gebhart/patrepeval huggingface dataset:
[Progress in the design of selective ATP-competitive kinase inhibitors]. (2007)

Kinases play crucial roles in the life of cell. Their functional abnormity usually leads to many human major diseases including tumors. The prospecting of ATP-competitive small-molecule kinase inhibitors targeting kinases of therapeutic interest has become the focus of researches. Due to the high conservation of the catalytic domain of kinases, the selectivity of kinase inhibitors is poor in general. However, along with the development of structural biology and computer-aided drug design, great progress in the research of selective, ATP-competitive kinase inhibitors has been achieved in recent years. In this account, the review has been made on the development of the design of selective kinase inhibitors.
Phase II study of metronomic chemotherapy (MC) with irinotecan (CPT-11) in patients with refractory metastatic colorectal cancer (MCRC). (2010)

e14109 Background: Tumor angiogenesis is one of the factors contributing to the growth and metastasis. In addition, it is a possible mechanism for repopulation of cells between cycles of standard chemotherapy, which leads to low efficiency of drug treatment in terms of overall survival. Therefore, inhibition of angiogenesis is a promising option of therapy for patients with metastatic disease. Methods: We conducted a phase II study of metronomic CPT-11 2.8 mg/m2/daily C.I. for 24 hours. There was no limit on the number of prior therapies. CT scans were performed every 6 weeks. Patients were treated until tumor progression or development of unacceptable toxicity. Serum was collected for measurement of endothelial progenitor cells (CD45-, CD105+, CD34+, CD59+, CD80+, CD86+). Results: 20 patients (pts) with MCRC were enrolled (12 female, 8 male), 17 of them were evaluated. Median age was 57.5 years (range 32-73). 6 (32.5%) pts had ECOG 2 and more. 60% of pts had 3 or more and 40% at least 2 prior chemotherapy lines. Toxicities included allergic reaction (1 G3), nausea (5 G1), vomiting (1 G1), diarrhea (3 G1), fatigue (1 G1), fever (1 G1), alopecia (1 G1). There were no treatment related deaths. There were no CR or PR. 9 of 17 pts had SD (53%). Median progression-free survival (PFS) was 103 (range 90-107) and 110 days (range 50-239) for 2nd and 3d lines chemotherapy, accordingly. The level of endothelial progenitor cells decreased with metronomic CPT-11 after 6 week evaluation from 0,008% to 0.005% (p = 0.17). Conclusions: Low-dose metronomic C.I. of irinotecan is well tolerated and leads to long-term median PFS in patients with MCRC failed to standard therapy. No significant financial relationships to disclose.
Polymorphism of Drug-Metabolizing Enzymes in Relation to Individual Susceptibility to Industrial Chemicals. (2000)

Polymorphism and the induction/inhibition of drug-metabolizing enzymes, such as cytochrome P450, aldehyde dehydrogenase (ALDH), glutathione S-transferase (GST), N-acetyltransferase (NAT), and NAD(P)H-quinone oxidoreductase (NQO1), were reviewed in relation to susceptibility to disease and to inter-individual difference in biological monitorings. A number of genetic and acquired factors can influence the susceptibility of an individual to chemicals, creating a so-called predisposition. Most cases in which genetic factors were present resulted from polymorphism of drug-metabolizing enzymes. However, conflicting reports have appeared on the relationship between polymorphism and risk of disease; in some cases, biologically plausible mechanisms linking genotypes and disease are not yet in evidence. Current findings based on biological monitoring of chemicals are insufficient to evaluate the relationship between genetic polymorphism and acquired risk when exposure has occurred in an occupational area. Investigation of such situations has generated data implicating GSTT1, GSTM1, NAT2, and NQO1 polymorphisms in biological monitoring of some chemicals; the ALDH2 polymorphism is the likely link between the genotype and the metabolism of low molecular aliphatic aldehydes. Although this polymorphism is limited in the case of Japanese as well as other Asian subjects, the inhibitors of ALDH2 activity such as trichloroethylene may produce a false polymorphism of this gene. As to the effect of factors influencing acquired predisposition, such as ethanol intake, intake of low carbohydrate diet or diabetes, corroborative epidemiological studies may be further required.
THE DETERMINATION OF CHROMIC OXIDE IN SAMPLES OF FEED AND EXCRETA BY ACID DIGESTION AND SPECTROPHOTOMETRY (1961)

