gebhart/patrepeval huggingface dataset:
Development of a drug-release strategy based on the reductive fragmentation of benzyl carbamate disulfides (1990)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDevelopment of a drug-release strategy based on the reductive fragmentation of benzyl carbamate disulfidesPeter D. Senter, Walter E. Pearce, and Robert S. GreenfieldCite this: J. Org. Chem. 1990, 55, 9, 2975–2978Publication Date (Print):April 1, 1990Publication History Published online1 May 2002Published inissue 1 April 1990https://pubs.acs.org/doi/10.1021/jo00296a082https://doi.org/10.1021/jo00296a082research-articleACS PublicationsRequest reuse permissionsArticle Views1937Altmetric-Citations65LEARN 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-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
Aggregation of Poly(p-phenylene ethynylene)s Containing Nonpolar and Amine Side Chains (2004)

ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTAggregation of Poly(p-phenylene ethynylene)s Containing Nonpolar and Amine Side ChainsRebecca B. Breitenkamp and Gregory N. TewView Author Information Department of Polymer Science and Engineering, University of Massachusetts, 120 Governors Drive, Amherst, Massachusetts 01003 Cite this: Macromolecules 2004, 37, 3, 1163–1165Publication Date (Web):January 16, 2004Publication History Received29 July 2003Revised19 November 2003Published online16 January 2004Published inissue 1 February 2004https://pubs.acs.org/doi/10.1021/ma0351017https://doi.org/10.1021/ma0351017brief-reportACS PublicationsCopyright © 2004 American Chemical SocietyRequest reuse permissionsArticle Views429Altmetric-Citations32LEARN 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-AlertscloseSupporting Info (2)»Supporting Information Supporting Information SUBJECTS:Absorption,Aggregation,Aromatic compounds,Interfaces,Polymers Get e-Alerts
Core−Shell Nanostructured Nanoparticle Films as Chemically Sensitive Interfaces (2001)

This paper reports the results of an investigation of vapor molecule sorption at different types of nanostructured nanoparticle films. Core-shell nanoparticles of two different core sizes, AU2-nm and Au5-nm, and molecular linkers of two different binding properties, 1,9-nonanedithiol and 11-mercaptoundecanoic acid, are utilized as building blocks for constructing chemically sensitive interfaces. The work couples measurements of two different transducers, interdigitated microelectrodes and quartz crystal microbalance, to determine the correlation of the electronic resistance change and the mass loading with vapor sorption. The responses to vapor sorption at these nanostructured interfaces are demonstrated to be dependent on the core size of nanoparticles and the chemical nature of linking molecules. The difference of molecular interactions of vapor molecules at the nanostructured interface is shown to have a significant impact on the response profile and sensitivity. For the tested vapor molecules, while there are small differences for the sorption of nonpolar and hydrophobic vapor molecules, there are striking differences for the sorption of polar and hydrophilic vapor molecules at these nanostructured interfacial materials. The implication of the findings to the delineation of design parameters for constructing core-shell nanoparticle assemblies as chemically sensitive interfacial materials is also discussed.
Tumor-selective proteotoxicity of verteporfin inhibits colon cancer progression independently of YAP1 (2015)

