gebhart/patrepeval huggingface dataset:
An omics perspective on drug target discovery platforms (2019)

The drug discovery process starts with identification of a disease-modifying target. This critical step traditionally begins with manual investigation of scientific literature and biomedical databases to gather evidence linking molecular target to disease, and to evaluate the efficacy, safety and commercial potential of the target. The high-throughput and affordability of current omics technologies, allowing quantitative measurements of many putative targets (e.g. DNA, RNA, protein, metabolite), has exponentially increased the volume of scientific data available for this arduous task. Therefore, computational platforms identifying and ranking disease-relevant targets from existing biomedical data sources, including omics databases, are needed. To date, more than 30 drug target discovery (DTD) platforms exist. They provide information-rich databases and graphical user interfaces to help scientists identify putative targets and pre-evaluate their therapeutic efficacy and potential side effects. Here we survey and compare a set of popular DTD platforms that utilize multiple data sources and omics-driven knowledge bases (either directly or indirectly) for identifying drug targets. We also provide a description of omics technologies and related data repositories which are important for DTD tasks.
Recent Development of Blue Fluorescent OLED Materials and Devices (2005)

Highlights of the recent development of highly efficient and robust blue fluorescent organic light-emitting device (OLED) materials and devices are reviewed with emphasis on work accomplished at the OLED Laboratory of Display Institute, National Chiao Tung University, Hsinchu, Taiwan, R.O.C.
Antibiotic susceptibility of potentially probiotic <i>Bifidobacterium</i> isolates from the human gastrointestinal tract (1998)

Sixteen Bifidobacterium isolates from the human gastrointestinal tract were assayed for susceptibility to 44 antibiotics by soft agar overlay disc diffusion on TPY agar. Five isolates (3/7 B. bifidum and 2/3 B. breve) exhibited atypical antibiotic susceptibility profiles. Poor growth in the agar overlay accounted for susceptibility of B. bifidum but not B. breve isolates. All other isolates were resistant to cefoxitin (30 micrograms), aztreonam (30 micrograms), vancomycin (30 micrograms), amikacin (30 micrograms), gentamicin (10 micrograms), kanamycin (30 micrograms), streptomycin (10 micrograms), fusidic acid (10 micrograms), trimethoprim (5 micrograms), norfloxacin (10 micrograms), nalidixic acid (30 micrograms), metronidazole (5 micrograms), polymyxin B (300 micrograms) and colistin sulphate (10 micrograms), and they were susceptible to the six penicillins studied, cephalothin (30 micrograms), cefuroxime (30 micrograms), cefaclor (30 micrograms), ceftizoxime (30 micrograms), cefotaxime (30 micrograms), bacitracin (10 micrograms), chloramphenicol (30 micrograms), erythromycin (15 micrograms), clindamycin (2 micrograms), rifampicin (5 micrograms) and nitrofurantoin (300 micrograms). In addition, they varied in their susceptibility to cephradine (30 micrograms), cephazolin (30 micrograms), cefoperazone (75 micrograms), ceftriaxone (30 micrograms), ofloxacin (5 micrograms) and furazolidone (15 micrograms). They were resistant, or only marginally moderately susceptible, to ceftazidime (30 micrograms), netilmicin (10 micrograms), sulphamethoxazole (100 micrograms), cotrimoxazole (25 micrograms) and ciprofloxacin (5 micrograms), and susceptible or marginally moderately susceptible to tetracycline (30 micrograms). All B. bifidum isolates were susceptible to cefixime (5 micrograms). Four microorganism-drug combinations were evaluated for beta-lactamase activity but its absence suggested that cell wall impermeability was responsible for cephalosporin resistance among bifidobacteria. The antibiotic susceptibility of B. animalis 25527T was similar to that of the human isolates.
The molecular basis of X-linked deafness type 3 (DFN3) in two sporadic cases: Identification of a somatic mosaicism for aPOU3F4 missense mutation (1997)

