gebhart/patrepeval huggingface dataset:
synthesis and Structure-Activity Relationships of 2,3-Benzodiazepines as AMPA Receptor Antagonists (2001)

There is increasing evidence of the potential therapeutic utility of glutamate receptor antagonists in the treatment of several neurodegenerative disorders, including stroke and epilepsy. In the last few years noncompetitive AMPA receptor antagonists have received considerable attention due to their therapeutic potentiality. The discovery of GYKI 52466, the prototype of noncompetitive AMPA receptor antagonists endowed with anticonvulsant and neuroprotective properties, induced growing interest on 2,3-benzodiazepine derivatives. This review covers the chemistry and pharmacology of this important class of AMPA receptor antagonists.
Abstract 5417: The identification of BMS-595, an orally active imidazo[1,2-b]pyridazine CK2 inhibitor with in vivo anti-tumor activity (2015)

Abstract CK2 is a highly conserved, and constitutively active family of serine/threonine kinases abnormally elevated in a wide variety of cancers and linked to poor prognosis and disease progression. The enzymes form as hetero-tetrameric complexes comprised of two highly related catalytic subunits (α or α´) with two regulatory β subunits in various combinations and distributions, depending on cell type. While CK2 plays a role in normal growth and development, deregulation of the enzymes has been shown to promote and maintain a malignant phenotype through mechanisms in both the anti-apoptotic and the pro-proliferative signaling pathways. CK2 has been reported to modulate the activity of several oncogenic transcription factors including CREB, Myc, Jun and Fos. Studies with RNAi and small molecule compounds have demonstrated tumor cell dependence on CK2. We sought to identify potent CK2 inhibitors to probe the function of CK2 in cancer-linked pathways and for evaluation in CK2 dependent tumor xenograft models. Herein we report SAR studies in the imidazo[1,2-b]pyridazine chemotype leading to the discovery of BMS-595, a highly potent and selective ATP-competitive CK2 inhibitor with a commensurate level of cellular potency. BMS-595 demonstrates strong PK/PD correlations and robust, oral anti-tumor efficacy in CK2-driven xenograft models at tolerated doses. Citation Format: Christine M. Tarby, Liqi He, Brian E. Fink, Andrew Nation, Yufen Zhao, Soong-Hoon Kim, Libing Chen, John S. Tokarski, Chiang Yu, Jonathan G. Pabalan, Urvashi V. Roongta, Jonathan Lippy, Mary Obermeier, Paul A. Elzinga, Aberra Fura, Benjamin Henley, Joseph J. Fargnoli, William R. Foster, Ashvinikumar V. Gavai, Tai W. Wong, John T. Hunt, Gregory D. Vite, Ashok V. Purandare, Brent A. Rupnow. The identification of BMS-595, an orally active imidazo[1,2-b]pyridazine CK2 inhibitor with in vivo anti-tumor activity. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 5417. doi:10.1158/1538-7445.AM2015-5417
Achieving Efficient CO2 Electrochemical Reduction on Tunable In(OH)3-Coupled Cu2O-Derived Hybrid Catalysts (2019)

Tunable In(OH)<sub>3</sub>-coupled Cu<sub>2</sub>O-derived hybrid catalysts are facilely synthesized to boost the selectivity and efficiency of the electrochemical CO<sub>2</sub> reduction reaction (CO<sub>2</sub>RR). The maximum faradaic efficiency (FE) of 90.37% for CO production is achieved at -0.8 V versus reversible hydrogen electrode. The mechanistic discussion suggests that the composition-dependent synergistic effect results in the enhanced selectivity for CO on the hybrid catalyst. By increasing the concentration of the electrolyte, a dramatically enhanced current density of 40.17 mA cm<sup>-2</sup> was achieved at -1.0 V in 0.7 M KHCO<sub>3</sub>. Furthermore, a KHCO<sub>3</sub> electrolyte with high concentration promotes the selectivity of CO<sub>2</sub>RR over the low overpotential range. At a low overpotential of 290 mV, the increased FE for CO of 74.05% is obtained in 0.7 M KHCO<sub>3</sub> as compared to that of 57.04% in 0.1 M KHCO<sub>3</sub>. Combining with the synergistic effect of the catalyst and the concentration effect of the electrolyte, the hybrid catalyst achieves high efficiency, high selectivity, and high stability for CO<sub>2</sub>RR.
Supporting High Bandwidth Applications with 60GHz Outdoor Picocells (2012)

