gebhart/patrepeval huggingface dataset:
Antagonists of the Luteinizing Hormone Releasing Hormone with Emphasis on Amino Acids in Position Five (1985)

Abstract Seventeen analogs of the luteinizing hormone releasing hormone (LHRH) have been synthesized, bioassayed, and compared for antiovulatory activity (AOA) in rats. The emphasis of design was replacement of Tyr 5 of LHRH. Position 5 has not been extensively studied. [N-Ac-D-2-Nal 1 , D-pClPhe 2 , D-3-Pal 3 , D-Arg 6 , D-Ala 10 ]-LHRH was the baseline for new designs. Comparison of the AOA's of the 17 analogs with the baseline revealed the two peptides with Phe 5 and 3-Pal 5 had equivalent AOA's, and were the best of the 17, and about 45% more potent than the baseline. Analogs with pClPhe 5 , oClPhe 5 , α-MepClPhe 5 , 2-Nal 5 , Trp 5 , and His 5 were less potent than the Phe 5 -and 3-Pal 5 -analogs. Based on the Phe 5 -analog, eight other analogs were synthesized with changes in positions 1, 2, 3 and 7 and although none were better than the baseline, 5/8 showed 20-60% AOA's at 250 ng and revealed optimum positions for new designs.
Lipophilic Modifications to Dinucleoside Polyphosphates and Nucleotides that Confer Antagonist Properties at the Platelet P2Y<sub>12</sub> Receptor (2008)

Platelet P2Y12 receptors play a central role in the regulation of platelet function and inhibition of this receptor by treatment with drugs such as clopidogrel results in a reduction of atherothrombotic events. We discovered that modification of natural and synthetic dinucleoside polyphosphates and nucleotides with lipophilic substituents on the ribose and base conferred P2Y12 receptor antagonist properties to these molecules producing potent inhibitors of ADP-mediated platelet aggregation. We describe methods for the preparation of these functionalized dinucleoside polyphosphates and nucleotides and report their associated activities. By analysis of these results and by deconstruction of the necessary structural elements through selected syntheses, we prepared a series of highly functionalized nucleotides, resulting in the selection of an adenosine monophosphate derivative (62) for further clinical development.
Structural Aspects for Evolution of β-Lactamases from Penicillin-Binding Proteins (2003)

Penicillin-binding proteins (PBPs), biosynthetic enzymes of bacterial cell wall assembly, and β-lactamases, resistance enzymes to β-lactam antibiotics, are related to each other from an evolutionary point of view. Massova and Mobashery (Antimicrob. Agents Chemother. 1998, 42, 1−17) have proposed that for β-lactamases to have become effective at their function as antibiotic resistance enzymes, they would have had to undergo structure alterations such that they would not interact with the peptidoglycan, which is the substrate for PBPs. A cephalosporin analogue, 7β-[N-Acetyl-l-alanyl-γ-d-glutamyl-l-lysine]-3-acetoxymethyl-3-cephem-carboxylic acid (compound 6), was conceived and synthesized to test this notion. The X-ray structure of the complex of this cephalosporin bound to the active site of the deacylation-deficient Q120L/Y150E variant of the class C AmpC β-lactamase from Escherichia coli was solved at 1.71 Å resolution. This complex revealed that the surface for interaction with the strand of peptidoglycan that acylates the active site, which is present in PBPs, is absent in the β-lactamase active site. Furthermore, insertion of a peptide in the β-lactamase active site at a location where the second strand of peptidoglycan in some PBPs binds has effectively abolished the possibility for such interaction with the β-lactamase. A 2.6 ns dynamics simulation was carried out for the complex, which revealed that the peptidoglycan surrogate (i.e., the active-site-bound ligand) undergoes substantial motion and is not stabilized for binding within the active site. These factors taken together disclose the set of structure modifications in the antibiotic resistance enzyme that prevent it from interacting with the peptidoglycan, en route to achieving catalytic proficiency for their intended function.
Order within order: Studies of semifluorinated block copolymers (1997)

