contradicts our previous results and the discussion of conduction mechanism returns to an impurity-concentration-related mechanism.
Photofrin uptake by murine macrophages. (1991)

The uptake of Photofrin by murine peritoneal macrophages in vivo and in vitro was examined. Cellular Photofrin content was measured either by performing a fluorometric assay or by using 14C-labeled drug. For comparison, the uptake of Photofrin by murine SCCVII tumor cells (squamous cell carcinoma) was also examined under the same conditions. The data demonstrate that macrophages have a much greater capacity for Photofrin uptake than SCCVII tumor cells. Photofrin contents at 24 h after drug administration (25 mg/kg) measured 420 +/- 90 (SD), 74 +/- 15, and 15 +/- 2 ng/micrograms of cell protein for peritoneal macrophages, tumor-associated macrophages, and SCCVII tumor cells, respectively. Factors that modify macrophage activity also influence the uptake of the drug by macrophages. The results support the assumption that Photofrin uptake by macrophages is dominated by phagocytosis of highly aggregated components of the drug. In vivo accumulated Photofrin material in peritoneal macrophages, tumor-associated macrophages, and tumor cells has shown very similar in vitro clearance from all three cell types. Only 20-30% of Photofrin was lost from the cells during the initial 24 h, mainly between 1 and 4 h of clearance incubation.
Generation of expressed sequence tags from a cDNA library of Coleus forskohlii for identification of genes involved in terpene biosynthesis (2015)

Coleus forskohlii (syn. Plectranthus barbatus) is a widely used medicinal plant and its main bioactive constituents are diterpenes forskolin and isoforskolin. The present study aimed to construct a cDNA library to identify expressed sequence tags related to terpene biosynthesis in C. forskohlii. We constructed a high quality normalized full-length cDNA library which reached the requirements (abundance, integrity, and library content) for isolating full-length genes. A total of 4 224 cDNA clones were sequenced and 2 394 unigenes were assembled with an average unigene size of 753 bp. A total of 2 100 (87.7 %) unigenes were functionally classified using gene ontologies, and 1 716 (71.7 %) unigenes were assigned to establish pathway associations in KEGG mapings. Notably, 64 unigenes putatively participated in the biosynthesis of secondary metabolites, in which 17 unigenes were identified that might be involved in the biosynthesis of the terpenoid backbone and monoterpenes, diterpenes, and triterpenes.
Differential Short-term Synaptic Plasticity and Transmission of Complex Spike Trains: to Depress or to Facilitate? (2000)

Experimental studies have revealed conspicuous short-term facilitation and depression that are expressed differentially at distinct classes of cortical synapses. To explore computational implications of synaptic dynamics, we investigated transmission of complex spike trains through a stochastic model of cortical synapse endowed with short-term facilitation and vesicle depletion. Inputs to the synapse model were either real spike train data recorded from the visual and prefrontal cortices of behaving monkeys, or were generated numerically with prescribed temporal statistics. We tested the hypothesis that short-term facilitation could enable synapses to filter out single spikes and favor bursts of action potentials. We found that the ratio between release probabilities for a burst spike and an isolated spike grows monotonically with increasing number of spikes per burst, and with increasing interval between isolated spikes. Burst detection is optimal when the facilitation time constant matches the average burst duration. Using fractal-like spike patterns characterized by long-term power-law temporal correlations and similar to those seen in sensory neurons, we found that facilitation increases correlation at short time scales. In contrast, depression leads to a dramatic reduction in temporal correlations at all time scales, and to a flat ('whitened') power spectrum, thereby decorrelating natural input signals.
The effects of an estrogen and glycolic acid cream on the facial skin of postmenopausal women: a randomized histologic study. (2003)

A prospective, randomized, double-blind study was conducted to determine if estradiol and glycolic acid creams produced a significant reversal of epidermal and dermal markers of aging and if the cumulative effect of the creams was greater than either alone. Sixty-five patients applied a cream containing 0.01% estradiol or 15% glycolic acid, alone or in combination, to one side of the face, and a vehicle cream to the opposite side, for 6 months. A 2-mm punch biopsy was obtained from the hairline of each patient and processed for analysis. The estradiol treatment produced a 23% increase in epidermal thickness (P = .00458); the glycolic acid, a 27% increase (P = .00467); and the combination, a 38% increase (P = .000181). All groups showed a statistically significant improvement in reversing markers (rete peg pattern, epidermal thickness) of skin aging. Although not statistically significant (P = .1), a cumulative effect was seen when estradiol and glycolic acid creams were used in combination.
Enhancement of voltage-controlled magnetic anisotropy through precise control of Mg insertion thickness at CoFeB|MgO interface (2017)

We studied the impact of different insertion layers (Ta, Pt, and Mg) at the CoFeB|MgO interface on voltage-controlled magnetic anisotropy (VCMA) effect and other magnetic properties. Inserting a very thin Mg layer of 0.1–0.3 nm yielded a VCMA coefficient of 100 fJ/V-m, more than 3 times higher than the average values of around 30 fJ/V-m reported in Ta|CoFeB|MgO-based structures. Ta and Pt insertion layers also showed a small improvement, yielding VCMA coefficients around 40 fJ/V-m. Electrical, magnetic, and X-ray diffraction results reveal that a Mg insertion layer of around 1.2 nm gives rise to the highest perpendicular magnetic anisotropy, saturation magnetization, as well as the best CoFe and MgO crystallinity. Other Mg insertion thicknesses give rise to either under- or over-oxidation of the CoFe|MgO interface; a strong over-oxidation of the CoFe layer leads to the maximum VCMA effect. These results show that precise control over the Mg insertion thickness and CoFe oxidation level at the CoFeB|MgO interface is crucial for the development of electric-field-controlled perpendicular magnetic tunnel junctions with low write voltage.
Electrochemistry in Room Temperature Ionic Liquids: A Review and Some Possible Applications (2006)

A review of electrochemistry in ionic liquids is presented, highlighting some particular examples, with the aim to compare any similarities and differences observed in RTILs to that observed in conventional solvents. The presence of impurities such as halide and water on the electrochemical window and viscosity of RTILs is discussed. Some fundamental electrochemical studies relating to mass transport, heterogeneous electron transfer kinetics and double-layer capacitance are compared to similar studies in conventional solvents, and the suitability of RTILs as solvents in electrochemical experiments is considered. The application of RTILs as replacements for conventional solvents in gas sensors is reviewed, focussing on the electrochemistry observed in RTILs for the following gases: oxygen, a mixture of oxygen and carbon dioxide, and ammonia. The low volatility and high thermal stability of RTILs renders them advantageous for the development of robust sensors under extreme conditions. Finally, the possibility for use of RTILs as solvents in electrosynthesis is discussed, focussing on two examples: the reactivity of electrogenerated bromine with cyclohexene, and the reduction of 4-nitrophenol. It is obvious that RTILs have the ability to offer many advantages over traditional solvents in the field of electrochemistry.