gebhart/patrepeval huggingface dataset:
Pyrazolodiazepines. III. 4-Aryl-1,6,7,8-tetrahydro-1,3-dialkylpyrazolo[3,4-e][1,4]diazepines as antidepressant agents (1981)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPyrazolodiazepines. III. 4-Aryl-1,6,7,8-tetrahydro-1,3-dialkylpyrazolo[3,4-e][1,4]diazepines as antidepressant agentsH. A. DeWald, S. Lobbestael, and B. P. H. PoschelCite this: J. Med. Chem. 1981, 24, 8, 982–987Publication Date (Print):August 1, 1981Publication History Published online1 May 2002Published inissue 1 August 1981https://pubs.acs.org/doi/10.1021/jm00140a013https://doi.org/10.1021/jm00140a013research-articleACS PublicationsRequest reuse permissionsArticle Views465Altmetric-Citations62LEARN 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
Increased level of phosphorylated akt measured by chemiluminescence-linked immunosorbent assay is a predictor of poor prognosis in primary breast cancer overexpressing ErbB-2 (2005)

Our findings demonstrate that, in breast cancer patients, Akt activation is associated with tumour proliferation and poor prognosis, particularly in the subset of patients with ErbB2-overexpressing tumours.
The structural behaviour of the nepheline family: (1) Sr and Ba aluminates (<i>M</i>Al<sub>2</sub>O<sub>4</sub>) (1982)

Abstract The structural relations of solid solutions in the series (Sr 1−x Ba x )Al 2 O 4 were studied using room- and high-temperature X-ray methods, infra-red spectroscopy, and DTA. At room temperature, SrAl 2 O 4 and solid solutions with x up to 0.31 are monoclinic, between x = 0.31 and 0.43 monoclinic and hexagonal forms coexist, and between x = 0.43 and 1.0 only hexagonal forms occur. On heating, a member of the monoclinic series of solid solutions transforms to hexagonal symmetry over a range of temperature within which both monoclinic and hexagonal forms coexist. The proportion of the hexagonal form increases instantaneously as the temperature is raised. The transformation temperature decreases with increasing BaAl 2 O 4 in solid solution and, in addition, the temperature width of the region of coexistence is markedly enlarged. SrAl 2 O 4 transforms over the range 665–705 °C and (Sr 0.7 Ba 0.3 )Al 2 O 4 over 170–405 °C. The DTA trace for SrAl 2 O 4 shows a peak at 677 °C. On cooling, the transformations show hysteresis of 15 to 25 °C. The coexisting monoclinic and hexagonal forms are believed to be isochemical, and discontinuities in cell parameters occur within the region of coexistence both in the compositional series at room temperature and in the elevated temperature transformation experiments. The low-to-high transformation is accompanied by a volume change of −0.2 to −0.3 %, and is believed to be first-order displacive with additional characteristics similar to those of martensitic transformations. The thermal expansion behaviour of structures in the (Sr,Ba)Al 2 O 4 , series indicates that two tilt systems are operative: co-operative rotation of tetrahedra about the c -axis, and tilting of tetrahedra relative to the 0001 plane. The results for the (Sr,Ba)Al 2 O 4 series are shown to be invaluable in reinterpreting the structural behaviour of members of the nepheline and leucite groups of minerals.
Effect of calcitriol on growth, differentiation, chemokine mRNA expression of cultured keratinocytes and on keratinocyte-T cell binding. (1994)

Calcitriol has recently been shown to be effective against psoriasis. However, its mode of action is not exactly known. The present study focused on the influence of calcitriol on growth, differentiation, chemokine mRNA and ICAM-1 mRNA expression of keratinocytes (KC) and on the binding of T-cells to keratinocytes. In vitro studies showed that calcitriol has a strong anti-proliferative effect and induces terminal differentiation. gamma-IP-10 and ICAM-1 mRNA were induced by gamma-IFN, an induction not influenced by calcitriol. Moreover, the functional expression of ICAM-1 on the KC cell surface as measured by a cell adhesion assay, was not influenced either. IL-8 and huGRO mRNAs were constitutively produced in KC, as was demonstrated after incubation with cycloheximide. Up-regulation of both IL-8 and huGRO mRNA by IL-1 alpha was also not affected by calcitriol. It is concluded that calcitriol has a strong antiproliferative activity and does not interfere with KC responsiveness to gamma-IFN and IL-alpha induced chemokine expression or with the adhesion of T-cells to keratinocytes.
Surface Glycolipid and Glycoprotein Antigens (1980)

