gebhart/patrepeval huggingface dataset:
THREE-COMPONENT PHOTORESISTS CONTAINING VINYL ETHER CROSSLINKING AGENTS (2001)

Thermal crosslinking reactivity and lithographic performance were investigated for three-component photoresists composed of a Brønsted acid-based binder polymer, a vinyl ether monomer as a crosslinking agent, and a photoacid generator. Poly(p-hydroxystyrene) (PHS) and poly(styrene-co-acrylic acid) (PST/PAA) were used as the binder polymers. The resists acted as highly sensitive, chemically amplified resists based on thermal crosslinking between a binder resin and a vinyl ether monomer and subsequent acidolytic cleavage of the crosslinks. The rate constants and activation energies for the thermal crosslinking reactions were determined, and the resists based on PST/PAA showed higher thermal crosslinking reactivity than PHS resists. The resists in this study exhibited high photosensitivity and afforded positive-tone images by alkaline development.
Ocular drug delivery (2006)

Drug delivery to the eye is hampered by anatomical factors, including the corneal epithelium, the blood-aqueous barrier and the blood-retinal barrier. This review aims to outline the major routes of ocular drug delivery, including systemic, topical, periocular and intravitreal. The pharmacokinetics, the disadvantages and the clinical relevance of these drug delivery routes have been emphasised. Recent advances in surgical techniques, therapeutic approaches and material sciences have produced exciting new therapies for ocular diseases. The role of ophthalmic drug formulation in targeting the desired ocular tissue and enhancing drug delivery by the chosen route whilst minimising side effects is also discussed.
Bisquinolines. 2. Antimalarial N,N-Bis(7-chloroquinolin-4-yl)heteroalkanediamines (1998)

N,N-Bis(7-chloroquinolin-4-yl)heteroalkanediamines 1-11 were synthesized and screened against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. These bisquinolines had IC50 values from 1 to 100 nM against P. falciparum in vitro. Six of the 11 bisquinolines were significantly more potent against the chloroquine-resistant W2 clone compared to the chloroquine-sensitive D6 clone. For bisquinolines 1-11 there was no relationship between the length of the bisquinoline heteroalkane bridge and antimalarial activity and no correlation between in vitro and in vivo antimalarial activities. Bisquinolines with alkyl ether and piperazine bridges were substantially more effective than bisquinolines with alkylamine bridges against P. berghei in vivo. Bisquinolines 1-10 were potent inhibitors of hematin polymerization with IC50 values falling in the narrow range of 5-20 microM, and there was a correlation between potency of inhibition of hematin polymerization and inhibition of parasite growth. Compared to alkane-bridged bisquinolines (Vennerstrom et al., 1992), none of these heteroalkane-bridged bisquinolines had sufficient antimalarial activity to warrant further investigation of the series.
Effects of brain natriuretic peptide on hemodynamics and renal function in dogs. (1990)

A new natriuretic peptide has been found in the porcine brain and termed brain natriuretic peptide (BNP). To examine the effects of BNP on the cardiovascular system and kidney as compared with alpha-hANP (ANP), BNP, and ANP (33, 167, 667 pmol/kg) were intravenously administered to anesthetized dogs. BNP dose-dependently decreased arterial pressure and left atrial pressure and dose-dependently increased heart rate, cardiac output, renal blood flow, urine volume, and sodium excretion. These effects were not significantly different from the effects of respective doses of ANP. To eliminate the possibility that these results were confounded by opposing actions of the baroreflex system, we performed additional experiments following sinoaortic denervation and vagotomy. These results also demonstrated no differences between the effects of BNP and ANP on the measured variables. Finally, we determined that the pharmacokinetics of exogenously injected BNP and ANP are indistinguishable. These findings lead to the possibility that BNP physiologically works in the body in the same manner as ANP.
Adaptive mobile access to context-aware services (2003)

