gebhart/patrepeval huggingface dataset:
Prodrugs of thymidylate synthase inhibitors: potential for antibody directed enzyme prodrug therapy (ADEPT). (1996)

Prodrugs of quinazoline antifolate thymidylate synthase (TS) inhibitors have been designed and synthesized for use in antibody-directed enzyme prodrug therapy (ADEPT). The syntheses of the alpha-linked dipeptides of two potent thymidylate synthase inhibitors, ZD1694 [N-[5-[N-(3,4-dihydro-2-methyl-4-oxoquinazolin-6- ylmethyl)-N-methylamino]-2-thenoyl]-L-glutamic acid] and ICI198583 ¿N-[4-[N-[(2-methyl-3,4-dihydro-4-oxo-6-quinazolinyl) methyl]-N-prop-2-ynylamino]benzoyl]-L-glutamic acid¿ are described. The alpha-carboxyl of the glutamic acid has been linked through an amide bond to an L-alanine or an L-glutamic acid. The alpha-linked L-dipeptide prodrugs were designed to be activated to their corresponding thymidylate synthase inhibitors at a tumour site by prior administration of a monoclonal antibody conjugated to the enzyme carboxypeptidase A (CPA). The viability of a colorectal cell line was monitored with the potential prodrugs in the presence or absence of CPA or with the parent drugs alone. All the dipeptides had greatly decreased cytotoxicity, with a deactivation of approximately 100-fold for the ZD1694 prodrugs and approximately 20-200-fold for the ICI198583 prodrugs. Activation of the alpha-linked L-alanine dipeptides with CPA led to a cytotoxicity enhancement of approximately 10-100 fold.
O-chain expression in the rough Brucella melitensis strain B115: induction of O-polysaccharide-specific monoclonal antibodies and intracellular localization demonstrated by immunoelectron microscopy (1992)

Spleen cells from mice infected with the rough Brucella melitensis strain B115 were fused with NSO myeloma cells. Hybridoma supernatants were screened in ELISA with cell walls (CW), sonicated cell extracts (CE) and rough lipopolysaccharide (R-LPS) of B. melitensis strain B115 and whole B. melitensis B115 cells. Surprisingly, 22 monoclonal antibodies (mAbs) reacting in ELISA with both CW and CE but not with R-LPS and bacterial cells were shown by immunoblot analysis and ELISA to react with smooth lipopolysaccharide (S-LPS). These mAbs also reacted in ELISA with O polysaccharides (OPS) from the smooth Brucella abortus strain 99 and the smooth B. melitensis strain 16M and thus recognize epitopes present on the O-chain. Proteinase K LPS preparations from B. melitensis B115 analysed by immunoblotting with one mAb (12G12) recognizing S-LPS of both A and M specificity displayed the typical S-LPS high-molecular-mass ladder pattern but no S-LPS was detected in the phenol/water/chloroform/light petroleum LPS preparation of the same strain. mAb 12G12, specific for S-LPS, and a mAb (A68/03F03/D05) specific for R-LPS were used to localize the O-chain and R-LPS expressed in B. melitensis strain B115 by immunoelectron microscopy. Immunogold labelling was observed at the surface of B. melitensis B115 cells with the anti-R-LPS mAb but not with the anti-S-LPS mAb. In ultrathin sections, immunogold labelling with the S-LPS specific mAb was observed in the cytoplasm and in the periphery of the cytoplasm, probably at the cytoplasmic membrane.(ABSTRACT TRUNCATED AT 250 WORDS)
Cryptosporidiosis: Clinical, Epidemiologic, and Parasitologic Review (1984)

Cryptosporidium, an intestinal protozoan parasite, is a well-known cause of diarrhea in animals but has been recognized only recently as a cause of human disease. Since 1976, 58 cases of cryptosporidiosis in humans have been reported; 18 of the patients had normal immune function, and 40 had various immunologic abnormalities, the most common of which, acquired immune deficiency syndrome (AIDS), occurred in 33 patients. Patients with normal immune function had self-limited diarrhea, but patients with immunologic abnormalities often developed severe, irreversible diarrhea; 22 patients have died. The diagnosis of cryptosporidiosis can now be made noninvasively, but increased diagnostic proficiency has led to little improvement in control or treatment of the disease. Although 23 compounds have been evaluated in experimentally infected animals and 20 drugs have been used in human clinical trials, no effective chemotherapeutic agent for cryptosporidiosis has been identified to date.
Synthesis and biological activity of LH-RH analogs substituted by alkyltryptophans at position 3. (1979)

