gebhart/patrepeval huggingface dataset:
Checkpoint kinase inhibitors: a patent review (2009 – 2010) (2011)

This is an exciting time for checkpoint kinase inhibitors, with several currently in Phase I or II clinical trials. Many of the CHK1 inhibitors contained within this patent review have shown preclinical efficacy in combination with DNA-damaging chemotherapies. CHK1 inhibitors have recently been demonstrated to be efficacious as single agents in preclinical models of tumors with constitutive activation of CHK1 or high intrinsic DNA damage due to replication stress. The level of newly published patent applications covering CHK1 and CHK2 inhibitors remains high and a diverse range of scaffolds has been claimed.
CD40 ligand is required for resolution of Pneumocystis carinii pneumonia in mice (1995)

The role of the CD40-CD40 ligand (CD40L) interaction in resolution of Pneumocystis carinii (PC) pneumonia (PCP) was assessed in a PC-infected severe combined immunodeficiency (SCID) mouse reconstitution model using an anti-CD40L mAb to block CD40L. SCID mice infected with PC were reconstituted with unfractionated spleen cells from immunocompetent donors and given either anti-CD40L mAb or an irrelevant control mAb. Mice given the control mAb resolved the PC infection, whereas those given the anti-CD40L mAb did not. That anti-CD40L mAb also inhibited PC-specific IgG production is consistent with the possibility that cognate CD4+ T cell-B cell interactions are important in PCP resolution. The experiment was then repeated, except that the PC-infected SCID mice were reconstituted with purified CD4+ T cells only. Again, the control mAb-treated group resolved the PCP, whereas mice treated with anti-CD40L mAb did not. In the second experiment, inhibition of resolution of PCP in the anti-CD40L mAb group was not the result of blocking CD4+ T cell-dependent activation of PC-specific B cells. The results are consistent with the possibility that resistance to PCP may involve interaction between B cells and CD4+ T cells via the CD40-CD40L pathway. However, results additionally indicate that inhibition of CD40-CD40L interaction ablates resistance to PCP by inhibiting the interaction of T cells with some cell other than B cells.
The relationship of N-linked glycosylation and heavy chain-binding protein association with the secretion of glycoproteins. (1987)

The relationship of N-linked glycosylation and association with heavy chain binding protein (BiP) to the secretion of Factor VIII (FVIII), von Willebrand Factor (vWF), and tissue plasminogen activator (tPA) was studied in Chinese hamster ovary (CHO) cells. FVIII has a heavily glycosylated region containing 20 clustered potential N-linked glycosylation sites. A significant proportion of FVIII was detected in a stable complex with BiP and not secreted. Deletion of the heavily glycosylated region resulted in reduced association with BiP and more efficient secretion. Tunicamycin treatment of cells producing this deleted form of FVIII resulted in stable association of unglycosylated FVIII with BiP and inhibition of efficient secretion. vWF contains 17 potential N-linked glycosylation sites scattered throughout the molecule. vWF was transiently associated with BiP and efficiently secreted demonstrating that CHO cells are competent to secrete a highly glycosylated protein. tPA, which has three utilized N-linked glycosylation sites, exhibited low level association with BiP and was efficiently secreted. Disruption of N-linked glycosylation of tPA by either site-directed mutagenesis or tunicamycin treatment resulted in reduced levels of secretion and increased association with BiP. This effect was enhanced by high levels of tPA expression. The glycosylation state and extent of association with BiP could be correlated with secretion efficiency.
CORES:  An Automated Method for Generating Three-Dimensional Models of Protein/Ligand Complexes (2004)