Industry research predicts that aggregate bandwidth requirements will increase by 1000-fold by 2020 [1]. This staggering growth is taxing mobile cellular networks past their limits and creating a capacity crisis [2]. Existing methods to increase capacity have
A Neural Network Based Approach for Inference and Verification of Transcriptional Regulatory Interactions (2006)

In this paper, we present a comprehensive neural network based modeling and validation framework for reverse engineering gene regulatory interactions. We employ two approaches, Gene Set Stochastic Sampling and Sensitivity Analysis, to infer these interactions. We first apply these methods to a simulated artificial dataset to ensure their correctness and accuracy. True biological interactions are then modeled by analyzing a rat hippocampus development dataset. Finally, we present a thorough computational methodology to test the validity and robustness of the inferred regulations through novel assemblies of relevant testing datasets.
Percutaneous Extra-Anatomic Nephrovesical Diversion: Preliminary Report* (1993)

We propose a new approach to total ureteric replacement based on the use of a new spiraled composite tube. This tube is inserted percutaneously into the renal pelvis, then tracked subcutaneously and introduced into the bladder via a short incision. The tube is maintained in place by anchoring its spirals along the subcutaneous tract, and only the two silicone extremities are in continuous contact with the urine. We have used this technique for total replacement of the ureter in one renal transplant patient with a follow-up of 8 months and no complication. A longer follow-up is obviously necessary, but this new, minimally invasive approach, using a newly designed tube, would appear to give a new lease of life to an old, abandoned principle.
Equipment for Harvesting, Transporting, Storing, and Feeding (1988)

Alfalfa and alfalfa-based forage account for almost 60% of the total tonnage of forages harvested in the USA. Area per farm, climatic conditions, type of terrain, and end use all have a direct effect on the type and size of equipment and on the harvest, storage, and feeding system used by farmers. The level of mechanization achieved in alfalfa harvesting, storage, and feeding depends on the type of harvest and storage system used and on the feeding needs of the producer. Large rectangular and large round balers and increased use of haylage have necessitated changes in methods for transporting alfalfa. Self-propelled models are used primarily by large dairy farmers, dehydrators, custom operators, and other operations where large quantities of alfalfa are harvested. Advances in computer capabilities have placed such systems analysis within reach of individual farmers and farm managers on home and office computers.
Combined MASS-DIMM instruments for atmospheric turbulence studies (2007)

Several site-testing programmes and observatories currently use combined Multi-Aperture Scintillation Sensor (MASS)-Differential Image Motion Monitor (DIMM) instruments for monitoring parameters of optical turbulence. The instrument is described here. After a short recall of the measured quantities and operational principles, the optics and electronics of MASS-DIMM, interfacing to telescopes and detectors, and operation are covered in some detail. Particular attention is given to the correct measurement and control of instrumental parameters to ensure valid and well-calibrated data, to the data quality and filtering. Examples of MASS-DIMM data are given, followed by the list of present and future applications.
Structure determination of the ordered (2 × 1) phase of NiSi surface alloy on Ni(111) using low-energy electron diffraction (2015)

The (2 × 1) structure of the two-dimensional nickel silicide surface alloy on Ni(111) was investigated using quantitative low-energy electron diffraction analysis. The unit cell of the determined silicide structure contains one Si and one Ni atom, corresponding to a chemical formula of NiSi. The Si atoms adopt substitutional face-centered cubic hollow sites on the Ni(111) substrate. The Ni–Si bond lengths were determined to be 2.37 and 2.34 Å. Both the alloy surface and the underlying first layers of Ni atoms exhibit slight corrugation. The Ni–Si interlayer distance is smaller than the Ni–Ni interlayer distance, which indicates that Si atoms and underlying Ni atoms strongly interact.
Accumulation of Vitamin C (Ascorbate) and Its Oxidized Metabolite Dehydroascorbic Acid Occurs by Separate Mechanisms (1995)