Considerable evidence indicates that changes in cell surface components occur during transformation of a normal cell into a malignant cell and that these changes determine some of the important properties of cancer cells. These properties include loss of contact inhibition, decrease in cell adhesion, increased growth, prolonged survival, expression of new antigens, and escape from immune destruction by the host. Cell surface carbohydrates are believed to be invovled in determining many of these properties. The carbohydrates of the cell surface have the potential to offer a multitude of individual specificities reflected in the cell surface antigens. This potential may be recognized by virtue of different monosaccharide content, linkages, sequence, and anomeric configurations seen in oligosaccharides of glycosphingolipids (GSL) and glycoproteins (GP). Carbohydrates are distributed among three classes of biochemical substances seen in the membranes, namely, GSL, GP, and mucopolysaccharides. Of these biochemical substances, GSLs and GPs are recognized as integral components of cell surface membranes (Leninger, 1968; Singer and Nicolson, 1972).
Drug-Eluting Fibers for HIV-1 Inhibition and Contraception (2012)

Multipurpose prevention technologies (MPTs) that simultaneously prevent sexually transmitted infections (STIs) and unintended pregnancy are a global health priority. Combining chemical and physical barriers offers the greatest potential to design effective MPTs, but integrating both functional modalities into a single device has been challenging. Here we show that drug-eluting fiber meshes designed for topical drug delivery can function as a combination chemical and physical barrier MPT. Using FDA-approved polymers, we fabricated nanofiber meshes with tunable fiber size and controlled degradation kinetics that facilitate simultaneous release of multiple agents against HIV-1, HSV-2, and sperm. We observed that drug-loaded meshes inhibited HIV-1 infection in vitro and physically obstructed sperm penetration. Furthermore, we report on a previously unknown activity of glycerol monolaurate (GML) to potently inhibit sperm motility and viability. The application of drug-eluting nanofibers for HIV-1 prevention and sperm inhibition may serve as an innovative platform technology for drug delivery to the lower female reproductive tract.
Contributions of individual mechanisms to fluoroquinolone resistance in 36 Escherichia coli strains isolated from humans and animals (1996)

Twenty-eight human isolates of Escherichia coli from Argentina and Spain and eight veterinary isolates received from the Ministry of Agriculture Fisheries and Foods in the United Kingdom required 2 to > 128 micrograms of ciprofloxacin per ml for inhibition. Fragments of gyrA and parC encompassing the quinolone resistance-determining region were amplified by PCR, and the DNA sequences of the fragments were determined. All isolates contained a mutation in gyrA of a serine at position 83 (Ser83) to an Leu, and 26 isolates also contained a mutation of Asp87 to one of four amino acids: Asn (n = 14), Tyr (n = 6), Gly (n = 5), or His (n = 1). Twenty-four isolates contained a single mutation in parC, either a Ser80 to Ile (n = 17) or Arg (n = 2) or a Glu84 to Lys (n = 3). The role of a mutation in gyrB was investigated by introducing wild-type gyrB (pBP548) into all isolates; for three transformants MICs of ciprofloxacin were reduced; however, sequencing of PCR-derived fragments containing the gyrB quinolone resistance-determining region revealed no changes. The analogous region of parE was analyzed in 34 of 36 isolates by single-strand conformational polymorphism analysis and sequencing; however, no amino acid substitutions were discovered. The outer membrane protein and lipopolysaccharide profiles of all isolates were compared with those of reference strains, and the concentration of ciprofloxacin accumulated (with or without 100 microM carbony cyanide m-chlorophenylhydrazone [CCCP] was determined. Twenty-two isolates accumulated significantly lower concentrations of ciprofloxacin than the wild-type E. coli isolate; nine isolates accumulated less then half the concentration. The addition of CCCP increased the concentration of ciprofloxacin accumulated, and in all but one isolate the percent increase was greater than that in the control strains. The data indicate that high-level fluoroquinolone resistance in E. coli involves the acquisition of mutations at multiple loci.
Cocaine Drives Aversive Conditioning via Delayed Activation of Dopamine-Responsive Habenular and Midbrain Pathways (2013)