We describe a new, automated method for building 3D models of small-molecule ligands complexed with proteins. Modeling templates are constructed from frameworks (i.e., ring systems and linkers) of ligands extracted from 3D structures of ligands complexed with proteins that are structurally related to the target protein. These templates are typically substructures of the target ligand and are used to build models that constrain the ligand's conformation and binding orientation in the active site of the target protein. The practical utility of the method is shown by demonstrating that most ligands containing related frameworks bind protein kinases in the same orientation. Moreover, models for 15 of 19 cdk2/ligand complexes in the protein data bank built using our method deviate from the X-ray structure by less than 2 A (rms). Finally, we show that over 70% of small-molecule protein kinase inhibitors published in J. Med. Chem. since 1993 can be modeled using a template extracted from a 3D protein kinase structure in the protein data bank.
Ovarian Cancer: Review of the National Institute for Clinical Excellence (NICE) Guidance Recommendations (2004)

The National Institute for Clinical Excellence (NICE), established in 1996 as a special Health Authority for England and Wales, provides the United Kingdom medical community with robust and reliable guidance on current "best practices" in medicine. Based on analyses of clinical efficacy, safety, and cost effectiveness, clinical guideline recommendations are developed in an attempt to standardize treatment of various diseases and medical conditions. To date, NICE has issued guidance for the use of three chemotherapeutic agents in the treatment of ovarian cancer: paclitaxel, topotecan, and pegylated liposomal doxorubicin. NICE guidance recommends surgery and adjuvant chemotherapy with paclitaxel/platinum combination therapy or platinum therapy alone as first-line treatment for ovarian cancer. NICE has also issued guidance recommending the use of topotecan or pegylated liposomal doxorubicin as second-line agents for the treatment of women with relapsed or refractory disease. Accounting for all available data, NICE guidance supports the appropriate roles of paclitaxel, topotecan, and pegylated liposomal doxorubicin in the treatment of advanced ovarian cancer.
Onboard locating system using real-time image processing for a self-navigating vehicle (1993)

An onboard location system for a self-navigating vehicle using signposts with bar codes placed along the routes is described. The system has two independent measuring subsystems. The first is a machine vision system composed of an onboard camera, an onboard image processing unit, and signposts. This subsystem measures location and direction of the vehicle by triangulation when the signposts are detected. The second is a dead-reckoning subsystem based on rotation counts for the right and left wheels. Data from these two subsystems are systematically combined by an extended Kalman filter. The experimental results show that an accurate and smooth estimation of the location and direction of the vehicle is obtained.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
A sampling valve for use in gas chromatography adaptable for high pressure or high temperature (1972)

A sampling valve for gases or liquids is described, which is capable of operating at high sample pressures (up to 74 kgf cm-2) or at high temperatures (up to 300 degrees C). For the high pressure operation a Kel F-Teflon-Molykote composite sealing material has been developed. Typical operating conditions are 62 degrees C and 35 kgf cm-2. When provided with sealings of commercially available polyimide the same valve can be used at temperatures as high as 300 degrees C and pressures of a few atmospheres. The valve is particularly suitable for studies in gas kinetics, since very small vapour or liquid samples can be injected directly from a reaction system into the gas chromatographic column.
Pulmonary drug delivery. Part II: The role of inhalant delivery devices and drug formulations in therapeutic effectiveness of aerosolized medications (2003)

Research in the area of pulmonary drug delivery has gathered momentum in the last several years, with increased interest in using the lung as a means of delivering drugs systemically. Advances in device technology have led to the development of more efficient delivery systems capable of delivering larger doses and finer particles into the lung. As more efficient pulmonary delivery devices and sophisticated formulations become available, physicians and health professionals will have a choice of a wide variety of device and formulation combinations that will target specific cells or regions of the lung, avoid the lung's clearance mechanisms and be retained within the lung for longer periods. It is now recognized that it is not enough just to have inhalation therapy available for prescribing; physicians and other healthcare providers need a basic understanding of aerosol science, inhaled formulations, delivery devices, and bioequivalence of products to prescribe these therapies optimally.
Determination of Thickness of a Self-Assembled Monolayer of Dodecanethiol on Au(111) by Angle-Resolved X-ray Photoelectron Spectroscopy (1998)

