gebhart/patrepeval huggingface dataset:
Concepts and Molecular Aspects in the Polypharmacology of PARP‐1 Inhibitors (2015)

Recent years have witnessed a renewed interest in PARP-1 inhibitors as promising anticancer agents with multifaceted functions. Particularly exciting developments include the approval of olaparib (Lynparza) for the treatment of refractory ovarian cancer in patients with BRCA1/2 mutations, and the increasing understanding of the polypharmacology of PARP-1 inhibitors. The aim of this review article is to provide the reader with a comprehensive overview of the distinct levels of the polypharmacology of PARP-1 inhibitors, including 1) inter-family polypharmacology, 2) intra-family polypharmacology, and 3) multi-signaling polypharmacology. Progress made in gaining insight into the molecular basis of these multiple target-independent and target-dependent activities of PARP-1 inhibitors are discussed, with an outlook on the potential impact that a better understanding of polypharmacology may have in aiding the explanation as to why some drug candidates work better than others in clinical settings, albeit acting on the same target with similar inhibitory potency.
Data from Antitumor Activity of a Kinesin Inhibitor (2023)

&lt;div&gt;Abstract&lt;p&gt;Several members of the kinesin family of microtubule motor proteins play essential roles in mitotic spindle function and are potential targets for the discovery of novel antimitotic cancer therapies. KSP, also known as &lt;i&gt;Hs&lt;/i&gt;Eg5, is a kinesin that plays an essential role in formation of a bipolar mitotic spindle and is required for cell cycle progression through mitosis. We identified a potent inhibitor of KSP, CK0106023, which causes mitotic arrest and growth inhibition in several human tumor cell lines. Here we show that CK0106023 is an allosteric inhibitor of KSP motor domain ATPase with a &lt;i&gt;K&lt;/i&gt;&lt;sub&gt;i&lt;/sub&gt; of 12 nm. Among five kinesins tested, CK0106023 was specific for KSP. In tumor-bearing mice, CK0106023 exhibited antitumor activity comparable to or exceeding that of paclitaxel and caused the formation of monopolar mitotic figures identical to those produced in cultured cells. KSP was most abundant in proliferating human tissues and was absent from cultured postmitotic neurons. These findings are the first to demonstrate the feasibility of targeting mitotic kinesins for the treatment of cancer.&lt;/p&gt;&lt;/div&gt;
OH-LIF measurement of H2/O2/N2 flames in a micro flow reactor with a controlled temperature profile (2014)

This paper presents combustion and ignition characteristic of H2/O2/N2 flames in a micro flow reactor with a controlled temperature profile. OH-LIF measurement was conducted to capture flame images. Flame responses were investigated for variable inlet flow velocity, U, and equivalence ratio, . Three kinds of flame responses were experimentally observed for the inlet flow velocities: stable flat flames (normal flames) in the high inlet flow velocity regime; unstable flames called Flames with Repetitive Extinction and Ignition (FREI) in the intermediate flow velocity regime; and stable weak flames in the low flow velocity regime, at = 0.6, 1.0 and 1.2. On the other hand, weak flame was not observed at = 3.0 by OH-LIF measurement. Computational OH mole fractions showed lower level at the rich conditions than those at stoichiometric and lean conditions. To examine this response of OH signal to equivalence ratio, rate of production analysis was conducted and four kinds of major contributed reaction for OH production: R3(O + H2 H + OH); R38(H + O2 O + OH); R46(H + HO2 2OH); and R86(2OH O + H2O), were found. Three reactions among them, R3, R38 and R46, did not showed significant difference in rate of OH production for different equivalence ratios. On the other hand, rate of OH production from R86 at = 3.0 was extremely lower than those at = 0.6 and 1.0. Therefore, R86 was considered to be a key reaction for the reduction of the OH production at = 3.0.
Increasing the human-computer bandwidth (2002)