Yes-associated protein 1 (YAP1) is a transcriptional coactivator in the Hippo signaling pathway. Increased YAP1 activity promotes the growth of tumors, including that of colorectal cancer (CRC). Verteporfin, a drug that enhances phototherapy to treat neovascular macular degeneration, is an inhibitor of YAP1. We found that verteporfin inhibited tumor growth independently of its effects on YAP1 or the related protein TAZ in genetically or chemically induced mouse models of CRC, in patient-derived xenografts, and in enteroid models of CRC. Instead, verteporfin exhibited in vivo selectivity for killing tumor cells in part by impairing the global clearance of high-molecular weight oligomerized proteins, particularly p62 (a sequestrome involved in autophagy) and STAT3 (signal transducer and activator of transcription 3; a transcription factor). Verteporfin inhibited cytokine-induced STAT3 activity and cell proliferation and reduced the viability of cultured CRC cells. Although verteporfin accumulated to a greater extent in normal cells than in tumor cells in vivo, experiments with cultured cells indicated that the normal cells efficiently cleared verteporfin-induced protein oligomers through autophagic and proteasomal pathways. Culturing CRC cells under hypoxic or nutrient-deprived conditions (modeling a typical CRC microenvironment) impaired the clearance of protein oligomers and resulted in cell death, whereas culturing cells under normoxic or glucose-replete conditions protected cell viability and proliferation in the presence of verteporfin. Furthermore, verteporfin suppressed the proliferation of other cancer cell lines even in the absence of YAP1, suggesting that verteporfin may be effective against multiple types of solid cancers.
Ultra-selective cycloaddition of dimethylfuran for renewable p-xylene with H-BEA (2013)

p-Xylene, the precursor for PET bottles, was synthesized at 90% yield by [4 + 2] cycloaddition of biomass-derived ethylene and dimethylfuran followed by subsequent dehydration with Beta zeolite.
Identification and elimination by site-directed mutagenesis of thermolabile aspartyl bonds in Aspergillus awamori glucoamylase (1995)

Both native Aspergillus niger glucoamylase and wild-type Aspergillus awamori glucoamylase expressed in Saccharomyces cerevisiae, which have identical primary structures, undergo hydrolysis at aspartyl bonds at low pH values and elevated temperatures. In native A.niger enzyme the Asp126-Gly127 bond was preferentially cleaved at pH 3.5, while at pH 4.5 cleavage of the Asp257-Pro258 and Asp293-Gly294 bonds was dominant. In wild-type A.awamori glucoamylase, cleavage of the latter was dominant at both pH 3.5 and 4.5. Site-directed mutations Asp126-->Glu and Gly127-->Ala in wild-type enzyme decreased specific activities by approximately 60 and 30%, respectively, and increased irreversible thermoinactivation rates 3- to 4-fold at pH 4.5. Replacement of Asp257 with Glu and Asp293 with Glu or Gln decreased specific activities by approximately 20%, but greatly reduced cleavage of the Asp257-Pro258 and Asp293-Gly294 bonds. The Asp257-->Glu mutant was produced very slowly and was more thermostable than wild-type glucoamylase at pH 4.5 up to 70 degrees C. Replacement of Asp293 with either Glu or Gln significantly raised protein production and slightly increased thermostability at pH 3.5 and 4.5, but not at pH 5.5.
Epitope-tagged Receptor Knock-in Mice Reveal That Differential Desensitization of α2-Adrenergic Responses Is because of Ligand-selective Internalization (2009)

Although ligand-selective regulation of G protein-coupled receptor-mediated signaling and trafficking are well documented, little is known about whether ligand-selective effects occur on endogenous receptors or whether such effects modify the signaling response in physiologically relevant cells. Using a gene targeting approach, we generated a knock-in mouse line, in which N-terminal hemagglutinin epitope-tagged alpha(2A)-adrenergic receptor (AR) expression was driven by the endogenous mouse alpha(2A)AR gene locus. Exploiting this mouse line, we evaluated alpha(2A)AR trafficking and alpha(2A)AR-mediated inhibition of Ca(2+) currents in native sympathetic neurons in response to clonidine and guanfacine, two drugs used for treatment of hypertension, attention deficit and hyperactivity disorder, and enhancement of analgesia through actions on the alpha(2A)AR subtype. We discovered a more rapid desensitization of Ca(2+) current suppression by clonidine than guanfacine, which paralleled a more marked receptor phosphorylation and endocytosis of alpha(2A)AR evoked by clonidine than by guanfacine. Clonidine-induced alpha(2A)AR desensitization, but not receptor phosphorylation, was attenuated by blockade of endocytosis with concanavalin A, indicating a critical role for internalization of alpha(2A)AR in desensitization to this ligand. Our data on endogenous receptor-mediated signaling and trafficking in native cells reveal not only differential regulation of G protein-coupled receptor endocytosis by different ligands, but also a differential contribution of receptor endocytosis to signaling desensitization. Taken together, our data suggest that these HA-alpha(2A)AR knock-in mice will serve as an important model in developing ligands to favor endocytosis or nonendocytosis of receptors, depending on the target cell and pathophysiology being addressed.
Study of the photochemical and in vitro phototoxicity of chlortalidone [2-chloro-5-(1-hydroxy-3-oxo-1-isoindolinyl)benzene sulfonamide]. (1999)

