gebhart/patrepeval huggingface dataset:
Deletion of the NH2-terminal residue converts monocyte chemotactic protein 1 from an activator of basophil mediator release to an eosinophil chemoattractant. (1996)

Chemotactic cytokines of the CC subfamily (CC chemokines) are considered as major mediators of allergic inflammation owing their actions on basophil and eosinophil leukocytes. The monocyte chemotactic protein (MCP) 1 is a potent inducer of mediator release from basophils but is inactive on eosinophils. To obtain information on the structural determinants of the activities of MCP-1, we have synthesized several NH2-terminally truncated analogues and tested their effects on basophils and eosinophils. Through deletion of the NH2-terminal residue, MCP-1(2-76) was obtained, which was a potent activator of eosinophils, as assessed by chemotaxis, cytosolic free Ca2+ changes, actin polymerization, and that induction of the respiratory burst. In contrast, the activity of MCP-1(2-76) on basophil leukocytes was dramatically decreased (50-fold) compared with that of full-length MCP-1. Deletion of the next residue led to total loss of activity on eosinophil and basophil leukocytes. Analogues with three or four residue deletions, MCP-1(4-76) and MCP-1(5-76), were again active on both cells, whereas all further truncation analogues, MCP-1(6-76) through MCP-1(10-76), were inactive. Thus, a minimal structural modification can change receptor and target cell selectivity of MCP-1. Our observations indicate that the recognition sites of CC chemokine receptors on eosinophils and basophils are similar, although they discriminate between MCP-1 and MCP-1(2-76) and suggest NH2-terminal processing as a potential mechanism for the regulation of CC chemokine activities.
Fluorine in medicinal chemistry (2007)

It has become evident that fluorinated compounds have a remarkable record in medicinal chemistry and will play a continuing role in providing lead compounds for therapeutic applications. This tutorial review provides a sampling of renowned fluorinated drugs and their mode of action with a discussion clarifying the role and impact of fluorine substitution on drug potency.
Norlanostane and Lanostane Glycosides from the Bulbs of Chionodoxa luciliae and Their Cytotoxic Activity. (2003)

Ten lanostane glycosides (1-10), including two new norlanostane glycosides (2 and 7) and a new lanostane glycoside with a spirolactone ring system (9), were isolated from the fresh bulbs of Chionodoxa luciliae (Liliaceae). The structures of the new compounds were determined on the basis of extensive spectroscopic analysis and the results of hydrolytic cleavage to be (23S)-3beta-[(O-beta-D-apiofuranosyl-(1-->2)-O-[beta-D-glucopyranosyl-(1-->3)]-O-beta-D-glucopyranosyl-(1-->2)-alpha-L-arabinopyranosyl-(1-->6)-beta-D-glucopyranosyl)oxy]-17alpha,23-epoxy-28,29-dihydroxy-27-norlanost-8-en-24-one (2), (23S)-17alpha,23-epoxy-29-hydroxy-3beta-[(O-alpha-L-rhamnopyranosyl-(1-->2)-O-[O-beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->3)]-O-beta-D-glucopyranosyl-(1-->2)-alpha-L-arabinopyranosyl-(1-->6)-beta-D-glucopyranosyl)oxy]-27-norlanost-8-ene-15,24-dione (7), and (23S,25R)-17alpha,23-epoxy-29-hydroxy-3beta-[(O-alpha-L-rhamnopyranosyl-(1-->2)-O-[beta-D-glucopyranosyl-(1-->3)]-O-beta-D-glucopyranosyl-(1-->2)-alpha-L-arabinopyranosyl-(1-->6)-beta-D-glucopyranosyl)oxy]lanost-8-en-23,26-olide (9), respectively. The cytotoxic activity of the isolated compounds against HSC-2 human oral squamous cell carcinoma cells are also reported.
Ultrahigh sensitivity magnetic field and magnetization measurements with an atomic magnetometer (2010)

We describe an ultrasensitive atomic magnetometer based on optically pumped potassium atoms operating in a spin-exchange relaxation free regime. We demonstrate magnetic field sensitivity of 160 aT/Hz1/2 in a gradiometer arrangement with a measurement volume of 0.45 cm3 and energy resolution per unit bandwidth of 44ℏ. As an example of an application enabled by such a magnetometer, we describe measurements of weak remnant rock magnetization as a function of temperature with a sensitivity on the order of 10−10 emu/cm3/Hz1/2 and temperatures up to 420°C.
Monodisperse Picoliter Droplets for Low-Bias and Contamination-Free Reactions in Single-Cell Whole Genome Amplification (2015)