Abstract Several new semifluorinated compounds and polymers modified with these groups were synthesized and investigated. The polymer supports for these mesomorphic groups were styrene‐diene block copolymers in which the semifluorinated groups were attached to a hydroxy‐modified diene block. The characteristics of the smectic phase formed and its effect on the self‐ordering behavior of the block copolymers were examined.
A dynamic resource allocation and media access control proposal for a multi-tier wireless ATM network (2002)

This paper presents a new protocol for controlling access to the shared radio medium in a multi-tier wireless ATM network. A multi-tier wireless ATM network provides seamless connectivity to the users in multiple geographic environments ranging from local area networks to wide area wireless networks. Dynamic resource allocating media access (DRAMA) provides full support for multiple traffic types with different priorities and for multiple connections per user. DRAMA benefits from statistical multiplexing and allows bursts up to the full channel bandwidth for data traffic. A full description of the protocol and simulation results are presented.
Lipid Oxidation Enhances the Function of Activated Protein C (2001)

Although lipid oxidation products are usually associated with tissue injury, it is now recognized that they can also contribute to cell activation and elicit anti-inflammatory lipid mediators. In this study, we report that membrane phospholipid oxidation can modulate the hemostatic balance. Oxidation of natural phospholipids results in an increased ability of the membrane surface to support the function of the natural anticoagulant, activated protein C (APC), without significantly altering the ability to support thrombin generation. Lipid oxidation also potentiated the ability of protein S to enhance APC-mediated factor Va inactivation. Phosphatidylethanolamine, phosphatidylserine, and polyunsaturation of the fatty acids were all required for the oxidation-dependent enhancement of APC function. A subgroup of thrombotic patients with anti-phospholipid antibodies specifically blocked the oxidation-dependent enhancement of APC function. Since leukocytes are recruited and activated at the thrombus or sites of vessel injury, our findings suggest that after the initial thrombus formation, lipid oxidation can remodel the membrane surface resulting in increased anticoagulant function, thereby reducing the thrombogenicity of the thrombus or injured vessel surface. Anti-phospholipid antibodies that block this process would therefore be expected to contribute to thrombus growth and disease.
Medium access control for full-duplex in wireless local area networks (2015)

Current wireless technologies strive to respond to the arising demand for the increase in mobile traffic. Recently, with the introduction of self-interference (SI) cancellation techniques, wireless full-duplex communication has become an attractive solution that doubles the spectral e ciency and enhances data rates. In this thesis, we present a medium access control (MAC) protocol, named Synchronized Contention Window Full-Duplex (S-CW FD) protocol for enabling full duplex communication in wireless local area networks (WLANs). The proposed S-CW FD protocol can not only work in ad hoc and infrastructure modes of IEEE 802.11 WLANs, but with the legacy nodes as well. In this work, saturated throughput of S-CW FD is derived based on a two dimensional Markov chain model, similar to Bianchi's, and those results are used to validate simulations in OPNET tool. Via detailed simulation experiments, the performance of S-CW FD is evaluated under different self-interference models and wireless network conditions. It is shown that when there are no hidden nodes in the network, the S-CW FD protocol can double the throughput of half-duplex IEEE 802.11, and in the presence of hidden nodes in the network, the throughput gain of full duplex over half-duplex can get as high as ten fold, even for moderate SI cancellation levels and heavy load. Comparisons with existing similar FD MAC protocols also indicate that the proposed S-CW FD protocol performs best under realistic network conditions and residual SI. Hence, S-CW FD stands out as a promising FD MAC protocol with a high chance of application in WLANs, not only for signiffcant performance improvements, but also for its exibility and backwards compatibility.
A photonic wide-band analog to digital converter (2002)

We describe how a tunable laser and common photonic components can perform the process of analog-to-digital conversion. The all-optical processing yields conversion rates orders of magnitude faster than the fastest electronic processor.
Homoarginine, kidney function and cardiovascular mortality risk (2014)

