gebhart/patrepeval huggingface dataset:
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors (1992)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNon-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitorsGeorge D. Hartman, Melissa S. Egbertson, Wasyl Halczenko, William L. Laswell, Mark E. Duggan, Robert L. Smith, Adel M. Naylor, Patricia D. Manno, Robert J. Lynch, and Cite this: J. Med. Chem. 1992, 35, 24, 4640–4642Publication Date (Print):November 1, 1992Publication History Published online1 May 2002Published inissue 1 November 1992https://pubs.acs.org/doi/10.1021/jm00102a020https://doi.org/10.1021/jm00102a020research-articleACS PublicationsRequest reuse permissionsArticle Views1233Altmetric-Citations247LEARN 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
Prospects for the genetic engineering of milk (1992)

Milk and milk products comprise a substantial fraction of the protein intake of the industrialised West. The establishment of germline manipulation techniques in cows offers opportunities for directly manipulating milk composition to produce products with enhanced nutritional and processing properties. The major milk proteins are encoded by a small number of abundantly expressed single-copy genes and a number of possible manipulations are described. Milk proteins exhibit complex interactions with each other and with other constituents of milk. It will, therefore, be necessary to utilise model systems to evaluate the consequences of these proposed changes before embarking upon the costly and time-consuming process of manipulating the bovine genome.
Zur Kenntnis der 2‐Amino‐1.3.4‐oxdiazole, IX. OXYDATION VON ALDEHYDSEMICARBAZOLEN ZU 2‐AMINO‐1.3.4‐OXDIAZOLEN UND DEREN ÜBERGANG IN 1‐ACYL‐SEMICARBAZIDE (1962)

Abstract Die bereits beschriebene Oxydation der Semicarbazone aromatischer Aldehyde zu 2‐Amino‐1.3.4‐oxdiazolen läßt sich auch auf aliphatische Aldehyde anwenden. — Die Bildung von Acylsemicarbaziden als Zwischenprodukte der Umwandlung von 2‐Amino‐1.3.4‐oxdiazolen in 1.2.4‐Triazolone durch alkalisches Verkochen wird bewiesen.
Purification and Functional Reconstitution with GTP-Binding Regulatory Proteins of Hexahistidine-Tagged Muscarinic Acetyicholine Receptors (m2 Subtype) (1996)

We have expressed human m2 muscarinic acetylcholine receptors tagged with six histidine residues at the carboxy-terminal region in insect cells (Sf9) and purified them using metal-immobilized Chelating Sepharose gels. Co(2+)-immobilized gels were found to be much more efficient for purification of m2 receptors than gels containing Ni2+ or other metal ions. Twenty-fold purification was attained by a simple, single-step procedure, and approximately 40% of solubilized receptors were recovered as a partially purified preparation with a specific activity of 1.6 nmol/mg of protein. Purified receptors were functionally active in that carbamylcholine stimulated binding of [35S]GTP gamma S to the G-protein G12 reconstituted in lipid vesicles with purified m2 receptors. The extent of stimulation of [35S] GTP gamma S binding to G12 by hexahistidine-tagged m2 receptors was essentially the same as that observed for m2 receptors that lack histidine tags. In addition, palmitoylation at the carboxy-terminal region was not impaired by the hexahistidine-tag fusion. The method described in this study should be applicable to the purification of other G-protein-coupled receptors in functionally active form.
Osteonecrosis after contact neodymium:yttrium aluminum garnet arthroscopic laser meniscectomy. (1997)

To our knowledge, this complication of laser arthroscopic meniscectomy has not been reported in the radiology literature. The clinical and MR imaging features of this important complication are described and possible causative mechanisms are discussed.
Randomized, placebo-controlled trial of the anti-tumor necrosis factor antibody fragment afelimomab in hyperinflammatory response during severe sepsis: The RAMSES Study (2001)

The IL-6 immunostrip test identified two distinct sepsis populations with significantly different mortality rates. A small (3.7%) absolute reduction in mortality rate was found in the afelimomab-treated patients. The treatment difference did not reach statistical significance.
Identification of select glucocorticoids as Smoothened agonists: Potential utility for regenerative medicine (2010)