With the advances of wireless communication, mobile computing will become ubiquitous. This will lend to adaptive computing, where electronic services support the user anytime, anywhere and in every form. Adaptive services must take the user requirements, the current geolocation, the situation he or she is facing, the available network connection and the associated usage costs into account. This very much relies on flexible and adaptive system mechanisms in the network. This paper presents the results of the ACTS AMASE (Agent-based Mobile Application Support Environment) project which has adapted a mobile agent system for the use in wireless networks to support mobile users. We concentrate on issues related to making mobile agent-based services aware to the context of the user. We examine (a) a mechanism that allows agents to adapt their behavior to the current situation in the wireless network, and (b) a system mechanism that automatically adapts agent execution to the given context. Finally, we present an overview of the current Europe-wide AMASE testbed and the realized application.
Poor Binding of a HER-2/neu Epitope (GP2) to HLA-A2.1 Is due to a Lack of Interactions with the Center of the Peptide (1999)

Class I major histocompatibility complex (MHC) molecules bind short peptides derived from proteins synthesized within the cell. These complexes of peptide and class I MHC (pMHC) are transported from the endoplasmic reticulum to the cell surface. If a clonotypic T cell receptor expressed on a circulating T cell binds to the pMHC complex, the cell presenting the pMHC is killed. In this manner, some tumor cells expressing aberrant proteins are recognized and removed by the immune system. However, not all tumors are recognized efficiently. One reason hypothesized for poor T cell recognition of tumor-associated peptides is poor binding of those peptides to class I MHC molecules. Many peptides, derived from the proto-oncogene HER-2/neu have been shown to be recognized by cytotoxic T cells derived from HLA-A2(+) patients with breast cancer and other adenocarcinomas. Seven of these peptides were found to bind with intermediate to poor affinity. In particular, GP2 (HER-2/neu residues 654-662) binds very poorly even though it is predicted to bind well based upon the presence of the correct HLA-A2.1 peptide-binding motif. Altering the anchor residues to those most favored by HLA-A2.1 did not significantly improve binding affinity. The crystallographic structure shows that unlike other class I-peptide structures, the center of the peptide does not assume one specific conformation and does not make stabilizing contacts with the peptide-binding cleft.
Slack-based heuristics for constraint satisfaction scheduling (1993)

Abstract: In this paper, we define and empirically evaluate new heuristics for solving the job shop scheduling i problem with non-relaxable time windows. The hypothesis underlying our approach is that by ap-j proaching the problem as one of establishing se-,:, quencing constraints between pairs of operations; requiring the same resource (as opposed to a proh-: lem of assigning start times t o each operation) and by exploiting previously developed analysis techniques for limiting search through the space i of possible sequencing decisions, simple, localized look-ahead techniques can yield problem solving performance comparable to currently dominating techniques that rely on more sophisticated anal-ysis of resource contention. We define a series of attention focusing heuristics based on simple anal-ysis of the temporal flexibility associated with dif-ferent sequencing decisions, and a similarly moti-vated heuristic for determining how to sequence a given operation pair. Performance results are reported on a suite of benchmark problems pre-: viously investigated by two advanced approaches, and our simplified look-ahead analysis techniques are shown to provide comparable problem solving leverage a t reduced computational cost.
The mouth‐feel properties of grape and apple proanthocyanidins in a wine‐like medium (2003)

Abstract A range of structurally defined apple and grape proanthocyanidins was isolated in sufficient amount to carry out a formal sensory descriptive analysis study. Purified proanthocyanidin fractions differed in chain length, degree of galloylation and epigallocatechin content. Astringency attributes of the preparations in a model wine medium were rated while the fractions were held in the mouth and after expectoration. The degree of polymerization appeared to be the variable that discriminated among the fractions to the greatest extent. It affected both the overall astringency and the different individual astringency attributes, with increased ‘drying’, ‘chalky’, ‘adhesive’ and ‘pucker’ characters correlating with increasing chain length. A rougher sensation with increased ‘coarseness’, ‘drying’ and ‘chalkiness’ correlated with an increased degree of galloylation of the fractions. The presence of epigallocatechin units in the proanthocyanidin tended to lower the ‘coarse’ perception. Copyright © 2003 Society of Chemical Industry
CRC Standard Probability and Statistics Tables and Formulae, Student Edition (2000)

