gebhart/patrepeval huggingface dataset:
Isolongifolenone: A Novel Sesquiterpene Repellent of Ticks and Mosquitoes (2009)

A naturally occurring sesquiterpene, isolongifolenone, derivatives of which have been used extensively as ingredients in the cosmetics industry, was discovered to effectively repel blood-feeding arthropods that are important disease vectors. We show that (-)-isolongifolenone deters the biting of the mosquitoes, Aedes aegypti (L.) and Anopheles stephensi Liston, more effectively than the widely used synthetic chemical repellent, N,N-diethyl-3-methyl benzamide (DEET), in laboratory bioassays. The compound also repelled blacklegged ticks, Ixodes scapularis Say, and lone star ticks, Amblyomma americanum (L.), as effectively as DEET. Isolongifolenone is easily synthesized from inexpensive turpentine oil feedstock. We are therefore confident that the compound has significant potential as an inexpensive and safe repellent for protection of large human populations against blood-feeding arthropods.
Peptide-mediated cellular delivery. (2000)

Peptide-mediated molecular therapeutic delivery systems have recently emerged as an alternative means to effectively substitute or augment present gene therapy technologies, e.g., TAT, VP22, engineered peptides. These systems show great promise for the elimination of the main bottleneck to safe, efficient, targeted gene therapy delivery and are able to efficiently introduce DNA, antisense peptide nucleic acids, oligonucleotides, small molecules and proteins into cells both in vitro and in vivo. They are versatile and easily designed to incorporate a number of specific attributes required for efficient cargo delivery. A fundamentally new property of these moieties will allow the therapeutic intervention in the biochemistry of the target cell without the need to alter its genome.
p65-activated Histone Acetyltransferase Activity Is Repressed by Glucocorticoids (2001)

Glucocorticoids acting through their specific receptor can either enhance or repress gene transcription. Dexamethasone represses interleukin-1beta-stimulated histone acetylation and granulocyte-macrophage colony-stimulating factor expression through a combination of direct inhibition of p65-associated histone acetyltransferase (HAT) activity and by recruiting histone deacetylase 2 (HDAC2) to the p65-HAT complex. Here we show that mifepristone, a glucocorticoid receptor partial agonist, has no ability to induce gene expression but represses interleukin-1beta-stimulated histone acetylation and granulocyte-macrophage colony-stimulating factor release by 50% maximally. Mifepristone was able to inhibit p65-associated HAT activity to the same extent as dexamethasone but failed to inhibit the natural promoter to an equal extent due to an inability to recruit HDAC2 to the p65-associated HAT complex. These data suggest that the maximal repressive actions of glucocorticoids require recruitment of HDAC2 to a p65-HAT complex. These data also suggest that pharmacological manipulation of specific histone acetylation status is a potentially useful approach for the treatment of inflammatory diseases.
Implementation and capabilities of a virtual interaction system (1998)

Virtual Interaction refers to a technique for interacting with computer generated graphics. Graphical objects are overlaid on live video of the user. A chromakey separates the user (foreground) from the background resulting in a silhouette of user. The computer causes the graphical objects to move in relation to the silhouette so that they appear to interact with the user. This paper presents the implementations of the system, some techniques for interaction and discusses using the system as a tool for physical therapy. 1.
Saccharomyces cerevisiae S288C Has a Mutation in FL08, a Gene Required for Filamentous Growth (1996)

Diploid strains of baker's yeast Saccharomyces cerevisiae can grow in a cellular yeast form or in filaments called pseudohyphae. This dimorphic transition from yeast to pseudohyphae is induced by starvation for nitrogen. Not all laboratory strains are capable of this dimorphic switch; many grow only in the yeast form and fail to form pseudohyphae when starved for nitrogen. Analysis of the standard laboratory strain S288C shows that this defect in dimorphism results from a nonsense mutation in the FLO8 gene. This defect in FLO8 blocks pseudohyphal growth in diploids, haploid invasive growth, and flocculation. Since feral strains of S. cerevisiae are dimorphic and have a functional FLO8 gene, we suggest that the flo8 mutation was selected during laboratory cultivation.
Suppression of anti-mouse immunoglobulin antibodies in subhuman primates receiving murine monoclonal antibodies against T cell antigens. (1987)