Topics discussed are high-definition television (HDTV), image compression, image density and dynamic range, and new application areas. HDTV will have a strong impact on the computing industry if it becomes a digital medium. It is certainly inevitable that HDTV will be digital, but it is as yet uncertain whether an intermediate analog standard will be attempted. In the computer industry, the economic impact may be very significant. Consumer volumes of VRAMs (video random-access and other key memories) components will have a strong affect on the chip market. VRAM architectures will also be influenced by the high bandwidth transfer rates required for HDTV. Displays will also be greatly affected. At a minimum, computer displays will have to change to a wider format, turning over the market.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
External Magnetic Field-Induced Mesoscopic Organization of Fe3O4 Pyramids and Carbon Sheets (2007)

The current investigation is centered on the thermal decomposition of iron(II) acetyl acetonate, Fe(C5H7O2)2, in a closed cell at 700 degrees C, which is conducted under a magnetic field (MF) of 10 T. The product is compared with a similar reaction that was carried out without a MF. This article shows how the reaction without a MF produces spherical Fe3O4 particles coated with carbon. The same reaction in the presence of a 10 T MF causes the rejection of the carbon from the surface of pyramid-shaped Fe3O4 particles, increases the Fe3O4 particle diameter, forms separate carbon particles, and leads to the formation of an anisotropic (long cigarlike) orientation of Fe3O4 pyramids and C sheets. The macroscopic orientation of Fe3O4 pyramids+C sheets is stable even after the removal of an external MF. The suggested process can be used to fabricate large arrays of uniform wires comprised of some magnetic nanoparticles, and to improve the magnetic properties of nanoscale magnetic materials. The probable mechanism is developed for the growth and assembly behavior of magnetic Fe3O4 pyramids+C sheets under an external MF. The effect of an applied MF to synthesize morphologically different, but structurally the same, products with mesoscopic organization is the key theme of the present paper.
Ivacaftor restores delayed mucociliary transport caused by Pseudomonas aeruginosa–induced acquired cystic fibrosis transmembrane conductance regulator dysfunction in rabbit nasal epithelia (2021)

In rabbit nasal epithelium, ivacaftor robustly stimulates CFTR-mediated Cl<sup>-</sup> secretion and normalizes ASL and CBF in PAO1-induced acquired CFTR dysfunction. Preclinical testing of CFTR potentiators as therapy for P aeruginosa rabbit sinusitis is planned.
Teaching an old dog new tricks: new directions in fundamental and applied closo-carborane anion chemistry (2019)

This feature article covers new directions in the fundamental and applied chemistry of the closo-carborane anions [HCB11H11]- and [HCB9H9]-, as well as some related chemistry with the dicarbolide ion [H2C2B9]2-. Specifically the manuscript will focus on summarizing the authors' as well as related novel contributions to the field. The application of such clusters as solution based electolytes for Mg batteries and related materials for ionic liquids will be discussed. In addition, the preparation of heterocycles and radicals fused to carborane anions will be discussed as well as various novel chemical transformations. Furthermore, new developments in anionic carboranyl phosphines and N-heterocyclic carbenes in the context of catalysis will be summarized.
Analytical and Biological Characterization of Supercoiled Plasmids Purified by Various Chromatographic Techniques (2005)

Supercoiled plasmids are an important component of gene-based delivery vehicles. A number of production methods for clinical applications have been developed, each resulting in very high-quality product with low levels of residual contaminants. There is, however, no consensus on the optimal methods to characterize plasmid quality, and further, to determine if these methods are predictive of either product stability or biological activity. We have produced two plasmids using four production purification methodologies based on PolyFlo and hydrophobic interaction chromatography (HIC), either alone or in tandem processes. In each case, the product was analyzed using standard molecular biological methods. We also performed a number of biophysical analyses such as dynamic light scattering (DLS), circular dichroism (CD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). Minimal differences were detected among the preparations based on the more standard molecular biological methods. Some small differences were detected, however, using biophysical techniques, particularly FTIR and DSC, which may reflect small variations in plasmid tertiary structure and thermal stability. Stability after heat exposure at 60 degrees C, exposure to fetal bovine serum and long-term storage at 4 degrees C varied between plasmids. One plasmid showed no difference in stability depending on the production process, but the other showed significant differences. Evaluation in vivo in models for gene immunization and gene therapy showed significant differences in the response depending on the method of purification. Preparations using a tandem process of PolyFlo used in two separation modes provided higher biological activity compared to a tandem HIC/PolyFlo process or either resin used alone in a single column process. These data indicate that the process by which supercoiled plasmids are made can influence plasmid stability and biological activity and emphasize the need for more rigorous methods to evaluate supercoiled plasmids as gene-delivery vehicles.
Circular High-Q Resonating Isotropic Strain Sensors with Large Shift of Resonance Frequency under Stress (2009)

