gebhart/patrepeval huggingface dataset:
Stable Phosphazenium Ions in Synthesis—an Easily Accessible, Extremely Reactive “Naked” Fluoride Salt (1991)

The strongest metal-free base is the cation 1, which can be prepared in a one-pot procedure from PCl5, NH4Cl, Me2NH, and NaBF4. Anion exchange affords 1-F, which mediates in the alkylation of an anionic allylic species produced from allyltrimethylsilane; furthermore, the unsolvated floride ion is an excellent proton-selective base for E2 eliminations.
A note on 'Efficient numerically stabilized rank-one eigenstructure updating' (and reply) (1991)

In the above-named paper, R.D. DeGroat and R.A. Roberts (see ibid., vol.38, no.2, p.301-16, Feb. 1990) developed a reorthogonalization scheme for stabilizing eigenstructure updating algorithms. The commenters show that only part of this scheme, namely the renormalization, is essential for the stability, so that a cheaper scheme, with roughly half as many computations, can perform equally well. DeGroat addresses two points raised by the commenters' work.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Monoclonal antibody to human high-molecular-weight kininogen recognizes its prekallikrein binding site and inhibits its coagulant activity (1989)

We developed a mouse monoclonal antibody (MoAb 115–21) to human high- molecular-weight kininogen (HK) that recognizes its prekallikrein binding site (residues 565 through 595 of HK). The corresponding synthesized 31-amino acid peptide (peptide IV) was recently shown to retain native HK's prekallikrein binding property. The same peptide bound factor XI also, although less avidly. Our MoAb recognizes purified HK, peptide IV, and the light chain moiety of HK (where the peptide IV resides), as shown by enzyme-linked immunosorbent assay (ELISA) and Western blotting experiments. The apparent dissociation constant for the HK and MoAb 115–21 interaction was 2.2 nmol/L. It does not recognize low-molecular-weight kininogen (LK) with which HK shares its heavy chain moiety or any antigens in human plasma congenitally deficient in kininogens. The binding of MoAb 115–21 to purified light chain of HK was competitively inhibited by peptide IV. In addition, the antibody inhibits HK-dependent clotting activity of normal human plasma and dextran sulfate-mediated activation of prekallikrein in plasma and retards cleavage of HK in normal plasma after contact activation with dextran sulfate. Also, purified Fab fragments of MoAb 115–21 inhibited the HK-dependent coagulant activity and dextran sulfate-mediated prekallikrein activation in normal plasma. Since the kd for HK-MoAb 115– 21 interaction is ten times lower than that of HK-prekallikrein, our data suggest that binding of MoAb 115–21 to HK's peptide IV site increases the free prekallikrein concentration in plasma and thus results in the decreased efficiency of factor XIIa-mediated activation of prekallikrein. Decreased levels of kallikrein thus formed may be responsible for the inhibition of HK-dependent clotting activity and the decrease in rate and extent of HK cleavage in normal plasma on contact activation with dextran sulfate. MoAb 115–21 may thus prove very useful, especially with its high affinity for HK, in further delineation of the role of HK and prekallikrein in contact activation and kinin-related human pathology.
Prostaglanin-E2 Potentiates the Suppressive Functions of Human Mononuclear Myeloid-Derived Suppressor Cells and Increases Their Capacity to Expand IL-10-Producing Regulatory T Cell Subsets (2019)