Users of statistics in their professional lives along with statistics students will welcome the CRC Standard Probability and Statistics Tables and Formulae, a concise, easy-to-use reference for basic statistics and probability. It contains all of the standardized statistical tables and formulae typically needed plus material on basic statistics topics, such as probability theory and distributions, regression, analysis of variance, nonparametric statistics, and statistical quality control. With this handy reference, readers can shift their focus from rote learning and memorization to the concepts they need to use statistics efficiently and effectively.
Modulation of A1 and A2B adenosine receptor activity: a new strategy to sensitise glioblastoma stem cells to chemotherapy (2014)

Therapies that target the signal transduction and biological characteristics of cancer stem cells (CSCs) are innovative strategies that are used in combination with conventional chemotherapy and radiotherapy to effectively reduce the recurrence and significantly improve the treatment of glioblastoma multiforme (GBM). The two main strategies that are currently being exploited to eradicate CSCs are (a) chemotherapeutic regimens that specifically drive CSCs toward cell death and (b) those that promote the differentiation of CSCs, thereby depleting the tumour reservoir. Extracellular purines, particularly adenosine triphosphate, have been implicated in the regulation of CSC formation, but currently, no data on the role of adenosine and its receptors in the biological processes of CSCs are available. In this study, we investigated the role of adenosine receptor (AR) subtypes in the survival and differentiation of CSCs isolated from human GBM cells. Stimulation of A1AR and A2BAR had a prominent anti-proliferative/pro-apoptotic effect on the CSCs. Notably, an A1AR agonist also promoted the differentiation of CSCs toward a glial phenotype. The differential effects of the two AR agonists on the survival and/or differentiation of CSCs may be ascribed to their distinct regulation of the kinetics of ERK/AKT phosphorylation and the expression of hypoxia-inducible factors. Most importantly, the AR agonists sensitised CSCs to the genotoxic activity of temozolomide (TMZ) and prolonged its effects, most likely through different mechanisms, are as follows: (i) by A2BAR potentiating the pro-apoptotic effects of TMZ and (ii) by A1AR driving cells toward a differentiated phenotype that is more sensitive to TMZ. Taken together, the results of this study suggested that the purinergic system is a novel target for a stem cell-oriented therapy that could reduce the recurrence of GBM and improve the survival rate of GBM patients.
Suppression of tuberculoimmunity in mice by Evans blue dye (1982)

Evans blue dye, which acts as an adjuvant in mice to promote induction of cell-mediated immunity, was found earlier to apparently act contrarily and decrease tuberculoimmunity. This phenomenon was investigated here in a long-term experiment examining the persistence of the suppressed immunity. Systemic suppression after injection of only 1 mg of dye was confirmed and was found to last for more than 2 weeks but less than 11 weeks. Localized evidence for dye-caused depression of tuberculoimmunity also was seen by the development in dye-injected mice immunized with emulsified whole bacilli of caseating tubercles at sites of pulmonary infection, a very rare type of pathology for tuberculosis in mice. The experiment, in addition, detected an aging-related decline in mice of resistance to tuberculosis evident by shortened survival, enlarged pulmonary tubercles, and increased susceptibility to systemic tuberculin reaction.
Number of CpG islands and genes in human and mouse. (1993)

Estimation of gene number in mammals is difficult due to the high proportion of noncoding DNA within the nucleus. In this study, we provide a direct measurement of the number of genes in human and mouse. We have taken advantage of the fact that many mammalian genes are associated with CpG islands whose distinctive properties allow their physical separation from bulk DNA. Our results suggest that there are approximately 45,000 CpG islands per haploid genome in humans and 37,000 in the mouse. Sequence comparison confirms that about 20% of the human CpG islands are absent from the homologous mouse genes. Analysis of a selection of genes suggests that both human and mouse are losing CpG islands over evolutionary time due to de novo methylation in the germ line followed by CpG loss through mutation. This process appears to be more rapid in rodents. Combining the number of CpG islands with the proportion of island-associated genes, we estimate that the total number of genes per haploid genome is approximately 80,000 in both organisms.
STRUCTURAL BASIS OF LECTIN-CARBOHYDRATE RECOGNITION (1996)