Murine monoclonal antibodies stimulate the production of human anti-mouse immunoglobulin antibodies (AMIA) when administered to patients. This limits their long-term usefulness as therapeutic and diagnostic agents. We report the use of three maneuvers to suppress AMIA against T cell-specific monoclonal antibodies in cynomolgus monkeys. Twelve monkeys received daily i.v. infusions of 1 mg each of anti-Leu-2a, -3a, and -5 on days 1 through 10. One group (control) received no suppressive regimen. The second group received cyclosporine, 12.5 mg/kg daily on days -7 to +14. The third group (PI) were passively immunized with 0.4 ml of hyperimmune monkey AMIA serum on days -7, -1, 2, 4, 6, and 8. The fourth group (TLI) received 1700 rad fractionated total lymphoid irradiation ending on day -1. The animals treated with TLI were markedly delayed in the onset of AMIA, which was suppressed to less than 1% of the control group. The AMIA specific for the constant region of animals receiving PI was also suppressed to one-third of control. The majority of the AMIA in all the animals was anti-idiotypic and wholly anti-idiotypic in the TLI animals.
Carbon Isotope Signature of Polycyclic Aromatic Hydrocarbons (PAHs):  Evidence for Different Sources in Tropical and Temperate Environments? (2002)

In tropical soils, naphthalene and, partly also, perylene occur at elevated concentrations while pyrolytic higher molecular weight PAHs are almost absent. We hypothesize that there are recent biological PAH sources in the tropical environment related with woody plants and termites. We used the C isotope signature of individual PAHs in temperate and tropical soils and in tropical wood and termite nests to distinguish different PAH sources. The mean delta13C values of the benzo[b+j+k]fluoranthenes and of benzo[a+e]pyrenes in temperate soils ranged between -24.6/1000 and -25.3/1000, being similar to values reported in the literature for PAHs with pyrolitic origin. The mean delta13C values of perylene decreased in the order temperate soils (-27.0/1000) > termite nests (-31.4/1000) > tropical soil (-32.4/1000), while those of naphthalene (-24.6/1000 to -26.2/1000) were similar among the tropical and temperate soils, tropical wood, and termite nests. Our results support the assumption that perylene in the tropical environment is recently biologically produced, as indicated by the depletion in 13C. The C isotope composition of naphthalene, however, cannot be used to distinguish different sources.
An improved synthesis of a methotrexate-albumin-791T/36 monoclonal antibody conjugate cytotoxic to human osteogenic sarcoma cell lines. (1986)

Improvements have been made in the synthesis of a drug-carrier-antibody conjugate using methotrexate as the drug, human serum albumin as the carrier, and a monoclonal antibody against a human osteogenic sarcoma cell line (791T/36). The improvements have resulted in a higher and more reproducible substitution of serum albumin by methotrexate, and improvements in the coupling of methotrexate covalently linked to human serum albumin to antibody resulting in a greater ease and efficiency of conjugation. The improvements have led to a conjugate of increased cytotoxicity while retaining the previously reported specificity. A conjugate is reported which shows cytotoxicity of 1.1 ng/ml (2.4 nM) with respect to methotrexate and 6 X 10(-11) M with respect to antibody in a clonogenic assay on 791T cells. This cytotoxicity is greater than that obtained using free methotrexate (2.8 ng/ml; 6.1 nM) and implies that drug cytotoxicity can be considered as the sum of drug uptake and the number of drug molecules required to kill a cell. This further suggests that antibodies could provide a potent delivery system for drugs which are poorly taken up by cells.
Deregulation and the New Zealand Agricultural Sector: A Review (1989)

Since July 1984 the New Zealand Government has been following a policy of disengagement and deregulation throughout the New Zealand economy. The impacts of the new policy have been felt at both the macro and the micro level. For the agricultural sector, a closer relationship to international prices and costs has been sought, with less industry assistance and direct support from the Government. With the removal of special privileges formerly enjoyed, the agricultural sector has also become more closely aligned with and vulnerable to changes in major macro parameters in the economy such as exchange rates, interest rates, inflation control and budget economies. The alignment of the agricultural economy with international prices and costs is likely to bring about a smaller and more competitive sector than was previously the case.
Neutral particle lithography: a simple solution to charge-related artefacts in ion beam proximity printing (2008)