We present circular architecture bioimplant strain sensors that facilitate a strong resonance frequency shift with mechanical deformation. The clinical application area of these sensors is for in vivo assessment of bone fractures. Using a rectangular geometry, we obtain a resonance shift of 330 MHz for a single device and 170 MHz for its triplet configuration (with three side-by-side resonators on chip) under an applied load of 3,920 N. Using the same device parameters with a circular isotropic architecture, we achieve a resonance frequency shift of 500 MHz for the single device and 260 MHz for its triplet configuration, demonstrating substantially increased sensitivity.
Immunological cross-reactivities of various anthracycline antibiotics against aclacinomycin a antisera. (1982)

Aclacinomycin A (ACM) antisera were obtained from the rabbits immunized with 4"'-deoxo-4"'-(R)-amino-ACM- or N,N-didemethyl-ACM-bovine serum albumin conjugate, and their immunoreactivities were tested with ACM-related anthracyclines. It was found that the binding ability with the ACM antisera was markedly decreased by the following structural changes in ACM: N,N-didemethylation of the rhodosamine moiety; 6-O- or 4-O-methylation; removal of the methoxycarbonyl group at C-10; hydroxylation at C-1, C-2 or C-11. It was less affected by some alterations in a side chain at C-9 or by deglycosidation of the terminal mono or disaccharide. The binding of the aglycone (aklavinone) was very weak.
Symshop: A Mobile Shopping Mall Application (2002)

The Frustrated Shopper Typical Experiences in a large shopping mall - Searching for the mall directory - Looking for merchandise - Looking for a sales assistant - Waiting for the cashier to check out items - Searching for promotional, discount items - Locating shopping partner who has wandered off separately, locating restrooms, etc - No idea what accessories match items - No time to shop leisurely!
A Completely Integrated 2.7GHz Voltage Controlled Oscillator with Low Phase Noise (2001)

and low-cost VCO is discussed. The VCO uses on-chip schottky diode varactors and regular bondwires for its resonator. The VCO was implemented for the local oscillator (LO) of a GPS receiver. The VCO oscillates at 2.7-GHz which is double the LO. This frequency is divided to generate I and Q components of the LO. The core VCO uses MOS devices and can easily be integrated in any standard CMOS process with better performance. Regular bondwires used to form the resonator makes the design compact and cost-effective. Also the high-Q bondwire inductance helps reduce the power and phase noise. An automatic amplitude control (AAC) loop has been used to control the amplitude of the oscillation. The implemented VCO has a phase noise of-112dBc/Hz at an offset of 200kHz from the 2.7GHz carrier and the core consumes 2.5mA from a 3V supply. 1
Reduction of Effective Pixel Pitch of Digital Micromirror Device for Lidar Transmitter and Receiver (2020)

Small pixel pitch with a large array size is highly anticipated for solid-state lidar transmitter and receiver. We demonstrate 2D beam steering with reduced effective pixel pitch by harnessing transitional state of the mirror array.
TOR signaling modulates Cdk8-dependent GAL gene expression in Saccharomyces cerevisiae (2020)