Many strong rewards, including abused drugs, also produce aversive effects that are poorly understood. For example, cocaine can produce aversive conditioning after its rewarding effects have dissipated, consistent with opponent process theory, but the neural mechanisms involved are not well known. Using electrophysiological recordings in awake rats, we found that some neurons in the lateral habenula (LHb), where activation produces aversive conditioning, exhibited biphasic responses to single doses of intravenous cocaine, with an initial inhibition followed by delayed excitation paralleling cocaine's shift from rewarding to aversive. Recordings in LHb slice preparations revealed similar cocaine-induced biphasic responses and further demonstrated that biphasic responses were mimicked by dopamine, that the inhibitory phase depended on dopamine D2-like receptors, and that the delayed excitation persisted after drug washout for prolonged durations consistent with findings in vivo. c-Fos experiments further showed that cocaine-activated LHb neurons preferentially projected to and activated neurons in the rostromedial tegmental nucleus (RMTg), a recently identified target of LHb axons that is activated by negative motivational stimuli and inhibits dopamine neurons. Finally, pharmacological excitation of the RMTg produced conditioned place aversion, whereas cocaine-induced avoidance behaviors in a runway operant paradigm were abolished by lesions of LHb efferents, lesions of the RMTg, or by optogenetic inactivation of the RMTg selectively during the period when LHb neurons are activated by cocaine. Together, these results indicate that LHb/RMTg pathways contribute critically to cocaine-induced avoidance behaviors, while also participating in reciprocally inhibitory interactions with dopamine neurons.
Integrin‐mediated adhesion of human articular chondrocytes to cartilage (2003)

Under the culture and seeding conditions studied, beta1, alpha 5 beta 1, and alpha v beta 5 integrins mediate human chondrocyte adhesion to cartilage. These chondrocyte integrins have a potential role in the initial adhesion and retention of chondrocytes at a cartilage defect site following clinical procedures of chondrocyte transplantation.
ADMINISTRATION OF RURAL ADJUSTMENT ASSISTANCE IN N.S.W. (1977)

A widening range of rural adjustment assistance measures is being utilised, thereby increasing the range of government organisations involved. In choosing between these measures additional government and non-government research is required, with proposed policies accounting for the division of responsibility for assistance that exists between government organisations. There is also a need for greater policy co-ordination between these organisations, and a proposal for the establishment of a N.S.W. Rural Adjustment Advisory Council is outlined.
Improvement of Apatite-Forming Ability of Titanium Metal Enriched with Calcium Ion on its Surface (2008)

It has been shown that titanium metal subjected to NaOH and heat treatments spontaneously forms a bonelike apatite on its surface in the living body and bonds to living bone. However, its apatite-forming ability was liable to decrease when the treated titanium metal was stored in humid environment. In the present study, the NaOH-treated titanium metal was soaked in a CaCl2 solution at 40°C for 24h, heat-treated at 600°C for 1h, and then soaked in ultrapure water at 80°C for 24h. Calcium titanate was formed on the surface of the titanium metal 1µm in thickness by these treatments. The resultant titanium metal showed high scratch resistance and high apatite-forming ability in a simulated body fluid. This high apatite-forming ability was maintained even after the titanium metal was kept in 95% relative humidity at 80°C for 1 week.
SpaceJMP (2016)