Neutral particle lithography (NPL) is a high resolution, proximity exposure technique where a broad beam of energetic neutral atoms floods a stencil mask and transmitted beamlets transfer the mask pattern to resist on a substrate. It preserves the advantages of ion beam lithography, including extremely large depth-of-field, sub-5 nm resist scattering, and the near absence of diffraction, yet is intrinsically immune to charge-related artefacts including line-edge roughness and pattern placement errors due to charge accumulation on the mask and substrate. This paper reviews the principles of NPL, surveys recent advances in the field and discusses applications involving insulating substrates, large proximity gaps or ultra-small features where the approach has particular advantages.
Neuroprotection of Photoreceptors by Minocycline in Light-Induced Retinal Degeneration (2004)

Minocycline is neuroprotective against light-induced loss of photoreceptors, possibly through the inhibition of retinal microglial activation.
Trends in A1C Concentrations Among U.S. Adults With Diagnosed Diabetes From 1999 to 2004 (2007)

A1C is formed when glucose reacts nonenzymatically with amino acids on hemoglobin. Its concentration represents an integrated measure of glucose concentration during hemoglobin's lifespan, which is about 2–3 months (1). Because A1C concentration predicts the risk for microvascular and macrovascular complications (2,3), it is used in the clinical setting to assess longer-term glycemic control among people with diabetes. Generally, A1C concentrations <7% are regarded as acceptable glycemic control (4).

Approximately 44% of U.S. adults with diagnosed diabetes had a concentration of A1C <7% during 1988–1994 compared with ∼36–37.0% during 1999–2000 (5,6). More recently, data from the National Committee for Quality Assurance showed steady increases in the percentage of patients receiving annual testing for A1C and decreases in the percentage of patients with poor glycemic control from 2000 to 2006 (7). Our objective was to examine trends in glycemic control among U.S. adults with diagnosed diabetes from 1999 to 2004.

The National Health and Nutrition Examination Survey (NHANES) 1999–2004 included nationally representative samples of the noninstitutionalized, civilian U.S. population, selected using a multistage, stratified sampling design (8). Participants were asked the following: “Other than during pregnancy, have you ever been told by a doctor or health professional that you have diabetes or sugar …
Selective Androgen Receptor Modulators in Drug Discovery: Medicinal Chemistry and Therapeutic Potential (2006)

Modulation of the androgen receptor has the potential to be an effective treatment for hypogonadism, andropause, and associated conditions such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and sexual dysfunction. Side effects associated with classical anabolic steroid treatments have driven the quest for drugs that demonstrate improved therapeutic profiles. Novel, non-steroidal compounds that show tissue selective activity and improved pharmacokinetic properties have been developed. This review provides an overview of current advances in the development of selective androgen receptor modulators (SARMs).
A fast super-resolution reconstruction algorithm for pure translational motion and common space-invariant blur (2001)

This paper addresses the problem of recovering a super-resolved image from a set of warped blurred and decimated versions thereof. Several algorithms have already been proposed for the solution of this general problem. In this paper, we concentrate on a special case where the warps are pure translations, the blur is space invariant and the same for all the images, and the noise is white. We exploit previous results to develop a new highly efficient super-resolution reconstruction algorithm for this case, which separates the treatment into de-blurring and measurements fusion. The fusion part is shown to be a very simple non-iterative algorithm, preserving the optimality of the entire reconstruction process, in the maximum-likelihood sense. Simulations demonstrate the capabilities of the proposed algorithm.
Removal of residual crosstalk components in blind source separation using LMS filters (2003)

The performance of blind source separation (BSS) using independent component analysis (ICA) declines significantly in a reverberant environment. The degradation is mainly caused by the residual crosstalk components derived from the reverberation of the jammer signal. This paper describes a post-processing method designed to refine output signals obtained by BSS. We propose a new method which uses LMS filters in the frequency domain to estimate the residual crosstalk components in separated signals. The estimated components are removed by non-stational spectral subtraction. The proposed method removes the residual components precisely, thus it compensates for the weakness of BSS in a reverberant environment. Experimental results using speech signals show that the proposed method improves the signal-to-interference ratio by 3 to 5 dB.
Distinct T‐cell subtypes induced with whole cell and acellular pertussis vaccines in children (1998)