Abstract Cdk8 of the RNA Polymerase II mediator complex regulates genes by phosphorylating sequence specific transcription factors. Despite conserved importance for eukaryotic transcriptional regulation, the signals regulating Cdk8 are unknown. Full induction of the yeast GAL genes requires phosphorylation of Gal4 by Cdk8, and we exploited this requirement for growth of gal3 yeast on galactose to identify mutants affecting Cdk8 activity. Several mutants from the screen produced defects in TOR signaling. A mutant designated g al f our throttle ( gft ) 1, gft1 , was identified as an allele of hom3 , encoding aspartokinase. Defects in gft1 / hom3 caused hypersensitivity to rapamycin, and constitutive nuclear localization of Gat1. Furthermore, mutations of tor1 or tco89 , encoding TORC1 components, also prevented GAL expression in gal3 yeast, and tco89 was determined to be allelic to gft7 . Disruption of cdc55 , encoding a subunit of PP2A regulated by TOR signaling, suppressed the effect of gft1 / hom3, gft7 / tco89 , and tor1 mutations on GAL expression in gal3 yeast, but not of cdk8 / srb10 disruptions or Gal4 S699A mutation. Mutations of gft1 / hom3 and tor1 did not affect kinase activity of Cdk8 in vitro , but caused loss of Gal4 phosphorylation in vivo . These observations demonstrate that TOR signaling regulates GAL induction through the activity of PP2A/ Cdc55, and are consistent with the contention that Cdk8-dependent phosphorylation of Gal4 S699 is opposed by PP2A/ Cdc55 dephosphorylation. These results provide insight into how induction of transcription by a specific inducer can be modulated by global nutritional signals through regulation of Cdk8-dependent phosphorylation.
Iterative Decoding for GERAN MBMS (2006)

Various advanced methods have been proposed to achieve sufficiently high throughput as well as reliability for multimedia broadcast multicast services (MBMS) within 3GPP RAN and GERAN. One of the methods which yield promising results with only marginal system modifications is based on outer Reed-Solomon (RS) coding on the radio link control (RLC) layer. For initial studies standard decoding algorithms based on erasure-only decoders have been employed. In order to further improve the performance, the system can be viewed as a serially concatenated code such that iterative decoding can be performed. Then, advanced receivers for MBMS over GERAN would incorporate soft-in soft-cut (SISO) decoders for both the inner convolutional code, as well as the outer RS code. Whereas for the convolutional code, standard SISO algorithms are applied, for the outer RS code a standard Berlekamp-Massey algorithm is modified to accept soft-input and to provide soft-output. With this modified iterative decoding strategy, simulations have shown gains of up to 14% in throughput on typical mobile radio channels.
Parkinson’s Disease Biomarkers: Perspective from the NINDS Parkinson’s Disease Biomarkers Program (2017)

Biomarkers for Parkinson's disease (PD) diagnosis, prognostication and clinical trial cohort selection are an urgent need. While many promising markers have been discovered through the National Institute of Neurological Disorders and Stroke Parkinson's Disease Biomarker Program (PDBP) and other mechanisms, no single PD marker or set of markers are ready for clinical use. Here we discuss the current state of biomarker discovery for platforms relevant to PDBP. We discuss the role of the PDBP in PD biomarker identification and present guidelines to facilitate their development. These guidelines include: harmonizing procedures for biofluid acquisition and clinical assessments, replication of the most promising biomarkers, support and encouragement of publications that report negative findings, longitudinal follow-up of current cohorts including the PDBP, testing of wearable technologies to capture readouts between study visits and development of recently diagnosed (de novo) cohorts to foster identification of the earliest markers of disease onset.
Development Guidance for Sign Design Standards (2012)

"This two-year project was designed to provide TxDOT with comprehensive review and update of mounting details and standards for large and small sign supports, and to provide a mechanism for TxDOT to quickly and effectively evaluate and address high priority needs related to sign support systems."
Systematic Post-assembly Modification of Graphene Oxide Paper with Primary Alkylamines (2010)

Graphene oxide paper can be systematically modified with alkylamines in both solution- and vapor-phase, with the latter process being significantly slower. After removal of physisorbed amine, the increases in gallery spacing, physical thickness, and mass of amine-modified papers can be directly correlated to the length of the intercalated alkyl chain. While the tensile strength of the modified papers slightly decreases with increasing amine lengths, their &amp;quot;effective graphene oxide moduli&amp;quot; were essentially unchanged, suggesting that graphene oxide is the sole contributor to the stiffness of amine-modified papers.
Biofeedback improves postural control recovery from multi-axis discrete perturbations (2012)

