gebhart/patrepeval huggingface dataset:
Effect of donor source on renal allograft function in children on triple immunosuppression (1994)

Results of renal transplantation using cadaver donors (CAD) are usually inferior to those using living related donors (LRD). We have previously reported 100% 1-year CAD and LRD graft survival using adult cadaver donors and triple immunosuppression. In the present study glomerular and tubular function of 23 LRD and 22 CAD grafts (median ages 3.5 and 2.6 years) were compared during 3 years after transplantation. Glomerular filtration rate (GFR) and renal plasma flow were lower in CAD grafts but remained stable in both groups. The mean GFRs were 87.3 and 63.2 ml/min/1.73 m2 at discharge and 82.8 and 72.5 ml/min/1.73 m2 at 36 months in LRD and CAD grafts respectively. No significant differences were found after 6 months. Tubular function was good in both groups. The only significant difference was in urate handling at 36 months (mean serum urate 396 mumol/l in CAD, 301 in LRD grafts, P < 0.05). Cyclosporin nephrotoxicity manifested as hyperkalaemia due to reduced distal potassium secretion and/or adrenal suppression. In conclusion, donor source had little effect on the development of progressive allograft dysfunction using adult CAD grafts and triple immunosuppression with CsA administered in three daily doses to preschool children.
Structure and Thermal Properties of Lithium Cyanate (2011)

Abstract The synthesis, structural, and thermal characterization of lithium cyanate are reported in this work. LiOCN forms crystals in the trigonal crystal system. The structure was solved in the space group R $\bar{3}$ m . It is isomorphous to the structure of sodium cyanate. In the temperature range from –90 °C up to the melting point no phase transition was observed. Furthermore the vibrational Raman spectrum was measured. The system KOCN‐LiOCN shows a dystecticum and the new phase was confirmed by powder X‐ray diffraction.
Sub-90 nm technologies-challenges and opportunities for CAD (2003)

Future high performance microprocessor design with technology scaling beyond 90 nm will pose two major challenges: (1) energy and power, and (2) parameter variations. Design practice will have to change from deterministic design to probabilistic and statistical design. This paper discusses circuit techniques and design automation opportunities to overcome the challenges.
Ruthenium Amide Complexes – Synthesis and Catalytic Activity in Olefin Metathesis and in Ring‐Opening Polymerisation (2018)

A set of olefin metathesis catalysts bearing a ruthenium amide moiety was synthesised. In the ruthenium amide form these complexes exhibit very low activity in standard metathesis reactions. However, a dramatic increase of activity was observed upon in situ activation with trimethylsilyl chloride or HCl, allowing successful application of such catalysts in a number of model ring‐closing metathesis, cross‐metathesis and enyne transformations. Moreover, such activated complexes proved to be very effective catalysts for bulk polymerisation of dicyclopentadiene (DCPD). The influence of factors such as temperature and the nature of additives on the properties of poly‐DCPD was examined.
High-dimensional index structures database support for next decade's applications (tutorial) (1998)

No abstract available.
Identification of p130 as an in VivoSubstrate of Receptor Protein-tyrosine Phosphatase α (2000)

We have employed a substrate trapping strategy to identify physiological substrates of the receptor protein-tyrosine phosphatase alpha (RPTPalpha). Here we report that a substrate-trapping mutant of the RPTPalpha membrane proximal catalytic domain (D1), RPTPalpha-D1-C433S, specifically bound to tyrosine-phosphorylated proteins from pervanadate-treated cells. The membrane distal catalytic domain of RPTPalpha (D2) and mutants thereof did not bind to tyrosine-phosphorylated proteins. The pattern of tyrosine-phosphorylated proteins that bound to RPTPalpha-D1-C433S varied between cell lines, but a protein of approximately 130 kDa was pulled down from every cell line. This protein was identified as p130(cas). Tyrosine-phosphorylated p130(cas) from fibronectin-stimulated NIH3T3 cells bound to RPTPalpha-D1-C433S as well, suggesting that p130(cas) is a physiological substrate of RPTPalpha. RPTPalpha dephosphorylated p130(cas) in vitro, and RPTPalpha co-localized with a subpopulation of p130(cas) to the plasma membrane. Co-transfection experiments with activated SrcY529F, p130(cas), and RPTPalpha or inactive, mutant RPTPalpha indicated that RPTPalpha dephosphorylated p130(cas) in vivo. Tyrosine-phosphorylated epidermal growth factor receptor was not dephosphorylated by RPTPalpha under these conditions, suggesting that p130(cas) is a specific substrate of RPTPalpha in living cells. In conclusion, our results provide evidence that p130(cas) is a physiological substrate of RPTPalpha in vivo.
Sperm-borne glutathione-S-transferase omega 2 accelerates the nuclear decondensation of spermatozoa during fertilization in mice† (2019)