The photodegradation process of the phototoxic diuretic drug chlorthalidone was studied. The products of its photolysis under UV-B were isolated and identified. Chlorthalidone was found to be active when examined by photohemolysis on human erythrocytes, but not in the presence of the isolated photoproducts. Inhibition of the photohemolysis process induced by chlorthalidone on addition of reduced glutathione (GSH) or ascorbic acid suggests the involvement of radicals species. The inhibition with 1,4-diazabycyclo [2.2.2] octane (DABCO), sodium azide (NaN3) sowie 2,5-dimethylfuran proof the participation of singlet oxygen (1O2) in this process.
CpG oligodeoxynucleotides improve the response to hepatitis B immunization in healthy and SIV-infected rhesus macaques (2004)

These findings support the development of clinical studies to assess the use of CpG ODN as an adjuvant for HBV vaccination in healthy and immunocompromised HIV-infected subjects.
XML BASED FRAMEWORK FOR CONTACT CENTER APPLICATIONS (2007)

W3C languages, VoiceXML and CCXML all play an important role in contact centers (CC) by simplifying the creation of CC applications. However, they cover only a subset of contact center functions, such as simple call control and interactive voice response (IVR) with automatic speech recognition. We discuss ways to complement VoiceXML and CCXML in order to cover all necessary contact center functions required to script end-to-end interactions in a consistent and seamless way. For this purpose we introduce an XML forms-based framework called XContact comprising the CC platform and applications, multi-script and multi-browsing, and interaction data processing. We also discuss how routing as a key CC capability can be scripted/captured within such framework in order to demonstrate the overall approach.
Growth factor delivery for oral and periodontal tissue engineering (2006)

The treatment of oral and periodontal diseases and associated anomalies accounts for a significant proportion of the healthcare burden, with the manifestations of these conditions being functionally and psychologically debilitating. Growth factors are critical to the development, maturation, maintenance and repair of craniofacial tissues, as they establish an extracellular environment that is conducive to cell and tissue growth. Tissue-engineering principles aim to exploit these properties in the development of biomimetic materials that can provide an appropriate microenvironment for tissue development. These materials have been constructed into devices that can be used as vehicles for delivery of cells, growth factors and DNA. In this review, different mechanisms of drug delivery are addressed in the context of novel approaches to reconstruct and engineer oral- and tooth-supporting structures, namely the periodontium and alveolar bone.
Dynamic coherent focus OCT with depth-independent transversal resolution (1999)

Abstract We present a new OCT technique which renders the transversal resolution depth independent. This is achieved by an optical setup which shifts the focus of the beam illuminating the object through the object depth without changing the path length in the corresponding interferometer arm. Therefore, the coherence gate remains at the beam focus without any readjustment of the reference arm. Depth resolution was tested with the help of microscopy cover-plates and transversal resolution was tested with the help of Ronchi rulings. Resolution was 100 lines mm−1 over an object depth of 430 μm. For a first demonstration of the properties of this dynamic coherent focus scheme in a biologic system a section of a human cornea was used. We expect that this technique can further be improved to obtain transversal resolution down to the 1-μm range
Expression of the mechanosensitive 2PK+ channel TREK‐1 in human osteoblasts (2005)

