gebhart/patrepeval huggingface dataset:
Matrix contraction by dermal fibroblasts requires syndecan 4: Insights into pathological scarring in chronic fibrotic disease (2006)

Chronic fibrotic diseases, such as diffuse systemic sclerosis (dSSc), are characterized by excessive scarring. The cell type that causes scarring is the myofibroblast. We show that fibroblasts isolated from scars of dSSc patients retain their myofibroblast phenotype in cell culture. We find that antagonizing transforming growth factor-beta receptor type I with the specific ALK5 inhibitor SB431542 alleviates the elevated matrix contraction by dSSc fibroblasts. dSSc fibroblasts show elevated ERK activation, and antagonizing MEK with U0126 suppresses the contractile abilities of dSSc dermal fibroblasts. TGFbeta-induced matrix contraction requires the proteglycan syndecan 4, as TGFbeta cannot induce a contractile phenotype in syndecan 4 −/ − dermal fibroblasts or induce phosphorylation of ERK. Lesional dSSc fibroblasts overexpress syndecan 4. Syndecan 4 siRNA reduces the activated phenotype of SSc fibroblasts. Thus antagonizing syndecan 4 would be expected to alleviate scarring in chronic fibrotic diseases, including dSSc.
Comparative Inhibition of Yeast Glutathione Reductase by Arsenicals and Arsenothiols (1997)

Tri(gamma-glutamylcysteinylglycinyl)trithioarsenite (AsIII(GS)3) is formed in cells and is a more potent mixed-type inhibitor of the reduction of glutathione disulfide (GSSG) by yeast glutathione (GSH) reductase than either arsenite (AsIII) or GSH. The present work examines the effects of valence and complexation of arsenicals with GSH or L-cysteine (Cys) upon potency as competitive inhibitors of the reduction of GSH disulfide (GSSG) by yeast GSH reductase. Trivalent arsenicals were more potent inhibitors than their pentavalent analogs, and methylated trivalent arsenicals were more potent inhibitors than was inorganic trivalent As. Complexation of either inorganic trivalent As or methylarsonous diiodide (CH3As(III)I2) with Cys or GSH produced inhibitors of GSH reductase that were severalfold more potent than the parent arsenicals. In contrast, dimethylarsinous iodide ((CH3)2As(III)I) was a more potent inhibitor than its complexes with either GSH or Cys. Complexes of CH3AsIII with GSH (CH3-AsIII(GS)2) or with Cys (CH3AsIII(Cys)2) were the most potent inhibitors, with Ki's of 0.009 and 0.018 mM, respectively. Inhibition of GSH reductase by arsenicals or arsenothiols was prevented by addition of meso-2,3-dimercaptosuccinic acid (DMSA) to a mixture of enzyme, GSSG, and inhibitor before addition of NADPH. DMSA added to the reaction mixture after NADPH reversed inhibition by (CH3)2As(III)I but had little effect on inhibition by CH3As(III)I2, Ch3AsIII(GS)2, CH3AsIII(Cys)2, or AsIII(GS)3. Partial redox inactivation of the enzyme with NADPH increased the inhibitory potency of CH3As(III)I2 and (CH3)2As(III)I and changed the mode of inhibition for CH3As(III)I2 from competitive to noncompetitive. The greater potency of methylated trivalent arsenicals and arsenothiols than of inorganic trivalent As suggests that biomethylation of As could yield species that inhibit reduction of GSSG and alter the redox status of cells.
Regulation of small intestinal glutamine transport by epidermal growth factor. (1993)