Whole genome amplification (WGA) is essential for obtaining genome sequences from single bacterial cells because the quantity of template DNA contained in a single cell is very low. Multiple displacement amplification (MDA), using Phi29 DNA polymerase and random primers, is the most widely used method for single-cell WGA. However, single-cell MDA usually results in uneven genome coverage because of amplification bias, background amplification of contaminating DNA, and formation of chimeras by linking of non-contiguous chromosomal regions. Here, we present a novel MDA method, termed droplet MDA, that minimizes amplification bias and amplification of contaminants by using picoliter-sized droplets for compartmentalized WGA reactions. Extracted DNA fragments from a lysed cell in MDA mixture are divided into 105 droplets (67 pL) within minutes via flow through simple microfluidic channels. Compartmentalized genome fragments can be individually amplified in these droplets without the risk of encounter with reagent-borne or environmental contaminants. Following quality assessment of WGA products from single Escherichia coli cells, we showed that droplet MDA minimized unexpected amplification and improved the percentage of genome recovery from 59% to 89%. Our results demonstrate that microfluidic-generated droplets show potential as an efficient tool for effective amplification of low-input DNA for single-cell genomics and greatly reduce the cost and labor investment required for determination of nearly complete genome sequences of uncultured bacteria from environmental samples.
Glycoantigens Induce Human Peripheral Tr1 Cell Differentiation with Gut-homing Specialization (2011)

The carbohydrate antigen (glycoantigen) PSA from an intestinal commensal bacteria is able to down-regulate inflammatory bowel disease in model mice, suggesting that stimulation with PSA results in regulatory T cell (Treg) generation. However, mechanisms of how peripheral human T cells respond and home in response to commensal antigens are still not understood. Here, we demonstrate that a single exposure to PSA induces differentiation of human peripheral CD4(+) T cells into type-Tr1 Tregs. This is in contrast to mouse models where PSA induced the production of Foxp3(+) iTregs. The human PSA-induced Tr1 cells are profoundly anergic and exhibit nonspecific bystander suppression mediated by IL-10 secretion. Most surprisingly, glycoantigen exposure provoked expression of gut homing receptors on their surface. These findings reveal a mechanism for immune homeostasis in the gut whereby exposure to commensal glycoantigens provides the requisite information to responding T cells for proper tissue localization (gut) and function (anti-inflammatory/regulatory).
Fetal cell microchimerism: helpful or harmful to the parous woman? (2003)

These data suggest the possibility that fetal microchimeric cells may also participate in the maternal physiological response to tissue injury. The medical consequences of pregnancy, therefore, appear to extend well beyond delivery.
Frequency doubling of Er-doped multimode fiber compressor-amplifiers (1998)

Summary form only given. We have demonstrated an efficient 5 times pulse compressor for medium power pulses in doped and undoped multimode (MM) fibers for the first time to our knowledge. There is no need for any external phase-control and the compressed pulses may be doubled with an efficiency of 50 percent.
Prostaglandin Endoperoxide H Synthases (Cyclooxygenases)-1 and −2 (1996)

Prostaglandin endoperoxide H synthases (PGHSs)1 catalyze the conversion of arachidonic acid and O2 to PGH2, the committed step in prostanoid biosynthesis (Fig. 1) (1). Before 1991, only one PGHS had been described, the isozyme now called PGHS-1, COX-1 (for cyclooxygenase-1) or the constitutive enzyme. At that time Simmons and Herschman and their colleagues discovered mRNAs whose expression was induced in chicken and mouse fibroblasts in response to src and tumor-promoting phorbol esters, respectively, and which encoded proteins having 60% amino acid sequence identity with PGHS-1.
Structural investigation and elucidation of new communesins from a marine‐derived Penicillium expansum Link by liquid chromatography/electrospray ionization mass spectrometry (2009)