TREK-1 is a mechanosensitive member of the two-pore domain potassium channel family (2PK+) that is also sensitive to lipids, free fatty acids (including arachidonic acid), temperature, intracellular pH, and a range of clinically relevant compounds including volatile anaesthetics. TREK-1 is known to be expressed at high levels in excitable tissues, such as the nervous system, the heart and smooth muscle, where it is believed to play a prominent role in controlling resting cell membrane potential and electrical excitability. In this report, we use RT-PCR, Western blotting and immunohistochemistry to confirm that human derived osteoblasts and MG63 cells express TREK-1 mRNA and protein. In addition, we show gene expression of TREK2c and TRAAK channels. Furthermore, whole cell patch clamp electrophysiology demonstrates that these cells express a spontaneously active, outwardly rectifying potassium "background leak" current that shares many similarities to TREK-1. The outward current is largely insensitive to TEA and Ba2+, and is sensitive to application of lysophosphatidylcholine (LPC). In addition, blocking TREK-1 channel activity is shown to upregulate bone cell proliferation. It is concluded that human osteoblasts functionally express TREK-1 and that these channels contribute, at least in part, to the resting membrane potential of human osteoblast cells. We hypothesise a possible role for TREK-1 in mechanotransduction, leading to bone remodelling.
Proposed N2 Toll Road in Pondoland : a reprieve (2005)

The Botanical Society of South Africa has stood by its position that the Environmental Impact Assessment process for the granting of permission for the building of the N2 Wild Coast Toll Road was 'fatally flawed'. The Society applauds the decision of the Minister of Environmental Affairs and Tourism, Marthinus van Schalkwyk, based on 223 appeals, to overturn the previous decision to proceed with the road. Congratulations to the Minister for this wise decision in the face of strong pressure to 'rubber-stamp' the former decision. This gives renewed hope that the promised transparent democratic processes, at least in the environmental sector, are going to be upheld in the future.
Characterization of Ubiquitinated Intraneuronal Inclusions in a Novel Belgian Frontotemporal Lobar Degeneration Family (2006)

The most common histologic feature in patients with frontotemporal lobar degeneration (FTLD) is intracellular brain inclusions of yet uncharacterized proteins that react with antiubiquitin (Ub) antibodies, but not with tau or synuclein (FTLD-U). We identified a four-generation Belgian FTLD family in which 8 patients had dominantly inherited FTLD. In one patient, we showed frontotemporal atrophy with filamentous Ub-positive intracellular inclusions in absence of tau pathology or any alterations in the levels of soluble tau. We characterized the cellular and subcellular localization and morphology of the inclusions. Ub-positive inclusions predominantly occurred within neurons (>97%), but were also observed within oligodendroglia (approximately 2%) and microglia (<1%), but not within astroglia. Regarding the subcellular localization, the intranuclear inclusions (INI) were up to approximately four-fold more frequent than the cytoplasmic inclusions, although the latter were more specific to neurons. The INIs frequently appeared spindle-shaped and 3-dimensional confocal reconstructions identified flattened, leaf-like structures. Ultrastructurally, straight 10- to 18-nm-diameter filaments constituted the spindle-shaped inclusions that occurred in close proximity to the nuclear membrane. Staining for HSP40, p62, and valosin/p97 was observed in only a minority of the inclusions. Whereas the precise nature of the protein remains elusive, characterization of such familial FTLD-U patients would be helpful in identifying a common denominator in the pathogenesis of familial and the more prevalent sporadic FTLD-U.
HIV phenotype & genotype data highlights Lake Maggiore meeting. (1998)

Researchers convened in Italy to discuss state-of-the-art antiretroviral treatment, the most recent data on the development of resistance in naive and experienced patients, and ways to reconstruct the immune system in the early and later stages of HIV disease. Participants reviewed data on a new generation of genotypic and phenotypic assays that portend a new model of care for guiding treatment decision-making in the face of treatment failure. Several papers described new mechanisms of resistance for nucleoside, nucleotide, nonucleotide reverse transcriptase inhibitors, and protease inhibitors. Other studies reported on the evolution of drug resistance, the problem of transmission of drug-resistant viruses, and the potency of regimen adjustments. Discussions revealed the need for academia and industry to continue to develop novel antiretroviral agents.
Characterizing and Optimizing Protease/Peptide Inhibitor Interactions, a New Application for Spot Synthesis (2000)