Seven analogs of luteinizing hormone-releasing hormone (LH-RH), in which the Trp residue at position 3 was replaced by various methyltryptophans and 1-ethyltryptophan, were synthesized and their LH-releasing activities were evaluated. All of these analogs showed reduced hormonal activity compared with synthetic LH-RH.
Metal induced crystallized poly-Si-based conductive bridge resistive switching memory device with one transistor and one resistor architecture (2015)

In this letter, the metal induced crystallization (MIC) process is used in the Si-based conductive bridging resistive random access memory (CBRAM) application. The amorphous Si (a-Si) is transformed to crystallized poly-silicon (poly-Si) at a low temperature by using Ni metal for inducing poly-Si to provide the resistive switching. The MIC process can produce a highly preferred orientation poly-Si film, which can create the exact paths or grain boundaries through the top and down electrodes in the present CBRAM device. The grain boundary in MIC poly-Si layer can confine the conductive filament of metal bridging growth in it, which can improve the switching fluctuation behavior in the nonvolatile memory application. Compared with the a-Si based device, a significant improvement in terms of resistive switching parameters such as stability and resistance distribution is demonstrated in the MIC poly-Si CBRAM device. Moreover, the well-behaved memory performance, such as high ON/OFF resistance ratio (4 order), a large AC endurance (106), and good retention characteristics (104 s at 125 °C) are achieved in the Cu/poly-Si/n+-Si CMOS compatible cross bar structure.
Microemulsions as potential drug delivery systems: a review. (2008)

By many estimates, up to 40 percent of new chemical entities discovered by the pharmaceutical industry are poorly soluble or lipophilic compounds. Solubilization of hydrophobic drugs with low aqueous solubility has been a major area of interest in recent years. Various solubilization techniques involve the use of co-solvents and surfactants along with pH adjustments. Applications of microemulsions have also drawn attention in the field of solubilization techniques. Microemulsions are optically isotropic and thermodynamically stable systems consisting of water, oil, a surfactant, and a co-surfactant and are known to enhance the bioavailability of drugs via topical and systemic routes. The objective of this review is to present briefly the possible applications of these novel systems of microemulsions. Most studies reported in the literature have investigated microemulsions intended for dermatological application because of the wider range of potential excipients.
Diamidino-.alpha.,.omega.-diphenoxyalkanes. Structure-activity relations for the inhibition of thrombin, pancreatic kallikrein, and trypsin (1973)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDiamidino-.alpha.,.omega.-diphenoxyalkanes. Structure-activity relations for the inhibition of thrombin, pancreatic kallikrein, and trypsinJ. D. Geratz, Alan C. Whitmore, Michael C. F. Cheng, and Claude PiantadosiCite this: J. Med. Chem. 1973, 16, 9, 970–975Publication Date (Print):September 1, 1973Publication History Published online1 May 2002Published inissue 1 September 1973https://pubs.acs.org/doi/10.1021/jm00267a003https://doi.org/10.1021/jm00267a003research-articleACS PublicationsRequest reuse permissionsArticle Views138Altmetric-Citations33LEARN 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
Photoinduced Phase Transition in an Organic Radical Crystal with Room-Temperature Optical and Magnetic Bistability (2003)

A phase control by photoirradiation is successfully achieved in a spin-Peierls system of the organic radical crystal, 1,3,5-trithia-2,4,6-triazapentalenyl (TTTA), which exhibits optical and magnetic bistability around room temperature with a large hysteresis loop. A nanosecond laser pulse is found to induce a transition from a diamagnetic low-temperature phase to a paramagnetic high-temperature phase both inside (296 K) and outside (11 K) the hysteresis loop. Comparison of the excitation energy dependence between transition efficiency and photoconductivity suggests that the photoinduced transition is driven by suppression of the spin-Peierls instability by the accumulation of photocarriers.
Development of the Implantable Glucose Sensor: What Are the Prospects and Why Is It Taking So Long? (1995)