Low homoarginine is strongly related to decreased kidney function, adverse cardiovascular events and death due to heart failure. The relationship between low homoarginine and adverse cardiovascular outcomes is most obvious when kidney function is impaired.
Calibrating Water Distribution Model Via Genetic Algorithms (2002)

Computer models have been built for the simulation of water distribution systems since the mid-1960s. However, a model needs to be calibrated before it can be used for analysis and operational study of a real system. Model calibration is a vitally important, but time consuming task. Over last two decades, several approaches using optimization techniques have been proposed for model calibrations. Although most of the methods can make the model agree with field observations, few are able to achieve a good level of calibration in terms of determining the correct model parameters (pipe roughness coefficients, junction demands and valve settings). The previously developed methods appear to be lacking versatility for users to accurately specify calibration task given real data for a real system. This paper proposes a comprehensive and flexible framework for calibrating hydraulic network model. Calibration tasks can be specified for a wat er distribution system according to data availability and model application requirements. It allows a user to (1) flexibly choose any combination of the model parameters such as pipe roughness, junction demand and link (pipes, valves and pumps) operational status, (2) easily aggregate model parameters to reduce the problem dimension for expeditious calculation, and (3) consistently specify boundary conditions and junction demand loadings that are corresponding to field data collection. A model calibration is then defined as an implicit nonlinear optimization problem, which is solved by employing a powerful genetic algorithm (GA), a generic search paradigm based on the principles of natural evolution and biological reproduction. Calibration solutions are obtained by minimizing the discrepancy between the model predicted and the field observed values of junction pressures and pipe flows. With this methodology, a modeler can be fully assisted during a calibration process, thus it is possible to achieve a good model calibration with high level of confidence. As a result, calibrated models can be developed for conducting system analysis and operational management. Example application is presented to demonstrate the efficacy and robustness of the genetic-based methodology for calibrating water distribution model.
Energy-band schemes of highly stable organic electroluminescent devices (1998)

Host-guest systems in organic electroluminescent (EL) devices have been studied. Organic EL cells doped with blue to red guest emitters were prepared and their characteristics and the energy bands of the materials were measured. A green EL cell doped with 2,3-quinacridone showed a maximum efficiency of 18.1 lm/W. A yellow EL cell doped with 5,6,11,12-tetraphenylnaphthacene (rubrene) showed a maximum efficiency of 14.4 lm/W and a half-decay time of 25000 h from 130 cd/m/sup 2/. The energy-band schemes of those cells were analyzed and requirements for the scheme and a guest emitter are discussed.
The 5q31 variants associated with psoriasis and Crohn's disease are distinct (2008)

Predisposition to psoriasis is known to be affected by genetic variation in HLA-C, IL12B and IL23R, but other genetic risk factors also exist. We recently reported three psoriasis-associated single nucleotide polymorphisms (SNPs) in the 5q31 locus, a region of high linkage disequilibrium laden with inflammatory pathway genes. The aim of this study was to assess whether other variants in the 5q31 region are causal to these SNPs or make independent contributions to psoriasis risk by genotyping a comprehensive set of tagging SNPs in a 725 kb region bounded by IL3 and IL4 and testing for disease association. Ninety SNPs, capturing 86.4% of the genetic diversity, were tested in one case-control sample set (467 cases/460 controls) and significant markers (P(allelic) < 0.05) (n = 9) were then tested in two other sample sets (981 cases/925 controls). All nine SNPs were significant in a meta-analysis of the combined sample sets. Pair-wise conditional association tests showed rs1800925, an intergenic SNP located just upstream of IL13 (Mantel-Haenszel P(combined) = 1.5 x 10(-4), OR = 0.77 [0.67-0.88]), could account for observed significant association of all but one other SNP, rs11568506 in SLC22A4 [Mantel-Haenszel P(combined) = 0.043, OR = 0.68 (0.47-0.99)]. Haplotype analysis of these two SNPs showed increased significance for the two common haplotypes (rs11568506-rs1800925: GC, P(combined) = 5.67 x 10(-6), OR = 1.37; GT, P(combined) = 6.01 x 10(-5), OR = 0.75; global haplotype P = 8.93 x 10(-5)). Several 5q31-region SNPs strongly associated with Crohn's disease (CD) in the recent WTCCC study were not significant in the psoriasis sample sets tested here. These results identify the most significant 5q31 risk variants for psoriasis and suggest that distinct 5q31 variants contribute to CD and psoriasis risk.
Master–slave interferometry for parallel spectral domain interferometry sensing and versatile 3D optical coherence tomography (2013)

