gebhart/patrepeval huggingface dataset:
Abstract 2524: Promising early-stage novel androgen receptor antagonists in head-head comparisons with Enzalutamide and Bicalutamide (2014)

Abstract Prostate cancer is the most common male cancer and the second leading cause of cancer-related deaths in developed countries. The androgen receptor (AR) is a key molecular target in the etiology and progression of the disease where the early stages of prostate cancer tumor growth are androgen dependent and respond well to androgen ablation and androgen receptor antagonists. However, castration-resistant prostate cancer (CRPC) typically develops in 1-2 years after androgen deprivation therapy and AR antagonist administration. Despite promising results from the recently approved second-generation AR antagonist Enzalutamide (MDV3100), CRPC remains a largely unmet medical need with less than a 15% 5-year survival rate. This poster introduces the discovery of a novel series of significantly structurally distinct small-molecule androgen antagonists from current therapeutics with promising biological profiles in (1) an FP binding assay, (2) a GeneBlazerTM functional assay and (3) a study of anti-proliferative activity against LNCaP cell growth. One of several promising compounds from a current collection of ∼100 analogs is exemplified by AR002. CompoundFP AR binding assay (IC50)GeneBlazerTM β-lactamase reporter assay (IC50)LNCAP cell growth inhibition (GI50)AR002328.7 nM557 nM2.3 μMEnzalutamide920 nM1150 nM11.65 μMBicalutamide145 nM1370 nM30.68 μM In summary, a novel class of AR antagonists has been identified, encouragingly demonstrating potent activity against AR and inhibition of cell growth in the prostate specific line LNCaP. Citation Format: Arthur Y. Shaw, Vijay Gokhale, Christopher Hulme, Steven P. Stratton. Promising early-stage novel androgen receptor antagonists in head-head comparisons with Enzalutamide and Bicalutamide. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 2524. doi:10.1158/1538-7445.AM2014-2524
Reperfusion injury in the endotoxin‐treated rat heart: reevaluation of the role of nitric oxide (1997)

1. The role of nitric oxide (NO) in ischaemia-reperfusion injury to the heart continues to be debated. 2. The role of NO released during endotoxemia on myocardial reperfusion injury was examined in rats given saline or lipopolysaccharide (LPS, 10 mg. kg-1). 3. Aortic rings from LPS-treated rats showed a markedly decreased contractile response to both noradrenaline (NA) and U46619, and a diminished relaxation response to acetylcholine, thrombin and aggregating platelets. Treatment of rat aortic rings from LPS-treated rats with the NO synthesis inhibitor N omega-nitro-L-arginine (L-NOARG) reversed the diminished contractile response to NE and U46619. 4. Before ischaemia-reperfusion, baseline force of cardiac contraction (FCC) and coronary perfusion pressure (CPP) were lower and coronary flow was higher in hearts from LPS-treated rats (all P < 0.05 vs. saline-treated group). Treatment of hearts from LPS-treated rats with L-NOARG increased baseline FCC and CPP. 5. After ischaemia-reperfusion, hearts from saline-treated rats showed a 36 +/- 5% fall in FCC, a 38 +/- 6% rise in CPP and a 38 +/- 5% fall in coronary flow, whereas hearts from LPS-treated rats revealed only a 16 +/- 9% fall in FCC, a 10 +/- 3% rise in CPP and a 20 +/- 4% fall in coronary flow (all P < 0.05 vs. changes in saline-treated group). Fewer hearts from LPS-treated rats developed reperfusion arrhythmias (6% vs. 60% hearts from saline-treated rats, P < 0.02). Myocardial superoxide dismutase activity was higher in the LPS-treated group (P < 0.05). 6. NO synthesis, measured as formation of nitrite, was higher (P < 0.05) in cardiac and aortic tissues from LPS-treated rats. Prostacyclin (PGI2) release in coronary effluent was greater in LPS-treated rat hearts (P < 0.05 vs. saline-treated rats). 7. Thus LPS-treated hearts demonstrate a basal decrease in FCC and coronary vascular resistance. These hearts demonstrate a modest protection from reperfusion injury. Induction of NO synthesis, and possibly PGI2 release, may underlie cardioprotection from ischaemia-reperfusion.
Adaptive Noise Equalizer with Equal-Loudness Compensation (2005)