Penicillium expansum is a ubiquitous species for which there are only few reports for chemical investigation in marine environments. Among the numerous secondary metabolites produced by this species, communesins represent a new class of cytotoxic and insecticidal indole alkaloids. In this study, we investigated a marine P. expansum strain exhibiting neuroactivity on a Diptera larvae bioassay. Bio-guided purification led to the isolation and the identification of communesin B as the main active compound by HRMS and 1H and 13C NMR. Liquid chromatography analyses with detection by electrospray ionization coupled with tandem mass spectrometry (LC/ESI-MS/MS) and high-resolution tandem mass spectrometry (LC/HRMS/MS) allowed the identification and characterization of four other known communesins (A, D, E and F) in the crude extract. A fragmentation model for dimethyl epoxide communesins was proposed after detailed interpretation of their MS/MS spectra. Further analyses of the extract using the modelled fragmentations led to the detection of seven new communesins found as minor compounds. Chemical structural elucidation of these new derivatives is discussed based on their fragmentation characteristics.
Altered immune responses in apolipoprotein E-deficient mice (2000)

Apolipoprotein E (apoE) is a 34 kDa glycosylated protein with multiple biological properties. In addition to its role in cholesterol transport, apoE has in vitro immunomodulatory properties. Recent data suggest that these immunomodulatory effects of apoE may be biologically relevant, and apoE-deficient mice have altered immune responses after bacterial inoculation and increased susceptibility to endotoxemia induced by lipopolysaccharide (LPS). To better understand the mechanism by which apoE-modulates immune responses, we tested the role of human apoE isoforms in assays of human T cell proliferation, and analyzed the immune responses of apoE-deficient mice. Both the E3 and E4 isoforms of apoE induced similar suppression of human lymphocyte function in assays of T cell proliferation, including mitogenic responses to phytohaemagglutin (PHA), stimulation of the T cell receptor with alphaCD3, and antigen-specific response to tetanus toxoid. ApoE-deficient mice showed no quantitative differences in thymic, splenic, or bone marrow lymphocyte populations, nor were there in vitro abnormalities in splenocyte proliferation after stimulation with alphaCD3 to suggest an inherent T cell defect in apoE-deficient mice. ApoE deficient animals, however, had significantly higher levels of antigen-specific IgM after immunization with tetanus toxoid, and impaired delayed type hypersensitivity responses as compared to control C57-BL/6 mice. These results support a growing body of evidence demonstrating an interplay between lipid metabolism and immune responses, and suggest that apoE plays a biologically relevant role in regulating humoral and cell-mediated immunity.
Y-Ba-Cu-O thin films prepared by a multilayer vacuum method (1988)

Polycrystalline Y-Ba-Cu-O thin films with a thickness of about 1 μm have been deposited on alumina substrates. The deposition was made by first sequentially evaporating Y/Ba/Cu layers followed by a heat treatment in an environment containing oxygen. The treated films were polycrystalline, and the electrical results showed an onset temperature of about 100 K and a zero-resistance temperature of 78 K for the films treated at 850 °C for 2 h in oxygen.
Hepatic Preneoplasia in Hepatitis B Virus Transgenic Mice (1994)

Hepatocarcinogenesis in hepatitis B virus transgenic mice was studied by means of a correlative cytomorphological and cytochemical approach at different time points in animals from 1 to 34 mo old. HBsAg-positive ground-glass hepatocytes emerged throughout the liver parenchyma in nearly all transgenic mice during the first 4 mo after birth. The panlobular expression of HBsAg persisted until foci of altered hepatocytes appeared (6 to 9 mo of age). Three different types of foci of altered hepatocytes-namely, glycogen-storage foci, mixed cell foci and glycogen-poor foci-developed. Hepatocellular adenomas and carcinomas appeared after 11 mo. Orcein staining revealed frequent transitions between ground-glass hepatocytes extensively expressing HBsAg and glycogen-storage (predominantly clear-cell) foci containing HBsAg-positive cytoplasmic components. Similar transitions between ground-glass hepatocytes and glycogenotic (clear) cells were often found in diffuse parenchymal glycogenosis at 11 or 12 mo. Remnants of HBsAg-positive material were also detected in mixed cell foci, glycogen-poor diffusely basophilic cell foci, hepatic adenoma and hepatocellular carcinoma. These findings suggest that ground-glass hepatocytes are the direct precursor of foci of altered hepatocytes and their neoplastic descendants. The extensive expression of HBsAg is gradually down-regulated during neoplastic transformation, just as the morphological the biochemical phenotypes of foci of altered hepatocytes, hepatic adenoma and hepatocellular carcinoma in transgenic mice resemble those described in chemical hepatocarcinogenesis. The predominant sequence of cellular changes leading from glycogen-storage (predominantly clear cell) foci to mixed cell foci, hepatic adenoma and hepatocellular carcinoma is characterized by a gradual decrease in the activities of glycogen synthase, phosphorylase, glucose-6-phosphatase and adenylate cyclase, whereas glucose-6-phosphate dehydrogenase and pyruvate kinase activities increase. These alterations indicate a shift from the glycogenotic state toward an increase in the pentose phosphate pathway and glycolysis.
Carotid Artery Wall Intima-Media Thickness Is Associated With Insulin-Mediated Glucose Disposal in Men at High and Low Coronary Risk (1995)