We conclude that EGF up-regulates amino acid transport activity in jejunal BBMVs, an event that is most likely caused by an increase in de novo biosynthesis of transporter protein. The increase in amino acid uptake not only may support de novo protein synthesis but, in the case of glutamine, also may be required for energy production and nucleotide biosynthesis.
Synthesis of a [1,5,1,5]platyrin, a 26.pi.-electron tetrapyrrolic annulene (1987)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of a [1,5,1,5]platyrin, a 26.pi.-electron tetrapyrrolic annuleneE. LeGoff and O. G. WeaverCite this: J. Org. Chem. 1987, 52, 4, 710–711Publication Date (Print):February 1, 1987Publication History Published online1 May 2002Published inissue 1 February 1987https://pubs.acs.org/doi/10.1021/jo00380a051https://doi.org/10.1021/jo00380a051research-articleACS PublicationsRequest reuse permissionsArticle Views135Altmetric-Citations38LEARN 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-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
ChemInform Abstract: Divergent Pathways of β, γ‐Unsaturated α‐Diazocarbonyl Compounds Catalyzed by Dirhodium and Lewis Acids Catalysts Separately or in Combination (2015)

Abstract Review: 73 refs.
Pressure-Controlled Solution Growth of Bulk GaN Crystals under High Pressure (2001)

We have developed the pressure-controlled solution growth (PC-SG) method and indicated the validity of this method for the growth of GaN single crystals. We have investigated the effect of the supersaturation of nitrogen atoms on the size of a GaN single crystal and its morphology. GaN single crystals with a surface area of about 120 mm2 and/or with good morphology were obtained at a rate of increase of nitrogen pressure less than 49 MPa/h. Structural and photoluminescence properties of GaN single crystals were examined and determined that these crystals with good morphology had good crystallinity. Furthermore, we have introduced a new high-pressure furnace and developed the multi-crucible system. The GaN single crystal with a surface area of 300 mm2 was obtained by natural nucleation. The GaN crystal with 47 mm diameter, whose normal axis was the (0001) plane, could be grown on a sapphire substrate.
Nanoscale lateral epitaxial overgrowth of GaN on Si (111) (2005)

We demonstrate that GaN can selectively grow by metalorganic chemical vapor deposition into the pores and laterally over the nanoscale patterned SiO2 mask on a template of GaN∕AlN∕Si. The nanoporous SiO2 on GaN surface with pore diameter of approximately 65 nm and pore spacing of 110 nm was created by inductively coupled plasma etching using anodic aluminum oxide template as a mask. Cross-section transmission electron microscopy shows that the threading-dislocation density was largely reduced in this nanoepitaxial lateral overgrowth region. Dislocations parallel to the interface are the dominant type of dislocations in the overgrown layer of GaN. A large number of the threading dislocations were filtered by the nanoscale mask, which leads to the dramatic reduction of the threading dislocations during the growth within the nano-openings. More importantly, due to the nanoscale size of the mask area, the very fast coalescence and subsequent lateral overgrowth of GaN force the threading dislocations to bend to the basal plane within the first 50 nm of the film thickness. The structure of overgrown GaN is a truncated hexagonal pyramid which is covered with six {11¯01} side facets and (0001) top surface depending on the growth conditions.
SOCS proteins, cytokine signalling and immune regulation (2007)

Suppressor of cytokine signalling (SOCS) proteins are inhibitors of cytokine signalling pathways. Studies have shown that SOCS proteins are key physiological regulators of both innate and adaptive immunity. These molecules positively and negatively regulate macrophage and dendritic-cell activation and are essential for T-cell development and differentiation. Evidence is also emerging of the involvement of SOCS proteins in diseases of the immune system. In this Review we bring together data from recent studies on SOCS proteins and their role in immunity, and propose a cohesive model of how cytokine signalling regulates immune-cell function.
Single-molecule studies of repressor–DNA interactions show long-range interactions (2005)

We have performed single-molecule studies of GFP-LacI repressor proteins bound to bacteriophage lambda DNA containing a 256 tandem lac operator insertion confined in nanochannels. An integrated photon molecular counting method was developed to determine the number of proteins bound to DNA. By using this method, we determined the saturated mean occupancy of the 256 tandem lac operators to be 13, which constitutes only 2.5% of the available sites. This low occupancy level suggests that the repressors influence each other even when they are widely separated, at distances on the order of 200 nm, or several DNA persistence lengths.
Contrast differences between scanning ion and scanning electron microscope images (2003)

