gebhart/patrepeval huggingface dataset:
Identification of new gonadotrophin-releasing hormone partial agonists (2006)

GnRH agonists or antagonists are currently utilized as therapeutic agents in a number of diseases. A side-effect of prolonged treatment with GnRH analogues is hypoestrogenism. In this study, we tested the in vitro potency of different GnRH analogues originally found to be partial agonists (i.e. analogues with decreased efficacy for activating or stimulating their cognate receptor) as well as novel analogues, to identify compounds that might potentially be useful for partial blockade of gonadotrophin release. Cultured COS-7 cells transiently expressing the rat or human GnRH receptor (GnRHR) were exposed to increasing concentrations (10(-8) to 10(-5) M) of GnRH analogues (c(4-10)[Asp4,DNal6,Dpr10]-GnRH; c(4-10) [Dpr4,DNal6,Asp10]-GnRH; c(4-10)[Cys(4,10),DNal6]-GnRH; c[Eaca1,DNal6]-GnRH; c[Gly1,DNal6]-GnRH; c[betaAla1,DTrp6]-GnRH; c[Dava1,DNal6]-GnRH; c[Gaba1, DNal6]-GnRH), and the ability of these analogues to provoke or antagonize GnRH-stimulated inositol phosphate production was assessed. With both human and rat GnRHRs, c[Eaca1,DNal6]-GnRH, c[Gly1,DNal6]-GnRH, c[betaAla1,DTrp6]-GnRH and c[Dava1,DNal6]-GnRH exhibited partial agonist activity (35-87% of the maximal efficacy shown by 10(-6) M GnRH), whereas c[Gaba1,DNal6]-GnRH behaved as a partial agonist with the human GnRHR and as full agonist with the rat GnRHR. c(4-10)[Asp4, DNal6,Dpr10]-GnRH and c(4-10)[Dpr4,DNal6,Asp10]-GnRH exhibited full antagonist activity with both GnRHRs, and c(4-10) [Cys(4,10),DNal6]-GnRH was a weak, partial agonist with the human GnRHR and a full antagonist with the rat GnRHR. With the exception of c[Gaba1,DNal6]-GnRH stimulation of the human GnRHR, and c[Dava1,DNal6]-GnRH and c[Gaba1, DNal6]-GnRH stimulation of the rat GnRHR, all partial agonists also exhibited antagonist activity in the presence of the exogenous full agonist. The results demonstrate that structurally similar analogues display variable potencies and efficacies in vitro for a specific GnRHR as well as for the human versus the rat GnRHR. Their ultimate in vivo usefulness to treat clinical conditions in which complete suppression of gonadotroph activity is not required remains to be investigated.
Current Management of Urolithiasis: Progress or Regress? (2002)

We believe this trend toward ureteroscopy is attributable to several factors: improved, smaller rigid and flexible ureteroscopes; the availability of more effective intracorporeal lithotripters (e.g., pneumatic and holmium laser), and the lack of development of lower cost, more effective SWL. This is an unfortunate trend, as we are moving away from the noninvasive treatment that was the hallmark of urolithiasis therapy at the beginning of the last decade toward more invasive endoscopic therapy. Increased research efforts in SWL technology are sorely needed.
Loss measurement of plasmonic modes in planar metal–insulator–metal waveguides by an attenuated total reflection method (2010)

We report experimental excitation and characterization of surface plasmon modes in planar metal-insulator-metal (MIM) waveguides. Our approach is based on determining the width of the reflection angular spectrum in the attenuated total reflection (ATR) configuration. Owing to its transverse character, the ATR configuration provides a more straightforward and simpler way to determine the loss of plasmonic modes in MIM structures, compared to using tapered end couplers with multiple waveguide samples or scanning near-field optical microscopy. In this Letter, two waveguide structures with Au claddings and 50/200 nm SiO(2) cores are investigated. The propagation lengths measured at λ = 1.55 μm are 5.7 and 18 μm, respectively, in agreement with the theoretical predictions.
Exploiting patterns of data magnitude for efficient image coding (2008)

In order to increase the computational efficiency of compression methods we have to consider that new hardware architectures increasingly rely more on wider data paths and parallel processing (e.g., SIMD and multi-core), than on faster clocks. Higher data throughputs are achieved with entropy coding methods that process larger amounts of information each time, and use context dependencies that are less complicated and that can be quickly updated. We propose a coding method with properties more suited to the new processors, that achieves better compression by exploiting patterns of data magnitude. We present experimental results on image coding implementations that take advantage of the fast decay of transform coefficient variance with frequency.
Process for the preparation of heterocyclyl chalcogenones via reaction of elemental sulfur, selenium, or tellurium with heterocyclic cationic species. (2010)

