gebhart/patrepeval huggingface dataset:
Taccalonolides E and A: Plant-derived steroids with microtubule-stabilizing activity. (2003)

During the course of a mechanism-based screening program designed to identify new microtubule-disrupting agents from natural products, we identified a crude extract from Tacca chantrieri that initiated Taxol-like microtubule bundling. Bioassay-directed purification of the extract yielded the highly oxygenated steroids taccalonolides E and A. The taccalonolides caused an increased density of cellular microtubules in interphase cells and the formation of thick bundles of microtubules similar to the effects of Taxol. Mitotic cells exhibited abnormal mitotic spindles containing three or more spindle poles. The taccalonolides were evaluated for antiproliferative effects in drug-sensitive and multidrug-resistant cell lines. The data indicate that taccalonolide E is slightly more potent than taccalonolide A in drug-sensitive cell lines and that both taccalonolides are effective inhibitors of cell proliferation. Both taccalonolides are poorer substrates for transport by P-glycoprotein than Taxol. The ability of the taccalonolides to circumvent mutations in the Taxol-binding region of beta-tubulin was examined using the PTX 10, PTX 22, and 1A9/A8 cell lines. The data suggest little cross-resistance of taccalonolide A as compared with Taxol, however, the data from the PTX 22 cell line indicate a 12-fold resistance to taccalonolide E, suggesting a potential overlap of binding sites. Characteristic of agents that disrupt microtubules, the taccalonolides caused G(2)-M accumulation, Bcl-2 phosphorylation, and initiation of apoptosis. The taccalonolides represent a novel class of plant-derived microtubule-stabilizers that differ structurally and biologically from other classes of microtubule-stabilizers.
Biochemical Characterization of a Class of Inhibitors of the Human Mitotic Kinesin KSP with a Novel Mechanism of Action (2006)

The motor protein kinesin spindle protein (KSP, also known as Eg5) plays a critical role in the establishment of the mitotic spindle. KSP is essential for the proper separation of spindle poles during mitosis and inhibition results in mitotic arrest and the formation of characteristic monoaster spindles. Prolonged mitotic arrest leads to apoptosis in tumor cells and tumor growth inhibition in xenograft mouse tumor models. Kinesin inhibitors are expected to be general antiproliferative agents effective in most cancers currently treated with anti‐microtubule agents. Several distinct classes of KSP inhibitors have been described previously in the public and patent literature; those that have been characterized as to mechanism of inhibition share a common induced‐fit allosteric binding site. In a high‐throughput screen for inhibitors of KSP, a novel class of thiazole‐containing inhibitors was identified. Unlike the previously described allosteric KSP inhibitors, the thiazoles described here show ATP competitive kinetic behavior and are presumed to bind within the nucleotide binding pocket. Although they bind to a pocket that is highly conserved across kinesins, these molecules exhibit significant selectivity for KSP over other kinesins and other ATP utilizing enzymes. Several of these compounds are active in cells and produce a phenotype similar to that observed with previously published allosteric inhibitors of KSP.
Preclinical Comparative Study of <sup>68</sup>Ga-Labeled DOTA, NOTA, and HBED-CC Chelated Radiotracers for Targeting PSMA (2016)

(68)Ga-labeled, low-molecular-weight imaging agents that target the prostate-specific membrane antigen (PSMA) are increasingly used clinically to detect prostate and other cancers with positron emission tomography (PET). The goal of this study was to compare the pharmacokinetics of three PSMA-targeted radiotracers: (68)Ga-1, using DOTA-monoamide as the chelating agent; (68)Ga-2, containing the macrocyclic chelating agent p-SCN-Bn-NOTA; and (68)Ga-DKFZ-PSMA-11, currently in clinical trials, which uses the acyclic chelating agent, HBED-CC. The PSMA-targeting scaffold for all three agents utilized a similar Glu-urea-Lys-linker construct. Each radiotracer enabled visualization of PSMA+ PC3 PIP tumor, kidney, and urinary bladder as early as 15 min post-injection using small animal PET/computed tomography (PET/CT). (68)Ga-2 demonstrated the fastest rate of clearance from all tissues in this series and displayed higher uptake in PSMA+ PC3 PIP tumor compared to (68)Ga-1 at 1 h post-injection. There was no significant difference in PSMA+ PC3 PIP tumor uptake for the three agents at 2 and 3 h post-injection. (68)Ga-DKFZ-PSMA-11 demonstrated the highest uptake and retention in normal tissues, including kidney, blood, spleen, and salivary glands and PSMA-negative PC3 flu tumors up to 3 h post-injection. In this preclinical evaluation (68)Ga-2 had the most advantageous characteristics for PSMA-targeted PET imaging.
Multiple-Agent Air/Ground Autonomous Exploration Systems (2007)