Regenerative medicine holds the promise of replacing damaged tissues largely by stem cell activation. Hedgehog signaling through the plasma membrane receptor Smoothened (Smo) is an important process for regulating stem cell proliferation. The development of Hedgehog-related therapies has been impeded by a lack of US Food and Drug Administration (FDA)-approved Smo agonists. Using a high-content screen with cells expressing Smo receptors and a beta-arrestin2-GFP reporter, we identified four FDA-approved drugs, halcinonide, fluticasone, clobetasol, and fluocinonide, as Smo agonists that activate Hedgehog signaling. These drugs demonstrated an ability to bind Smo, promote Smo internalization, activate Gli, and stimulate the proliferation of primary neuronal precursor cells alone and synergistically in the presence of Sonic Hedgehog protein. Halcinonide, fluticasone, clobetasol, and fluocinonide provide an unprecedented opportunity to develop unique clinical strategies to treat Hedgehog-dependent illnesses.
Wi-fi backscatter (2014)

RF-powered computers are small devices that compute and communicate using only the power that they harvest from RF signals. While existing technologies have harvested power from ambient RF sources (e.g., TV broadcasts), they require a dedicated gateway (like an RFID reader) for Internet connectivity. We present Wi-Fi Backscatter, a novel communication system that bridges RF-powered devices with the Internet. Specifically, we show that it is possible to reuse existing Wi-Fi infrastructure to provide Internet connectivity to RF-powered devices. To show Wi-Fi Backscatter's feasibility, we build a hardware prototype and demonstrate the first communication link between an RF-powered device and commodity Wi-Fi devices. We use off-the-shelf Wi-Fi devices including Intel Wi-Fi cards, Linksys Routers, and our organization's Wi-Fi infrastructure, and achieve communication rates of up to 1 kbps and ranges of up to 2.1 meters. We believe that this new capability can pave the way for the rapid deployment and adoption of RF-powered devices and achieve ubiquitous connectivity via nearby mobile devices that are Wi-Fi enabled.
2-Aminoethoxydiphenyl Borate Activates and Sensitizes the Heat-Gated Ion Channel TRPV3 (2004)

Six of the mammalian transient receptor potential (TRP) ion channel subtypes are nonselective cation channels that can be activated by increases or decreases in ambient temperature. Five of them can alternatively be activated by nonthermal stimuli such as capsaicin [transient receptor potential vanilloid 1 (TRPV1)] or hypo-osmolarity (TRPV2 and TRPV4). No nonthermal stimuli have yet been described for TRPV3, a warmth-gated ion channel expressed prominently in skin keratinocytes. Here, we demonstrate that 2-aminoethoxydiphenyl borate (2-APB), a compound used to inhibit store-operated Ca2+ channels and IP3 receptors, produces robust activation of recombinant TRPV3 in human embryonic kidney 293 cells with an EC50 of 28 microm. 2-APB also sensitizes TRPV3 to activation by heat, even at subthreshold concentrations. In inside-out membrane patches from TRPV3-expressing cells, 2-APB increases the open probability of TRPV3. Also, whereas heat alone is capable of activating TRPV3-mediated currents in only a small proportion of primary mouse keratinocytes, 2-APB activates heat-evoked, TRPV3-mediated currents in the majority of these cells. Together, these findings identify 2-APB as the first known chemical activator of TRPV3 and enhance the notion that TRPV3 participates in the detection of heat by keratinocytes.
Adverse drug reactions: types and treatment options. (2003)