Recent clinical trials have demonstrated that new generation acellular pertussis vaccines can confer protection against whooping cough. However, the mechanism of protective immunity against Bordetella pertussis infection induced by vaccination remains to be defined. We have examined cellular immune responses in children immunized with a range of acellular and whole cell pertussis vaccines. Immunization of children with a potent whole-cell vaccine induced B. pertussis-specific T cells that secreted interferon-gamma (IFN-gamma), but not interleukin-5 (IL-5). In contrast, T cells from children immunized with acellular pertussis vaccines secreted IFN-gamma and/or IL-5 following stimulation with B. pertussis antigens in vitro. These observations suggest that protective immunity conferred by whole-cell vaccines, like natural immunity, is mediated by type 1 T cells, whereas the mechanism of immune protection generated with acellular vaccines may be more heterogeneous, involving T cells that secreted type 1 and type 2 cytokines.
Mechanism and Utility of an RNA-Cleaving DNA Enzyme (1998)

We previously reported the in vitro selection of a general-purpose RNA-cleaving DNA enzyme that exhibits a catalytic efficiency (kcat/KM) exceeding that of any other known nucleic acid enzyme [Santoro, S. W. and Joyce, G. F. (1997) Proc. Natl. Acad. Sci. U.S.A. 94, 4262-4266]. This enzyme contains approximately 30 deoxynucleotides and can cleave almost any RNA substrate under simulated physiological conditions, recognizing the substrate through two Watson-Crick binding domains. The kinetics of cleavage under conditions of varying pH, choice of divalent metal cofactor, and divalent metal concentration are consistent with a chemical mechanism involving metal-assisted deprotonation of a 2'-hydroxyl of the substrate, leading to substrate cleavage. Kinetic measurements reveal that the enzyme strongly prefers cleavage of the substrate over ligation of the two cleavage products and that the enzyme's catalytic efficiency is limited by the rate of substrate binding. The enzyme displays a high level of substrate specificity, discriminating against RNAs that contain a single base mismatch within either of the two substrate-recognition domains. With appropriate design of the substrate-recognition domains, the enzyme exhibits a potent combination of high substrate sequence specificity and selectivity, high catalytic efficiency, and rapid catalytic turnover.
Styrylquinoline Derivatives:  A New Class of Potent HIV-1 Integrase Inhibitors That Block HIV-1 Replication in CEM Cells (1998)

On the basis of the fact that several polynucleotidyl transferases, related to HIV integrase, contain in their active site two divalent metal cations, separated by ca. 4 A, new potential HIV integrase inhibitors were designed, in which a quinoline substructure is linked to an aryl nucleus possessing various hydroxy substitution patterns, by means of an ethylenic spacer. Although the most active compounds contain the catechol structure, this group is not essential for the activity, since compound 21 that lacks such a moiety is a potent drug, implicating the presence of a different pharmacophore. The most promising styrylquinolines thus synthesized inhibit HIV-1 integrase in vitro at micromolar or submicromolar concentrations and block HIV replication in CEM cells, with no significant cellular toxicity in a 5-day period assay. These inhibitors are active against integrase core domain-mediated disintegration, suggesting that fragment 50-212 is their actual target. These new styrylquinolines may provide lead compounds for the development of novel antiretroviral agents for AIDS therapeutics, based upon inhibition of HIV integrase. They might also be used in the elucidation of the mechanism of inhibition of this enzyme; e.g., they could serve as candidates for cocrystallization studies with HIV integrase.
Platelet Angiotensin II Binding Sites and Early Detection of Preeclampsia (1998)