Heterocyclic chalcogenones were prepd. by reaction of S, Se, or Te with ionic liqs. or salts [I; Ra = (substituted) alkyl, cycloalkyl, aryl, aralkyl, alkylaryl; Q = (unsatd.) (substituted) linker to form a ring of 5-10 members; X- = anion selected from conjugate bases of HX having a pKa value of &gt;2.5]. Thus, 1-butyl-3-methylimidazolium acetate was heated with stoichiometric S at 75° for 48 h to give 1-butyl-3-methylimidazole-2-thione. [on SciFinder(R)]
Unsupervised prominence prediction for speech synthesis (2013)

We propose an unsupervised prominence prediction method for expressive speech synthesis. Prominence patterns are learned by statistical analysis of prosodic features extracted from speech data. The advantages of our unsupervised datadriven prominence prediction include: easy adaptation to new speakers, speech styles, and even languages without requiring expert knowledge or complicated linguistic rules. In this approach, first, prominence predictive prosodic features are extracted at the foot level. Next, the extracted prosodic features are clustered, each cluster representing a prominence level. Based on just-noticeable-differences of prosodic features, the optimal number of perceptually distinct prominence levels is determined. Finally, the proposed prominence prediction is applied to prosody prediction for unit selection speech synthesis. Perceptual evaluation results show a preference for a 4-level unsupervised prominence prediction over a rule-based baseline in terms of naturalness and expressiveness of synthesized speech.
Traffic Incident Detection Based on Extreme Machine Learning (2017)

ABSTRACT

Traffic incident detection is an essentialpart of the intelligenttransportation systemand attracts lots of attention from researchers in different areas. To reduce the computation and to avoid overfitting of the traditional feed-forward neural network, an extreme machine learning is implemented to detect traffic incidents. Using the real-world data, the proposed model is compared with feed-forward neural network and other two commonly used models by several evaluation criteria. The results indicate the proposed model has the highest accuracy, detection rate and lowest false alarm rate. Moreover, it consumes less time. In conclusion, the performance of the proposed model is better than other benchmark models and suit to detect traffic incidents.
Enhanced Complexity and Catalytic Efficiency in the Hydrolysis of Phosphate Diesters by Rationally Designed Helix‐Loop‐Helix Motifs (2008)

HJ1, a 42-residue peptide that folds into a helix-loop-helix motif and dimerizes to form a four-helix bundle, successfully catalyzes the cleavage of "early stage" DNA model substrates in an aqueous solution at pH 7.0, with a rate enhancement in the hydrolysis of heptyl 4-nitrophenyl phosphate of over three orders of magnitude over that of the imidazole-catalyzed reaction, k(2)(HJ1)/k(2)(Im) = 3135. The second-order rate constant, k(2)(HJ1) was determined to be 1.58x10(-4) M(-1) s(-1). The catalyst successfully assembles residues that in a single elementary reaction step are capable of general-acid and general-base catalysis as well as transition state stabilization and proximity effects. The reactivity achieved with the HJ1 polypeptide, rationally designed to catalyze the hydrolysis of phosphodiesters, is based on two histidine residues flanked by four arginines and two adjacent tyrosine residues, all located on the surface of a helix-loop-helix motif. The introduction of Tyr residues close to the catalytic site improves efficiency, in the cleavage of activated aryl alkyl phosphates as well as less activated dialkyl phosphates. HJ1 is also effective in the cleavage of an RNA-mimic substrate, uridine-3'-2,2,2-trichloroethyl phosphate (leaving group pK(a) = 12.3) with a second-order rate constant of 8.23x10(-4) M(-1) s(-1) in aqueous solution at pH 7.0, some 500 times faster than the reaction catalyzed by imidazole, k(2)(HJ1)/k(2)(Im) = 496.
Lateral Interbody Fusion for Treatment of Discogenic Low Back Pain: Minimally Invasive Surgical Techniques (2012)