Numerous aspects of the wet acidic digestion procedure for the assay of Cr 2 O 3 in feed and excreta samples have been investigated; these included time and temperature of heating, the effects of sulphuric acid concentration, and the wavelengths at which optical densities are read. On the basis of the findings, modifications of the procedure have been adopted.As the optical densities of dichromate solutions, which are the end products of the digestion, are influenced by their sulphuric acid molarities, it is essential that such molarities be kept relatively constant. Reading of optical densities at 350 mμ permits a much greater sensitivity in the assay than does the use of a wavelength of 444 mμ. Standard curves with correlation coefficients of 1.000 between Cr 2 O 3 concentration and optical density were obtained consistently, demonstrating a high degree of precision. When a 3-gram sample of feed and a 1-gram sample of excreta are employed, the observed ratio [Formula: see text] must be corrected as follows:Corrected ratio = (observed ratio × 1.110) − 0.045. This correction accounts for the background light absorption at 350 mμ attributable to the feed and excreta.The modified method was found to give comparable results to the sodium fusion technique with evidence of slight advantages over the latter.
Practice Parameter: Assessing patients in a neurology practice for risk of falls (an evidence-based review) (2008)

Patients with neurologic or general conditions associated with an increased risk of falling should be asked about recent falls and further examined for the presence of specific neurologic deficits that predict falls, which include gait and balance disorders; deficits of lower extremity strength, sensation, and coordination; and cognitive impairments. If substantial risks of falls are identified, appropriate interventions that are described in other evidence-based guidelines may be considered.
Modeling the Maillard Reaction: Schiff Base Formation (2005)

10.1196/annals.1333.104
Disentangling Trainability and Generalization in Deep Neural Networks (2019)

A longstanding goal in the theory of deep learning is to characterize the conditions under which a given neural network architecture will be trainable, and if so, how well it might generalize to unseen data. In this work, we provide such a characterization in the limit of very wide and very deep networks, for which the analysis simplifies considerably. For wide networks, the trajectory under gradient descent is governed by the Neural Tangent Kernel (NTK), and for deep networks the NTK itself maintains only weak data dependence. By analyzing the spectrum of the NTK, we formulate necessary conditions for trainability and generalization across a range of architectures, including Fully Connected Networks (FCNs) and Convolutional Neural Networks (CNNs). We identify large regions of hyperparameter space for which networks can memorize the training set but completely fail to generalize. We find that CNNs without global average pooling behave almost identically to FCNs, but that CNNs with pooling have markedly different and often better generalization performance. These theoretical results are corroborated experimentally on CIFAR10 for a variety of network architectures and we include a colab notebook that reproduces the essential results of the paper.
Pathogenic Mechanisms Associated With Different Clinical Courses of Multiple Sclerosis (2019)

In the majority of patients multiple sclerosis starts with a relapsing remitting course (RRMS), which may at later times transform into secondary progressive disease (SPMS). In a minority of patients the relapsing remitting disease is skipped and the patients show progression from the onset (primary progressive MS, PPMS). Evidence obtained so far indicate major differences between RRMS and progressive MS, but no essential differences between SPMS and PPMS, with the exception of a lower incidence in the global load of focal white matter lesions and in particular in the presence of classical active plaques in PPMS. We suggest that in MS patients two types of inflammation occur, which develop in parallel but partially independent from each other. The first is the focal bulk invasion of T- and B-lymphocytes with profound blood brain barrier leakage, which predominately affects the white matter, and which gives rise to classical active demyelinated plaques. The other type of inflammation is a slow accumulation of T-cells and B-cells in the absence of major blood brain barrier damage in the connective tissue spaces of the brain, such as the meninges and the large perivascular Virchow Robin spaces, where they may form aggregates or in most severe cases structures in part resembling tertiary lymph follicles. This type of inflammation is associated with the formation of subpial demyelinated lesions in the cerebral and cerebellar cortex, with slow expansion of pre-existing lesions in the white matter and with diffuse neurodegeneration in the normal appearing white or gray matter. The first type of inflammation dominates in acute and relapsing MS. The second type of inflammation is already present in early stages of MS, but gradually increases with disease duration and patient age. It is suggested that CD8<sup>+</sup> T-lymphocytes remain in the brain and spinal cord as tissue resident cells, which may focally propagate neuroinflammation, when they re-encounter their cognate antigen. B-lymphocytes may propagate demyelination and neurodegeneration, most likely by producing soluble neurotoxic factors. Whether lymphocytes within the brain tissue of MS lesions have also regulatory functions is presently unknown. Key open questions in MS research are the identification of the target antigen recognized by tissue resident CD8<sup>+</sup> T-cells and B-cells and the molecular nature of the soluble inflammatory mediators, which may trigger tissue damage.
Band-to-Band Tunnel Transistor Design and Modeling for Low Power Applications (2012)