Drug hypersensitivity results from interactions between a pharmacologic agent and the human immune system. These types of reactions constitute only a small subset of all adverse drug reactions. Allergic reactions to medications represent a specific class of drug hypersensitivity reactions mediated by IgE. Immune-mediated drug reactions may be discussed generally in the Gell and Coombs classification system, a widely accepted conceptual framework for understanding complex immune reactions. However, some reactions involve additional, poorly understood mechanisms that are not easily classified. Identifiable risk factors for drug hypersensitivity reactions include age, female gender, concurrent illnesses, and previous hypersensitivity to related drugs. Drug hypersensitivity is a clinical diagnosis based on available data. Laboratory testing may be useful, with skin testing providing the greatest specificity. Treatment is largely supportive and includes discontinuation of the offending medication, symptomatic treatment, and patient education. Patients with penicillin allergy should avoid carbapenems, and caution should be used in prescribing cephalosporins in these patients. Reactions to radiocontrast media can be limited by pretreatment with prednisone, diphenhydramine, and either ephedrine or a histamine H2-receptor antagonist.
Towards a theory of natural language interfaces to databases (2003)

The need for Natural Language Interfaces to databases (NLIs) has become increasingly acute as more and more people access information through their web browsers, PDAs, and cell phones. Yet NLIs are only usable if they map natural language questions to SQL queries correctly. As Schneiderman and Norman have argued, people are unwilling to trade reliable and predictable user interfaces for intelligent but unreliable ones. In this paper, we introduce a theoretical framework for reliable NLIs, which is the foundation for the fully implemented Precise NLI. We prove that, for a broad class of semantically tractable natural language questions, Precise is guaranteed to map each question to the corresponding SQL query. We report on experiments testing Precise on several hundred questions drawn from user studies over three benchmark databases. We find that over 80% of the questions are semantically tractable questions, which Precise answers correctly. Precise automatically recognizes the 20% of questions that it cannot handle, and requests a paraphrase. Finally, we show that Precise compares favorably with Mooney's learning NLI and with Microsoft's English Query product
Performance requirements of physically strenuous occupations: validating minimum standards for muscular strength and endurance (2004)

Employment rights legislative mandates passed in the USA over the last three decades emphasize the importance of validating performance standards for physically strenuous occupations. This study validated minimally acceptable standards for the muscular strength and endurance necessary to perform fire suppression activities. Incumbent firefighters (n=153) selected for key demographic characteristics completed a simulated set of firefighting tasks (Fire Suppression Evolution) and then a Predictor Test Battery of physical abilities tests. Regression analysis revealed that three predictor test items (hose drag/high rise pack carry; arm lift; arm endurance) combined to significantly predict performance time of the Fire Suppression Evolution (p < or =0.01). Firefighters (n=41) rating videotaped performance times of the Fire Suppression Evolution determined that more than one-half a standard deviation slower than the mean time established by the incumbents reflected unacceptable performance. Approximately 80% of incumbent firefighters passed the minimally acceptable performance standard. Use of the 3-predictor test battery would correctly identify 89% of successful performers and 72% of unsuccessful performers. This study demonstrates that validation of minimal physical performance standards will identify a cohort of individuals with a high probability of not being able to perform critical fire suppression activities. This finding has important implications for examining the relationship between physical performance standards and medical and economic outcomes.
HLA-A0201 and HLA-B7 binding peptides in the EBV-encoded EBNA-1, EBNA-2 and BZLF-1 proteins detected in the MHC class I stabilization assay. Low proportion of binding motifs for several HLA class I alleles in EBNA-1 (1995)