Low back pain is one of the most common ailments in the general population, which tends to increase in severity along with aging. While few patients have severe enough symptoms or underlying pathology to warrant surgical intervention, in those select cases treatment choices remain controversial and reimbursement is a substancial barrier to surgery. The object of this study was to examine outcomes of discogenic back pain without radiculopathy following minimally-invasive lateral interbody fusion. Twenty-two patients were treated at either one or two levels (28 total) between L2 and 5. Discectomy and interbody fusion were performed using a minimallyinvasive retroperitoneal lateral transpsoas approach. Clinical and radiographic parameters were analyzed at standard pre- and postoperative intervals up to 24 months. Mean surgical duration was 72.1 minutes. Three patients underwent supplemental percutaneous pedicle screw instrumentation. Four (14.3%) stand-alone levels experienced cage subsidence. Pain (VAS) and disability (ODI) improved markedly postoperatively and were maintained through 24 months. Segmental lordosis increased significantly and fusion was achieved in 93% of levels. In this series, isolated axial low back pain arising from degenerative disc disease was treated with minimally-invasive lateral interbody fusion in significant radiographic and clinical improvements, which were maintained through 24 months.
Determining the Mechanical Properties of Rat Skin with Digital Image Speckle Correlation (2004)

&lt;i&gt;Background:&lt;/i&gt; Accurate measurement of the mechanical properties of skin has numerous implications in surgical repair, dermal disorders and the diagnosis and treatment of trauma to the skin. Investigation of facial wrinkle formation, as well as research in the areas of skin aging and cosmetic product assessment can also benefit from alternative methodologies for the measurement of mechanical properties. &lt;i&gt;Objective:&lt;/i&gt; A noncontact, noninvasive technique, digital image speckle correlation (DISC), has been successfully introduced to measure the deformation field of a skin sample loaded by a material test machine. With the force information obtained from the loading device, the mechanical properties of the skin, such as Young’s modulus, linear limitation and material strength, can be calculated using elastic or viscoelastic theory. &lt;i&gt;Methods:&lt;/i&gt; The DISC method was used to measure the deformation of neonatal rat skin, with and without a glycerin-fruit-oil-based cream under uniaxial tension. &lt;i&gt;Results:&lt;/i&gt; Deformation to failure procedure of newborn rat skin was recorded and analyzed. Single skin layer failures were observed and located by finding the strain concentration. Young’s moduli of freshly excised rat skin, cream-processed rat skin and unprocessed rat skin, 24 h after excision, were found with tensile tests to be 1.6, 1.4 and 0.7 MPa, respectively. &lt;i&gt;Conclusion:&lt;/i&gt; Our results have shown that DISC provides a novel technique for numerous applications in dermatology and reconstructive surgeries.
Intumescent Reaction Mechanisms (1985)

An extensive experimental program has been conducted on intumescent systems where the components have been varied systematically. Small plates were coated with the various formulations, exposed to a heat source typical of aviation fuel fires, and the temperature-time history of the substrate recorded. Concurrently, a simplified mathematical model was developed for an intumes cing system which has given insight to the fundamental mechanisms of in tumescence. The model and the results of the experimental program demonstrate certain desirable features of intumescent systems.
High speed packet forwarding compiled from protocol independent data plane specifications (2016)

P4 is a high level language for programming network switches that allows for great flexibility in the description of packet structure and processing, independent of the specifics of the underlying hardware. In this demo, we present our prototype P4 compiler in which the hardware independent and hardware specific functionalities are separated. We have identified the requisites of the latter, which form the interface of our target specific Hardware Abstraction Library (HAL); the compiler turns P4 code into a target independent core program that is linked to this library and invokes its operations. The two stage separation improves portability: to support a new architecture, only the hardware dependent library has to be implemented. In the demo, we demonstrate the flexibility of our compiler with a HAL for Intel DPDK, and show the packet processing and forwarding performance of compiled switches in different scenarios.
PROTEINASES AS PROBABLY FACTORS OF REGULATION OF COMPETITIVE RELATIONS AMONG MICROORGANISMS (2018)

ПРОТЕАЗЫ КАК ВЕРОЯТНЫЕ ФАКТОРЫ РЕГУЛЯЦИИ КОНКУРЕНТНЫХ ОТНОШЕНИЙ СРЕДИ МИКРООРГАНИЗМОВ
Efficiency Improvement for Path Detection and Tracking Algorithm in a Time-Varying Channel (2015)

This paper revisits estimation and tracking of channel parameters of multiple-input multiple-output (MIMO) systems. Since initialization of channel parameters has always been regarded as a computationally complex problem, we develop a new parameter initialization method that exploits the nature of the data structure of channel measurements. For medium or large problems it leads to a more than 500 times runtime acceleration for parameter initialization. We show that the runtime of the new initialization method increases much more slowly compared with that of the traditional initialization method when the dimensions of measurement data or search grids grow.
IPv6 over BLUETOOTH(R) Low Energy (2015)