The contrasts of scanning ion microscope images (Ga+ ion) at 30 keV are compared to those of scanning electron microscope images at 30 keV. Remarkable differences are observed in the surface sensitivity, crystal orientation, and atomic number effects of target material. The examples are shown by the secondary electron images and the origins of those differences are discussed on the basis of the different interactions of those particles with solid.
The histology research of the relationship between different corpus luteum types and the follicular development from cattle ovary (2001)

The results were as following: 1)There were differences function between different types of corpus luteum from the ovaries. 2)There were significant differences between different types of corpus luteum and numbers of different period follicles. 3)There were no significant differences between the different types of corpus luteum and the diameters of different period follicles.
Monoclonal Antibody Recognizing Pre‐S(2) Epitope of Hepatitis B Virus: Characterization of Pre‐S(2) Epitope and Anti‐Pre‐S(2) Antibody (1986)

A hybrid cell line producing monoclonal antibodies recognizing an epitope encoded by the pre-(S)2 region of hepatitis B virus (HBV) genome was obtained by fusion of mouse myeloma cells with lymphocytes from mice immunized with HBV. The monoclonal antibody Mo-F124 secreted from the hybrid line reacted with the pre-S(2) epitope expressed on the surface of both viral and recombinant HBsAg particles--pre-S(2) and S gene product--localised on 34 kD glycoprotein of the viral envelope. The pre-S(2) epitope was sensitive to digestion with V8 protease from Staphylococcus aureus. The enzyme abolished reactivity with Mo-F124 and polymerized human serum albumin (pHSA) binding activity of recombinant particles. Mo-F124 antibody was used to develop highly sensitive radioimmunoassays for determination of pre-S(2) epitope and anti-pre-S(2) antibody in sera of hepatitis B patients. Detection of a pre-S(2) epitope by the monoclonal antibody-based assay in the early phase of acute HBV infection correlated well with the presence of markers of active viral replication (HBeAg, HBV DNA). The appearance of anti-pre-S(2) antibody, usually in the third month after onset of symptoms, was followed by elimination of circulating HBsAg and seroconversion to anti-HBs in all tested cases of uncomplicated acute hepatitis followed by recovery. Anti-pre-S(2) response was not observed in patients with chronic hepatitis B or acute HBV infection progressing to chronic disease. The observed correlation of anti-pre-S(2) response with recovery suggests that the pre-S(2) epitope may represent one of the epitopes inducing antibodies that neutralize the hepatitis B virus.
Ductal Heterogeneity of Cytokeratins, Gene Expression, and Cell Death in the Rat Ventral Prostate (1990)

The rat ventral prostate is a complex gland composed of numerous ducts. The epithelial cells that line the lumen of the ducts are surrounded by stromal cells. The epithelial cells display a characteristic morphology that is dependent on their anatomical location within the ducts; the cells that line the lumen in the region of the ducts close to the urethra (the proximal region) are cuboidal, while those in the distal regions of the ducts are tall columnar cells. We have examined the regional expression of two genes that are expressed in the prostate: prostate steroid-binding protein (PSBP; a marker for androgen-dependent protein synthesis) and TRPM-2 (a marker for programmed cell death). We have demonstrated that the expression of PSBP, in the presence of androgens, and TRPM-2, in the absence of androgens, is restricted to the luminal epithelial cells in the distal regions of the prostatic ducts. Neither of the genes is expressed in the proximal regions of the ducts. In view of the probable effects of the epithelial-stromal interactions in the gland we have also characterized the cytokeratin composition of the epithelial cells lining the prostatic ducts. We have established that the basal epithelial cells of the prostate are primarily localized in the proximal region of the ducts. We propose that these cells may attenuate the influence of the stromal cells on the luminal epithelium and exert a negative influence on the cytodifferentiation of the secretory epithelial cells. The results also suggest that PSBP, which has been considered to be an androgen-dependent gene may, in fact, be a sequence that is constitutively expressed in the luminal cells that die in the absence of androgens. This has significant implications on the mechanism of androgen action in the rat ventral prostate.
NRF2-mediated Notch pathway activation enhances hematopoietic reconstitution following myelosuppressive radiation (2014)

