gebhart/patrepeval huggingface dataset:
Antimuscarinic Potency and Bladder Selectivity of PNU‐200577, a Major Metabolite of Tolterodine (1997)

PNU-200577 (labcode DD 01 [(R)-N, N-diisopropyl-3-(2-hydroxy-5-hydroxymethylphenyl)-3-phenylpropanamine ) is a major pharmacologically active metabolite of tolterodine, a new muscarinic receptor antagonist intended for the treatment of an overactive bladder. In vitro, PNU-200577 produced a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips (KB = 0.84 nM; pA2 = 9.14). In vivo, PNU-200577 was significantly more potent at inhibiting acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50 15 and 40 nmol.kg-1, respectively; P < 0.01). In radioligand binding studies carried out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, PNU-200577 was not selective for any muscarinic receptor subtype. Thus, PNU-200577 is similar to tolterodine in terms of antimuscarinic potency, functional selectivity for the urinary bladder in vivo and absence of selectivity for muscarinic receptor subtypes in vitro. The results of this study clearly indicate that PNU-200577 contributes to the therapeutic action of tolterodine, in view of its high antimuscarinic potency, similar serum concentration and lower degree of protein binding.
Oxidative Stress, <i>hogg1</i> Expression and NF‐κB Activity in Cells Exposed to Low Level Chromium (2003)

Chromium compounds are carcinogenic to the human lung, although the detailed biochemical mechanism is still unclear. To understand the carcinogenic mechanism in cells exposed to low level hexavalent chromium, we measured the generation of reactive oxygen species (ROS) and 8-hydroxydeoxyguanosine (8-OH-dG), the transcription of hogg1, which encodes an 8-OH-dG repair protein, and NF-kappaB activation levels in the A549 human lung epithelial cell line after exposure to Cr (VI) at concentrations of 12.5 to 800 microM. In A549 cells, ROS levels and DNA binding by NF-kappaB increased in proportion to the concentration of Cr (VI). These increases were diminished by pretreatment with catalase, superoxide dismutase, or D-mannitol, but the levels of 8-OH-dG and expression of hogg1 did not change significantly with Cr (VI) exposure. These results suggest that the induction of ROS and the activation of NF-kappaB are important in the carcinogenic mechanism of Cr (VI), but it is unlikely that Cr (VI) concentrations below 800 microM increase 8-OH-dG levels or the expression of hogg1.
Unified system for optimizing the transmission of technical data flow from railway vehicles (2012)

The main fields of research in this article cover the execution of some diagnose, control, data base, analyse and management systems applied to the locomotives. These systems monitor the following: the vehicle's position in the land and the actual speed; the technical parameters for the electric traction motors and the auxiliary services, main command circuits, the voltage in the live wire; the storage of data concerning the power consumption and the status of the “dead-man” safety system; the storage of data concerning the activity of the on-board personnel and its audio and video communication with the traffic control. The research cover as well the transmission, reception and complete analyse of all the parameters discussed above, at the traffic control level, by the human operator which supervises the running vehicles.
Design and Fabrication of Three-Dimensional Scaffolds for Tissue Engineering of Human Heart Valves (2008)

We developed a new fabrication technique for 3-dimensional scaffolds for tissue engineering of human heart valve tissue. A human aortic homograft was scanned with an X-ray computer tomograph. The data derived from the X-ray computed tomogram were processed by a computer-aided design program to reconstruct a human heart valve 3-dimensionally. Based on this stereolithographic model, a silicone valve model resembling a human aortic valve was generated. By taking advantage of the thermoplastic properties of polyglycolic acid as scaffold material, we molded a 3-dimensional scaffold for tissue engineering of human heart valves. The valve scaffold showed a deviation of only +/-3-4% in height, length and inner diameter compared with the homograft. The newly developed technique allows fabricating custom-made, patient-specific polymeric cardiovascular scaffolds for tissue engineering without requiring any suture materials.
Photon detectors with large dynamic range and at near-infrared wavelength for direct detection space lidars (2009)