It is unknown whether ascorbate alone (vitamin C), its oxidized metabolite dehydroascorbic acid alone, or both species are transported into human cells. This problem was addressed using specific assays for each compound, freshly synthesized pure dehydroascorbic acid, the specially synthesized analog 6-chloroascorbate, and a new assay for 6-chloroascorbate. Ascorbate and dehydroascorbic acid were transported and accumulated distinctly; neither competed with the other. Ascorbate was accumulated as ascorbate by sodium-dependent carrier-mediated active transport. Dehydroascorbic acid transport and accumulation as ascorbate was at least 10-fold faster than ascorbate transport and was sodium-independent. Once transported, dehydroascorbic acid was immediately reduced intracellularly to ascorbate. The analog 6-chloroascorbate had no effect on dehydroascorbic acid transport but was a competitive inhibitor of ascorbate transport. The Ki for 6-chloroascorbate (2.9-4.4 microM) was similar to the Km for ascorbate transport (9.8-12.6 microM). 6-Chloroascorbate was itself transported and accumulated in fibroblasts by a sodium-dependent transporter. These data provide new information that ascorbate and dehydroascorbic acid are transported into human neutrophils and fibroblasts by two distinct mechanisms and that the compound available for intracellular utilization is ascorbate.
Ophthalmic Manifestations of Amyotrophic Lateral Sclerosis (An American Ophthalmological Society Thesis). (2015)

Histopathologic analysis of ALS eyes and mice with the UBQLN2(P497H) mutation, as well as OCT measurements, supports involvement of the anterior visual pathway. We identified pathologies, including intraretinal deposits and axonal loss. pRNFL and total macular thinning found on OCT correlated with disease duration. A pattern of vision loss specific for ALS was not identified. This study confirms ocular involvement in patients and transgenic animals with ALS/dementia.
Blind binary masking for reverberation suppression in cochlear implants (2013)

A monaural binary time-frequency (T-F) masking technique is proposed for suppressing reverberation. The mask is estimated for each T-F unit by extracting a variance-based feature from the reverberant signal and comparing it against an adaptive threshold. Performance of the estimated binary mask is evaluated in three moderate to relatively high reverberant conditions (T60 = 0.3, 0.6, and 0.8 s) using intelligibility listening tests with cochlear implant users. Results indicate that the proposed T-F masking technique yields significant improvements in intelligibility of reverberant speech even in relatively high reverberant conditions (T60 = 0.8 s). The improvement is hypothesized to result from the recovery of the vowel/consonant boundaries, which are severely smeared in reverberation.
One night of partial sleep deprivation affects habituation of hypothalamus and skin conductance responses (2014)

Sleep disturbances are prevalent in clinical anxiety, but it remains unclear whether they are cause and/or consequence of this condition. Fear conditioning constitutes a valid laboratory model for the acquisition of normal and pathological anxiety. To explore the relationship between disturbed sleep and anxiety in more detail, the present study evaluated the effect of partial sleep deprivation (SD) on fear conditioning in healthy individuals. The neural correlates of 1) nonassociative learning and physiological processing and 2) associative learning (differential fear conditioning) were addressed. Measurements entailed simultaneous functional MRI, EEG, skin conductance response (SCR), and pulse recordings. Regarding nonassociative learning, partial SD resulted in a generalized failure to habituate during fear conditioning, as evidenced by reduced habituation of SCR and hypothalamus responses to all stimuli. Furthermore, SCR and hypothalamus activity were correlated, supporting their functional relationship. Regarding associative learning, effects of partial SD on the acquisition of conditioned fear were weaker and did not reach statistical significance. The hypothalamus plays an integral role in the regulation of sleep and autonomic arousal. Thus sleep disturbances may play a causal role in the development of normal and possibly pathological fear by increasing the susceptibility of the sympathetic nervous system to stressful experiences.
Sub-second heat inactivation of coronavirus (2020)