Myeloid-derived suppressor cells (MDSC) emerged as major factors driving the tumor progression due to numerous immunosuppressive mechanisms they possess. Prostaglandin (PG)E2 is shown critical for the induction of MDSC and their suppressive functions <i>in vivo</i>, but it is poorly understood how it affects the capacity of MDSC to induce different subsets of regulatory T cells (Treg). By using a novel protocol for the generation of mononuclear (M)-MDSC, we showed that PGE2 potentiates the GM-CSF/IL-6-dependent induction of CD33<sup>+</sup>CD11b<sup>+</sup>HLA-DR<sup>-</sup>CD14<sup>+</sup> M-MDSC <i>in vitro</i>. PGE2 diminished the capacity of GM-CSF/IL-6 M-MDSC to produce proinflammatory cytokines upon activation and augmented their capacity to produce IL-27, IL-33, and TGF-β. These results correlated with an increased potential of GM-CSF/IL-6/PGE2 M-MDSC to suppress T cell proliferation, expand alloreactive Th2 cells, and reduce the development of alloreactive Th17 and cytotoxic T cells. Interestingly, GM-CSF/IL-6/PGE2 M-MDSC displayed a lower capacity to induce TGF-β-producing FoxP3<sup>+</sup> regulatory Treg compared to GM-CSF/IL-6 M-MDSC, as a consequence of reduced IDO-1 expression. In contrast, GM-CSF/IL-6/PGE2 M-MDSC potentiated IL-10 production by CD8<sup>+</sup>T, Th2, and particularly CD4<sup>+</sup>FoxP3<sup>-</sup> type 1 Treg, the latter of which depended on ILT3 and ILT4 expression. Cumulatively, PGE2 potentiated the suppressive phenotype and functions of GM-CSF/IL-6-induced M-MDSC and changed the mechanisms involved in Treg induction, which could be important for investigating new therapeutic strategies focused on MDSC-related effects in tumors and autoimmune diseases.
Uniformity of the Splicing Pattern of the E6/E7 Transcripts in Human Papillomavirus Type 16-transformed Human Fibroblasts, Human Cervical Premalignant Lesions and Carcinomas (1990)

We utilized the RNA polymerase chain reaction (PCR) to analyse the transcripts of the E6/E7 open reading frames of human papillomavirus type 16 (HPV-16). Total RNA was isolated from 14 cervical squamous carcinomas, nine cervical intraepithelial neoplasias and from human fibroblasts transformed with different HPV-16 constructs. In all specimens two spliced transcripts were detected. Sequence analysis of the cloned PCR products showed that both transcripts were generated by splicing out an intron in E6, from nucleotides (nt) 226 to 409 in one transcript and from nt 226 to 526 in the other. The major transcript present in all RNA specimens had the smallest intron in E6. The RNA PCR described here is the method of choice for analysing splice and donor sites in tissue specimens where a limited amount of RNA is available. Results obtained with transformed cells revealed no difference in splicing whether HPV-16 was controlled by its homologous promoter or by a heterologous promoter, the Rous sarcoma virus long terminal repeat.
Estimation of ten-year risk of fatal cardiovascular disease in Europe: the SCORE project (2003)

The SCORE risk estimation system offers direct estimation of total fatal cardiovascular risk in a format suited to the constraints of clinical practice.
On a Potential Global Role for Vitamin K-dependent γ-Carboxylation in Animal Systems (2001)

The vitamin K-dependent gamma-carboxylation of glutamate to gamma-carboxyglutamate was originally well characterized in the mammalian blood clotting cascade. gamma-Carboxyglutamate has also been found in a number of other mammalian proteins and in neuropeptides from the venoms of marine snails belonging to the genus Conus, suggesting wider prevalence of gamma-carboxylation. We demonstrate that an open reading frame from a Drosophila melanogaster cDNA clone encodes a protein with vitamin K-dependent gamma-carboxylase activity. The open reading frame, 670 amino acids in length, is truncated at the C-terminal end compared with mammalian gamma-carboxylase, which is 758 amino acids. The mammalian gene has 14 introns; in Drosophila there are two much shorter introns but in positions precisely homologous to two of the mammalian introns. In addition, a deletion of 6 nucleotides is observed when cDNA and genomic sequences are compared. In situ hybridization to fixed embryos indicated ubiquitous presence of carboxylase mRNA throughout embryogenesis. Northern blot analysis revealed increased mRNA levels in 12-24-h embryos. The continued presence of carboxylase mRNA suggests that it plays an important role during embryogenesis. Although the model substrate FLEEL is carboxylated by the enzyme, a substrate containing the propeptide of a Conus carboxylase substrate, conantokin G, is poorly carboxylated. Its occurrence in vertebrates, molluscan systems (i.e. Conus), and Drosophila and the apparently strong homology between the three systems suggest that this is a highly conserved and widely distributed post-translational modification in biological systems.
Immobilized Polydiacetylene Vesicles on Solid Substrates for Use as Chemosensors (2003)

Polydiacetylene‐based chemosensors are prepared by assembling liposomes of diacetylene monomers with terminal amine groups on an aldehyde‐modified glass substrate, and polymerizing them by irradiation with UV light. Incubation of the immobilized film sensor in a poly(acrylic acid) solution results in a color change from the original blue (solid line in Figure) to the red phase (broken line).
Heat and moisture exchangers and the body temperature: a peroperative study (1990)