A new method is presented that uses parallel peptide array synthesis on cellulose membranes to characterize protease/peptide inhibitor interactions. A peptide comprising P5-P4' of the third domain of turkey ovomucoid inhibitor was investigated for both binding to and inhibition of porcine pancreatic elastase. Binding was studied directly on the cellulose membrane, while inhibition was measured by an assay in microtiter plates with punched out peptide spots. The importance of each residue for binding or inhibition was determined by substitutional analyses, exchanging every original amino acid with all other 19 coded amino acids. Seven hundred eighty individual peptides were investigated for binding behavior to porcine pancreatic elastase, and 320 individual peptides were measured in inhibition experiments. The results provide new insights into the interaction between the ovomucoid derived peptide and subsites in the active site of elastase. Combining these data with length analysis we designed new peptides in a step-wise fashion which in the end not only inhibited elastase 400 times more strongly than the original peptide, but are highly specific for the enzyme. In addition, the optimized inhibitor peptide was protected against exopeptidase attack by substituting D-amino acids at both termini.
Personalized ranking metric embedding for next new POI recommendation (2015)

The rapidly growing of Location-based Social Networks (LBSNs) provides a vast amount of check-in data, which enables many services, e.g., point-of-interest (POI) recommendation. In this paper, we study the next new POI recommendation problem in which new POIs with respect to users' current location are to be recommended. The challenge lies in the difficulty in precisely learning users' sequential information and personalizing the recommendation model. To this end, we resort to the Metric Embedding method for the recommendation, which avoids drawbacks of the Matrix Factorization technique. We propose a personalized ranking metric embedding method (PRME) to model personalized check-in sequences. We further develop a PRME-G model, which integrates sequential information, individual preference, and geographical influence, to improve the recommendation performance. Experiments on two real-world LBSN datasets demonstrate that our new algorithm outperforms the state-of-the-art next POI recommendation methods.
Accelerator Applications in a Nuclear Renaissance (2003)

Three martensitic candidate target materials, namely Alloys EP-823 and HT-9, and Type 422 stainless steel have been tested to evaluate their susceptibility to stress corrosion cracking (SCC), hydrogen embrittlement (HE) and localized corrosion (pitting and crevice) in aqueous solutions of different pH values at ambient and elevated temperatures. The SCC behavior of smooth and notched tensile specimens was evaluated by using both constant-load and slow-strain-rate (SSR) testing techniques. The susceptibility to localized corrosion was determined by cyclic potentiodynamic polarization (CPP) method. The extent and morphology of cracking were analyzed by scanning electron microscopy (SEM). The results of SSR testing indicate that the time-to-failure, the percent elongation and the percent reduction in area were significantly reduced in the 90oC acidic solution. However, the magnitude of the true failure stress was increased in the presence of a notch due to a smaller area at the root of the notch. Constant-load SCC testing in the 90oC acidic solution showed cracking within 30 days. SEM micrographs of all broken specimens revealed intergranular brittle failure at the primary fracture face. The results of CPP experiments are currently being analyzed, that will be presented along with the overall test data.
Effects of poloxamer on the gelation of silk fibroin (2000)

The influence of the concentration of poloxamer 407, the pH and the temperature on the gelation of silk fibroin (SF) were studied. It was found that the gelation of SF occurred in the presence of poloxamer at pH value of 7.0 while gelation of SF itself did not occur. The gelation time of SF was shortened with increasing the poloxamer concentration and the temperature. The sol-gel transition of SF became reversible with an addition of poloxamer. From infrared (IR) and circular-dichroism (CD) spectroscopy measurements, it was found that a conformational change of the SF in the SF/poloxamer system from random coil to β-structure was accelerated after forming a polymer complex with the poloxamer. The crystallinity of the poloxamer was reduced by SF from X-ray diffraction measurements.