Space-based lidar instruments must be able to detect extremely weak laser return signals from orbital distance. The signals have a wide dynamic range caused by the variability in atmospheric transmission and surface reflectance under a fast moving spacecraft. Ideally, lidar detectors should be able to detect laser signal return pulses at the single photon level and produce linear output for multiple photon events. They should have high quantum efficiency in the nearinfrared wavelength region where high-pulse-energy space-qualified lasers are available. Silicon avalanche photodiode (APD) detectors have been used in most space lidar receivers to date. Their sensitivity is typically hundreds of photons per pulse at 1064 nm, and is limited by the quantum efficiency, APD gain noise, dark current, and preamplifier noise. NASA is investigating photon-sensitive near-infrared detectors with linear response for possible use on the next generation direct-detection space lidars. We have studied several types of linear mode avalanche photodiode detectors that are sensitive from 950 nm to 1600 nm and potentially viable for near term space lidar missions. We present our measurement results and a comparison of their performance.
Substrate Specificity of the Lanthipeptide Peptidase ElxP and the Oxidoreductase ElxO (2014)

The final step in lanthipeptide biosynthesis involves the proteolytic removal of an N-terminal leader peptide. In the class I lanthipeptide epilancin 15X, this step is performed by the subtilisin-like serine peptidase ElxP. Bioinformatic, kinetic, and mass spectrometric analysis revealed that ElxP recognizes the stretch of amino acids DLNPQS located near the proteolytic cleavage site of its substrate, ElxA. When the ElxP recognition motif was inserted into the noncognate lanthipeptide precursor NisA, ElxP was able to proteolytically remove the leader peptide from NisA. Proteolytic removal of the leader peptide by ElxP during the biosynthesis of epilancin 15X exposes an N-terminal dehydroalanine on the core peptide of ElxA that hydrolyzes to a pyruvyl group. The short-chain dehydrogenase ElxO reduces the pyruvyl group to a lactyl moiety in the final step of epilancin 15X maturation. Using synthetic peptides, we also investigated the substrate specificity of ElxO and determined the 1.85 Å resolution X-ray crystal structure of the enzyme.
A meta-model for software development resource expenditures (1981)

One of the basic goals of software engineering is the establishment of useful models and equations to predict the cost of any given programming project. Many models have been proposed over the last several years, but, because of differences in the data collected, types of projects and environmental factors among software development sites, these models are not transportable and are only valid within the organization where they were developed. This result seems reasonable when one considers that a model developed at a certain environment will only be able to capture the impact of the factors which have a variable effect within that environment. Those factors which are constant at that environment, and therefore do not cause variations in the productivity among projects produced there, may have different or variable effects at another environment.This paper presents a model-generation process which permits the development of a resource estimation model for any particular organization. The model is based on data collected by that organization which captures its particular environmental factors and the differences among its particular projects. The process provides the capability of producing a model tailored to the organization which can be expected to be more effective than any model originally developed for another environment. It is demonstrated here using data collected from the Software Engineering Laboratory at the NASA/Goddard Space Flight Center.
Synthesis and Antitumor Cytotoxicity Evaluation of Novel Thiazole‐Containing Glycosylated Polyamides (2003)

Abstract Certain thiazole‐containing water‐soluble glycosylated polyamides were synthesized and preliminary anti‐cancer evaluation carried out by NCI against three types of cancer‐cells. Glycosyl moieties were introduced onto the polyamide backbone in order to increase the water‐solubility of the longer polymers. This necessitated the development of novel synthetic methods. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003)
Biosystematics of two new species of unusually coloured Australian mygalomorph spiders, Arbanitis (Araneae: Idiopidae), from south-western Australia (2000)

(Uploaded by Plazi from the Biodiversity Heritage Library) No abstract provided.
Planning and Simulation of Neurosurgery in a Virtual Reality Environment (2000)