Memory-centric computing demands careful organization of the virtual address space, but traditional methods for doing so are inflexible and inefficient. If an application wishes to address larger physical memory than virtual address bits allow, if it wishes to maintain pointer-based data structures beyond process lifetimes, or if it wishes to share large amounts of memory across simultaneously executing processes, legacy interfaces for managing the address space are cumbersome and often incur excessive overheads. We propose a new operating system design that promotes virtual address spaces to first-class citizens, enabling process threads to attach to, detach from, and switch between multiple virtual address spaces. Our work enables data-centric applications to utilize vast physical memory beyond the virtual range, represent persistent pointer-rich data structures without special pointer representations, and share large amounts of memory between processes efficiently.
Supertoughened Polylactide Binary Blend with High Heat Deflection Temperature Achieved by Thermal Annealing above the Glass Transition Temperature (2017)

Through thermal annealing above the glass transition temperature, a supertoughened binary blend with the highest notched Izod impact strength of 98 KJ/m2 was achieved, which was about 52 times of that of neat polylactide (PLA; 1.9 KJ/m2). The binary blend was composed of biocompatible and biodegradable PLA and ethylene–acrylic ester–glycidyl methacrylate terpolymer (EGMA) elastomer at the composition of 80/20 PLA/EGMA. For one toughened binary blend with the notched Izod impact strength of 94 KJ/m2, its tensile elongation at break was kept above 120%. Moreover, this supertoughened binary blend also displayed a much higher heat deflection temperature for application. Thermal annealing induced crystallization of the PLA matrix in the blend, and a linear correlation between the notched Izod impact strength and crystallinity was revealed. The possible toughening mechanism for the PLA/EGMA 80/20 blend with thermal annealing was analyzed from the viewpoint of negative pressure effects, as imposed on EGMA elastomeric particles during the quench process and thermal annealing thereafter. Decreases of the glass transition temperatures for the EGMA elastomeric particles in the blend were observed for both the quench and thermal annealing processes, which originated from asymmetric thermal shrinkages between the EGMA elastomeric phase and PLA matrix phase.
Grafting Efficiency of Lignin-Grafted-Polyacrylic Acid (2015)

Agriculture biomasses have been successfully converted into value-added products such as biocomposite plastics, furniture, papers and textiles. However, only the cellulose parts of these lignocellulosic materials are being used while other components such as lignin and wax are discarded. For a tropical country like Malaysia, banana stem is one of the sources of biomasses. Like other biomasses-based products, only cellulose part of banana stem is used while the lignin portion is discarded due to overly hydrophilic character. This water-loving property of lignin can be manipulated into specific application such as water absorbent for waste treatment. This research is aimed to synthesis water absorbent-based lignin from banana stem. The lignin had been extracted from banana stem using Kraft process prior to grafted with acrylic acid monomer (AA) in order to increase its water absorbency. The reaction was carried out via free radical polymerization in the presence of hydrogen peroxide (H 2 O 2 ) as initiator and ammonium iron (II) sulfate hexahydrate as catalyst. The reaction temperature was set at 60°C. Grafting efficiency of polyacrylic acid (PAA) onto lignin backbone was determined by varying the amounts of AA monomer, lignin and initiator. The highest grafting percentage was acquired at 60% with the amount of 6ml acrylic acid, 2ml initiator and 0.2g lignin respectively.
Blind OFDM channel estimation through linear precoding: a subspace approach (2003)

A blind channel estimation method for OFDM systems is proposed. By introducing a linear precoder before the IFFT operation, a low-rank structure is created in the received post-DFT signal. Then subspace properties can be explored to identify the channel up to a scalar ambiguity.
Cavity quantum electrodynamics effects in electrically driven high-Q micropillar cavities (2008)

We realized high-quality electrically pumped mircopillar cavities featuring pronounced cQED effects, such as weak coupling and high-beta lasing. The high quality of the electrically contacted micropillars allowed the observation of strong coupling via electro-optical resonance-tuning.
Information content best characterises the hemispheric selectivity of the inferior parietal lobe: a meta-analysis (2020)