As the physical dimensions of the MOSFET have been scaling, the supply voltage has not scaled accordingly and thus the power density has been continuously increasing. This is mainly due to the fact that transistor operation requires carriers to go over the source side potential barrier which limits the subthreshold swing of a MOSFET to 60mV/dec at room temperature and thus inhibits the scaling of the threshold voltage. Tunneling devices utilizing the band-to-band tunneling mechanism have been known to overcome this fundamental limit.In this thesis, the tunneling field-effect-transistor (TFET) is explored to replace conventional MOSFETs for low power applications. The band-to-band tunneling mechanism is looked into in order to develop a more accurate tunneling model that considers the change in effective mass during the transition between the conduction and valence band. Device simulator parameters are modified with this model and are used in designing the TFET. The silicon P-I-N structure TFET is studied through simulation and various experimental splits as a baseline for the TFET development. High tunneling currents are measured from a short channel device with a flash and spike anneal combination and a novel silicided source TFET using silicide induced dopant segregation is shown to achieve sub-60mV/dec subthreshold swing. Measurement and analysis methods of the transistor current and subthreshold swing to verify the TFET are discussed. Lower band gap Ge devices and Strained Si/Ge hetero-structure devices utilizing a lower effective bandgap are also explored to improve the performance of the TFET.
A Comparison of Semipermeable Microcapsules and Standard Dialysers for Use in Separation (1974)

Abstract Dialysers with membranes of the coil, plate, or capillary configurations are most commonly used in separation procedures. Inrecent years, there is the development of a new class of dialys is system in the form of semipermeable microcapsules (1,2,3, 4). It is the purpose of this paper to discuss this new dialys is system and to compare it with standard dialysers.
<i>In Vitro</i>Activity of LY 333328 Against Anaerobic Gram-Positive Bacteria (1999)

LY 333328 is a new semisynthetic glycopeptide with reported activity against aerobic Gram-positive cocci such as enterococci, pneumococci, streptococci and staphylococci. The present investigation was undertaken to determine the in vitro activity of LY 333328 against 178 Gram-positive anaerobic bacteria recently isolated from human infections. The activity was compared with that of vancomycin, teicoplanin, cefoxitin, imipenem, clindamycin and metronidazole. Peptostreptococci (48 strains): LY 333328, range 0.016-1.0 mg/l; vancomycin, 0.125-2.0 mg/l; teicoplanin, 0.032-2.0 mg/l; cefoxitin, 0.064-8.0 mg/l; imipenem, 0.016-0.064 mg/l; clindamycin, 0.016-1.0 mg/l; metronidazole, 0.125-8.0 mg/l. Propionibacterium acnes (31 strains): LY 333328, range 0.032-0.125 mg/l; vancomycin, 0.25-0.5 mg/l; teicoplanin, 0.25-0.5 mg/l; cefoxitin, 0.125-1.0 mg/l; imipenem, 0.032-0.064 mg/l; clindamycin, 0.016-0.064 mg/l; metronidazole, 32-> or =64 mg/l. Clostridium difficile (50 strains): LY 333328, range 0.016-2.0 mg/l; vancomycin, 0.5-4.0 mg/l; teicoplanin, 0.064-0.5 mg/l; cefoxitin, 64-128 mg/l; imipenem, 8.0 mg/l; clindamycin, 0.25-128 mg/l; metronidazole, 0.125-0.25 mg/l. Clostridium perfringens (49 strains): LY 333328, range 0.016-2.0 mg/l; vancomycin, 0.025-4.0 mg/l; teicoplanin, 0.064-4.0 mg/l; cefoxitin, 0.5-1.0 mg/l; imipenem, 0.016-0.5 mg/l; clindamycin, 0.008-1.0 mg/l; metronidazole, 1.0-4.0 mg/l. LY 333328 had an excellent in vitro activity against anaerobic Gram-positive bacteria.
Low power bus encoding with crosstalk delay elimination [SoC] (2003)