The development of an implantable glucose sensor for use in diabetes was first suggested in the 1960s (1–3). The sensor would provide an alternative to the present discrete methods of glucose determination that are based on intermittent blood sampling. Continuous glucose sensing would be particularly important in the detection and management of hypoglycemia. It would also allow early detection of hyperglycemia and provide a basis for insulin administration at more appropriate dosages and timing or for automatic insulin delivery from a pump. An implantable glucose sensor could also be used in parallel with other existing or potential forms of insulin replacement, such as transplantation or hybrid islet devices.
Long-Term Rescue of Retinal Structure and Function by Rhodopsin RNA Replacement with a Single Adeno-Associated Viral Vector in P23H RHO Transgenic Mice (2012)

Many mutations in the human rhodopsin gene (RHO) cause autosomal dominant retinitis pigmentosa (ADRP). Our previous studies with a P23H (proline-23 substituted by histidine) RHO transgenic mouse model of ADRP demonstrated significant improvement of retinal function and preservation of retinal structure after transfer of wild-type rhodopsin by AAV. In this study we demonstrate long-term rescue of retinal structure and function by a single virus expressing both RHO replacement cDNA and small interfering RNA (siRNA) to digest mouse Rho and human P23H RHO mRNA. This combination should prevent overexpression of rhodopsin, which can be deleterious to photoreceptors. On the basis of the electroretinogram (ERG) response, degeneration of retinal function was arrested at 2 months postinjection, and the response was maintained at this level until termination at 9 months. Preservation of the ERG response in P23H RHO mice reflected survival of photoreceptors: both the outer nuclear layer (ONL) and outer segments of photoreceptor cells maintained the same thickness as in nontransgenic mice, whereas the control injected P23H eyes exhibited severe thinning of the ONL and outer segments. These findings suggest that delivery of both a modified cDNA and an siRNA by a single adeno-associated viral vector provided long-term rescue of ADRP in this model. Because the siRNA targets human as well as mouse rhodopsin mRNAs, the combination vector may be useful for the treatment of human disease.
Sensitive detection of bacterial transcription initiation sites and differentiation from RNA processing sites in the pheromone-induced plasmid transfer system of Enterococcus faecalis. (1996)

A method was developed to detect 5' ends of bacterial RNAs expressed at low levels and to differentiate newly initiated transcripts from processed transcripts produced in vivo. The procedure involves use of RNA ligase to link a specific oligoribonucleotide to the 5' ends of cellular RNAs, followed by production of cDNA and amplification of the gene of interest by PCR. The method was used to identify the precise sites of transcription initiation within a 10-kb region of the pheromone-inducible conjugative plasmid pCF10 of Enterococcus faecalis. Results confirmed the 5' end of a very abundant, constitutively produced transcript (from prgQ) that had been mapped previously by primer extension and defined the initiation point of a less abundant, divergently transcribed message (from prgX). The method also showed that the 5' end of a pheromone-inducible transcript (prgB) that had been mapped by primer extension was generated by processing rather than new initiation. In addition, the results provided evidence for two promoters, 3 and 5 kb upstream of prgB, and indicated that only the transcripts originating 5 kb upstream may be capable of extending to prgB.
Regression of fetal cerebral abnormalities by primary cytomegalovirus infection following hyperimmunoglobulin therapy (2008)

The outcomes of the infants born to HIG-treated mothers support the efficacy of HIG as a treatment for CMV-infected fetuses with ultrasound cerebral abnormalities.
Ceria Based Nano-Scale Catalysts For Water-Gas Shift (WGS) Reaction (2004)

This paper describes our research efforts towards the preparation of high surface area ceria oxide (CeO2) containing catalysts for fuel processing and therefore for fuel cells applications. In the present work, we present a simple. single step flame synthesis method to prepare high surface area ceria based fuel reformation catalysts using aqueous solutions of metal acetate precursors. The specific surface areas of the synthesized powders are in the range of 130 and 163(meter squared)/g. High-resolution transmission electron microscopic (TEM) characterization showed that the particle sizes for the ceria materials are in the range of 3 and 10 nm. X-ray diffraction (XRD) and X-ray photoelectron spectra show the presence of transition metal oxide in the as prepared catalysts. The catalysts also test for water-gas-shift (WGA) reaction.
Human neurological cancer cells express interleukin‐4 (IL‐4) receptors which are targets for the toxic effects of IL4‐pseudomonas exotoxin chimeric protein (1994)