We apply equal-loudness compensation to the adaptive active noise equalizer (ANE). Previous works have focused mainly on using an adaptive gain factor to control the degree of noise reduction or amplification. In order to have a more accurate perception of the actual attenuation or amplification of the noise level, equal-loudness compensation is incorporated into the gain factor. This approach provides an improved performance as compared to the conventional ANE, in term of perceived loudness of the residual noise.
Dynamic Superresolution Optical Lattice Microscopy (2005)

The potential for high-speed superresolution fluorescence microscopy through the combination of optical lattice excitation with methods such as stimulated emission depletion, total internal reflection, and multidimensional localization is considered theoretically.
The Impact of Kitchen and Food Service Preparation Practices on the Volatile Aroma Profile in Ripe Tomatoes: Effects of Refrigeration and Blanching (2019)

Both refrigeration and blanching of red-stage tomatoes are common practices in Japan home kitchens and in food service operations. However, little is reported on the impact of such practices on aroma profiles in tomato fruits. In this study, ‘FL 47’ tomatoes at red stage were dipped in 50 °C hot water for 5 minutes or exposed to 5 °C for 4 days to simulate consumer handling of tomato in food service or home kitchens, respectively. Of the 42 volatile compounds detected, refrigeration generally suppressed production of aldehydes, alcohols, oxygen-containing heterocyclic compounds, and nitrogen- and oxygen-containing heterocyclic compounds, including the following abundant and/or important volatiles: pentanal, 3-methylbutanal, 2-methylbutanal, hexanal, cis -3-hexenal, trans -2-hexenal, 2- phenylacetaldehyde, pentanol, 3-methylbutanol, 2-phenylethanol, 1-penten-3-one, gera-nial, and geranylacetone. On the other hand, the production of aldehydes, alcohols, hydrocarbons, oxygen-containing heterocyclic compounds, and nitrogen- and oxygen-containing heterocyclic compounds was reduced by blanching, associated with low concentrations of 2-methylbutanal, pentanal, cis -3-hexenal, trans -2-hexenal, 2-phenyl-acetaldehyde, pentanol, 2-methylbutanol, and 2-phenylethanol. These results indicate that a short blanching or refrigeration of tomatoes substantially impacts tomato aroma quality.
A wafer-bonded hybrid silicon quantum dot laser (2016)

We present a wafer-bonded hybrid-silicon quantum-dot laser. Continuous-wave operation up to 100 °C and a threshold current density of 227 A/cm2 at room temperature are observed. Efficient coupling to a passive silicon waveguide is demonstrated. These devices are a key component in next generation supercomputers.
Two competing queues with linear costs and geometric service requirements: the μc-rule is often optimal (1985)

A discrete-time model is presented for a system of two queues competing for the service attention of a single server with infinite buffer capacity. The service requirements are geometrically distributed and independent from customer to customer as well as from the arrivals. The allocation of service attention is governed by feedback policies which are based on past decisions and buffer content histories. The cost of operation per unit time is a linear function of the queue sizes. Under the model assumptions, a fixed prioritization scheme, known as the μc -rule, is shown to be optimal for the expected long-run average criterion and for the expected discounted criterion, over both finite and infinite horizons. Two different approaches are proposed for solving these problems. One is based on the dynamic programming methodology for Markov decision processes, and assumes the arrivals to be i.i.d. The other is valid under no additional assumption on the arrival stream and uses direct comparison arguments. In both cases, the sample path properties of the adopted state-space model are exploited.
A method to deliver patterned electrical impulses to Schwann cells cultured on an artificial axon (2019)