Our results suggest that an increase in intimamedia thickness, as a possible expression of early atherosclerosis, is negatively related to insulin sensitivity.
Studies on the anti-inflammatory activity and ulcerogenic adverse effect of thiazole derivatives, especially 2-amino-thiazoleacetic acid derivatives. (1984)

A series of derivatives of 4-arylthiazole acetic acid and 2-aminothiazole were studied with respect of their antiinflammatory effect in rat carrageenin edema. Some active compounds were found, which suppressed the paw edema formation strongly, and two compounds were selected, 4-(4-chlorophenyl)-2-phenylaminothiazole acetic acid (Compd. 29) and 4-(4-chlorophenyl)-2-diethylaminothiazole acetic acid (Compd. 71) for further detailed studies. These compounds (Compd. 29 and Compd. 71) moderately inhibited the denaturation of albumin with heat-treatment. Hyperthermic lysis of erythrocytes were strongly inhibited with both Compds. 29 and 71 in the wide range of concentrations (5 X 10(-5) mol/l-5 X 10(-4) mol/l), while their related compound, Compd. 2 (fentiazac) and the reference drugs, ibuprofen, phenylbutazone and flufenamic acid, were either ineffective or stimulatory at the higher concentration. Compds. 29 and 71 inhibited strongly both trypsin and chymotrypsin activities, which differed from the above reference drugs qualitatively and quantitatively. The adverse effect on the gastrointestinal membrane was less with Compd. 29 and Compd. 71 compared with fentiazac and ibuprofen. Compd. 29 especially gave the preferable results with almost no gastric damage at the higher dosage together with its good anti-edematous activity. The characteristics of Compds. 29 and 71 are discussed in terms of the correlation between anti-inflammatory effect and ulcerogenic effect and also of the clinical application.
A PRIMER ON ANTENATAL TESTING FOR NEONATAL NURSES (2006)

Parents and healthcare providers are challenged to understand the mechanisms of, and predictors for preterm delivery. In addition to the epidemiologic implications, on a practical level, the ability to predict preterm delivery may help the neonatal team triage to assure bed availability, and to predict and provide appropriate staffing for new admissions. On an individual patient level, understanding the maternal history, including antenatal risk factors and relevant monitoring and testing, is an important foundation for subsequent neonatal care. A number of new diagnostic testing tools are being used in obstetric practice to enhance the ability to predict preterm delivery. The results of fetal fibronectin and ultrasound measurement of cervical length are increasingly used to triage obstetrical patients. Results of these tests may prompt transfer to a tertiary facility. Part 1 of this 2-part series will describe antenatal testing techniques used to predict preterm delivery (PTD), as well as highlight the emerging developments in maternal serum testing. Further, a recent treatment option for preterm labor, 17 alpha-hydroxyprogesterone caproate, will also be discussed.
3D thermoplastic elastomer microfluidic devices for biological probe immobilization (2011)