The importance of conditioning the inhaled gas for maintaining the body temperature during artificial respiration was investigated. The mean body temperature (MBT) was deduced from readings from five measuring sites, four of which were situated at the skin and the fifth in the rectum. Temperature recordings were made every 15th min. Twenty patients were admitted to the study. In 10 patients a heat and moisture exchanger was used (the HME group), and the other 10 were ventilated without an HME (the control group). The patients were normoventilated, and a non-rebreathing system was used. All operations were made in the ENT-region of the body. Great care was taken to avoid variation of external factors that may affect the MBT. We found that the MBT decreased 0.2 degrees C/h less in the HME group than in the control group. If corrections were made for differences in amounts of fluids given and age factors, a difference in heat loss of 41.6 kJ/h between the two groups could be derived from this figure. This difference was statistically significant. Our finding correlated fairly well with a predicted reduction of heat loss of 26.0 kJ/h for the type of HME used. A certain margin of error seemed to be inevitable in measuring body temperatures, and the reason for this is discussed. Our results support the fact that the investigation is adequately designed, and that the heat conserved with an HME is rather low.
Plasmodium falciparum gene encoding a protein similar to the 78-kDa rat glucose-regulated stress protein. (1988)

Genes homologous to heat shock protein 70 have been described in parasitic protozoa. It has been proposed that they may be important to the parasite as it moves from the vertebrate host at 37 degrees C to the insect. We now describe a genomic DNA clone isolated from Plasmodium falciparum that encodes a protein similar in sequence to a mammalian heat shock-related protein, the 78-kDa glucose-regulated protein of rat and hamster. The gene is expressed during the erythrocytic stage in both asexual and sexual parasites (RNA blot analysis) and a 72-kDa protein is immunoprecipitated from erythrocytic stage parasites. Importantly, the sequence of the clone is similar to the canonical sequence at the carboxyl termini of glucose-regulated proteins of mammals that determines their localization within endoplasmic reticulum. Since the parasite sequence has only three (Asp-Glu-Leu) of the four carboxyl-terminal amino acids, its location and its function within the parasite remain to be determined.
Azaphilones Inhibit Tumor Promotion by 12-O-Tetradecanoylphorbol-13-Acetate in Two-Stage Carcinogenesis in Mice (1994)

Monascorubrin (an azaphilone derivative) was isolated from Monascus anka, 'Monascus pigment', a natural pigment of food additivies, was extracted from Monasucs spp., and chaetoviridin A, one of the azaphilones, was isolated from Chaetomium globosum var. flavo-viridae. Application of 1 microgram of 12-O-tetradecanoylphorbol-13-acetate (TPA), a tumor promoting agent, to the mouse ear resulted in induction of inflammation. Among monascorubrin and related compounds assayed, monascorubrin, chaetoviridin A and its related compounds inhibited the inflammatory activity of TPA in mice. The 50% inhibitory dose of these compounds for TPA-induced inflammation was 0.4-1.5 mumol. Furthermore, monascorubrin (2 mumol), chaetoviridin A (2 mumol) and Monascus pigment (1 mg) markedly suppressed the promoting effect of TPA (1 microgram) on skin tumor formation in mice initiated with 7,12-dimethylbenz[a]anthracene (50 micrograms). It is assumed that the inhibition of tumor promotion by monascorubrin, chaetoviridin A and Monascus pigment is due to anti-inflammatory activity.
Cytoplasmic RNA modulators of an inside-out signal-transduction cascade (1999)

A vaccinia virus-based RNA expression system enabled high-level cytoplasmic expression of RNA aptamers directed against the intracellular domain of the beta2 integrin LFA-1, a transmembrane protein that mediates cell adhesion to intercellular adhesion molecule-1 (ICAM-1). In two different cell types, cytoplasmic expression of integrin-binding aptamers reduced inducible cell adhesion to ICAM-1. The aptamers specifically target, and thereby define, a functional cytoplasmic subdomain important for the regulation of cell adhesion in leukocytes. Our approach of aptamer-controlled blocking of signaling pathways in vivo could potentially be applied wherever targeted modulation of a signal-transduction cascade is desired.
Electron-transporting materials for organic electroluminescent and electrophosphorescent devices (2004)