In deep-submicron (DSM) technology, minimizing the propagation delay and power consumption on buses are two of the most important design objectives in system-on-chip (SoC) design. In particular, coupling effects between wires on the bus cause serious problems such as crosstalk delay, noise, and power consumption. Most of the previous works on bus encoding are targeted either (1) to minimize the power consumption on the bus or (2) to minimize the crosstalk delay, but not both. In this paper, we propose a new bus encoding algorithm which not only minimizes the dynamic power consumption on the bus but also eliminates the crosstalk delay. We achieve the combined objective of (1) and (2) by analyzing, formulating and solving the problem of minimizing a weighted sum of the self transition and cross-coupled transition activities on bus in the context of the concept of self-shield encoding (whose fundamental theory is well studied recently by B. Victor and K. Keutzer (Proc. ICCAD, 2001)). From experiments using a set of benchmark designs, it is shown that the proposed encoding technique consumes 15.4%-47.4% less power over the existing techniques, while totally eliminating the crosstalk delays.
Polypeptides. Part XXV. Synthesis of isariin (1974)

O-(Glycyl-L-valyl-D-leucyl-L-alanyl-L-valyl)-D- and L-3-hydroxydodecanoic acids (D- and L-isoisariic acids) have been synthesised and their cyclisation has been studied. D-Isoisariic acid was converted through its acid chloride into a cyclopeptolide indistinguishable from isariin, a metabolite of Isaria cretacea. High pressure liquid chromatography was necessary for the isolation of the product from the reaction mixture and facilitated comparison with the natural material. Attempts to cyclise D-isoisariic acid by other methods were unsuccessful.
Abstracts (1992)

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There You Go! - Estimating Pointing Gestures In Monocular Images For Mobile Robot Instruction (2006)

In this paper, we present a neural architecture that is capable of estimating a target point from a pointing gesture, thus enabling a user to command a mobile robot to a specific position in his local surroundings by means of pointing. In this context, we were especially interested to determine whether it is possible to implement a target point estimator using only monocular images of low-cost Webcams. The feature extraction is also quite straightforward: We use a gabor jet to extract the feature vector from the normalized camera images; and a cascade of multi layer perceptron (MLP) classifiers as estimator. The system was implemented and tested on our mobile robotic assistant HOROS. The results indicate that it is in fact possible to realize a pointing estimator using monocular image data, but further efforts are necessary to improve the accuracy and robustness of our approach
Comparison of Percoll, mini-Percoll and swim-up methods for sperm preparation from abnormal semen samples (1992)

Two methods of density gradient centrifugation, Percoll (P) and mini-Percoll (MP), were compared with the swim-up technique for preparing spermatozoa from each of 40 abnormal semen samples. P and MP produced similar results with a mean recovery of spermatozoa with progressive motility which was significantly higher (18-19%) than that achieved with swim-up (5%). However, the swim-up method resulted in the recovery of spermatozoa with a higher mean motility (89 versus 58%), velocity (69 versus 56 microns/s), percentage with normal morphology (22 versus 16%) and intact acrosomes (61 versus 36%) than P and MP. The mean amplitude of lateral head displacement was the only characteristic of spermatozoa in semen which correlated with the recoveries of motile spermatozoa. Combining MP and swim-up methods for 10 samples produced a higher recovery (11 versus 6.9%) of spermatozoa with significantly better mean motility (94 versus 87%) than did swim-up alone. Although P and MP resulted in greater yields of motile spermatozoa than the swim-up preparation, the latter procedure selected higher proportions of spermatozoa with improved characteristics (velocity, intact acrosomes and normal morphology) which correlate with fertilization rates in vitro. It is concluded that P and MP are not superior to swim-up. However, sequential MP and swim-up preparation improves yields of high quality spermatozoa from some abnormal semen samples and therefore has potential for improving fertilization rates.
Experimental verification of source-mask optimization and freeform illumination for 22-nm node static random access memory cells (2011)