We have investigated two unrelated males with X-linked deafness type 3 (DFN3) for mutations in the POU3F4 gene. In one patient, we observed a mutation that is predicted to result in an Arg330Ser amino acid substitution. In another DFN3 patient, a somatic mosaicism for an Arg323Gly amino acid substitution was found. This mosaicism was detected in two independently established EBV immortalized B cells and peripheral blood lymphocytes (PBLs). Semiquantitative analysis showed that approximately 50% of the PBLs of this patient carry the mutation. We hypothesize that the Arg323Gly mutation occurred very early in embryogenesis, before the differentiation of cells involved in hematopoiesis and inner ear development. In both patients, the missense mutations are situated in the POU homeodomain and are predicted to disrupt the DNA binding of the POU3F4 protein. All nine point mutations thus far described were found in the POU domains of POU3F4. Since these domains constitute only 35% of the open reading frame of POU3F4, there is a statistically significant preference for mutations in the POU-specific and POU homeodomain.
Selectively fired, tubing-conveyed perforating guns save rig time (1993)

Selective firing of tubing-conveyed perforating (TCP) guns during drill stem tests (DSTs) added flexibility and saved costs for Marathon Oil Co. As an example, in the Garland field in Wyoming, the guns allowed perforating multiple zones in one trip. This saved 1 1/2--2 days/well in rig time and $25,000--30,000/well in electric wire line and DST tool charges. For international offshore operations, savings of $200,000/well appear possible. Savings result not only from perforating multiple zones, but also from arbitrarily setting firing patterns with or without zone isolation. The paper describes the testing of equipment, the design of the guns, firing heads, crossover assembly, pressure isolation sub, control line, and select-fire sub, and applications for the guns.
Granulatimide and Isogranulatimide, Aromatic Alkaloids with G2 Checkpoint Inhibition Activity Isolated from the Brazilian Ascidian <i>Didemnum </i><i>granulatum</i>:  Structure Elucidation and Synthesis (1998)

Crude methanol extracts of the ascidian Didemnum granulatum collected in Brazil showed activity in a new screen for G2 cell cycle checkpoint inhibitors. Bioassay-guided fractionation of the extract yielded the known alkaloids didemnimides A (1) and D (2), the new alkaloid didemnimide E (3), and a new G2 checkpoint inhibitor. Two candidate structures for the inhibitor, named granulatimide (4) and isogranulatimide (5), have been prepared via a short and efficient biomimetic synthesis involving the photolysis of didemnimide A (1). The synthesis revealed that the correct structure for the naturally occurring G2 checkpoint inhibitor is isogranulatimide (5). Granulatimide (4), the other candidate structure, was also found to be a G2 checkpoint inhibitor, and it was subsequently detected in chromatographic fractions associated with purification of D. granulatum alkaloids. Granulatimide (4) and isogranulatimide (5) represent the first examples of a new class of G2 specific cell cycle checkpoint inhibitors and the first ones identified through a rational screening program.
Low-power chip interconnection by dynamic termination (1995)

A low-power dynamic termination scheme is proposed and demonstrated as a way to reduce power dissipation for high-speed data transport. In this scheme, the transmission lines are terminated only if the signals change. The gate of a switching MOS transistor connected to a termination resistor is driven by differentiating the transmission signal with a resistor and a capacitor. The power dissipation of the terminating resistor can be reduced to 1/5 in the conventional determination scheme, and overshoot can be reduced to 1/5 that in the open scheme. This scheme is promising for use with palm-top equipment, facilitating high-speed low power operation.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Fabrication of Robust Biomolecular Patterns by Reactive Microcontact Printing on <i>N</i>‐Hydroxysuccinimide Ester‐Containing Polymer Films (2006)