One of the requirements for efficient organic electroluminescent devices (OLEDs) is balanced charge injection from the two electrodes and efficient transport of both holes and electrons within the luminescent layer in the device structure. Many of the common luminescent conjugated polymers, e.g. derivatives of poly(phenylenevinylene) and poly(fluorene), are predominantly hole transporters (i.e. p-dopable). This article gives a brief overview of organic electroluminescence and electrophosphorescence and provides a more detailed consideration of ways in which electron transport in these systems has been enhanced by the incorporation of electron-deficient (i.e. n-dopable) small molecules and polymers into the devices, either as blends or by covalent attachment of sub-units to the luminophore or as an additional electron-transporting, hole-blocking (ETHB) layer adjacent to the cathode. The chemical structures of these systems are presented and their roles are assessed. Most of these ETHB molecules are electron-deficient aromatic nitrogen-containing heterocycles, e.g. derivatives of 1,3,4-oxadiazole, pyridine, pyrimidine, pyrazine, quinoline, etc. Non-aromatic thiophene-S,S-dioxide derivatives are also discussed. The article is written from an organic chemist's perspective.
A 34-amino acid peptide of the third component of complement mediates properdin binding. (1988)

Abstract In this study, a peptide of 34 amino acids from the Mr 40,000 C terminus alpha-chain fragment of C3 was found to mediate properdin (P) binding. Treatment of the Mr 40,000 fragment with CNBr generated one major Mr 17,000 fragment that was capable of binding P. Amino acid sequence data placed the Mr 17,000 fragment within residues 1385 to 1540 of the C3 sequence. After analyzing this sequence for highly conserved segments within the C3 from other species (which bind P) and segments of low similarity within human C4, mouse C5, and alpha2-macroglobulin (which do not bind P), a 34-amino acid (1402 to 1435) peptide was synthesized. This synthetic peptide bound to P and inhibited its binding to C3b. In addition, it exhibited negative regulatory activity on the alternative pathway as it inhibited the lysis of rabbit erythrocytes by normal human serum. These results show that the P-binding site is located within the residues 1402 to 1435 of the C3 sequence.
Super-Liquid-Repellent Surfaces Prepared by Colloidal Silica Nanoparticles Covered with Fluoroalkyl Groups (2005)

A simple and easy method to prepare super-liquid-repellent surfaces is proposed. Sol-gel films were prepared by hydrolysis and condensation of alkoxysilane compounds. Both surface energy and roughness were controlled using colloidal silica particles and fluoroalkylsilane. When the fractional amounts of both colloidal silica and fluoroalkylsilane were optimized in the films, the film surface exhibited repellency to both water and oil. Finally, it was shown that the method proposed here would be applied to a simple one-pot coating for a uniform large area, and be useful for practical use.
The Genetics of the Mediterranean Fruit Fly:1 a “White Pupae” Mutant2 (1979)

Journal Article The Genetics of the Mediterranean Fruit Fly: a "White Pupae" Mutant Get access Yoram Rössler Yoram Rössler The "Israel Cohen" Institute for Biological Control, Citrus Marketing Board, Rehovot, Israel. Search for other works by this author on: Oxford Academic Google Scholar Annals of the Entomological Society of America, Volume 72, Issue 5, 15 September 1979, Pages 583–585, https://doi.org/10.1093/aesa/72.5.583 Published: 15 September 1979 Article history Received: 08 March 1978 Published: 15 September 1979
Finite Mixture Models (2000)

The important role of finite mixture models in the statistical analysis of data is underscored by the ever-increasing rate at which articles on mixture applications appear in the statistical and general scientific literature. The aim of this article is to provide an up-to-date account of the theory and methodological developments underlying the applications of finite mixture models. Because of their flexibility, mixture models are being increasingly exploited as a convenient, semiparametric way in which to model unknown distributional shapes. This is in addition to their obvious applications where there is group-structure in the data or where the aim is to explore the data for such structure, as in a cluster analysis. It has now been three decades since the publication of the monograph by McLachlan &amp; Basford (1988) with an emphasis on the potential usefulness of mixture models for inference and clustering. Since then, mixture models have attracted the interest of many researchers and have found many new and interesting fields of application. Thus, the literature on mixture models has expanded enormously, and as a consequence, the bibliography here can only provide selected coverage.
Efficient cyclopropanation of C60 starting from malonates (1997)

The direct treatment of C60 with malonates in the presence of CBr4 and diazabicyclo[5.4.0]undec-7-ene (DBU) leads to an efficient conversion to methanofullerenes, which is demonstrated with the syntheses of monoadducts and highly symmetric hexaadducts in good yields.
Phosphorylation of D-glucose in Escherichia coli mutants defective in glucosephosphotransferase, mannosephosphotransferase, and glucokinase (1975)