The use of customized illumination modes is part of the pursuit to stretch the applicability of immersion ArF lithography. Indeed, a specific illumination source shape that is optimized for a particular design leads to enhanced imaging results. Recently, freeform illumination has become available through pixelated diffractive optical elements or through ASML's programmable illuminator system (FlexRayTM) allowing for virtually unconstrained intensity distribution within the source pupil. In this paper, the benefit of freeform over traditional illumination is evaluated, by applying source mask co-optimization (SMO) for an aggressive use case and wafer-based verification. For a 22-nm node SRAM of 0.099 and 0.078 μm2 bit cell area, the patterning of the full contact and metal layer into a hard mask is demonstrated with the application of SMO and freeform illumination. In this work, both pixelated diffractive optical elements and FlexRay are applied. Additionally, the match between the latter two is confirmed on wafer, in terms of critical dimension and process window.
An Historian's Approach to the Origins of the Castle in England (1969)

(1969). An Historian's Approach to the Origins of the Castle in England. Archaeological Journal: Vol. 126, No. 1, pp. 131-148.
The Chemistry of Vitamin E. XXXIII. A New Synthesis of 6-Hydroxychromans, Including α-Tocopherol<sup>1</sup> (1942)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTThe Chemistry of Vitamin E. XXXIII. A New Synthesis of 6-Hydroxychromans, Including α-Tocopherol1Lee Irvin Smith and Henry C. MillerCite this: J. Am. Chem. Soc. 1942, 64, 2, 440–445Publication Date (Print):February 1, 1942Publication History Published online1 May 2002Published inissue 1 February 1942https://pubs.acs.org/doi/10.1021/ja01254a056https://doi.org/10.1021/ja01254a056research-articleACS PublicationsRequest reuse permissionsArticle Views120Altmetric-Citations8LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Error Correction Codes In Wireless Sensor Network: An Energy Aware Approach (2010)

Link reliability and transmitted power are two important design constraints in wireless network design. Error control coding (ECC) is a classic approach used to increase link reliability and to lower the required transmitted power. It provides coding gain, resulting in transmitter energy savings at the cost of added decoder power consumption. But the choice of ECC is very critical in the case of wireless sensor network (WSN). Since the WSNs are energy constraint in nature, both the BER and power consumption has to be taken into count. This paper develops a step by step approach in finding suitable error control codes for WSNs. Several simulations are taken considering different error control codes and the result shows that the RS(31,21) fits both in BER and power consumption criteria.
Quantitative determination of Young's modulus on a biphase polymer system using atomic force microscopy (2000)

Atomic force microscopy (AFM) is currently used to investigate polymer surface morphology, to obtain roughness parameters or to map the qualitative differenceces of surface properties. Some previous studies have attempted to determine quantitatively the elastic surface properties, but the difficulty with AFM is that the contact geometry is not very well known, due to the complexity of the mechanical system composed of the cantilever–tip set and the solid surface. We propose here a relative method for measuring the Young's modulus E of a polymer surface by AFM indentation, involving a calibration step obtained from a set of standards constituted by pure polymers with known modulus. Contact stiffness, indentation at peak load and shape of unloading curve are obtained for each reference polymer, leading to a linear relationship between E and a function of these parameters. This calibration curve allows the unknown Young's modulus values of the different phases at the surface of a biphase polymer system to be determined. The force volume mode was used to record force curves. Compared to classical indentation techniques, the force volume mode gives the advantage of imaging surface domains exhibiting elasticity differences. Thus, the elastic modulus can be quantified with a spatial resolution on a nanometric scale. Copyright © 2000 John Wiley & Sons, Ltd.