In Brief Objective To determine if platelet angiotensin II binding density during the second or third trimester of pregnancy can be used as a marker for early detection of women who will develop preeclampsia. Methods We collected blood samples from 412 nulliparous pregnant women during their second or third trimesters. They were classified in four groups after delivery: noromtensive (n = 297), transient hypertensive (n = 54), preeclamptic (w = 39), and chronic hypertensive (n = 22). We also studied 35 nonpregnant women and 122 women in the peripartum period. The binding capacity of platelet angiotensin II receptors was analyzed in each patient. Results In normotensive pregnancies, there was a significant decrease in mean (± standard error of the mean [SEM]) platelet binding in the second trimester (1.6 ± 0.2 fmol/109 cells) compared with nonpregnant women (3.3 ± 0.7 fmol/109 cells). No statistical differences were observed in the mean (± SEM) number of platelet angiotensin II binding sites between the groups studied in the third trimester (normal: 1.7 ± 0.1 fmol/109 cells; transient hypertensive: 2.3 ± 0.4 fmol/109 cells; preeclamptic: 1.6 ± 0.4 fmol/109 cells, and chronic hypertensive: 1.6 ± 0.6 fmol/109 cells), nor were any significant differences found in second-trimester values. At cutoff levels providing identical sensitivities, angiotensin II binding showed significantly lower positive predictive values than mean arterial pressure (P < .05). With this study's sample size, we could have demonstrated an improvement in positive predictive values of 20% with a statistical power (1-β) of 90%. Conclusion The measurement of platelet angiotensin II receptor density cannot be recommended for the early detection of preeclampsia. Platelet angiotensin II receptor density does not predict later development of preeclampsia.
Genotypes and Sequence Variants of Human Papillomavirus DNAs from Human Immunodeficiency Virus Type I-Infected Women with Cervical Intraepithelial Neoplasia (1992)

Human papillomavirus (HPV) DNA was found in cervicovaginal lavage fluids from 9 of 11 human immunodeficiency virus type 1 (HIV-1)-seropositive female prostitutes with cervical intraepithelial neoplasia (CIN) in Kinshasa, Zaire. Since 7 yielded complex nucleic acid hybridization results consistent with mixed HPV infections, limited sequencing of HPV DNA was used to identify the HPVs present. Three of HPV 16 and 1 each of HPV 18, 31, 33, and 56 and ME180-HPV were identified by sequencing in 8 samples. Each of these genotypes has been found in specimens from HIV-1-seronegative women with CIN. Some DNAs had nucleic acid and amino acid sequence variations relative to the reference HPVs, but the variants were closely related to variants that have been found in HIV-1-seronegative women. Variant amino acids were found predominantly at three positions in one 40-amino-acid segment of the L1 open reading frame sequenced. The predominant HPV 16 variant observed has been found rarely in other countries.
Regulation of muscarinic receptor function in developing oligodendrocytes by agonist exposure (2003)

1 Oligodendrocytes, the myelin forming cells in the CNS, express muscarinic acetylcholine receptors (mAChR), primarily M3, coupled to various signal transduction pathways. 2 In the present study we have investigated whether mAChR undergo functional agonist-induced regulation in cultured oligodendrocyte progenitors and differentiated oligodendrocytes. 3 The muscarinic agonist, carbachol (CCh) caused a time-dependent desensitization of phosphoinositide (PI) hydrolysis, and the internalization and down-regulation of receptors. Short-time desensitization (5 min) of PI hydrolysis occurred without receptor internalization and reached 54% by 1 h. The same treatment decreased cell surface receptors labelled with the non-permeable ligand [(3)H]-NMS by 47%, while total receptor density ([(3)H]-scopolamine binding) decreased by 30%. Longer CCh treatment down-regulated receptors by 70% and desensitized the PI response by 80%. 4 Although protein kinase C (PKC) activation desensitized mAChR, CCh-mediated desensitization was independent of PKC. 5 Inhibition of receptor endocytosis by low temperature during the pre-stimulation period or in the presence of hyperosmotic sucrose (0.5 M) blocked desensitization, receptor internalization and down-regulation. 6 Recovery of surface mAChR and their functional activity following down-regulation was slow, returning to control levels by 24 h after agonist removal. In progenitor cells, dose-response curves for CCh-mediated PI hydrolysis and c-fos mRNA expression showed that newly synthesized mAChR were supersensitive after recovery. 7 Overall, the present results provide evidence of functional agonist-mediated mAChR regulation in brain oligodendroglial cells.
Arabinogalactan proteins contribute to the immunostimulatory properties of New Zealand honeys (2012)

The immunostimulatory activity of kanuka honey may be particularly dependent on AGPs derived from the nectar of kanuka flowers.