Bluetooth Smart is the brand name for the Bluetooth low energy feature in the Bluetooth specification defined by the Bluetooth Special Interest Group. The standard Bluetooth radio has been widely implemented and available in mobile phones, notebook computers, audio headsets, and many other devices. The low-power version of Bluetooth is a specification that enables the use of this air interface with devices such as sensors, smart meters, appliances, etc. The lowpower variant of Bluetooth has been standardized since revision 4.0 of the Bluetooth specifications, although version 4.1 or newer is required for IPv6. This document describes how IPv6 is transported over Bluetooth low energy using IPv6 over Low-power Wireless Personal Area Network (6LoWPAN) techniques.
Limbic progesterone receptor activity enhances neuronal excitability and seizures (2021)

Activation of PRs expressed in the EC and hippocampus increased neuronal excitability and worsened seizures. These receptors may play a role in catamenial epilepsy.
Ultrasound stiffness and perfusion markers correlate with tumor volume responses to immunotherapy (2023)

Immunotherapy has revolutionized the treatment of dozens of cancers and became a standard of care for some tumor types. However, the majority of patients do not benefit from current immunotherapeutics and many develop severe toxicities. Therefore, the identification of biomarkers to classify patients as likely responders or non-responders to immunotherapy is a timely task. Here, we test ultrasound imaging markers of tumor stiffness and perfusion. Ultrasound imaging is non-invasive and clinically available and can be used both for stiffness and perfusion evaluation. In this study, we employed syngeneic orthotopic models of two breast cancers, a fibrosarcoma and a melanoma, to demonstrate that ultrasound-derived measures of tumor stiffness and perfusion (i.e., blood volume) correlate with the efficacy of immune checkpoint inhibition (ICI) in terms of changes in primary tumor volume. To modulate tumor stiffness and perfusion and thus, get a range of therapeutic outcomes, we employed the mechanotherapeutic tranilast. Mechanotherapeutics combined with ICI are advancing through clinical trials, but biomarkers of response have not been tested until now. We found the existence of linear correlations between tumor stiffness and perfusion imaging biomarkers as well as strong linear correlations between the stiffness and perfusion markers with ICI efficacy on primary tumor growth rates. Our findings set the basis for ultrasound biomarkers predictive of ICI therapy in combination with mechanotherapeutics. STATEMENT OF SIGNIFICANCE: Hypothesis: Monitoring Tumor Microenvironment (TME) mechanical abnormalities can predict the efficacy of immune checkpoint inhibition and provide biomarkers predictive of response. Tumor stiffening and solid stress elevation are hallmarks of tumor patho-physiology in desmoplastic tumors. They induce hypo-perfusion and hypoxia by compressing tumor vessels, posing major barriers to immunotherapy. Mechanotherapeutics is a new class of drugs that target the TME to reduce stiffness and improve perfusion and oxygenation. In this study, we show that measures of stiffness and perfusion derived from ultrasound shear wave elastography and contrast enhanced ultrasound can provide biomarkers of tumor response.
Measurement of In‐Grain Orientation Gradients by EBSD and Comparison with Finite Element Results (2003)

EBSD orientation mapping over large sample areas (see Figure for a close‐up of three grains extracted from an orientation map) gives the basis data for a statistical evaluation on orientation gradients developed within grains of a cold‐rolled aluminum plate. This data set serves as a counterpart for finite‐element simulations for checking whether the orientation gradients observed can be attributed to the interaction of adjacent grains. Although the tendency of the simulations fits the experiment, the amplitude of the orientation spread is always underestimated, whatever the initial orientation of grains.
Chelation-Tamoxifen Conjugates for Imaging of Estrogen Receptors (2021)