The postacrosomal sheath (PAS) of the perinuclear theca (PT) is the first compartment of the sperm head to solubilize into the ooplasm upon sperm-oocyte fusion, implicating its constituents in zygotic development. This study investigates the role of one such constituent, glutathione-S-transferase omega 2 (GSTO2), an oxidative-reductive enzyme found in the PAS and perforatorial regions of the PT. GSTO2 uses the conjugation of reduced glutathione, an electron donor shown to be compulsory in sperm disassembly within the ooplasm. The proximity of GSTO2 to the condensed sperm nucleus led us to hypothesize that this enzyme may facilitate nuclear decondensation by reducing disulfide bonds before the recruitment of GSTO enzymes from within the ooplasm. To test this hypothesis, we utilized a cell permeable isozyme-specific inhibitor, which fluoresces when bound to the active site of GSTO2, to functionally inhibit spermatozoa before performing intracytoplasmic sperm injections (ICSI) in mice. The technique allowed for targeted inhibition of solely PT-residing GSTO2, as all that is required for complete zygotic development is the injection of the mouse spermatozoon head. ICSI showed that inhibition of PT-anchored GSTO2 caused a delay in sperm nuclear decondensation, and further resulted in untimely embryo cleavage, and an increase in fragmentation beginning at the morula stage. The confounding effects of these developmental delays ultimately resulted in decreased blastocyst formation. This study implicates PT-anchored GSTO2 as an important facilitator of nuclear decondensation and reinforces the notion that the PAS-PT is a critical sperm compartment harboring molecules that facilitate zygotic development.
Ca2+ coupling in vascular smooth muscle: Mg2+ and buffer effects on contractility and membrane Ca2+ movements (1982)

An examination of the literature, over the past two decades, reveals that (1) in studies of different types of vascular smooth muscles, Mg2+ is often either left out of physiological salt solutions or reduced in concentration compared with that in blood; and (2) when excitation--contraction coupling processes have been examined in isolated vascular tissues and cells, a number of artificial (synthetic) amine and organic zwitterion buffers have often been substituted for the naturally occurring bicarbonate and phosphate anions found in the blood and in cells. The influence of extracellular magnesium ions ([Mg2+]0) on tone, contractility, reactivity, and divalent cation movements in vascular smooth muscles, and how they may relate to certain vascular disease states, is reviewed. Data are presented and reviewed which indicate that many of the most commonly used artificial buffers (e.g., Tris, HEPES, MOPS, Bicine, PIPES, imidazole) can exert adverse effects on contractility and reactivity of certain arterial and venous smooth muscles. The data reviewed herein suggest that [Mg2+]0 and membrane Mg are important in the regulation of vascular tone, vascular reactivity, and in control of Ca uptake, content, and distribution in smooth muscle cells. [HCO3-]0 and (or) PO4(2-) anions may be important for normal maintenance of excitability and reactivity and in the control of Ca uptake, content, and distribution in smooth muscle cells.
Synthesis of chiral GABAA receptor subtype selective ligands as potential agents to treat schizophrenia as well as depression (2018)