Glioblastoma, glioma or neuroblastoma cells were examined for the expression of IL-4 receptors (IL-4R) by flow cytometric analysis and 125I-IL-4 binding. These cancer cell lines expressed IL-4R which were of high affinity (KD = 700 x 10(-12) M) on glioblastoma cells. To investigate the function of these receptors and to target potent cytotoxic antitumor agents to human neurological cancers, we utilized IL4-PE4E, which is composed of IL-4 and mutant Pseudomonas exotoxin (IL4-PE4E). This chimeric molecule was cytotoxic toward human glioblastoma, neuroblastoma and glioma tumor cells in a dose-dependent manner. The cytotoxicity of IL4-PE4E was specific, since it was neutralized by excess IL-4, and by an anti-IL-4 monoclonal antibody in all types of brain tumor tested. IL2-PE4E and IL6-PE4E were not cytotoxic, nor was an IL4-PE4E mutant lacking ADP-ribosylating activity, indicating the IL4-PE4E-mediated cytotoxicity of the brain tumor cells required both IL-4R binding and enzymatic toxin activity. These data indicate that human neurological cancer cells express IL-4R which are targets for the cytotoxic effects of IL4-toxin. In addition, our data also suggest that IL4-PE4E should be studied further as a potential treatment for human neurological cancers.
Surfimage (1998)

for cozienf-based image Tetieval, most of the cument systems aTe "tigid", i.e. they rettieve a fied set of images as Tesponse to a given que~and an image featuTe. We introduce S=fitaage, a useT-fiendly, genetic and flw-ble content-based image TetievaI system. Stiiatage wes the que~-by-sample appToach for ~ettieving images and integrate advanced ~eatuTessuch as image signatuTe combination, classification, multiple queti~and queq Refinement. The classic and advanced featuTes of SMiraage aTe detaild in the papeT. Stiiraage has been eztensive[y t~ted oz dozens of databas~and p~oauced ezcellent Tetm-evalTe-S-dts; a sample of Tetm"evaTau~ts h pr~ented here. I
Recent trends in pediatric Haemophilus influenzae type B infections in Canada. Immunization Monitoring Program, Active (IMPACT) of the Canadian Paediatric Society and the Laboratory Centre for Disease Control. (1996)

The prevalence of Hib infections reported by the IMPACT centres has declined greatly since the introduction of vaccination programs. However, deaths and complications continue to occur, attesting to the need to vaccinate all eligible infants and children against this virulent pathogen.
SoftBridge in action: the first Deaf telephony pilot (2003)

The effect of thyroidectomy on the activity of liver alcohol dehydrogenase and on the rate of ethanol elimination was determined in the rat. Thyroidectomy resulted in a marked increase in liver alcohol dehydrogenase activity. Three isoenzymes of alcohol dehydrogenase activity were demonstrated in thyroidectomized animals by starch gel electrophoresis, as compared with two in sham-operated control animals. Triiodothyronine administration decreased the enzyme activity in control animals, and suppressed the enhanced activity in thyroidectomized animals. Inhibition of alcohol dehydrogenase by triiodothyronine in vitro was found to be competitive with respect to NAD+ and uncompetitive with respect to ethanol in both contrast and thyroidectomized animals. Thyroidectomy did not result in any changes in the rate of ethanol elimination. The cytosolic free NAD+/NADH ratio decreased after ethanol administration in both control and thyroidectomized animals, while the mitochondrial-free NAD+/NADH ratio decreased only in the control animals. These results indicate that the thyroid is a repressor of liver alcohol dehydrogenase activity. A defect in the transfer of reducing equivalents from the cytosol to the mitochondria appears to limit the rate of ethanol elimination in thyroidectomized animals with increased liver alcohol dehydrogenase activity.
Performance of microstrip patch antenna withelectrically thick laminated glass superstrate (1994)

The effects of a laminated glass superstrate on both the radiation pattern and the impedance bandwidth of a microstrip patch antenna are reported. It is shown that nulls that appear in the radiation pattern of the antenna, due to surface wave effects, can be successfully eliminated by the use of a layer of resistive film. The bandwidth of the antenna is significantly increased to ~20% while the gain is maintained at 5–6 dB.
Bacterial Isolation by Lectin-Modified Microengines (2011)