Conventional spectral domain interferometry (SDI) methods suffer from the need of data linearization. When applied to optical coherence tomography (OCT), conventional SDI methods are limited in their 3D capability, as they cannot deliver direct en-face cuts. Here we introduce a novel SDI method, which eliminates these disadvantages. We denote this method as Master - Slave Interferometry (MSI), because a signal is acquired by a slave interferometer for an optical path difference (OPD) value determined by a master interferometer. The MSI method radically changes the main building block of an SDI sensor and of a spectral domain OCT set-up. The serially provided signal in conventional technology is replaced by multiple signals, a signal for each OPD point in the object investigated. This opens novel avenues in parallel sensing and in parallelization of signal processing in 3D-OCT, with applications in high- resolution medical imaging and microscopy investigation of biosamples. Eliminating the need of linearization leads to lower cost OCT systems and opens potential avenues in increasing the speed of production of en-face OCT images in comparison with conventional SDI.
Garbage-first garbage collection (2004)

Garbage-First is a server-style garbage collector, targeted for multi-processors with large memories, that meets a soft real-time goal with high probability, while achieving high throughput. Whole-heap operations, such as global marking, are performed concurrently with mutation, to prevent interruptions proportional to heap or live-data size. Concurrent marking both provides collection completeness and identifies regions ripe for reclamation via compacting evacuation. This evacuation is performed in parallel on multiprocessors, to increase throughput.
Virtual Network Provisioning Over Distance-Adaptive Flexible-Grid Optical Networks [Invited] (2014)

In software-defined optical networks (SDONs), network services are provided in terms of virtual optical networks (VONs). VON provisioning requires additional considerations regarding their optical characteristics and constraints compared to virtual networks offered in the electrical domain. In this paper, we present a new VON provisioning procedure that is specifically designed for distance-adaptive flexible-grid optical networks. Simulations show up to three times increase in network capacity by leveraging the combined effect of flexible node mapping and distance-adaptive modulation.
Model-based compressive sensing for signal ensembles (2009)

Compressive sensing (CS) is an alternative to Shannon/Nyquist sampling for acquiring sparse or compressible signals. Instead of taking N periodic samples, we measure M ¿ N inner products with random vectors and then recover the signal via a sparsity-seeking optimization or greedy algorithm. A new framework for CS based on unions of subspaces can improve signal recovery by including dependencies between values and locations of the signal's significant coefficients. In this paper, we extend this framework to the acquisition of signal ensembles under a common sparse supports model. The new framework provides recovery algorithms with theoretical performance guarantees. Additionally, the framework scales naturally to large sensor networks: the number of measurements needed for each signal does not increase as the network becomes larger. Furthermore, the complexity of the recovery algorithm is only linear in the size of the network. We provide experimental results using synthetic and real-world signals that confirm these benefits.
ChemInform Abstract: 5,11‐DIMETHYL‐2,9‐BIS(PHENYLACETYL)‐5,11‐DIAZATETRACYCLO(6.2.2.02,7.04,9)DODECANE, A POTENT, NOVEL ANALGESIC (1977)