A nuclear disaster may result in exposure to potentially lethal doses of ionizing radiation (IR). Hematopoietic acute radiation syndrome (H-ARS) is characterized by severe myelosuppression, which increases the risk of infection, bleeding, and mortality. Here, we determined that activation of nuclear factor erythroid-2-related factor 2 (NRF2) signaling enhances hematopoietic stem progenitor cell (HSPC) function and mitigates IR-induced myelosuppression and mortality. Augmenting NRF2 signaling in mice, either by genetic deletion of the NRF2 inhibitor Keap1 or by pharmacological NRF2 activation with 2-trifluoromethyl-2'-methoxychalone (TMC), enhanced hematopoietic reconstitution following bone marrow transplantation (BMT). Strikingly, even 24 hours after lethal IR exposure, oral administration of TMC mitigated myelosuppression and mortality in mice. Furthermore, TMC administration to irradiated transgenic Notch reporter mice revealed activation of Notch signaling in HSPCs and enhanced HSPC expansion by increasing Jagged1 expression in BM stromal cells. Administration of a Notch inhibitor ablated the effects of TMC on hematopoietic reconstitution. Taken together, we identified a mechanism by which NRF2-mediated Notch signaling improves HSPC function and myelosuppression following IR exposure. Our data indicate that targeting this pathway may provide a countermeasure against the damaging effects of IR exposure.
Development and Validation of a High-Performance Liquid Chromatography Method for the Evaluation of Niflumic Acid Cross-Reactivity of Two Commercial Immunoassays for Cannabinoids in Urine (2010)

Niflumic acid is a nonsteroidal, anti-inflammatory drug widely prescribed in Greece. We recently noticed that this drug cross-reacts for cannabinoids in a kinetic interaction of microparticles in a solution (KIMS) immunoassay method but does not in an enzyme multiplied immunoassay technique (EMIT) immunoassay method. The objective of the study was to develop and validate a high-performance liquid chromatographic method in order to evaluate niflumic acid cross-reactivity in two commercial immunoassays for cannabinoids in urine, both in niflumic acid standards as well as in urine specimens obtained from subjects receiving niflumic acid. Urine niflumic acid standards were prepared in drug-free urine at 13 concentrations ranging from 1.25 to 1000 microg/mL. The standards gave presumptive positive cannabinoids results when analyzed by the KIMS immunoassay method when the concentration was above 2.5 microg/mL. None of the prepared standards gave a false-positive cannabinoid result when analyzed by the EMIT immunoassay method. By applying a 50 ng/mL cutoff for cannabinoids in these assays, all 55 urine specimens collected from the 5 subjects who participated gave negative results by the EMIT and false-positive results by the KIMS immunoassay method. It is concluded that KIMS is more prone to cross-reactions by niflumic acid compared to EMIT. Therefore, all positive screening tests for cannabinoids obtained by KIMS should be confirmed by another technique.
Spread Spectrum and Time Division Multiple Access Satellite Communications (1977)

Although time division multiple access (TDMA) satellite communication provides the highest traffic capacity per satellite and offers efficient transmission of a wide variety of services, it suffers from network timing and ranging requirements and message security. On the other hand, spread spectrum multiple access (SSMA) satellite communication is suited for reliable random access and tactical transmission systems. Orthogonal functions such as Rademacher, Haar, and Walsh, or pseudonoise sequence coding of amplitude and phase of the analog message or code division of baseband signals, frequency and time hopping are among the several methods employed for spread spectrum communications. A combination of TDMA and SSMA can be used for asynchronous and reliable transmission of digital or analog signals.
Short-chain dehydrogenases/reductases (SDR) (1995)