Autonomous systems of multiple-agent air/ground robotic units for exploration of the surfaces of remote planets are undergoing development. Modified versions of these systems could be used on Earth to perform tasks in environments dangerous or inaccessible to humans: examples of tasks could include scientific exploration of remote regions of Antarctica, removal of land mines, cleanup of hazardous chemicals, and military reconnaissance. A basic system according to this concept (see figure) would include a unit, suspended by a balloon or a blimp, that would be in radio communication with multiple robotic ground vehicles (rovers) equipped with video cameras and possibly other sensors for scientific exploration. The airborne unit would be free-floating, controlled by thrusters, or tethered either to one of the rovers or to a stationary object in or on the ground. Each rover would contain a semi-autonomous control system for maneuvering and would function under the supervision of a control system in the airborne unit. The rover maneuvering control system would utilize imagery from the onboard camera to navigate around obstacles. Avoidance of obstacles would also be aided by readout from an onboard (e.g., ultrasonic) sensor. Together, the rover and airborne control systems would constitute an overarching closed-loop control system to coordinate scientific exploration by the rovers.
Unsupervised Approach for Autonomous Pavement-Defect Detection and Quantification Using an Inexpensive Depth Sensor (2012)

Current pavement condition–assessment procedures are extensively time consuming and laborious; in addition, these approaches pose safety threats to the personnel involved in the process. In this study, a RGB-D sensor is used to detect and quantify defects in pavements. This sensor system consists of a RGB color image, and an infrared projector and a camera that act as a depth sensor. An approach, which does not need any training, is proposed to interpret the data sensed by this inexpensive sensor. This system has the potential to be used for autonomous cost-effective assessment of road-surface conditions. Various road conditions including patching, cracks, and potholes are autonomously detected and, most importantly, quantified, using the proposed approach. Several field experiments have been carried out to evaluate the capabilities, as well as the limitations of the proposed system. The global positioning system information is incorporated with the proposed system to localize the detected defects. This approach has the potential to be deployed as a supplementary sensor system in pavement surface–assessment vehicles and reduce the operation cost.
3D laser optoacoustic ultrasonic imaging system for research in mice (LOUIS-3DM) (2014)

In this work we introduce an improved prototype of three-dimensional imaging system that combines optoacoustic tomography (OAT) and laser ultrasound tomography (LUT) to obtain coregistered maps of tissue optical absorption and speed of sound (SoS). The OAT scan is performed by a 360 degree rotation of a mouse with respect to an arc-shaped array of ultrasonic transducers. A Q-switched laser system is used to establish optoacoustic illumination pattern appropriate for deep tissue imaging with a tunable (730-840 nm) output wavelengths operated at 10 Hz pulse repetition rate. A 532 nm wavelength output, being mostly absorbed within a narrow superficial layer of skin, is used to outline the visualized biological object. Broadband laser ultrasound emitters are arranged in another arc pattern and are positioned opposite and orthogonal to the array of transducers. This imaging geometry allows reconstruction of volumes that depict SoS distributions from the measured time of flight data. The reconstructed LUT images can subsequently be employed by an optoacoustic reconstruction algorithm to compensate for acoustic wavefield aberration and thereby improve accuracy of the reconstructed images of the absorbed optical energy. The coregistered OAT-LUT imaging is validated in a phantom and live mouse using a single-slice system prototype.
Abstract 4842: Lysosomal-associated protein multispanning transmembrane 5 gene (LAPTM5) is associated with spontaneous regression of neuroblastomas (2010)