The results show that among the displays evaluated in this study, no one tactor column configuration was optimal for standing tasks involving discrete surface perturbations. Feedback produced larger effects on body tilt versus center of pressure parameters. Furthermore, the subjects' performance worsened when erroneous feedback was provided, suggesting that vibrotactile stimulation applied to the torso is actively processed and acted upon rather than being responsible for simply triggering a stiffening response.
A method for impact assessment of faults on the performance of field-oriented control drives: A first step to reliability modeling (2010)

In this paper, the effects of certain component faults on the performance of three-phase inverter-fed induction motors are analyzed under indirect field-oriented control. Simulations of faults in the current sensors, speed encoder, three-phase inverter, and motor are presented. Sample hardware faults verifying the simulation results are also presented. Performance requirements are set based on typical performance measures of electric vehicles. These requirements are then used to determine whether or not the system survives a fault. A simple fault detection and isolation scheme using multiple speed encoders is also tested. The construction of a Markov reliability model of the overall system is a direct application of the results, and allows quantifying global reliability measures.
On-line fault detection of sensor measurements (2004)

On-line fault detection in sensor networks is of paramount importance due to the convergence of a variety of challenging technological, application, conceptual, and safety related factors. We introduce a taxonomy for classification of faults in sensor networks and the first on-line model-based testing technique. The approach is generic in the sense that it can be applied on an arbitrary system of heterogeneous sensors with an arbitrary type of fault model, while it provides a flexible tradeoff between accuracy and latency. The key idea is to formulate on-line testing as a set of instances of a non-linear function minimization and consequently apply nonparametric statistical methods to identify the sensors that have the highest probability to be faulty. The optimization is conducted using the Powell nonlinear function minimization method. The effectiveness of the approach is evaluated in the presence of random noise using a system of light sensors.
Studies towards the Biomimetic Synthesis of Ginsenoyne L; Efficient Synthesis of 2'-epi-Ginsenoyne L (2003)

Abs tract -The biomimetic synthesis of 2'-epi-gynsenyone L has been accomplished in 7 steps and in good yield through the novel use of bis-acetylenic enones as hetero Diels-Alder dienes for the mild and easy generation of dihydropyrans.As part of our continuous efforts in the biomimetic synthesis of natural products, 1 we have become interested in the biomimetic synthesis of gynsenoyne L (1).Ginsenoyne L (1) was isolated in 2000 by Hirakura and coworkers in 6.8x10 -5 % yield from the roots of Panax ginseng, and its structure proposed on the basis of 2-D NMR spectral analysis, and NMR spectral data comparison with panaxydol (2). 2 Panax ginseng is an important plant in traditional oriental medicine for the treatment of diabetes, as well as, psychiatric and neurological disorders. 3
Down‐regulation of monocytic VLA‐4 leads to a decreased adhesion to VCAM‐1 (1993)

The alpha 4 beta 1 integrin VLA-4 is expressed on practically all leukocytes, except on mature granulocytes. Here we show that in vitro treatment of monocytic cells with phorbol-12-myristate-13-acetate (PMA) leads to a selective decrease in the VLA-4 alpha-chain expression, both at the RNA and protein level. Meanwhile the expression of beta 1 and that of alpha 5, another alpha-chain associating with beta 1, was seen to increase. The decrease of alpha 4 expression was restricted to monocytic cells, and was not observed on other VLA-4-positive cells tested (MOLT-4 T cells and HOS sarcoma cells). The down-regulation of the VLA-4 alpha-chain was followed by a decreased binding capacity of the cells to recombinant VCAM-1. This data indicates that while previous findings show that the integrin-dependent adhesion may rapidly be regulated by altering the avidity of the interacting molecules, their quantitative modulation also has a clear impact on adhesion.
CVD barriers for Cu with nanoporous ultra low-k: integration and reliability (2003)

The drive for greater integrated circuit performance has led to the need for faster interconnect systems, the development of porous ultra low-k dielectrics and thin CVD barriers. The porous structure and lower modulus of low-k dielectrics has made integration a greater challenge. In this paper, we report on an initial feasibility study on of a new spin-on nanoporous low-k dielectric with a CVD TiN(Si) barrier, for Cu dual damascene integration.