ADVERTISEMENT RETURN TO ISSUEPREVNoteDetermination of Thickness of a Self-Assembled Monolayer of Dodecanethiol on Au(111) by Angle-Resolved X-ray Photoelectron SpectroscopyToshihiro Kondo, Masatoshi Yanagida, Katsuaki Shimazu, and Kohei UosakiView Author Information Physical Chemistry Laboratory, Division of Chemistry, Graduate School of Science, Hokkaido University, Sapporo 060-0810, Japan, and Division of Material Science, Graduate School of Environmental Earth Science, Hokkaido University, Sapporo 060-0810, Japan Cite this: Langmuir 1998, 14, 19, 5656–5658Publication Date (Web):August 27, 1998Publication History Received4 May 1998Revised7 July 1998Published online27 August 1998Published inissue 1 September 1998https://pubs.acs.org/doi/10.1021/la980517chttps://doi.org/10.1021/la980517cbrief-reportACS PublicationsCopyright © 1998 American Chemical SocietyRequest reuse permissionsArticle Views1850Altmetric-Citations49LEARN 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 SUBJECTS:Alcohols,Gold,Layers,Molecules,Thickness Get e-Alerts
A genetic method for defining DNA-binding domains: application to the nuclear receptor NGFI-B. (1993)

A method is described that allows for rapid and efficient generation of functional mutations in DNA-binding domains of proteins. The target DNA-binding domain is attached to the Gal4p transcriptional-activating domain and expressed in yeast. The binding site recognized by the target domain is placed upstream of a gene that produces a protein toxic to yeast cells, so that the chimeric protein activates its expression, providing a selection against DNA-binding domain function. The chimeric protein also activates expression of a gene necessary for histidine prototrophy, using a second DNA-binding domain included in the chimera (lexA), providing a selection against general activator mutations. Therefore, requiring growth in the absence of histidine focuses mutations to the target DNA-binding domain. This method was applied to the DNA-binding domain of the nuclear receptor NGFI-B. Nearly all mutations obtained concurred with previous studies of NGFI-B and other nuclear receptors, verifying the functional validity of the mutational profile obtained. In addition, by coupling this selection scheme with the two-hybrid system [Chien, C.-t., Bartel, P. L., Sternglanz, R. & Fields, S. (1991) Proc. Natl. Acad. Sci. USA 88, 9578-9582], mutations that alter protein interaction domains could also be obtained.
Analysis of acrylamide and mechanisms of its formation in deep-fried products (2002)

A reliable and sensitive gas chromatography-mass spectrometry method was developed for the determination of acrylamide, a toxic compound recently discovered in baked, fried or grilled food. Satisfactory results for repeatability and recoveries were obtained by this method. The limit of detection for acrylamide was 15 μg/kg food and recoveries were between 95 to 103%. The improved method was then employed to study the influence of heat, heating time and type of frying oil on the formation of acrylamide during the deep frying of French fries. In this matrix acrylamide formation was promoted by heating in a time-dependent manner. It appeared that acrylamide arose, when reducing sugars, dimethylpolysiloxane or partial glycerides were present. Three mechanisms of formation are discussed in this context. Although the mechanistic complexity increases dramatically in the presence of various food components, some recommendations can be given to minimize acrylamide levels in deep fried products.
Nucleotide sequence and functional map of pE194, a plasmid that specifies inducible resistance to macrolide, lincosamide, and streptogramin type B antibodies (1982)