Abstract Background; Neuroblastoma (NB) is the most frequently occurring solid tumor in children, and shows heterogeneous clinical behavior. Favorable tumors, which are usually detected by mass screening based on increased levels of catecholamines in urine, regress spontaneously via programmed cell death (PCD) or mature through differentiation into benign ganglioneuroma (GN). In contrast, advanced-type NB tumors often grow aggressively, despite intensive chemotherapy. Understanding the molecular mechanisms of PCD during spontaneous regression in favorable NB tumors, as well as identifying genes with a pro-death role, is a matter of urgency for developing novel approaches to the treatment of advanced-type NB tumors. Key findings; We found that the expression of lysosomal associated protein multispanning transmembrane 5 (LAPTM5) was usually down-regulated due to DNA methylation in an NB cell-specific manner, but up-regulated in degenerating NB cells within locally regressing areas of favorable tumors detected by mass-screening. Experiments in vitro showed that not only a restoration of its expression but also the accumulation of LAPTM5 protein, was required to induce non-apoptotic cell death with autophagic vacuoles and lysosomal destabilization with lysosomal-membrane permeabilization (LMP) in a caspase-independent manner. While autophagy is a membrane-trafficking pathway to degrade the proteins in lysosomes, the LAPTM5-mediated lysosomal destabilization with LMP leads to an interruption of autophagic flux, resulting in the accumulation of immature autophagic vacuoles, p62/SQSTM1, and ubiqitinated proteins as substrates of autophagic degradation. In addition, ubiquitin-positive inclusion bodies appeared in degenerating NB cells. Conclusions; We propose a novel molecular mechanism for PCD with the accumulation of autophagic vacuoles due to LAPTM5-mediated lysosomal destabilization. LAPTM5-induced cell death is lysosomal cell death with impaired autophagy, not cell death by autophagy, so-called autophagic cell death. Thus LAPTM5-mediated PCD is closely associated with the spontaneous regression of NBs and opens new avenues for exploring innovative clinical interventions for this tumor. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 2010 Apr 17-21; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2010;70(8 Suppl):Abstract nr 4842.
Tolerogenic citrullinated peptide for arthritis (2015)

Disease-specific autoantibodies directed against post-translation citrullinated proteins/peptides (ACPAs) are specific serological markers for rheumatoid arthritis (RA) and have been accepted as one of the classification criteria for the disease. Beyond diagnosis these autoantibodies have also been shown also to predict disease severity. These autoantibodies can be detected several years prior to the clinical onset of RA, with increasing titers overtime, as disease onset is established.
Soluble epoxide hydrolase and epoxyeicosatrienoic acids modulate two distinct analgesic pathways (2008)

During inflammation, a large amount of arachidonic acid (AA) is released into the cellular milieu and cyclooxygenase enzymes convert this AA to prostaglandins that in turn sensitize pain pathways. However, AA is also converted to natural epoxyeicosatrienoic acids (EETs) by cytochrome P450 enzymes. EET levels are typically regulated by soluble epoxide hydrolase (sEH), the major enzyme degrading EETs. Here we demonstrate that EETs or inhibition of sEH lead to antihyperalgesia by at least 2 spinal mechanisms, first by repressing the induction of the COX2 gene and second by rapidly up-regulating an acute neurosteroid-producing gene, StARD1, which requires the synchronized presence of elevated cAMP and EET levels. The analgesic activities of neurosteroids are well known; however, here we describe a clear course toward augmenting the levels of these molecules. Redirecting the flow of pronociceptive intracellular cAMP toward up-regulation of StARD1 mRNA by concomitantly elevating EETs is a novel path to accomplish pain relief in both inflammatory and neuropathic pain states.
Bacteriocins reduce<i>Campylobacter jejuni</i>colonization while bacteria producing bacteriocins are ineffective (2008)