Abstract The fabrication of robust biomolecule microarrays by reactive microcontact printing (μCP) on spin‐coated thin films of poly( N ‐hydroxysuccinimidyl methacrylate) (PNHSMA) on oxidized silicon and glass is described. The approach combines the advantages of activated polymer thin films as coupling layers, characterized by high reactivity and high molecular loading, with the versatility and flexibility of soft lithography. The transfer of amino end‐functionalized poly(ethylene glycol) (PEG) from oxidized poly(dimethylsiloxane) elastomer stamps to PNHSMA films is shown by Fourier transform infrared spectroscopy, X‐ray photoelectron spectroscopy, fluorescence microscopy, and ellipsometry measurements to result in covalent coupling and identical grafting densities, as found previously for coupling from solution. The PEG‐protected areas effectively inhibit the adsorption of fluoresceinamine, bovine serum albumin, as well as 25‐mer DNA, while the unreacted N ‐hydroxysuccinimidyl methacrylate ester groups retain their reactivity towards primary amino groups. Biomolecule microarrays have been thus conveniently fabricated in a two‐step procedure. The hybridization of target DNA to immobilized probe DNA in micropatterns proves the concept of reactive μCP on activated polymer films for obtaining robust platforms for biomolecule immobilization and screening.
Upper-Extremity Volume Measurements in Women With Lymphedema: A Comparison of Measurements Obtained Via Water Displacement With Geometrically Determined Volume (2002)

Volume of an edematous UE calculated by geometric formulas correlated strongly with volume determined by water displacement. Although strongly correlated, the measurements obtained by the 2 methods did not agree.
Phase II study of DHA-paclitaxel (TXP) as first line chemotherapy in patients with hormone refractory prostate cancer (HRPC) (2004)

4657 Background: DHA-paclitaxel (Taxoprexin) is a covalent conjugate of paclitaxel and docosahexaenoic acid that has greater tumor specificity in pre-clinical models than paclitaxel. The conjugate accumulates in tumor tissue where it is cleaved to paclitaxel. The objective of this multi-center study was to evaluate the efficacy and tolerability of TXP as first line therapy in patients with HRPC. Methods: Thirty-six patients, median age 70y (range 56–86) PS 0 (12), PS 1 (24) with advanced HRPC and no previous cytotoxic treatment were enrolled. Patients were required to have adequate renal, hepatic and bone marrow function and measurable disease. TXP was administered iv over 2 hours q21 days at one of two doses, 1100 mg/m2 (14), 900 mg/m2 (22) . Results: Fifty-one courses (mean 3.6) were administered at 1100 mg/m2 and 65 courses (mean 2.9) at 900 mg/m2. Neutropenia was the primary toxicity and was dose limiting: 12 of 14 (86%) patients treated at 1100 mg/m2 had grade 3/4 neutropenia vs. 9 of 22 (41%) at 900 mg/m2. Thirty-two patients were evaluable for response: at 900 mg/m2, PR 1/19 (5%), SD 8/19 (42%) PSA 1/19 (5%); at 1100 mg/m2, PR 2/13 (15%), SD 7/13 (54%), PSA 1/13 (7%). Median survival is 17.5 months. Conclusions: The combination of objective responses and lengthy survival suggests that TXP is active in the treatment of patients with HRPC. (Supported by American Regent.) Author Disclosure Employment or Leadership Consultant or Advisory Stock Ownership Honoraria Research Funding Expert Testimony Other Remuneration Luitpold Pharmaceuticals, Inc. Protarga, Inc.
The flavonoid luteolin inhibits niacin‐induced flush (2008)

Niacin (7.5 mg per rat, equivalent to a human dose of 1750 mg per 80 kg) maximally increased ear temperature to 1.9+/-0.2 degrees C at 45 min. Quercetin and luteolin (4.3 mg per rat; 1000 mg per human), administered i.p. 45 min prior to niacin, inhibited the niacin effect by 96 and 88%, respectively. Aspirin (1.22 mg per rat; 325 mg per human) inhibited the niacin effect by only 30%. Niacin almost doubled plasma PGD2 and 5-HT, but aspirin reduced only PGD2 by 86%. In contrast, luteolin inhibited both plasma PGD2 and 5-HT levels by 100 and 67%, respectively. CONCLUSIONS AND IMPLICATIONS. Niacin-induced skin temperature increase is associated with PGD2 and 5-HT elevations in rats; luteolin may be a better inhibitor of niacin-induced flush because it blocks the rise in both mediators.
Design and Implementation of 150 W AC/DC LED Driver with Unity Power Factor, Low THD, and Dimming Capability (2019)