Information from the brain travels back and forth along peripheral nerves in the form of electrical impulses generated by neurons and these impulses have repetitive patterns. Schwann cells in peripheral nerves receive molecular signals from axons to coordinate the process of myelination. There is evidence, however, that non-molecular signals play an important role in myelination in the form of patterned electrical impulses generated by neuronal activity. The role of patterned electrical impulses has been investigated in the literature using co-cultures of neurons and myelinating cells. The co-culturing method, however, prevents the uncoupling of the direct effect of patterned electrical impulses on myelinating cells from the indirect effect mediated by neurons. To uncouple these effects and focus on the direct response of Schwann cells, we developed an in vitro model where an electroconductive carbon fiber acts as an artificial axon. The fiber provides only the biophysical characteristics of an axon but does not contribute any molecular signaling. In our "suspended wire model", the carbon fiber is suspended in a liquid media supported by a 3D printed scaffold. Patterned electrical impulses are generated by an Arduino 101 microcontroller. In this study, we describe the technology needed to set-up and eventually replicate this model. We also report on our initial in vitro tests where we were able to document the adherence and ensheath of human Schwann cells to the carbon fiber in the presence of patterned electrical impulses (hSCs were purchased from ScienCell Research Laboratories, Carlsbad, CA, USA; ScienCell fulfills the ethic requirements, including donor's consent). This technology will likely make feasible to investigate the response of Schwann cells to patterned electrical impulses in the future.
NOTES perforated viscus repair is feasible and requires lower peritoneal pressures than laparoscopy in a porcine model (2009)

Moran, Erica A. MD; Gostout, Christopher J. MD; Bingener, Juliane MD Author Information
Flexible Quasi‐2D Perovskite/IGZO Phototransistors for Ultrasensitive and Broadband Photodetection (2019)

Organic-inorganic hybrid perovskites (PVKs) have recently emerged as attractive materials for photodetectors. However, the poor stability and low electrical conductivity still restrict their practical utilization. Owing to the quantum-well feature of two-dimensional (2D) Ruddlesden-Popper PVKs (2D PVKs), a promising quasi-2D PVK/indium gallium zinc oxide (IGZO) heterostructure phototransistor can be designed. By using a simple ligand-exchange spin-coating method, quasi-2D PVK fabricated on flexible substrates exhibits a desirable type-II energy band alignment, which facilitates effective spatial separation of photoexcited carriers. The device exhibits excellent photoresponsivity values of >10<sup>5</sup> A W<sup>-1</sup> at 457 nm, and broadband photoresponse (457-1064 nm). By operating the device in the depletion regime, the specific detectivity is found to be 5.1 × 10<sup>16</sup> Jones, which is the record high value among all PVK-based photodetectors reported to date. Due to the resistive hopping barrier in the quasi-2D PVK, the device can also work as an optoelectronic memory for near-infrared information storage. More importantly, the easy manufacturing process is highly beneficial, enabling large-scale and uniform quasi-2D PVK/IGZO hybrid films for detector arrays with outstanding ambient and operation stabilities. All these findings demonstrate the device architecture here provides a rational avenue to the design of next-generation flexible photodetectors with unprecedented sensitivity.
Effects of a 10 T External Magnetic Field on the Thermal Decomposition of Fe, Ni, and Co Acetyl Acetonates (2008)

The current investigation is centered on the thermal decomposition (700 degrees C) of acetyl acetonates of Ni, Co, and Fe in a closed reactor that was conducted by employing an external magnetic field (MF) of 10T. Interestingly, reactions of Co and Ni acetyl acetonates under a 10T MF produce Co and Ni nanoparticles (NPs) coated with carbon, while Fe acetyl acetonate produces Fe3O4 uncoated with carbon. Additionally, it is observed that all the as-formed magnetic particles tend to align in one dimension along applied MF; thus, this process can be used to fabricate large arrays of magnetic nanoparticles. The effect of an applied MF to synthesize morphologically and compositionally different products from corresponding precursors with their mesoscopic organization is the key theme of the present paper, explained with a plausible mechanism.
A 2 ns access, 500 MHz 288 Kb SRAM macro (2002)

High speed level-1 cache applications demand fast single cycle access times and short cycles. Novel circuits that deliver fast access times and self-resetting CMOS (SRCMOS) techniques that deliver fast cycle times are described. Two key elements for fast access times are: fast signal conversion from static CMOS to SRCMOS and fast signal conversion from SRCMOS to static CMOS. These conversions are performed by the input receiver and output driver circuits. A two-stage address decode scheme to minimize gate complexity and a high performance "late select 4-to-1" mux in front of the output drivers are also key elements. A "Sense and Hold Amplifier" (SHA) is used to perform pulse alignment with the asynchronous "late select" signal. The critical redundancy compare path is designed to be as fast as the primary word line decode path in order to minimize any impact on performance. SRCMOS circuitry allows for fast cycle operation without the use of a centrally controlled clocking scheme. Only the receivers are clocked and all subsequent circuits are triggered by pulses generated from preceding stages. Extensive sharing of reset circuitry is employed to minimize the overhead of SRCMOS. The SRAM includes a programmable "Array-Built-In-Self-Test" (ABIST) sub-macro which allows extensive test pattern coverage and access time evaluation at cycle speed.
ChemInform Abstract: Enzymatic Formation of Dicarbonyl Sugars: C‐2 Oxidation of 1→6 Disaccharides Gentiobiose, Isomaltose and Melibiose by Pyranose 2‐Oxidase from Trametes multicolor. (2000)