Broiler chickens are widely considered an important source of human exposure to Campylobacter jejuni because of the high numbers found colonizing the chicken gut and the consequent contamination of processed carcasses.We hoped to intervene in C. jejuni gut colonization by using a defined probiotic. Chicken intestinal contents were screened for diverse bacterial isolates that manifested C. jejuni inhibition. These antagonistic bacteria were fed directly to chickens before or after C. jejuni challenge. The prophylactic probiotic treatments were effective only when very low challenge levels of C. jejuni were used. Otherwise, probiotic treatments failed to reduce C. jejuni colonization. Regardless of treatment, as birds further aged C. jejuni numbers soon approached the levels observed in the control birds. We sought an alternative approach, as commercial broilers may be exposed to infectious levels of C. jejuni at any time during production. Two of our most promising antagonistic isolates, Lactobacillus salivarius NRRL B-30514 and Paenibacillus polymyxa NRRL B-30509, were further studied for effectiveness in reducing C. jejuni in chickens. When 250 mg of purified bacteriocins (produced by these organisms)/kg feed were fed therapeutically to chickens colonized with C. jejuni, colonization was reduced by at least one million-fold. Treatments with viable probiotic bacterial cultures were ineffective in reducing C. jejun i in chickens, while bacteriocin treatment from these corresponding bacteria substantially reduced C. jejuni colonization in the live birds. Key words: bacteriocin, Campylobacter jejuni, colonization, probiotic, broiler chicken, competitive exclusion, Lactobacillus salivarius, Paenibacillus polymyxa
Method for producing heat-resistant semi-inorganic compounds (1983)

The method for producing a heat resistant, semi-inorganic compound is discussed. Five examples in which various alcohols, phenols, and aromatic carbonic acids are used to test heat resistance and solubility are provided.
Electrical conductivity and permittivity maps of brain tissues derived from water content based on T<sub>1</sub>‐weighted acquisition (2016)

Human brain and phantom EP images suggest that water content is a dominating factor in determining the electrical properties of tissues. Despite possible literature inaccuracies, the proposed method offers EP maps that can provide complementary information to current approaches, to facilitate EPT scans in clinical applications. Magn Reson Med 77:1094-1103, 2017. © 2016 International Society for Magnetic Resonance in Medicine.
Evaluation of Pheromone Dispensers for Use in Gypsy Moth Detection (Lepidoptera: Lymantriidae)2 (1992)

Seven controlled-release dispenser formulations containing 500 μg of gypsy moth pheromone (+)-disparlure, were compared in laboratory and field tests. Pheromone release rates, residual pheromone contents, and male moth captures in traps baited with the dispensers were compared following pre-aging of the dispensers in a greenhouse at 35 °C for 0, 4, 12, and 16 wk. The laminate dispenser, now used in USDA detection traps, became less attractive over time as its pheromone release rate and content dropped below the threshold values previously reported as necessary for effective attraction. A polyvinyl chloride coated twine dispenser produced high male moth captures and gave release rates and residual contents above these thresholds (30 ng/h release rate and 100 μg content) at all aging periods. The tube-A dispenser was the most effective of the new commercially prepared formulations, followed by the membrane and tube-B whose male moth captures and release rates tended to increase with aging time. The capsule and film dispensers were the least effective of the formulations tested.
Active Specific Immunotherapy of Malignant Melanoma with Anti‐idiotypic Monoclonal Antibodies (1993)

In this study, we have utilized the human high molecular weight-melanoma associated antigen (HMW-MAA) as a target for active specific immunotherapy with mouse anti-idiotypic (anti-id) monoclonal antibodies (mAb) in patients with malignant melanoma. After having summarized the characteristics of HMW-MAA which account for its selection as a target for immunotherapy, we describe the development and characterization of mouse anti-id mAb MK2-23 which bears the internal image of HMW-MAA. Furthermore, we describe the results of the first clinical trial performed with mouse anti-id mAb MK2-23 in patients with malignant melanoma.
Quantitation of Soybean Allergens Using Tandem Mass Spectrometry (2010)