B lymphocytes immortalized with EBV in vitro, lymphoblastoid cell lines (LCL), express eight EBV-encoded proteins, EBV nuclear antigens -1 to -6 (EBNA-1 to -6), and latent membrane proteins 1 and 2 (LMP 1 and 2). After appropriate stimulations of blood lymphocytes from seropositive individuals, MHC-restricted cytotoxic T cells (CTL), which lyse LCL cells, can be generated in vitro. Such CTLs can recognize EBNA-2 to -6, and LMP 1 and 2, but not EBNA-1-derived peptides presented on the cell surfaces. We posed the question whether this exceptional feature of EBNA-1 is due to lack of MHC class I binding peptides. A computer search for 11 human leukocyte antigen (HLA) alleles showed that EBNA-1 has a lower number and lower proportion of relevant binding motifs to several alleles than EBNA-2 to -6 and LMP 1 and 2. The low motif numbers in EBNA-1 is in line with its apparent failure to generate a CTL response, and it may be the consequence of immunoselection allowing the existence of EBV genome-carrying B cells in the immunocompetent hosts. The binding capacities of synthetic peptides of EBNA-1 and -2 and of the immediate early lytic cycle protein BZLF-1 to HLA-A0201 (A2) and HLA-B7 molecules were tested in an MHC stabilization assay. The peptide transporter-deficient T2 line, which expresses a low level of HLA-A2 and its HLA-B7 transfectant subline, were used for this purpose because specifically bound peptides elevate the surface expression of these MHC molecules. Of five synthetic nonamer EBNA-1 peptides which include the relevant binding motif, four bound to A2. In a series of 20-amino acid-long overlapping EBNA-1 peptides none showed binding to A2, while eight peptides bound to B7. Two 20-amino acid-long EBNA-2 and seven BZLF-1 peptides were identified as A2 binders, and four EBNA-2 and eight BZLF-1 peptides bound to B7. Thus, we have exclude the possibility that the inability of the EBNA-1 protein to generate HLA-restricted CTLs could be due to the lack of HLA class I binding peptides in its sequence. The finding that several EBNA-1 peptides could bind to these two HLa molecules does not, however, necessarily reflect the natural situation because the peptides may not be processed and/or transported to the cell surfaces. We have stimulated lymphocytes of healthy donors with relevant HLA types with the autologous LCL.(ABSTRACT TRUNCATED AT 400 WORDS)
Markedly Enhanced Recyclability of Osmium Catalyst in Asymmetric Dihydroxylation Reactions by Using Macroporous Resins Bearing Both Residual Vinyl Groups and Quaternary Ammonium Moieties. (2005)

Abstract For Abstract see ChemInform Abstract in Full Text.
Triglyceride synthesis: insights from the cloning of diacylglycerol acyltransferase (2000)

Although the biochemistry of triglyceride synthesis has been studied for decades, an understanding of the molecular processes involved has been lacking. The recent cloning of a gene encoding acyl coenzyme A : diacylglycerol acyltransferase, an enzyme that catalyses the final step in triglyceride synthesis, has opened this area to molecular investigation and has begun to provide new insights into triglyceride metabolism.
Blood Pressure and Functional Recovery in Acute Ischemic Stroke (1998)

These results suggest that complete recovery in ischemic stroke is facilitated by a moderate blood pressure reduction when brain edema develops, most likely as the result of a more adequate cerebral perfusion pressure. Conversely, stroke worsening due to pharmacological hypoperfusion is exceptional.
ROC curves in evaluation of serum fibrosis indices for hepatic fibrosis (2002)

Serum fibrosis indices can indicate tendency of hepatic fibrosis, but it cannot replace liver biopsy. However, as diagnostic markers, more efficient serum fibrosis indices for the diagnosis of hepatic fibrosis need to be explored.
MALDI Mass Spectrometry Combined with Avidin−Biotin Chemistry for Analysis of Protein Modifications (1998)

A general mass spectrometric method that combines purification and analysis in one step is described for the rapid and sensitive determination of protein modification that involves covalent attachment of a modifying group. In this method, the modifying group is first labeled with a biotin moiety, and the covalent interaction of this group with the targeted protein results in a biotinylated product. The modified protein can then be subjected to enzymatic digestion, followed by the isolation of the biotinylated peptide based on a previously described MALDI method incorporating the avidin-biotin interaction (Schriemer, D. C.; Li, L. Anal. Chem. 1996, 68, 3382-3387). To illustrate the validity of the method, a study of a model system was undertaken, involving the interaction between avian skeletal muscle troponin C and a sulfhydryl-specific biotinylation reagent. It is shown that isolation of a modified peptide with an immobilized avidin product could be achieved, even in the presence of an excess of contaminating protein. Exoproteases could be added to the crude tryptic digest to generate peptide ladders, each containing biotin, which could be analyzed by the avidin-biotin/MALDI method for sequence information. Complementary sequence information could be obtained from the application of this technique in a tandem sector/time-of-flight mass spectrometer for MALDI MS/MS analysis, which allowed for the identification of the modification site.
Hybrid Wavelet-PSO-ANFIS Approach for Short-Term Wind Power Forecasting in Portugal (2010)