This paper presents the implementation of a two-stage light-emitting diode (LED) driver based on commercial integrated circuits (IC). The presented LED driver circuit topology, which is designed to drive a 150 W LED module, consists of two stages: AC-DC power factor correction (PFC) stage and DC/DC power converter stage. The implementation of the PFC stage uses IC NCP1608, which uses the critical conduction mode to guarantee a unity input power factor with a wide range of input voltages. The DC/DC power converter with soft-switching characteristics for the entire load range uses IC FLS2100XS. Furthermore, the design of an electromagnetic interference (EMI) filter for the LED driver and the dimming control circuit are discussed in detail. The hardware prototype, an LED lighting system, with a rated power of 150 W/32 V from a nominal 220 V/50 Hz AC voltage supply was tested to show the effectiveness of the design. The presented LED driver was tested for street lighting, and the experimental results show that the power factor (PF) was higher than 0.97, the total harmonics distortion (THD) was lower than 7%, and the efficiency was 91.7% at full load. The results prove that the performance of the presented LED driver complies with the standards: IEC61000-3-2 and CIRSP 15:2009.
N-acetylneuraminic acid estimation in human serum by neuraminidase and resorcinol/ferric(III) chloride reagent in hydrochloric solution. (1994)

By the method described the serum concentration of the protein-bound or the total N-acetylneuraminic acid can be determined. The estimation of the protein-bound N-acetylneuraminic acid is a specific method. In comparison to the Arzneibuch (D.L.) GDR-method (Vol. 2, Akademie Verlag Berlin, 1985) based on Svennerholm (Biochim. Biophys. Acta 24 (1957) 604-611) the advantages of our estimation are: high stability of the dye complex during a period of at least one hour for a final concentration of at least 6.0 mol/l hydrochloric acid; omission of the time-consuming resuspension of the protein precipitation and the extraction of the dye product with n-amyl alcohol; and the lack of diminution of the monosaccharide influence.
A Simple Route to Unsymmetrically Substituted 1,2,4,5-Tetrazines (1994)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA Simple Route to Unsymmetrically Substituted 1,2,4,5-TetrazinesStephen C. Fields, Marshall H. Parker, and W. Randal EricksonCite this: J. Org. Chem. 1994, 59, 26, 8284–8287Publication Date (Print):December 1, 1994Publication History Published online1 May 2002Published inissue 1 December 1994https://doi.org/10.1021/jo00105a059Request reuse permissionsArticle Views719Altmetric-Citations15LEARN 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 InReddit PDF (564 KB) Get e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
A generic software platform for controlling collaborative robotic system using XML-RPC (2006)

This paper describes a software platform used for controlling any set of collaborative robots. The platform is specially designed for users without special skills on hardware design or communication topics. The platform provides a standard to simplify the addition of new hardware devices. The system runs over Linux operating system; it is accessible through different programming languages. Calls among architecture processes are performed using XML-RPC. Data transport is TCP-IP based; therefore the system is accessible from a conventional Internet link. Some experiments are performed in order to detect the programming languages that better fit in the architecture and the better web server for operating. It was found that php, in comparison with C language, reduces more than three times the speed of call processing, and more that seven times in comparison with c-sharp language (MONO implementation). Using CGI to access an Apache server is twice faster than using s standalone server
Parenteral Iron and Recombinant Human Erythropoietin Therapy to Stimulate Erythropoiesis in Patients Undergoing Repair of Hip Fracture (1996)

We have previously demonstrated the value of erythropoietin therapy and oral iron supplementation coupled with autologous blood donation in patients undergoing elective orthopaedic procedures. For patients undergoing non-elective surgery such as repair of hip fracture, however, alternative approaches to blood conservation must be developed. To investigate one approach, patients undergoing surgical repair of hip fracture were administered parenteral iron (Iron Dextran USP, 100 mg daily by continuous intravenous infusion) and recombinant human erythropoietin (EPO, 150 u/kg subcutaneously daily) during hospitalization in order to stimulate erythropoiesis. Of nine evaluable patients, three showed evidence of low iron stores. The median total iron therapy administered was 500 mg (the equivalent of 2 1/2 blood units). The median total EPO dose administered was 737 u/kg. The median estimated red blood cell volume produced by the combined therapy was 398 ml (the equivalent of two blood units). Six of eight patients who had reticulocyte data available showed increases in reticulocyte counts. The median admission and discharge hematocrit levels were 35.2% and 31.8%, respectively. Six of nine patients did not require allogeneic blood units. We conclude that parenteral iron supplementation and EPO therapy can stimulate effective erythropoiesis in hip fracture patients, and provide a possible approach to blood conservation in these non-elective surgical patients.
Angiotensin AT<sub>4</sub> ligands are potent, competitive inhibitors of insulin regulated aminopeptidase (IRAP) (2003)