Our understanding of the inferior parietal lobe (IPL) remains challenged by inconsistencies between neuroimaging and neuropsychological perspectives. To date, others assume that hemispheric specialisation of the IPL is linked with the type of processing; attention processing in the right hemisphere; memory retrieval and semantic judgement in the left hemisphere. Here, we provide compelling evidence associating the type of information being processed with the recruitment of each hemisphere's IPL. In a meta-analysis, we classify 121 previous fMRI reports of IPL activity arising from episodic memory retrieval, according to the type of information that characterises each fMRI contrast. We demonstrate that the left IPL is more consistently associated with retrieval of the semantic (95% of eligible contrasts) than perceptual aspects of memory (83%). In contrast, the right IPL is more consistently associated with the retrieval of perceptual (97%), than semantic aspects of memory (43%). This work revises assumptions of how the IPL contributes to healthy cognition and has major implications for IPL-related neuropsychological deficits.
Effect of GR32191, a potent thromboxane receptor antagonist, on exercise induced bronchoconstriction in asthma. (1991)

Previous work suggests a role for mast cell derived mediators in exercise induced asthma. The contribution of newly generated contractile prostaglandins to exercise induced asthma was assessed by using a potent and orally active thromboxane (TP1) receptor antagonist, GR32191. The effect of 120 mg GR32191 on exercise induced asthma was observed in 12 asthmatic subjects. For the exercise challenge the subjects performed six minutes of treadmill exercise, breathing dry air at a work load that had previously been shown to induce a fall in FEV1 of 25% or more from the pre-exercise baseline. No effect of GR32191 on pre-exercise baseline airway calibre was evident. There was no significant difference in the mean maximum percentage fall in FEV1 from baseline after exercise between drug and placebo (placebo 30.2%, GR32191 day 31.6%). It is concluded that the thromboxane antagonist GR32191 has no effect on exercise induced asthma. This suggests that prostaglandins, including PGD2, that act via the thromboxane receptor do not have an important role in exercise induced asthma.
Tuning the performance of I/O-intensive parallel applications (1996)

Getting good I/0 performance from parallel programs is a critical problem for many application domains. In this paper, we report our experience tuning the I/0 performance of four application programs from the areas of satellite-data processing and linear algebra. After tuning, three of the four applications achieve application-level 1/0 rates of over 100 MB/s on 16 processors. The total volume of 1/0 required by the programs ranged from about 75 MB to over 200 GB. We report the lessons learned in achieving high I/0 performance from these applications, including the need for code restructuring, local disks on every node and knowledge of future I/0 requests. We also report our experience on achieving high performance on peer-to-peer configurations. Finally, we comment on the necessity of complex I/0 interfaces like collective I/0 and strided requests to achieve high performance.
The Loop Connecting Metal-Binding Domains 3 and 4 of ATP7B Is a Target of a Kinase-Mediated Phosphorylation (2009)

Cu-ATPase ATP7B (Wilson's disease protein) transports copper into the trans-Golgi network for biosynthetic incorporation into ceruloplasmin and sequesters excess copper to endocytic vesicles for further export out of the cell. The activity and intracellular location of ATP7B are regulated by copper levels; the trafficking of ATP7B between cellular compartments is coupled to changes in the level of protein phosphorylation. Neither the nature of the kinase(s) phosphorylating ATP7B nor the location of phosphorylation sites is known. We demonstrate that the membrane-bound ATP7B is phosphorylated by an ATP-dependent, GTP-independent kinase that can be either soluble or membrane-associated. Mg(2+) or Mn(2+) is necessary for kinase activity. We further show that the recombinant N-terminal domain of ATP7B (N-ATP7B) is a specific target for a kinase-mediated phosphorylation in vitro and in cells. Although exogenous addition of copper is not required for kinase activity, copper binding to N-ATP7B markedly alters the exposure of loops connecting the metal-binding subdomains (MBDs) to proteolysis and facilitates phosphorylation by 25-30%. MBD1-2 and MBD4-5 linkers become protected, while MBD2-3 and MBD3-4 regions remain exposed. A significant, 5-fold increase in the level of phosphorylation is also observed for the ATP7B variant that lacks the 29 kDa N-terminal fragment (mostly likely comprised of MBD1-3). Analysis of phosphorylated peptides by two-dimensional gel electrophoresis and mass spectrometry points to the loop connecting MBD3 and MBD4 as a region of phosphorylation. Altogether, the results suggest a mechanism in which kinase-mediated phosphorylation of ATP7B is controlled by a conformational state of N-ATP7B.