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.
The state of melanoma: challenges and opportunities (2016)

The Melanoma Research Foundation (MRF) has charted a comprehensive assessment of the current state of melanoma research and care. Intensive discussions among members of the MRF Scientific Advisory Council and Breakthrough Consortium, a group that included clinicians and scientists, focused on four thematic areas - diagnosis/early detection, prevention, tumor cell dormancy (including metastasis), and therapy (response and resistance). These discussions extended over the course of 2015 and culminated at the Society of Melanoma Research 2015 International Congress in November. Each of the four groups has outlined their thoughts as per the current status, challenges, and opportunities in the four respective areas. The current state and immediate and long-term needs of the melanoma field, from basic research to clinical management, are presented in the following report.
Burrowing is a sensitive behavioural assay for monitoring general wellbeing during dextran sulfate sodium colitis in laboratory mice (2013)

An impaired intestinal epithelial barrier is thought to be a major factor in the pathogenesis of human inflammatory bowel disease (IBD). IBD is frequently investigated by inducing a damaged barrier in murine models of colitis. This can be done by feeding mice with dextran sulfate sodium (DSS) polymers in their drinking water. Refinement measures should focus on alleviating unnecessary suffering during this probably painful condition. Appropriate parameters are needed to decide when to terminate the experiments. Our aim was to investigate whether a change in burrowing behaviour is a sensitive measure of animal welfare in murine models of colitis. Acute colitis was induced in C57BL/6 mice with 2.0% DSS over nine days. The burrowing test is based on the species-typical behaviour of mice to spontaneously displace items from tubes within their home cage. As a burrowing apparatus, a water bottle (250 mL, 150 mm length, 55 mm diameter) filled with 138-142 g of pellets of the animal's diet was used. The presence of intestinal inflammation as a result of acute DSS-induced colitis was confirmed by a decrease in body weight, colon length and an increase of murine endoscopic index of colitis severity, histological score and spleen weight in the group receiving DSS as compared with the control group. An onset of intestinal inflammation correlated with a significant decrease in burrowing behaviour (P < 0.05). Altered adrenal gland histology indicated stress as a result of acute colitis. Our findings provide evidence that changes of spontaneous burrowing behaviour correlate with the onset of inflammation in acute DSS-induced colitis.
Inhibition of Enzymatic Browning in Fresh Fruit and Vegetable Juices by Soluble and Insoluble Forms of β-Cyclodextrin Alone or in Combination with Phosphates (1996)

Soluble and insoluble forms of β-cyclodextrin (β-CD) can be used to inhibit enzymatic browning of fresh raw apple, pear, white grape, and celery juice. The anti-browning effects of soluble CDs were concentration-dependent. Concentrations (1−1.5% w/v) of soluble (un-derivatized, hydroxyethyl, or maltosyl) β-CD substantially inhibited browning of Granny Smith apple juice held at room temperature for several hours while untreated juice browned in minutes. Higher concentrations (4−10%) of soluble β-CD derivatives completely inhibited the browning of apple juice held for 1 day under these conditions. The effectiveness of β-CD was greatly enhanced by the presence of phosphate-containing compounds. Hence, only 1% levels of soluble β-CD (in the presence of 0.25−0.5% phosphate compound) completely inhibited browning in apple juice held for 1 day at room temperature or for up to 2−3 weeks at 4 °C. Treatment of apple, pear, white grape, and celery juice with an insoluble form of β-CD, either in a batchwise or flow-through process, resulted in juices free of CDs that resisted browning indefinitely. Keywords: Enzymatic browning; inhibition; cyclodextrins; vegetable and fruit juice; phosphates; phytic acid
LET Dependence of Single Event Transient Pulse-Widths in SOI Logic Cell (2009)