Lectins are responsible for cell surface sugar recognition in bacteria, animals, and plants. Examples include bacterial toxins; animal receptors that mediate cell-cell interactions, uptake of glycoconjugates, and pathogen neutralization; and plant toxins and mitogens. The structural basis for selective sugar recognition by members of all of these groups has been investigated by x-ray crystallography. Mechanisms for sugar recognition have evolved independently in diverse protein structural frameworks, but share some key features. Relatively low affinity binding sites for monosaccharides are formed at shallow indentations on protein surfaces. Selectivity is achieved through a combination of hydrogen bonding to the sugar hydroxyl groups with van der Waals packing, often including packing of a hydrophobic sugar face against aromatic amino acid side chains. Higher selectivity of binding is achieved by extending binding sites through additional direct and water-mediated contacts between oligosaccharides and the protein surface. Dramatically increased affinity for oligosaccharides results from clustering of simple binding sites in oligomers of the lectin polypeptides. The geometry of such oligomers helps to establish the ability of the lectins to distinguish surface arrays of polysaccharides in some instances and to crosslink glycoconjugates in others.
The Concise Guide toPHARMACOLOGY2013/14: Enzymes (2013)

The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of the key properties of over 2000 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. The full contents can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.12444/full. Enzymes are one of the seven major pharmacological targets into which the Guide is divided, with the others being G protein-coupled receptors, ligand-gated ion channels, ion channels, nuclear hormone receptors, catalytic receptors and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. A new landscape format has easy to use tables comparing related targets. It is a condensed version of material contemporary to late 2013, which is presented in greater detail and constantly updated on the website www.guidetopharmacology.org, superseding data presented in previous Guides to Receptors and Channels. It is produced in conjunction with NC-IUPHAR and provides the official IUPHAR classification and nomenclature for human drug targets, where appropriate. It consolidates information previously curated and displayed separately in IUPHAR-DB and the Guide to Receptors and Channels, providing a permanent, citable, point-in-time record that will survive database updates.
Opposing Regulatory Roles of Complement Factor 5 in the Development of Bleomycin-Induced Pulmonary Fibrosis (2005)

The mechanisms of idiopathic pulmonary fibrosis pathogenesis, a chronic and progressive interstitial lung disease, remain elusive. The complement system, a crucial arm of the innate immune response, plays a pivotal role in several pathological disorders; however, the contribution of individual complement components to lung fibrosis has not yet been examined. Complement factor 5 (C5) and its cleavage product C5a are critical mediators in inflammatory diseases. Thus, to evaluate the role of C5 in lung fibrosis, we compared congenic C5-sufficient and C5-deficient mice in a well-characterized murine model of bleomycin-induced pulmonary fibrosis. C5-deficient mice had an exaggerated inflammatory phenotype compared with C5-sufficient mice during acute bleomycin-induced lung injury. These findings suggest a protective and anti-inflammatory role for C5, which was linked to the regulation of matrix metalloproteinases involved in cell migration. In contrast, C5 had a detrimental effect during chronic stages of bleomycin-induced injury, indicating a profibrotic role for C5. This deleterious activity for C5 was associated with expression of the fibrogenic cytokine TGF-beta1 and matrix metalloproteinase-3, an important mediator in fibroblast contraction. Altogether, our data reveal novel and opposing roles for C5 in both inflammation and tissue repair. Furthermore, these findings provide insight into the development of new therapeutic strategies for idiopathic pulmonary fibrosis patients.
Interferon-gamma regulates an antigen specific for endothelial cells involved in lymphocyte traffic. (1986)