New template-based self-propelled gold/nickel/polyaniline/platinum (Au/Ni/PANI/Pt) microtubular engines, functionalized with the Concanavalin A (ConA) lectin bioreceptor, are shown to be extremely useful for the rapid, real-time isolation of Escherichia coli (E. coli) bacteria from fuel-enhanced environmental, food, and clinical samples. These multifunctional microtube engines combine the selective capture of E. coli with the uptake of polymeric drug-carrier particles to provide an attractive motion-based theranostics strategy. Triggered release of the captured bacteria is demonstrated by movement through a low-pH glycine-based dissociation solution. The smaller size of the new polymer-metal microengines offers convenient, direct, and label-free optical visualization of the captured bacteria and discrimination against nontarget cells.
Array-based comparative genomic hybridization reveals recurrent chromosomal aberrations and Jab1 as a potential target for 8q gain in hepatocellular carcinoma (2005)

Hepatocellular carcinoma (HCC) is one of the major malignancies worldwide. We have previously characterized global gene expression patterns in HCC using microarrays. Here, we report the analysis of genomic DNA copy number among 49 HCC samples using BAC array-based comparative genomic hybridization (CGH). We observed recurrent and characteristic chromosomal aberrations, including frequent DNA copy number gains of 1q, 6p, 8q and 20q, and losses of 4q, 8p, 13q, 16q and 17p. We correlated gene expression with array CGH data, and identified a set of genes whose expression levels correlated with common chromosomal aberrations in HCC. Especially, we noticed that high expression of Jab1 in HCC significantly correlated with DNA copy number gain at 8q. Quantitative microsatellite analysis further confirmed DNA copy number gain at the Jab1 locus. Overexpression of Jab1 in HCC was also validated using real-time RT-PCR, and Jab1 protein levels were studied by immunohistochemistry on tissue microarrays. Functional analysis in HCC cell lines demonstrated that Jab1 may regulate HCC cell proliferation, thereby having a potential role in HCC development. In conclusion, this study shows that arraybased CGH provides high resolution mapping of chromosomal aberrations in HCC, and demonstrates the feasibility of correlating array CGH data with gene expression data to identify novel oncogenes and tumor suppressor genes.
Human Transcription Factor hTAFII150 (CIF150) Is Involved in Transcriptional Regulation of Cell Cycle Progression (1999)

Here we present evidence that CIF150 (hTAF(II)150), the human homolog of Drosophila TAF(II)150, plays an important and selective role in establishing gene expression patterns necessary for progression through the cell cycle. Gel filtration experiments demonstrate that CIF150 (hTAF(II)150) seems to be less tightly associated with human transcription factor IID than hTAF(II)130 is associated with hTAF(II)250. The transient functional knockout of CIF150 (hTAF(II)150) protein led to cell cycle arrest at the G(2)/M transition in mammalian cell lines. PCR display analysis with the RNA derived from CIF150-depleted cells indicated that CIF150 (hTAF(II)150) is required for the transcription of only a subset of RNA polymerase II genes. CIF150 (hTAF(II)150) directly stimulated cyclin B1 and cyclin A transcription in cotransfection assays and in vitro assays, suggesting that the expression of these genes is dependent on CIF150 (hTAF(II)150) function. We defined a CIF150 (hTAF(II)150) consensus binding site and demonstrated that a CIF150-responsive cis element is present in the cyclin B1 core promoter. These results suggest that one function of CIF150 (hTAF(II)150) is to select specific RNA polymerase II core promoter elements involved in cell cycle progression.
Immunohistochemical Detection of Porcine Rotavirus Using Immunogold Silver Staining (IGSS) (1992)

Immunogold silver staining (IGSS) was applied for the detection of porcine group A rotavirus in formalin-fixed paraffin-embedded tissue sections of small intestine. Prior to the application of IGSS, the reactivity of protein A-gold as a marker was tested with group-specific antiserum in immunogold electron microscopy. Immune aggregates were intensely and specifically labeled with the gold complex. Application of IGSS to tissue sections resulted in specific dark staining of villous enterocytes infected by group A rotavirus. This method also proved effective for the detection of rotaviral antigen in infected cultured cells. The IGSS method may be suitable for routine diagnostic detection of rotaviral infections and may have application for detection of other viral pathogens of veterinary importance.