<b><i>Background:</i></b> The differential diagnosis of estrogen receptor-positive (ER+) pathway-activated systems by using a labeled antiestrogen helps to select the patients for optimal response to endocrine therapy and to discontinue the treatment when resistance occurs. The authors' purpose was to synthesize chelator-tamoxifen conjugates for imaging ER (+) diseases. <b><i>Materials and Methods:</i></b> A hydroxypropyl linker was incorporated between either cyclam or cyclam diacetic acid and tamoxifen analog to produce SC-05-L-1 (Z-1-(1,4,8,11-tetraazacyclotetradecan-1-yl)-3-((5-(4-(2-(diethylamino)ethoxy)phenyl)-4,5-diphenylpent-4-en-1-yl)oxy)propan-2-ol) and SC-05-N-1 (Z-2,2'-(4-(3-((5-(4-(2-(diethylamino)ethoxy)phenyl)-4,5-diphenylpent-4-en-1-yl)oxy)-2-hydroxy-propyl)-1,4,8,11-tetraazacyclotetradecane-1,8-diyl)diacetic acid), respectively. <i>In vitro</i> cell uptake and cell/media ratios of <sup>99m</sup>Tc-SC-05-L-1 and <sup>99m</sup>Tc- SC-05-N-1 in ER (+) ovarian cancer cells (TOV-112D and OVCAR3) were performed. To ascertain the specificity of cell uptake, the cell uptake was blocked with estrone. <i>In vivo</i> <sup>99m</sup>Tc-SC-05-L-1 or <sup>99m</sup>Tc-SC-05-N-1 single-photon emission computed tomography/computed tomography was conducted in tumor-bearing rodents and compared to <sup>18</sup>F-fluoro-2-deoxy-d-glucose (<sup>18</sup>F-FDG) positron emission tomography/magnetic resonance imaging (a reference technology). <b><i>Results:</i></b> The radiochemical purities of <sup>99m</sup>Tc-SC-05-L-1 and <sup>99m</sup>Tc-SC-05-N-1 were greater than 99% (<i>n</i> = 10). <sup>99m</sup>Tc-SC-05-L-1 had higher cell/media ratios than <sup>99m</sup>Tc-SC-05-N-1 in OVCAR-3 ER (+) cells. The cell uptake of <sup>99m</sup>Tc-SC-05-L-1 was blocked 80% by estrone indicating an ER-mediated process occurred. <sup>99m</sup>Tc-SC-05-N-1 was further selected for <i>in vivo</i> imaging studies due to higher maximum tolerated dose and superior water solubility than <sup>99m</sup>Tc-SC-05-L-1. <sup>99m</sup>Tc-SC-05-N-1 showed higher tumor uptake and tumor/muscle count density ratios than <sup>18</sup>F-FDG in tumor-bearing rodents. <b><i>Conclusion:</i></b> <sup>99m</sup>Tc-SC-05-N-1 showed better differential diagnosis of ovarian tumors than <sup>18</sup>F-FDG, indicating great promising in chelator-tamoxifen conjugate for ER pathway-directed systems imaging.
Therapeutic Potential of Targeting Metabotropic Glutamate Receptors for Parkinson’s Disease (2012)

Parkinson's disease (PD) is a progressive neurological disorder predominantly characterized by motor symptoms including bradykinesia and resting tremor. The gold standard of treatment for PD remains dopamine replacement therapy, which eventually fails due to continued progression of the disease and the development of debilitating side effects. Recent breakthroughs are providing the first major advances in the development of fundamentally new pharmacological strategies for the treatment of PD that do not rely on dopamine replacement strategies, but rather aim to reduce the overactive indirect pathway within the basal ganglia. In this article, we will review the role of metabotropic glutamate receptors within the basal ganglia and discuss the potential for modulation of metabotropic glutamate receptors as a treatment for PD.
Autonomous Data Collection With Timed Communication Constraints for Unmanned Underwater Vehicles (2021)

This letter studies the problem of data collection where an autonomous underwater vehicle (AUV) is required to inspect several goals while staying within the communication range of an unmanned surface vehicle (USV) moving along a predefined path. A reward is associated with each inspected goal, and, so the overall objective is to increase the sum of the rewards. The proposed planner takes the AUV dynamics and the obstacles into account in order to generate collision-free and dynamically-feasible trajectories that enable the AUV to inspect multiple goals while maintaining communication with the USV. When not all the goals can be inspected, the planner generates trajectories that increase the sum of the rewards. The proposed planner constructs a roadmap equipped with time information in order to facilitate navigation and maintain communication in complex 3D environments. A crucial aspect is an effective coupling of discrete search with sampling-based motion planning. Specifically, a multi-goal discrete search is proposed to effectively compute roadmap paths that increase the sum of the rewards. These paths then guide the sampling-based expansion of a motion tree. Experiments using complex 3D environments and an AUV model defined by nonlinear second-order differential equations indicate the efficiency of the planner to inspect an increasing number of goals.