Angiotensin IV (Ang IV) exerts profound effects on memory and learning, a phenomenon ascribed to its binding to a specific AT4 receptor. However the AT4 receptor has recently been identified as the insulin-regulated aminopeptidase (IRAP). In this study, we demonstrate that AT4 receptor ligands, including Ang IV, Nle1-Ang IV, divalinal-Ang IV, and the structurally unrelated LVV-hemorphin-7, are all potent inhibitors of IRAP catalytic activity, as assessed by cleavage of leu-beta-naphthylamide by recombinant human IRAP. Both Ang IV and divalinal-Ang IV display competitive kinetics, indicating that AT4 ligands mediate their effects by binding to the catalytic site of IRAP. The AT4 ligands also displaced [125I]-Nle1-Ang IV or [125I]-divalinal1-Ang IV from IRAP-HEK293T membranes with high affinity, which was up to 200-fold greater than in the catalytic assay; this difference was not consistent among the peptides, and could not be ascribed to ligand degradation. Although some AT4 ligands were subject to minor cleavage by HEK293T membranes, none were substrates for IRAP. Of a range of peptides tested, only vasopressin, oxytocin, and met-enkephalin were rapidly cleaved by IRAP. We propose that the physiological effects of AT4 ligands result, in part, from inhibition of IRAP cleavage of neuropeptides involved in memory processing.
Laboratory diagnostic testing for Borrelia burgdorferi infection. (2011)

<title>Abstract</title> This chapter describes the different serological tests and direct assays used for the laboratory diagnosis of <italic>Borrelia burgdorferi</italic> infection. The appropriate use of diagnostic tests is discussed.
New technical solutions in nanotechnology. Part 2 (2016)

The new technical solutions including inventions in the area of nanotechnology and nanomaterials are efficiently applied in communal and housing services as well as in construction and other joint fields. The invention «The diagnostics method for defects on the metal surfaces (RU 2581441)» refers to the methods used to detect defects and cracks on the surface of metal equipment and pipe lines. The suspension of metal nanoparticles is consistently applied on the surface of controlled object following direction from the bigger diameter to the smaller one. The nanoparticles possess the photoluminescence property and their shape is spheric with different diameters. After each application the surface is dried and excessive particles are removed. Then rowwise scanning of object surface is executed with the ray of femtosecond laser and at the same time the intensity of the two-photon luminescence signal is registered in every studied area fixing the location of this area and obtaining the map of glow intensity distribution of nanoparticles exited by the laser radiation. The maps shows the zones with the maximal glow intensity, the coor dinates and shape of the determined glow zone make it possible to determine the coordinates and shape of the defect and the size of its intersection is considered to be equal to relative diameter of the applied nanoparticles at this application stage. The technical stage is increased reliability and credibility of the study. The specialists may be also interested in the following inventions: the method to produce forged pieces from fire-resistant granulated alloys (RU 2583564); the method to produce nanocomposite with double shape memory effect based on monocrystals of ferromagnetic alloy (RU 2583560); the method to produce nanostructured titanium-nickel-zirconium coatings with shape memory (RU 2583222); the method to produce nanocomposites based on golden nanoparticles covered with coating of silica oxide and quantum points (RU 2583022); the nethod to produce polymer composite based on oriented carbon nanotubes (RU 2560382); the method to produce ferromagnetic metal nanoparticles with hard isolation coating (RU 2582870); the method of synthesis of endohedral fullerenes (RU 2582697); the optical measurement system and the method of quantitative measurement of critical size for nanodimensional objects (RU 2582484); the method to produce nanostructured coating and the equipment for its realization (RU 2575667) et al.