Soybean (Glycine max) seed contain some proteins that are allergenic to humans and animals. However, the concentration of these allergens and their expression variability among germplasms is presently unknown. To address this problem, 10 allergens were quantified from 20 nongenetically modified commercial soybean varieties using parallel, label-free mass spectrometry approaches. Relative quantitation was performed by spectral counting and absolute quantitation was performed using multiple reaction monitoring (MRM) with synthetic, isotope-labeled peptides as internal standards. During relative quantitation analysis, 10 target allergens were identified, and five of these allergens showed expression levels higher than technical variation observed for bovine serum albumin (BSA) internal standard (∼11%), suggesting expression differences among the varieties. To confirm this observation, absolute quantitation of these allergens from each variety was performed using MRM. Eight of the 10 allergens were quantified for their concentration in seed and ranged from approximately 0.5 to 5.7 μg/mg of soy protein. MRM analysis reduced technical variance of BSA internal standards to approximately 7%, and confirmed differential expression for four allergens across the 20 varieties. This is the first quantitative assessment of all major soybean allergens. The results show the total quantity of allergens measured among the 20 soy varieties was mostly similar.
All-optical associative memory with shift invariance and multiple-image recall (1987)

We present experimental results from an all-optical associative memory that combines holography and phase conjugation. The device has the capability to recall a complete image when merely a portion of the stored image is input to the system. Multiple superimposed two-dimensional images with gray scale can be stored and recalled. In addition, we have demonstrated the system's invariance to translation of the input images.
Distortion Analyzer-A New Tool for Assessing and Improving Electrodynamic Transducer (2000)

The dominant nonlinear distortions in loudspeakers, headphones and other actuators are predictable and are closely related with the general principle, particular design, materials and assembling techniques applied to the transducer. The Distortion Analyzer uses novel system identification techniques to measure the large signal parameters of the expanded loudspeaker model, the instantaneous state signals and the distortion components generated by each nonlinearity. This information is crucial for assessing the performance of transducer in the large signal domain as well as for finding the physical causes of the distortion to improve the transducer in respect with sound quality, weight, size and cost.
Multi-degree optical node for effective utilization of optical transponders in WDM mesh networks (2010)

Multi-degree optical node configuration is proposed to utilize optical transponders more effectively. Number of optical transponders per fiber link can be reduced to the half of the number of all the wavelength channels.
Silicon Heterojunction Solar Cells and p‐type Crystalline Silicon Wafers: A Historical Perspective (2022)

The first reports of both boron–oxygen (BO)‐related light‐induced degradation (BO‐LID) and amorphous/crystalline silicon heterojunction (SHJ) solar cell fabrication date back to the early 1970s. However, the complete development of the “modern” SHJ structure took place well before BO defect stabilization processes were developed. Due to the susceptibility of p‐type Czochralski (Cz)‐grown silicon to BO‐LID, such wafers were deemed unsuitable for SHJ solar cells. In addition to stability issues, lower charge carrier lifetimes due to contamination and challenges with surface passivation posed barriers to the adoption of p‐type wafers in SHJ applications. Herein, these three key challenges are discussed in detail. Kinetic modeling and experimental results reveal the severe impact of BO‐LID in p‐type SHJ solar cells and provide possible explanations as to why earlier attempts using p‐type wafers might have failed. The role of gettering and advanced hydrogenation in stabilizing BO defects in SHJ solar cells is demonstrated experimentally. Finally, a summary of the effective surface recombination velocities reported in the literature for hydrogenated intrinsic amorphous silicon passivation of p‐ and n‐type crystalline silicon wafers is presented. Based on these findings, the potential of p‐type wafers to enable a next‐generation of high‐efficiency solar cells featuring carrier‐selective contacts is discussed.
Multicolor holographic imaging with a white-light source (1977)

A simple technique is described by which holograms have been made that reconstruct bright, multicolor images of three-dimensional objects when illuminated with a white-light source. The only sacrifice involved is vertical parallax, which is relatively unimportant.
Incentive-based demand response approach for aggregated demand side participation (2016)

This paper proposes a novel incentive-based demand response (DR) program that can be utilized by a service provider (SP) to procure capacity resources from its subscribed customers in terms of a load reduction. By providing incentives in advance, the SP can induce customers to participate in the program and voluntarily determine the quantity of load reduction to be sold to the SP. Stackelberg game theory is adopted to capture the interactions between the SP and its customers. The optimal incentives were determined analytically, and each customer's optimal load reduction was also decided accordingly. Simulation results showed that the proposed incentive-based DR approach is effective in determining optimal incentives for an SP to procure the required capacity resources.