pE194 is a small plasmid (isolated originally in Staphylococcus aureus) which confers erythromycin-inducible resistance to macrolide, lincosamide, and streptogramin type B (MLS) antibiotics. The nucleotide sequence of pE194 contains 3,728 base pairs (bp), corresponding to a molecular mass of 2.4 million daltons. By means of site-specific cleavage with restriction endonucleases and cloning resultant fragments, determinants of the two major biological functions of p E194, i.e., inducible MLS resistance and replication, could be localized and assigned to specific sequences in the plasmid. Restriction endonuclease TaqI cut pE194 at three sites. TaqI fragment A (1,443 bp) contained the determinant for inducible MLS resistance, whereas TaqI fragment B (1,354 bp) contained a determinant necessary for plasmid replication. Regulatory mutations resulting in constitutive expression of MLS resistance mapped in TaqI fragment A, whereas a mutation associated with elevated plasmid copy number was mapped in TaqI fragment B. Also mapping in TaqI fragment B was a plasmid replication determinant comprising two sets of inverted complementary repeat sequences, one of which spanned 124 bp and was adjacent to a second smaller set which was rich in guanine and cytosine residues. pE194 contained six open reading frames which were theoretically capable of coding for proteins with maximum molecular masses as follows (in daltons): A, 48,300; B, 29,200; C, 14,000; D, 13,900; E, 12,600; and F, 2,700. Insertion of plasmid pBR322 into the single PstI site located in frame A of pE194 resulted in a composite plasmid which could replicate in both Bacillus subtilis and Escherichia coli, suggesting that an intact polypeptide A is dispensable for both replication of pE194 and for MLS resistance. Frame B specified inducible MLS resistance, whereas frame F specified the putative peptide associated with the proposed B determinant translational attenuator. The extent to which frames C, D, and E, all contained in TaqI fragment B, were translated into polypeptide products is not known; however, a base change in frame E was found in a comparison between the high-copy-number mutant, cop-6, and the wild-type strains.
The morphology of human pronuclear embryos is positively related to blastocyst development and implantation (2000)

Human embryos are selected for transfer using morphology at the cleaving and blastocyst stages. Zygote morphology has been related to implantation and pregnancy. The aim of this study was to relate pronuclear morphology to blastocyst development. Zygotes were scored according to distribution and size of nucleoli within each nucleus. Zygotes displaying equality between the nuclei had 49.5% blastocyst formation and those with unequal sizes, numbers or distribution of nucleoli had 28% blastocyst formation. Cleaving embryos that were selected initially by zygote morphology and secondarily by morphology on day 3 had increased implantation (IR) and pregnancy rates (PR; 31 and 57%), compared with those selected by morphology alone (19 and 33% respectively; P: < 0.01). There was a significant difference between zygote-scored and non-scored cycles on day 3 (PR: 57 versus 33%; IR: 31 versus 19%) and on day 5 (PR: 73 versus 58%; IR; 52 versus 39%). Zygote scoring can maintain pregnancy rates for both day 3 and day 5 transfers, increase implantation rates and reduce the numbers of embryos required to achieve a pregnancy.
Differential scanning calorimetry studies of irradiated polyethylene: II. The effect of oxygen (1984)

Abstract The effect of absorbed doses of ionizing radiation up to 2MGy in the presence of air on the melting behavior of high‐ and low‐density polyethylene was analyzed from data obtained by differential scanning calorimetry. Thermal measurements were made during the first melting after irradiation. The first melting temperature of polyethylene irradiated in air decreased with increasing absorbed dose. Above approximately 0.6 MGy bimodal endotherms were observed for high‐density polyethylene. The heat of fusion remained unchanged after irradiation in air for absorbed doses of less than 2 MGy. Bimodal endotherms were not obtained for low density polyethylene samples irradiated in air. The changes in melting temperature and the appearance of bimodal endotherms are related to the radiation chemistry of polyethylene in the presence of oxygen.
Agricultural and Food Chemistry: The Road Ahead (1988)

ADVERTISEMENT RETURN TO ISSUEPREVArticleAgricultural and Food Chemistry: The Road AheadCharles Brine and Harry PrebludaCite this: J. Agric. Food Chem. 1988, 36, 4, 875–879Publication Date (Print):July 1, 1988Publication History Published online14 January 2005Published inissue 1 July 1988https://pubs.acs.org/doi/10.1021/jf00083a600https://doi.org/10.1021/jf00083a600research-articleACS PublicationsRequest reuse permissionsArticle Views81Altmetric-Citations1LEARN 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
Addressing insulin resistance in Type 1 diabetes (2008)