Microfluidics has emerged as a valuable tool for the high-resolution patterning of biological probes on solid supports. Yet, its widespread adoption as a universal biological immobilization tool is still limited by several technical challenges, particularly for the patterning of isolated spots using three-dimensional (3D) channel networks. A key limitation arises from the difficulties to adapt the techniques and materials typically used in prototyping to low-cost mass-production. In this paper, we present the fabrication of thin thermoplastic elastomer membranes with microscopic through-holes using a hot-embossing process that is compatible with high-throughput manufacturing. The membranes provide the basis for the fabrication of highly integrated 3D microfluidic devices with a footprint of only 1 × 1 cm(2). When placed on a solid support, the device allows for the immobilization of up to 96 different probes in the form of a 10 × 10 array comprising isolated spots of 50 × 50 μm(2). The design of the channel network is optimized using 3D simulations based on the Lattice-Boltzmann method to promote capillary action as the sole force distributing the liquid in the device. Finally, we demonstrate the patterning of DNA and protein arrays on hard thermoplastic substrates yielding spots of excellent definition that prove to be highly specific in subsequent hybridization experiments.
Improving Book OCR by Adaptive Language and Image Models (2012)

In order to cope with the vast diversity of book content and typefaces, it is important for OCR systems to leverage the strong consistency within a book but adapt to variations across books. We describe a system that combines two parallel correction paths using document-specific image and language models. Each model adapts to shapes and vocabularies within a book to identify inconsistencies as correction hypotheses, but relies on the other for effective cross-validation. Using the open source Tesseract engine as baseline, results on a large data set of scanned books demonstrate that word error rates can be reduced by 25 percent using this approach.
Substrate specificity of enzymes in organic solvents vs. water is reversed (1986)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSubstrate specificity of enzymes in organic solvents vs. water is reversedAleksey. Zaks and Alexander M. KlibanovCite this: J. Am. Chem. Soc. 1986, 108, 10, 2767–2768Publication Date (Print):May 1, 1986Publication History Published online1 May 2002Published inissue 1 May 1986https://pubs.acs.org/doi/10.1021/ja00270a053https://doi.org/10.1021/ja00270a053research-articleACS PublicationsRequest reuse permissionsArticle Views811Altmetric-Citations209LEARN 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
Environmental degradation of biodegradable polyesters. IV. The effects of pores and surface hydrophilicity on the biodegradation of poly(ϵ‐caprolactone) and poly[(R)‐3‐hydroxybutyrate] films in controlled seawater (2003)

Abstract Poly(ϵ‐caprolactone) (PCL) and poly[( R )‐3‐hydroxybutyrate] ( R ‐PHB) films with pores and hydrophilic surfaces were prepared by the water extraction of poly(ethylene oxide) from as‐cast blend films (1:1) and by the alkali treatment of as‐cast nonporous films, respectively. These films, as well as as‐cast nonporous PCL and R ‐PHB films, were biodegraded in static seawater kept at 25°C, and their biodegradation was monitored with gravimetry, gel permeation chromatography (GPC), and scanning electron microscopy. The pores or highly hydrophilic surfaces of the PCL and R ‐PHB films enhanced their biodegradation in seawater. Moreover, GPC measurements could be used to trace the biodegradation in seawater when the biodegradation proceeded to a great extent. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 90: 587–593, 2003
A Combination of Grape Extract, Green Tea Extract and l‐Carnitine Improves High‐fat Diet‐induced Obesity, Hyperlipidemia and Non‐alcoholic Fatty Liver Disease in Mice (2011)

To develop a therapeutic agent for obesity-related metabolic disorders, a mixture of dietary components was prepared, including grape extract, green tea extract and l-carnitine (RGTC), and its effects on obesity, hyperlipidemia and non-alcoholic fatty liver disease examined. The RGTC dramatically inhibited the high-fat diet (HFD)-induced increase in body weight and fat in C57BL/6 mice, whereas food consumption was not affected by RGTC treatment. The RGTC also concentration-dependently suppressed the HFD-induced increase in plasma lipids, such as low-density lipoprotein cholesterol and triglycerides. In addition, increases in liver weight and liver steatosis were returned to normal by RGTC treatment in HFD-fed C57BL/6 mice. The plasma levels of glutamic-oxaloacetic transaminase and glutamic-pyruvic transaminase were also significantly down-regulated by RGTC treatment. These results suggest that RGTC suppressed HFD-induced obesity, hyperlipidemia and non-alcoholic fatty liver disease, suggesting that RGTC supplementation might be a promising adjuvant therapy for the treatment of these metabolic disorders.