Short-chain dehydrogenases/reductases (SDR) constitute a large protein family. Presently, at least 57 characterized, highly different enzymes belong to this family and typically exhibit residue identities only at the 15-30% level, indicating early duplicatory origins and extensive divergence. In addition, another family of 22 enzymes with extended protein chains exhibits part-chain SDR relationships and represents enzymes of no less than three EC classes. Furthermore, subforms and species variants are known of both families. In the combined SDR superfamily, only one residue is strictly conserved and ascribed a crucial enzymatic function (Tyr 151 in the numbering system of human NAD(+)-linked prostaglandin dehydrogenase). Such a function for this Tyr residue in SDR enzymes in general is supported also by chemical modifications, site-directed mutagenesis, and an active site position in those tertiary structures that have been characterized. A lysine residue four residues downstream is also largely conserved. A model for catalysis is available on the basis of these two residues. Binding of the coenzyme, NAD(H) or NADP(H), is in the N-terminal part of the molecules, where a common GlyXXXGlyXGly pattern occurs. Two SDR enzymes established by X-ray crystallography show a one-domain subunit with seven to eight beta-strands. Conformational patterns are highly similar, except for variations in the C-terminal parts. Additional structures occur in the family with extended chains. Some of the SDR molecules are known under more than one name, and one of the enzymes has been shown to be susceptible to native, chemical modification, producing reduced Schiff base adducts with pyruvate and other metabolic keto derivatives. Most SDR enzymes are dimers and tetramers. In those analyzed, the area of major subunit contacts involves two long alpha-helices (alpha E, alpha F) in similar and apparently strong subunit interactions. Future possibilities include verification of the proposed reaction mechanism and tracing of additional relationships, perhaps also with other protein families. Short-chain dehydrogenases illustrate the value of comparisons and diversified research in generating unexpected discoveries.
Fiber-optic bus-oriented single-hop interconnections among multi-transceiver stations (1991)

The merits of the single-path selective-broadcast interconnection (SBI) implemented in fiber-optic technology are explored. This is a static, passive, fiber-optic interconnection among a set of stations, each equipped with multiple transmitters, and receivers. It uses c/sup 2/ buses, each interconnecting a subset of the stations, and provides a single optical path between any two stations. Thus, it succeeds in decoupling transmission rate from aggregate network throughput. It offers substantial advantages in power budget and the maximum number of stations that can be connected without repeaters and amplifiers. When compared with c buses, each interconnecting all stations, this SBI is attractive in terms of the required passive fiber-optic components such as fiber segments and star couplers. For a fixed power budget, the capacity of this SBI is optimal among bus-oriented single-hop interconnections for both a uniform traffic pattern and worst-case unknown skew.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors (2011)

The R- and S-enantiomer of N-(4-(3-(1-ethyl-3,3-difluoropiperidin-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-4-yloxy)-3-fluorophenyl)-2-(4-fluorophenyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide are novel MET kinase inhibitors that have been investigated as potential anticancer agents. The effect of the chirality of these compounds on preclinical in vivo pharmacokinetics and toxicity was studied. The plasma clearance for the S-enantiomer was low in mice and monkeys (23.7 and 7.8 mL min(-1) kg(-1), respectively) and high in rats (79.2 mL min(-1) kg(-1)). The R/S enantiomer clearance ratio was 1.5 except in rats (0.49). After oral single-dose administration at 5 mg kg(-1) the R/S enantiomer ratio of AUC(inf) was 0.95, 1.9 and 0.41 in mice, rats and monkeys, respectively. In an oral single-dose dose-ranging study at 200 and 500 mg kg(-1) and multi-dose toxicity study in mice plasma AUC exposure was approximately 2- to 3-fold higher for the R-enantiomer compared to the S-enantiomer. Greater toxicity of the S-enantiomer was observed which appeared to be due to high plasma C(min) values and tissue concentrations approximately 24 h after the final dose. Both enantiomers showed low to moderate permeability in MDCKI cells with no significant efflux, no preferential distribution into red blood cells and similar plasma protein binding in vitro. Overall, the differences between the enantiomers with respect to low dose pharmacokinetics and in vitro properties were relatively modest. However, toxicity results warrant further development of the R-enantiomer over the S-enantiomer.