A series of novel imidazobenzodiazepine analogs of the lead chiral ligand SH-053-2'F-<i>S</i>-CH<sub>3</sub> (<b>2</b>), an α2/α3/α5 (Bz)GABA (A)ergic receptor subtype selective ligand, which reversed PCP-induced prepulse inhibition (PPI) of acoustic startle, were synthesized. These chiral (<i>S</i>)-CH<sub>3</sub> ligands are targeted for the treatment of schizophrenia and depression. These new ligands were designed by modifying the liable ester functionality in <b>2</b> to improve the metabolic stability, cytotoxicity, and activity as compared to <b>2</b>. Based on the data to date, the most promising ligands are the <i>N</i>-cyclopropyl amide GL-I-55 (<b>8c</b>) and the methyl bioisostere GL-I-65 (<b>9a</b>). The <i>in vitro</i> metabolic stability, cytotoxicity and <i>in vivo</i> locomotor effects are described in this report. Based on these results, <b>8c</b> and <b>9a</b> are the most promising for further <i>in vivo</i> pharmacology.
Isoquinoline thiosemicarbazone displays potent anticancer activity with in vivo efficacy against aggressive leukemias (2020)

A potent class of isoquinoline-based α-N-heterocyclic carboxaldehyde thiosemicarbazone (HCT) compounds has been rediscovered; based upon this scaffold, three series of antiproliferative agents were synthesized through iterative rounds of methylation and fluorination modifications, with anticancer activities being potentiated by physiologically relevant levels of copper. The lead compound, <b>HCT-13</b>, was highly potent against a panel of pancreatic, small cell lung carcinoma, prostate cancer, and leukemia models, with IC<sub>50</sub> values in the low-to-mid nanomolar range. Density functional theory (DFT) calculations showed that fluorination at the 6-position of <b>HCT-13</b> was beneficial for ligand-copper complex formation, stability, and ease of metal-center reduction. Through a chemical genomics screen, we identify DNA damage response/replication stress response (DDR/RSR) pathways, specifically those mediated by ataxia-telangiectasia and Rad3-related protein kinase (ATR), as potential compensatory mechanism(s) of action following <b>HCT-13</b> treatment. We further show that the cytotoxicity of <b>HCT-13</b> is copper-dependent, that it promotes mitochondrial electron transport chain (mtETC) dysfunction, induces production of reactive oxygen species (ROS), and selectively depletes guanosine nucleotide pools. Lastly, we identify metabolic hallmarks for therapeutic target stratification and demonstrate the <i>in vivo</i> efficacy of <b>HCT-13</b> against aggressive models of acute leukemias in mice.
Novel TMEM98 mutations in pedigrees with autosomal dominant nanophthalmos. (2015)

A recent report identified a single TMEM98 missense mutation in a nanophthalmos pedigree. Our discovery of two additional TMEM98 mutations confirms the important role of the gene in the pathogenesis of autosomal dominant nanophthalmos.
Magnetization preparation during the steady state: Fat‐saturated 3D TrueFISP (2001)

A novel fat saturation scheme is proposed which combines spectral fat saturation with a steady-state 3D true Fast Imaging with Steady Precesson (TrueFISP) sequence. Fat saturation consisted of a conventional frequency-selective excitation pulse surrounded by spoiler gradients. This saturation block was periodically repeated within a continuously running TrueFISP sequence. Except for the fat signals, the steady-state signal formation and the resulting image contrast of TrueFISP was not modified by the periodically inserted fat saturation block. This was achieved by a alpha/2 flip-back pulse before the fat saturation block, which stores the established steady-state transverse magnetization as pure longitudinal magnetization. After fat saturation this longitudinal magnetization was excited by a alpha/2 preparation pulse to continue the TrueFISP acquisition. The resulting images show contrast identical to conventional TrueFISP images, but without the usually very bright fat signals. The short repetition time allows acquisition of a 3D data set of the abdomen within a single breath-hold.
Supplementary Figure 2 from SMAC Mimetic (JP1201) Sensitizes Non–Small Cell Lung Cancers to Multiple Chemotherapy Agents in an IAP-Dependent but TNF-α–Independent Manner (2023)