Single event transient (SET) pulse-widths were measured as a function of linear energy transfer (LET) by using pulse capture circuits and simulated with mixed-mode 3-D device simulations. We found that the carrier recombination process dominates the LET dependence of the pulse-widths.
1376-P: Comparison of a-Cell Response to Intravenous or Oral Glucose in Nondiabetic Humans (2022)

Type 2 Diabetes (T2DM) and prediabetes are characterized by β-cell and α-cell dysfunction which can occur independently. Defects in α-cell response to rising glucose can be evaluated with an oral or intravenous challenge: the former reflects normal physiology, the latter is unaffected by incretins or gut motility. We compared Glucagon Secretion Rate (GSR) in response to rising glucose during a Graded Glucose Infusion (GGI) and an Oral Glucose Tolerance Test (OGTT) . We studied 39 non-diabetic, weight-stable subjects (53 ± 2 yrs, 29 ± 1 Kg/M2) , with different fasting and glucose tolerance status. All subjects underwent a 75g OGTT and a GGI, with glucose infusion doubling every hour for 4 hours. GSR was calculated by deconvolution from plasma concentrations of glucagon on both study days (GSRGGI and GSROGTT) . The suppression of GSRGGI could be described with a single-exponential relationship between GSR and glucose concentrations. The slope of the log-transformed secretion line allows estimation of the change in glucose necessary to suppress GSR by 50% (G50) . This index of suppressibility is elevated in people with impaired fasting glucose compared to normal fasting glucose (2.7 ± 0.2 vs. 3.8 ± 0.4 mmol/L, p=0.01) . Intriguingly, GSROGTT, exhibited a delayed response to rising glucose (compared to GSRGGI) , during the early part of the OGTT. However, the relationship of GSROGTT to glucose did not differ from that of GSRGGI during the fasting state and at the time of peak postprandial suppression. This allowed the calculation of G50 during the OGTT, which was similar to that observed during the GGI (R2=0.66) and correlated with weight, age and fasting glucose (R2=0.49) . These data demonstrate the ability of a novel index (G50) , to reproducibly quantify α-cell suppression by oral or intravenous glucose in non-diabetic subjects. Future studies will be necessary to determine if this relationship also applies to T2DM and how gastrointestinal and other factors alter the rate of GSR suppression during an OGTT. Disclosure M.C.Laurenti: None. A.Manduca: None. C.Cobelli: None. C.Dalla man: Research Support; Becton, Dickinson and Company, Sanofi-Aventis Deutschland GmbH. A.Vella: Advisory Panel; Crinetics Pharmaceuticals, Inc., Rezolute, Inc., vTv Therapeutics, Zealand Pharma A/S, Other Relationship; Novo Nordisk. Funding National Institutes of Health (DK078646, DK116231)
Phase-oriented control of a modular 3-Phase 3-level 4-leg inverter AC power source supplying floating or grounded loads (2013)

A control scheme for a high-performance three-phase AC power source is presented. The four-leg inverter output stage uses three bridge legs to generate the phase output voltages with reference to the neutral point potential, which is defined by the fourth bridge leg. The inverter is controlled using a phase-oriented control in order to achieve precise control of each output phase with unbalanced voltages and any kind of load. The neutral potential is controlled for maximum modulation range in case of floating load and controlled to zero for grounded load. The control scheme for the input PWM rectifier stage considers the control of the zero sequence voltage in order to prevent the appearance of circulating currents through the ground loop when the load star point is connected to ground. The control of the circulating currents also allows the safe parallel connection of two or more AC sources. Simulation results under balanced and unbalanced conditions demonstrate the performance of the AC source in terms of output voltage control and prevention of circulating ground currents.
Self-Consistent Amplitude Calibration of Miras-SMOS (2018)

Using land-sea transitions as two-level targets, the gain parameter of the three Noise Injection Radiometers (NIR) installed in instrument MIRAS onboard ESA's SMOS satellite are independently estimated. The reference data for this calibration is the average antenna temperature measured simultaneously by the other MIRAS receivers operating as total power radiometers. Individually, the retrieved parameters show similar values to the nominal sky-calibrated ones, but long-term series of data reveal different seasonal behavior, suggesting that external maneuvers may have a non-negligible impact on the NIR front-end stability.