Type 1 diabetes is recognised to include an element of insulin resistance. Insulin resistance is an independent risk factor for the development of macro- and microvascular complications of Type 1 diabetes and may also contribute to the development of the disease. This understanding comes at a time when the incidence of Type 1 diabetes appears to be rising and the public health burden from its vascular complications is high. A variety of safe and efficacious manoeuvres are available to redress insulin resistance in Type 2 diabetes. So far however, clinical trials addressing insulin resistance in Type 1 diabetes have been small with only short periods of follow-up. Regardless, these trials have yielded promising results. This review examines the evidence for insulin resistance in the pathophysiology of Type 1 diabetes and its complications, the problems associated with its measurement, and summarizes the trials aimed at reducing insulin resistance in Type 1 diabetes. This includes a meta-analysis of controlled trials of adjuvant metformin in Type 1 diabetes.
A Simple Cipher Governs DNA Recognition by TAL Effectors (2009)

TAL effectors of plant pathogenic bacteria in the genus Xanthomonas bind host DNA and activate genes that contribute to disease or turn on defense. Target specificity depends on an effector-variable number of typically 34 amino acid repeats, but the mechanism of recognition is not understood. We show that a repeat-variable pair of residues specifies the nucleotides in the target site, one pair to one nucleotide, with no apparent context dependence. Our finding represents a previously unknown mechanism for protein-DNA recognition that explains TAL effector specificity, enables target site prediction, and opens prospects for use of TAL effectors in research and biotechnology.
Recycled Materials for Port Construction (1992)

The concept of utilizing recycled materials is presented. Types of materials which may be applicable are described, as well as, typical projects utilizing these materials.
Projected motion group for vision (1993)

For the image understanding and patten recognitions, it is important to extract invariant features from given images corresponding to various transformations. Once the invariant features are obtained, we can estimate motion parameters and/or categorize objects into equivalent classes based on some criterions. So many techniques to extract invariant features are proposed, and most of them need exact matching between an image before transformation and another image after transformation. But this matching process is not easy to perform. Then we propose a group theoretical method, which does not require a matching process. In this paper, we show the bases of the representation of the perspective projected motion group and those of the spherical projected motion group explicitly.
Recombinant human platelet- derived growth factor-BB: a promising role for fibroblast cell attachment in chronic periodontitis. A concentration-dependent effect on human cell adhesion: SEM study (2009)

The present study is aimed to test minimum threshold rhPDGF-BB concentration required to obtain greater root surface biocompatibility and most suitable condition for fibroblast cell attachment and growth in chronic periodontitis. MATERIAL AND METHOD: Proximal surfaces of twenty selected periodontitis teeth were prepared and divided into four groups (ten specimens/each): - I: untreated diseased (control); II: scaling & root planning (SRP); III: SRP then rhPDGF-BB application (50ng/ml); IV: SRP then rhPDGF-BB application (25ng/ml). Fibroblasts were pooled on root specimens, then specimens were incubated. Results of both cell count and shape were assessed by SEM and evaluated repeatedly within a representative standard area. RESULTS: Group II: showed a comparable negative effect, since no significant differences found.Group III: showed a significant positive effect, higher than both groups I & II but lower than group IV. Group IV: demonstrated the best results for cell quantity & quality, where it had favorable significant differences when compared to all others. CONCLUSION: rhPDGF-BB with 25ng/ml concentration showed a more positive effect in getting higher fibroblast cell count & more healthy cell shape than rhPDGF-BB (50ng/ml). A promising role of rhPDGF-BB (25ng/ml) as good modulating agent for fibroblast cell attachment in chronic periodontitis may be suggested