The VIVIAN system allows users to work with complex imaging data in a fast, comprehensive, and intuitive manner. The 3-D interaction of this virtual reality environment is essential to the efficient assembly of surgically relevant spatial information from the data derived from multiple imaging techniques. The usefulness of the system is highly dependent on the accurate coregistration of the data and the real-time speed of the interaction.
Mathematical Methods and Algorithms for Signal Processing (1999)

I. INTRODUCTION AND FOUNDATIONS. 1. Introduction and Foundations. II. VECTOR SPACES AND LINEAR ALGEBRA. 2. Signal Spaces. 3. Representation and Approximation in Vector Spaces. 4. Linear Operators and Matrix Inverses. 5. Some Important Matrix Factorizations. 6. Eigenvalues and Eigenvectors. 7. The Singular Value Decomposition. 8. Some Special Matrices and Their Applications. 9. Kronecker Products and the Vec Operator. III. DETECTION, ESTIMATION, AND OPTIMAL FILTERING. 10. Introduction to Detection and Estimation, and Mathematical Notation. 11. Detection Theory. 12. Estimation Theory. 13. The Kalman Filter. IV. ITERATIVE AND RECURSIVE METHODS IN SIGNAL PROCESSING. 14. Basic Concepts and Methods of Iterative Algorithms. 15. Iteration by Composition of Mappings. 16. Other Iterative Algorithms. 17. The EM Algorithm in Signal Processing. V. METHODS OF OPTIMIZATION. 18. Theory of Constrained Optimization. 19. Shortest-Path Algorithms and Dynamic Programming. 20. Linear Programming. APPENDIXES. A. Basic Concepts and Definitions. B. Completing the Square. C. Basic Matrix Concepts. D. Random Processes. E. Derivatives and Gradients. F. Conditional Expectations of Multinomial and Poisson r.v.s.
Effect of 4 days of mouth rinsing with delmopinol or chlorhexidine on the vitality of plaque bacteria (1992)

Delmopinol is a new surface active anti-plaque agent that has demonstrated a low antimicrobial effect in vitro. By use of a vitality staining technique, the antimicrobial effect on bacteria in plaque samples was tested after rinsing with delmopinol or chlorhexidine. 6 healthy male subjects volunteered to rinse for 4 days using a double-blind cross-over study design with a wash-out period between the rinsing regimens. No oral hygiene measures were allowed during the test periods and each test period started with a professional tooth cleaning procedure 2 days before the start of rinsing to allow for plaque formation. Rinsing was performed with 0.2% delmopinol hydrochloride or 0.2% chlorhexidine digluconate 2 x a day. Small samples of plaque were collected from the buccal surfaces of premolars and 1st molars before the first rinse on day 1 and then before and 1, 2, 4, 7, and 24 h after the last rinse on the 4th day. The plaque samples were immediately stained with propidium iodide and fluorescein diacetate to visualize dead and vital microorganisms respectively. The vitality of the microflora was evaluated using a fluorescence microscope. The baseline vitality values were 91% for chlorhexidine and 86% for delmopinol. At day 4, the plaque vitality for chlorhexidine was approximately 40% up to 4 h and 50% at 7 h and 60% at 24 h after the last rinse. Corresponding values for plaque vitality after delmopinol rinsing were between 70 and 80% on all sampling occasions.(ABSTRACT TRUNCATED AT 250 WORDS)
Structural and functional roles of highly conserved serines in human lipoprotein lipase. Evidence that serine 132 is essential for enzyme catalysis (1991)