ABSTRACT Heat treatment denatures viral proteins that comprise the virion, making virus incapable of infecting a host. Coronavirus (CoV) virions contain single-stranded RNA genomes with a lipid envelope and 4 proteins, 3 of which are associated with the lipid envelope and thus are thought to be easily denatured by heat or surfactant-type chemicals. Prior studies have shown that a temperature of as low as 75 °C and treatment duration of 15 min can effectively inactivate CoV. The applicability of a CoV heat inactivation method greatly depends on the length of time of a heat treatment and the temperature needed to inactivate the virus. With the goal of finding conditions where sub-second heat exposure of CoV can sufficiently inactivate CoV, we designed and developed a simple system that can measure sub-second heat inactivation of CoV. The system is composed of capillary stainless-steel tubing immersed in a temperature-controlled oil bath followed by an ice bath, through which virus solution can be flowed at various speeds. Flowing virus solution at different speeds, along with a real-time temperature monitoring system, allows the virus to be accurately exposed to a desired temperature for various durations of time. Using mouse hepatitis virus (MHV), a beta-coronavirus, as a model system, we identified that 85.2 °C for 0.48 s exposure is sufficient to obtain &gt; 5 Log 10 reduction in viral titer (starting titer: 5 × 10 7 PFU/mL), and that when exposed to 83.4 °C for 0.95 s, the virus was completely inactivated (zero titer, &gt; 6 Log 10 reduction). IMPORTANCE Three coronaviruses (CoVs) have now caused global outbreaks within the past 20 years, with the COVID19 pandemic caused by SARS-CoV-2 still ongoing. Methods that can rapidly inactivate viruses, especially CoVs, can play critical roles in ensuring public safety and safeguarding personal health. Heat treatment of viruses to inactive them can be an efficient and inexpensive method, with the potential to be incorporated into various human-occupied spaces. In this work, a simple system that can heat-treat viruses for extremely short period was developed and utilized to show that sub-second exposure of CoV to heat is sufficient to inactivate CoV. This opens up the possibility of developing instruments and methods of disinfecting CoV in diverse settings, including rapid liquid disinfection and airborne virus disinfection. The developed method can also be broadly utilized to assess heat sensitivity of viruses other viral pathogens of interest and develop sub-second rapid heat inactivation approaches.
Nanofibers based on polymers for energy harvesting and smart labels (2022)

Nanofibers based on polymers are widely used in different fields, including cosmetics, electronics, sensing, medicine, phtonics, energy and filtration. These materials have a 1D character and exhibit tailorable physico-chemical properties which enables their use in multifunctional devices. They are characterized by properties such as, high surface to volume ratio, large area coverage and low-cost manufacturing which makes their use already widespread in industry. Here I report on our research on nanofibers made by spinning technologies assisted by electric fields, which exhibits photonic functions and energy harvesting/sensing capabilities1. An additional exploited application relies on their use as photoprogrammable material, based on an epoxy-based negative photoresist. Intelligent, flexible, paper-based labels, capable to operate by visual contrast and indicate inappropriate time-temperature exposure of perishable food and drugs are demonstrated2. The research leading to these results has received funding from the European Research Council under the European Union’s Horizon 2020 Research and Innovation Programme (Grant Agreement no. 682157, “xPRINT”) and the Italian Minister of University and Research PRIN 2017PHRM8X and 20173L7W8K projects. References 1 L. Persano et al., Advanced Materials 2017, 29, 1701031, 10.1002/adma.201701031. 2 L. Romano et al. Nature Communications 2020, 11, 5991, https://doi.org/10.1038/s41467-020-19676-y.
Carnosine in primary afferents of the olfactory system: an autoradiographic and biochemical study (1982)