One of the most striking examples of localized vascular differentiation is exhibited by specialized lymphoid organ venules that mediate the extravasation of circulating lymphocytes from the blood. These vessels are characterized by cuboidal or "high" endothelial cell morphology and are unique in their functional capacity to interact with migrating lymphocytes, regulating both the rate and specificity of lymphocyte traffic through particular regions of the body. We describe here a monoclonal antibody, MECA-325, that defines an endothelial cell differentiation antigen selectively expressed on high endothelium in the mouse. Thus an antigen defining a specific functional subset of endothelial cells has been found. Furthermore, we demonstrate that the MECA-325 antigen can be induced in mouse lung or bone marrow-derived endothelial cell lines in vitro by interferon-gamma but not by interferon-beta, interleukin-1, or endothelial cell mitogens. The results define a unique marker associated with differentiated endothelial cells mediating lymphocyte traffic from the blood, and they provide evidence that the specialized phenotype of these high endothelial cells may be induced and controlled by local factors associated with immune activity.
Characterization of the copper-thiolate cluster in yeast metallothionein and two truncated mutants. (1988)

Cu-metallothionein was purified from Saccharomyces cerevisiae harboring plasmids containing mutated CUP1 metallothionein genes resulting in deletions at the carboxy-terminal end of the polypeptide. The truncated polypeptides are recovered as polypeptides of 35 and 48 residues in length. The Cu-S cluster in the wild-type metallothionein and the two truncates were characterized. The truncated proteins, designated T35 and T48, contain 4 and 2 fewer cysteinyl residues, respectively, compared to the 12 cysteines in wild-type metallothionein; yet the mutant molecules bind Cu(I) ions in a stoichiometry comparable to the wild-type protein, i.e. 7-8 mol eq. The Cu(I) ions bound to T48 are as tenaciously bound as those bound to the wild-type molecule. The electronic transitions in the ultraviolet are similar for Cu-T48 and the wild-type protein. Both mutants and wild-type Cu-protein exhibit luminescence. The corrected emission maxima occurs at 609 nm with a corrected excitation peak near 277 nm. The luminescence quantum yield and lifetime of fluorescence decay of Cu-T48 and wild-type Cu-metallothionein are similar. The absolute quantum yield of the wild-type Cu-protein luminescence is 0.0058 and has a 440-ns lifetime. The similar fluorescence rate constant in the two molecules suggests they possess a similar chromophore. The Cu-T35 protein is more labile than Cu-T48 or the wild-type protein in the association of Cu(I) ions and the air sensitivity of the electronic transitions and luminescence. Although T48 lacks 2 of the 12 cysteines in the wild-type protein, we are unable to detect any differences in the properties of the native metal clusters in the two molecules; T35 lacking 4 cysteinyl residues forms a Cu(I) cluster with properties significantly different from the wild-type molecule. Properties of the Cu-thiolate cluster were also studied in Cu(I)-reconstituted samples. The cluster in wild-type metallothionein forms in all-or-nothing fashion. This conclusion is based on copper binding stoichiometry and luminescence studies. The relative quantum yield of samples with intermediate Cu(I) levels was constant, consistent with all-or-none cluster formation.
A MEMS nanoplotter with high-density parallel dip-pen nanolithography probe arrays (2002)

We report on the development of a nanoplotter that consists of an array of microfabricated probes for parallel dip-pen nanolithography. Two types of device have been developed by using microelectromechanical systems micromachining technology. The first consists of 32 silicon nitride cantilevers separated by 100 µm, while the second consists of eight boron-doped silicon tips separated by 310 µm. The former offers writing and imaging capabilities, but is challenged with respect to tip sharpness. The latter offers smaller linewidths and increased imaging capabilities at the expense of probe density. Parallel generation of nanoscopic monolayer patterns with a minimum linewidth of 60 nm has been demonstrated using an eight-pen microfabricated probe array.
Ketogenic Diet for the Treatment of Refractory Epilepsy in Children: A Systematic Review of Efficacy (2000)

Although controlled trials are lacking, the evidence is sufficient to determine that the ketogenic diet is efficacious in reducing seizure frequency in children with refractory epilepsy.