Genetic studies show that Escherichia coli has three enzymes capable of phosphorylating glucose: soluble adenosine 5'-triphosphate-dependent glucokinase, which plays only a minor role in glucose metabolism; an enzyme II, called glucosephosphotransferase, with high specificity for the D-glucose configuration; and another enzyme II, called mannosephosphotransferase, with broader specificity. The former enzyme II is active on glucose and methyl-alpha-glucopyranoside, whereas the latter is active on D-glucose, D-mannose, 2-deoxy-D-glucose, D-glucosamine, and D-mannosamine. Mutations leading to loss of glucosephosphotransferase activity and designated by the symbol gpt are between the purB and pyrC markers in a locus previously called cat. The locus of mutations to loss of mannosephosphotransferase, mpt, is between the eda and fadD genes. Mutations to loss of glucokinase, glk, are between the ptsI and dsd genes.
ShieldFS (2016)

Preventive and reactive security measures can only partially mitigate the damage caused by modern ransomware attacks. Indeed, the remarkable amount of illicit profit and the cyber-criminals' increasing interest in ransomware schemes suggest that a fair number of users are actually paying the ransoms.
Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras (2016)

Selective degradation of proteins by proteolysis targeting chimeras (PROTACs) offers a promising potential alternative to protein inhibition for therapeutic intervention. Current PROTAC molecules incorporate a ligand for the target protein, a linker, and an E3 ubiquitin ligase recruiting group, which bring together target protein and ubiquitinating machinery. Such hetero-bifunctional molecules require significant linker optimization and possess high molecular weight, which can limit cellular permeation, solubility, and other drug-like properties. We show here that the hetero-bifunctional molecule can be formed intracellularly by bio-orthogonal click combination of two smaller precursors. We designed a tetrazine tagged thalidomide derivative which reacts rapidly with a <i>trans</i>-cyclo-octene tagged ligand of the target protein in cells to form a cereblon E3 ligase recruiting PROTAC molecule. The in-cell click-formed proteolysis targeting chimeras (CLIPTACs) were successfully used to degrade two key oncology targets, BRD4 and ERK1/2. ERK1/2 degradation was achieved using a CLIPTAC based on a covalent inhibitor. We expect this approach to be readily extendable to other inhibitor-protein systems because the tagged E3 ligase recruiter is capable of undergoing the click reaction with a suitably tagged ligand of any protein of interest to elicit its degradation.
Determination of the Acid Strength of Binary Oxide Catalysts Using Temperature-Programmed Desorption of Pyridine (1997)

Abstract The temperature-programmed desorption of pyridine (Py-TPD) was performed for measuring the acid strength and acid amount of binary oxide catalysts. First, the optimum measurement conditions were determined by comparing the TPD spectra with the infrared spectra of adsorbed pyridine measured under the same conditions in order to minimize the shift in the desorption temperature and contribution of physically absorbed and/or weakly held pyridine. The following conditions were found to be optimum: purging at 423 K for 2 h, W/F (W, sample weight; F, flow rate of the carrier) of 100 mg/150 cm 3 min −1, and a heating rate of 5 K min−1. This method was applied then to a series of binary mixed oxide catalysts. The amount of desorbed pyridine was 15—24% of the full coverage of pyridine on the catalyst surface with few exceptions. The highest acid strength, determined from the Py-TPD spectra, was well-correlated to that determined from a color change of Hammett indicators. The potential of the Py-TPD for determining the acid strength and the acid amount on binary oxide catalysts is discussed.
Viral protein R of HIV-1 (1999)

Viral protein R (Vpr) of HIV-1 belongs to a class of so called 'accessory' proteins, originally thought to be dispensable for virus replication, at least in vitro. Indeed, viruses with mutated or deleted Vpr replicate well in transformed T cell lines. However, recently published results reveal several important functions performed by Vpr, which are critical for HIV-1 replication in vivo. Vpr plays an important role in regulating nuclear import of the HIV-1 pre-integration complex, and is required for virus replication in non-dividing cells. Vpr also induces cell cycle arrest in proliferating cells, stimulates virus transcription, and regulates activation and apoptosis of infected cells. These diverse functions are mediated by the interaction of Vpr with different cellular proteins, many of which carry the WxxF amino acid motif. The molecular events underlying the activity of Vpr are reviewed in this article.