Abstract Das Dinitril des Diazatetracyclododecans (I) ergibt bei der Umsetzung mit Benzylmagnesiumchlorid (II) das Phenylacetylderivat (III), aus dem über die Urethane (IV) und (V) weitere Derivate hergestellt werden.
The Industrial Potential of Extreme Thermophiles (1988)

New Zealand has extensive thermal regions which, unlike those of other parts of the world, are easily accessible at all seasons of the year. The hot springs of these regions are diverse in mineral composition, acidity and temperature. Only bacteria can live at temperatures higher than 65°C, and those growing optimally at 65°C or higher are called extreme thermophiles. Currently biochemical and physiological studies of extremely thermophilic bacteria are being made by the Thermophile Research Unit at the University of Waikato alongside studies of the ecology of the hot springs from which the bacteria are isolated.KeywordsCorn StoverThermophilic BacteriumMesophilic BacteriumGlucose IsomeraseHigh Fructose Corn SyrupThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
Transition metal catalyzed alternating copolymerizations of olefins and co (1995)

Abstract Well defined Pd(II) catalysts of the type (N′N)Pd(CH 3 )(Solv.) + B(Ar f ) 4 ‐ (Ar f = −3, 5‐(CF 3 ) 2 C 6 H 3 ) have been prepared for living alternating copolymerizations of olefins with CO. This talk will focus on the mechanistic details of chain growth as elucidated by 1 H and 13 C NMR spectroscopy, model studies of key migratory insertion steps and synthesis and properties of various copolymers and block copolymers based on styrenes, CH 2 =CHC 6 H 4 X [X = p ‐C(CH 3 ) 3 , p ‐OC(O)CH 3 , p ‐OC(O)C‐t‐Bu), p ‐NHC(O)(C‐t‐Bu)]. Use of the catalysts based on the C 2 symmetric, homochiral ligand 2, 2'‐bis[2‐[4(S)‐(Alkyl)‐1, 3‐oxazolinyl]]propane [Alkyl = CH 3 , CH(CH 3 ) 2 ] produces a copolymer, 1, with a highly isotactic microstructure and high optical activity in contrast to achiral ligands such as 1,10‐phenanthroline which produce copolymers with predominantly syndiotactic microstructure.
An imaging system for quantitive surface temperature mapping using two-color thermographic phosphors (1988)

A technique for obtaining detailed quantitative temperature distributions on test models in hypersonic wind tunnels is presented. This technique is based on the ratio of blue to green (450, 520 nm) emission from an UV (365 nm) excited phosphor coating. Separately filtered images are recorded from a three-tube color camera, utilizing off-the-shelf front-end video optics to discriminate wavelengths. Two demonstration studies in a 31-inch Mach 10 tunnel are discussed. One study presents the windward surface temperature-time history for a transatmospheric vehicle, and the other illustrates nosetip heating on a spherically blunted slender cone.
Strategies for preventing porcine xenograft rejection: recent progress and future developments (1997)

Interest in xenotransplantation (the use of animal organs for transplantation) has been revived because of the severe shortage of human donor organs, and pigs are currently thought to be the species most suitable for widespread use. Recent insights into the mechanisms underlying vascular rejection, endothelial cell activation and cellular responses to xenogeneic tissue have led to the development of novel methods designed to inhibit immune-mediated xenograft rejection. The first clinical trials of porcine organs are expected within the next few years, once outstanding questions about the safety of transplanted pig tissues have been addressed. They will herald a new era in medical practice, characterised by the practical application of modern molecular and genetic techniques to solve clinical problems. In the future, it is hoped that these same techniques may resolve some of the problems currently associated with long-term systemic immunosuppression and serve to inhibit the progress of chronic rejection, the process that currently limits the lifespan of transplanted allografts. This article reviews the pathophysiology of xenograft rejection and highlights the novel strategies to prevent hyperacute xenograft rejection that are likely to be useful in clinical practice. Other strategies designed to inhibit later stages of xenograft rejection are also presented, with emphasis on the need for graft-specific or ‘tailored’ immunosuppression. Areas where future development is likely are also discussed.