Previous in vivo studies have shown that beta-alanine is incorporated specifically into the dipeptide L-carnosine (beta-alanyl-L-histidine). In the present study, we administered beta-[3H]alanine to the nasal cavity of hamsters and used biochemical analyses to identify the radioactively labeled compounds in the olfactory epithelium and olfactory bulb and autoradiography to demonstrate the localization and transport of the label in the primary afferents of the olfactory system. The olfactory epithelium and lamina propria were labeled intensely 6 hr after intranasal beta-[3H]alanine administration. At this survival time, 61% of the radioactivity in the olfactory epithelium was present in the carnosine fraction, while 37% of the label remained in the beta-alanine fraction. After 24-hr and 4-day survival periods, greater than 82% of the radioactivity was present in the carnosine fraction, and the olfactory receptors and bundles of axons were labeled preferentially. The olfactory nerve and glomerular layers of the main olfactory bulb were labeled intensely at 6 and 24 hr after beta-[3H]alanine administration; much less label was present in these layers at 4 days survival. At all three of these survival times, greater than 84% of the radioactivity in the olfactory bulb was present in the carnosine fraction. No label was present in the olfactory epithelium or bulb 18 days after beta-[3H]alanine administration. While the autoradiographic labeling over the structures of the accessory olfactory system was consistently less intense than that over the main olfactory system structures, the patterns of labeling were similar over the four survival times. Intranasal alpha-[3H]alanine administration resulted in some labeling in the primary afferent fibers, but the labeling did not have the specificity nor the same time course over the four survival times that was observed after beta-[3H]alanine administration. The results are consistent with the hypothesis that carnosine is a neurotransmitter or neuromodulator in the olfactory neurons. The results also suggest that carnosine may play a similar role in the vomeronasal neurons.
All-fibre 3 x 3 acousto-optic switch (1995)

We report an all-fibre 3 x 3 acousto-optic switch. The maximum drive power required is 4 mW, the switching time is 100µs and the insertion loss is less than 0.5 dB.
Atlas: a framework for large scale automated mapping and localization (2004)

This thesis describes a scalable robotic navigation system that builds a map of the robot’s environment on the fly. This problem is also known as Simultaneous Localization and Mapping (SLAM). The SLAM problem has as inputs the control of the robot’s motion and sensor measurements to features in the environment. The desired output is the path traversed by the robot (localization) and a representation of the sensed environment (mapping). The principal contribution of this thesis is the introduction of a framework, termed Atlas, that alleviates the computational restrictions of previous approaches to SLAM when mapping extended environments. The Atlas framework partitions the SLAM problem into a graph of submaps, each with its own coordinate system. Furthermore, the framework facilitates the modularity of sensors, map representations, and local navigation algorithms by encapsulating the implementation specific algorithms into an abstracted module. The challenge of loop
Developing Language Resources for a Transnational Digital Government System (2018)

We describe ongoing efforts towards developing language resources for a transnational digital government project aimed at applying information technology (IT) to a problem of international concern: detecting and monitoring activities related to the transnational movement of illicit drugs. The project seeks to support information sharing, coordination and collaboration among government agencies within a country and across national boundaries by combining a variety of technologies including a distributed query processor with form-based and conversational user interfaces, a language translation system, an event server for event filtering and notification, and an event-trigger-rule server. The prototype system is being developed by U.S. universities in collaboration with an international agency and with universities and government agencies in Belize and the Dominican Republic. This paper focuses on the linguistic resources and their use in Example-Based Machine Translation (EBMT). We are in the process of developing an English- Spanish parallel corpus, focused on the domain of information elicited and used at border crossings, to fuel the EBMT system. While significant parallel corpora are available for these two languages in the newswire domain, they were found to be of very limited use for the border crossings application, spurring the need to develop our own resources.
Figure S7 from The Elongin BC Complex Negatively Regulates AXL and Marks a Differentiated Phenotype in Melanoma (2023)

&lt;p&gt;Modulation of AXL neither affects cell proliferation nor sensitivity to MEK inhibition.&lt;/p&gt;