The structure of human lipoprotein lipase was recently deduced from its cDNA sequence. It contains 8 serine residues (residues 45, 132, 143, 172, 193, 244, 251, and 363) that are absolutely conserved in both lipoprotein lipase and hepatic lipase across all species studied. The high homology between lipoprotein lipase, hepatic lipase, and pancreatic lipase suggests that the catalytic functions of these enzymes share a common mechanism and that one of the 8 conserved serines in human lipoprotein lipase must play a catalytic role as does serine 152 in the case of pancreatic lipase (Winkler, F. K., D'Arcy, A., and Hunziker, W. Nature 343, 771-774). We expressed wild-type and site-specific mutants of human lipoprotein lipase in COS cells in vitro. We produced two to four substitution mutants involving each of the 8 serines and assayed a total of 22 mutants for both enzyme activity and the amount of immunoreactive enzyme mass produced. Immunoreactive lipase was detected in all cases. With the exception of Ser132, for each of the 8 serine mutants we studied, at least one of several mutants at each position showed detectable enzyme activity. All three substitution mutants at Ser132, Ser----Thr, Ser----Ala, and Ser----Asp, were totally inactive. Ser132 occurs in the consensus sequence Gly-Xaa-Ser-Xaa-Gly present in all serine proteinases and in human pancreatic lipase. The x-ray crystallography structure of human pancreatic lipase suggests that the analogous serine residue in human pancreatic lipase, Ser152, is the nucleophilic residue essential for catalysis. Our biochemical data strongly support the conclusion that Ser132 in human lipoprotein lipase is the crucial residue required for enzyme catalysis. The observed specific activities of the variants involving the other seven highly conserved serines in human lipoprotein lipase are consistent with the interpretation that this enzyme has a three-dimensional structure very similar to that of human pancreatic lipase.
1,4-Addition reaction of organolithium and -magnesium compounds to .alpha.,.beta.-unsaturated thioamides (1978)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT1,4-Addition reaction of organolithium and -magnesium compounds to .alpha.,.beta.-unsaturated thioamidesYoshinao Tamaru, Toshiro Harada, Hiromitsu Iwamoto, and Zenichi YoshidaCite this: J. Am. Chem. Soc. 1978, 100, 16, 5221–5223Publication Date (Print):August 1, 1978Publication History Published online1 May 2002Published inissue 1 August 1978https://pubs.acs.org/doi/10.1021/ja00484a059https://doi.org/10.1021/ja00484a059research-articleACS PublicationsRequest reuse permissionsArticle Views221Altmetric-Citations54LEARN 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
Learn Java now (1996)

Learn Java Now provides a tutorial for programming with the Microsoft implementation of Java. It covers the language basics, windowing techniques, and use of classes. An integrated package, it features a special edition of the software on disk.
Hydrogen Peroxide Is Essential for Estrogen-Deficiency Bone Loss and Osteoclast Formation (2004)

We recently found that estrogen deficiency leads to a lowering of thiol antioxidant defenses in rodent bone. Moreover, administration of agents that increase the concentration in bone of glutathione, the main intracellular antioxidant, prevented estrogen-deficiency bone loss, whereas depletion of glutathione by buthionine sulfoximine administration provoked substantial bone loss. To analyze further the mechanism by which antioxidant defenses modulate bone loss, we have now compared expression of the known antioxidant enzymes in osteoclasts. We found that glutathione peroxidase 1 (Gpx), the enzyme primarily responsible for the intracellular degradation of hydrogen peroxide, is overwhelmingly the predominant antioxidant enzyme expressed by osteoclasts and that its expression was increased in bone marrow macrophages by receptor activator of nuclear factor-kappaB ligand (RANKL) and in osteoclasts by 17beta-estradiol. We therefore tested the effect of overexpression of Gpx in osteoclasts by stable transfection of RAW 264.7 (RAW) cells, which are capable of osteoclastic differentiation in response to RANKL, with a Gpx-expression construct. Osteoclast formation was abolished. The Gpx expression construct also suppressed RANKL-induced nuclear factor-kappaB activation and increased resistance to oxidation of dihydrodichlorofluorescein by exogenous hydrogen peroxide. We therefore tested the role of hydrogen peroxide in the loss of bone caused by estrogen deficiency by administering pegylated catalase to mice. We found that catalase prevented ovariectomy-induced bone loss. These results suggest that hydrogen peroxide is the reactive oxygen species responsible for signaling the bone loss of estrogen deficiency.
Faithful Reconstruction of Application Behavior Based on Event Traces in the LiteOS Operating System (2008)