The increased integration of wind power into the electric grid, as it occurs today in Portugal, poses new challenges due to its intermittency and volatility. Wind power forecasting plays a key role in tackling these challenges. A novel hybrid approach, combining wavelet transform, particle swarm optimization, and an adaptive-network-based fuzzy inference system, is proposed in this paper for short-term wind power forecasting in Portugal. A thorough comparison is carried out, taking into account the results obtained with seven other approaches. Finally, conclusions are duly drawn.
Immunohistochemical and Clinical Characterization of the Basal-Like Subtype of Invasive Breast Carcinoma (2004)

A panel of four antibodies (ER, HER1, HER2, and cytokeratin 5/6) can accurately identify basal-like tumors using standard available clinical tools and shows high specificity. These studies show that many basal-like tumors express HER1, which suggests candidate drugs for evaluation in these patients.
Do daily threshold trend fluctuations of epicardial leads correlate with pacing and sensing characteristics in paediatric patients? (2007)

High amplitudes of daily Deltafluctuation correlate with higher and increasing pacing thresholds and lower impedances. Theoretically, this results from electrode microinstability on the epicardial surface. A decrease of the steroid-eluting potency of the electrode can be hypothesized to cause higher daily Deltafluctuation beyond a lead age of 5 years. Potential implications of marked daily Deltafluctuation are short-term follow-up and lead replacement in the presence of high pacing thresholds.
Distribution and Prevalence of Hyperpolarization-Activated Cation Channel (HCN) mRNA Expression in Cardiac Tissues (1999)

HCN cation channel mRNA expression was determined in the rabbit heart and neonatal and adult rat ventricle using RNase protection assays. In the rabbit SA node, the dominant HCN transcript is HCN4, representing >81% of the total HCN message. HCN1 is also expressed, representing >18% of the total HCN mRNA. Rabbit Purkinje fibers contained almost equal amounts of HCN1 and HCN4 transcripts with low levels of HCN2, whereas rabbit ventricle contained predominantly HCN2. The SA node contained 25 times the total HCN message of Purkinje fibers and 140 times the total HCN message of ventricle. No reports of hyperpolarization-activated current (If) exist in rabbit Purkinje fibers, and we could not record If in rabbit ventricular myocytes. To investigate the possible role of isoform switching in determining the voltage dependence of If, we determined the prevalence of HCN isoforms in neonatal and adult rat ventricle. We had previously determined the threshold for activation of If to be approximately -70 mV in neonatal rat ventricle and -113 mV in adult rat ventricle. In both neonatal and adult rat ventricle, only HCN2 and HCN4 transcripts are present. The ratio of HCN2 to HCN4 is approximately 5:1 in the neonate and 13:1 in the adult. Taken together, these results suggest that different cardiac regions express different isoforms of the HCN family. The HCN1 and HCN4 isoforms are most closely associated with a depolarized threshold for If activation, whereas the HCN2 isoform is associated with a more negative activation curve.
Tear Dynamics Model (2007)

Most of the predicted results agree with the reported experimental results, at least qualitatively. However, some predictions disagree with experiments suggesting that further improvements in the model are needed. The model developed in this paper can improve our understanding of tear dynamics and also serve as a tool to evaluate the efficacy of various modalities at treating dry eyes.
The production and crystallization of the human leukocyte antigen class II molecules HLA-DQ2 and HLA-DQ8 complexed with deamidated gliadin peptides implicated in coeliac disease (2007)

The major histocompatibility complex (MHC) class II molecules HLA-DQ2 and HLA-DQ8 are key risk factors in coeliac disease, as they bind deamidated gluten peptides that are subsequently recognized by CD4+ T cells. Here, the production and crystallization of both HLA-DQ2 and HLA-DQ8 in complex with the deamidated gliadin peptides DQ2 alpha-I (PQPELPYPQ) and DQ8 alpha-I (EGSFQPSQE), respectively, are reported.