Visibility has been a key challenge for wireless sensor network applications. Deployed on the extremely resource-constrained mote platform, such applications may fail unexpectedly, or exhibit behavior different from their intended goals. To help understand why such problems occur, we design and implement an event trace logger based on the LiteOS operating system, which allows us to partially reconstruct application behavior after execution, such as which path it took for an IF statement, its invocation history of the kernel system calls, and its dynamics across multiple nodes. We plan to demonstrate the usefulness of this event trace logger and its translator using a multi-hop routing application.
Relaying in Butterfly Networks: Superposition constellation design for Wireless Network Coding (2015)

Wireless Physical Layer Network Coding (WNC) techniques exploit the inherent nature of wireless channels to improve the performance of wireless communication systems. Unlike conventional Network Coding, in WNC the transmitted signals constructively interact directly in the constellation space, thus inducing specific requirements on the source constellation design. Suitable multi-source constellations should enable direct decoding of WNC functions of user data (from the observed superimposed constellations at receiving nodes) and simultaneously they should allow delivery of partial information to nodes with worse channel conditions (exploiting the natural broadcast property of wireless channels). Source constellations possessing both the aforementioned attributes simultaneously can be desirable in a WNC-based system and thus proper constellation design can become a relatively challenging task. In this paper we focus on this problem and we introduce a systematic constellation design algorithm for a 5-node Wireless Butterfly Network (WBN) with WNC processing, where the basic principles of multi-source constellation design for WNC systems can be demonstrated. We show that the proposed constellations outperform the conventional approaches over the whole range of SNR conditions in the system.
Expression of double-stranded-RNA-specific RNase III of Escherichia coli is lethal to Saccharomyces cerevisiae (1988)

The gene for the double-stranded RNA (dsRNA)-specific RNase III of Escherichia coli was expressed in Saccharomyces cerevisiae to examine the effects of this RNase activity on the yeast. Induction of the RNase III gene was found to cause abnormal cell morphology and cell death. Whereas double-stranded killer RNA is degraded by RNase III in vitro, killer RNA, rRNA, and some mRNAs were found to be stable in vivo after induction of RNase III. Variants selected for resistance to RNase III induction were isolated at a frequency of 4 X 10(-5) to 5 X 10(-5). Ten percent of these resistant strains had concomitantly lost the capacity to produce killer toxin and M dsRNA while retaining L dsRNA. The genetic alteration leading to RNase resistance was localized within the RNase III-coding region but not in the yeast chromosome. These results indicate that S. cerevisiae contains some essential RNA which is susceptible to E. coli RNase III.
Passive network as a complex-voltage generator in four quadrants (1975)

In single-channel and multichannel measurement systems, operating at an audio or low radio frequency, it is often necessary to adjust either the polar or cartesian components of the voltage in one or more of the channels to establish an initial set of conditions. A passive network is described that provides independent and precise control of the real and imaginary components of its output voltage. It can also be used as a generator of a complex voltage in any of the four quadrants with similar control of the cartesian components from a zero condition. Alternatively, if the real and imaginary components of the network's output are fed to a suitable sine/cosine potentiometer, the output voltage can be adjusted continuously in phase with constant modulus, and the latter parameter can be controlled independently by means of an attenuator. A brief description is given of the results obtained with an experimental network that was constructed to prove the theory at 1 MHz. A modified Kelvin-Varley voltage divider is also described that provides equal voltage increments with a constant voltage overlap between adjacent steps. If three capacitors in the network are switched, then it can be made to cover at least three decades in frequency. It is suggested that, for the frequency range from 50 Hz to about 50 kHz, when operating in the complex-voltage-generator mode, it could replace the mutual inductance of the conventional quadrant potentiometer. Also, in the case of multiport network analysers, operating at a fixed intermediate frequency, it could be used as an analogue vector voltmeter, in which the generated voltage is nulled against the network's response voltages. A further possible application is to precision inductance voltage dividers for either error-signal cancellation or the intercomparison of dividers of this type.