&lt;p&gt;PDF file - 671K, A, H358, D, H1819, G, H2887 treated with gemcitabine alone (brown circles), or treated with gemcitabine in the presence of 10 mM JP1201 (red diamonds), luciferase siRNA (black circles), cIAP1 siRNA (blue triangles), cIAP2 siRNA (grey triangles), XIAP siRNA (green squares), or the combination of cIAP1, cIAP2, and XIAP siRNA (orange squares). B, H358, E, H1819, H, H2887 treated with paclitaxel alone (brown circles), or treated with paclitaxel in the presence of 10 mM JP1201 (red diamonds), luciferase siRNA (black circles), cIAP1 siRNA (blue triangles), cIAP2 siRNA (grey triangles), XIAP siRNA (green squares), or the combination of cIAP1, cIAP2, and XIAP siRNA (orange squares). C, H358, F, H1819, I, H2887 treated with vinorelbin alone (brown circles), or treated with vinorelbine in the presence of 10 mM JP1201 (red diamonds), luciferase siRNA (black circles), cIAP1 siRNA (blue triangles), cIAP2 siRNA (grey triangles), XIAP siRNA (green squares), or the combination of cIAP1, cIAP2, and XIAP siRNA (orange squares).&lt;/p&gt;
Nanoimprint of Proton Exchange Membrane for MEMS-based Fuel Cell Application (2007)

It is difficult to achieve large surface reaction area in MEMS-based fuel cell because of volume and material limits. In this work, we put forward a novel method to get large surface reaction area in MEMS-based fuel cell. The novel method consisted of the formation of fine pattern in proton exchange membrane by nanoimprint technology. We modified the surface of Nafion <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">reg</sup> 117 membrane by thermal nanoimprint. MEMS-based direct methanol fuel cell of the nanoimprint membrane showed greatly improved performance. The as-achieved performance was much better than the state-of-the-art of MEMS-based direct methanol fuel cell with planar electrode. Maximum power density had been improved by about 10 times. The nanoimprint technology shows innovative advantages due to low cost and simple process.
Enhanced stability of a chimeric hepatitis B core antigen virus-like-particle (HBcAg-VLP) by a C-terminal linker-hexahistidine-peptide (2018)

These findings establish the genetically simply transferable C-terminal polyhistidine-peptide as a general stabilizing element for chimeric HBcAg-VLPs to increase their suitability.
ChemInform Abstract: Aluminum(III) Chloride‐Catalyzed Reaction of 1,1,1‐Trichloroethane with Aromatic Compounds: A Facile Synthesis of Symmetrical 1,1‐Diphenylethylenes. (2001)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Vascular 05 (2002)

Aim: Leucocyte adhesion to the endothelium is implicated in the pathogenesis of IRI in several vascular beds, including skeletal muscle. The magnitude and time course of expression of adhesion molecules such as E- and P-selectin is an important and rate-limiting step in the pathogenesis of IRI. Methods: A dual radiolabelled monoclonal antibody (mAb) technique was used to quantify E- and P-selectin expression in (a) rat hindlimbs with tourniquet-induced ischaemia for 4 h, followed by 3, 6 or 24 h of reperfusion, (b) the non-ischaemic hindlimb and (c) the small bowel in rats exposed to IRI and a sham protocol of IRI. Results: There was no significant increase in E-selectin expression, regardless of reperfusion time when compared to sham animals or the non-ischaemic hindlimb. No E-selectin expression was detected in the small bowel of animals of either experimental or sham protocols. In contrast a significant increase in P-selectin expression was observed in the ischaemic limb: 3.1, 4.3 and 1.7 ng mAb g−1 compared to the non-ischaemic limb: 0.2, 0.1 and 0.1 ng mAb g−1, at 3, 6 and 24 h, respectively. P-selectin expression was significantly raised in the small bowel at 3-h reperfusion: 0.6 ng mAb g−1 tissue versus 0.5 ng mAb g−1 tissue for sham. Conclusion: Skeletal muscle IRI is associated with a significant increase in P– but not E-selectin expression in the injured hindlimb and small bowel. This differential response may be related to platelet accumulation in tissues exposed to IRI.
Brain insulin sensitivity is linked to adiposity and body fat distribution (2020)

To read the full abstract: Nat Commun. 2020;11(1):1841. Published 2020 Apr 15. doi: https://pubmed.ncbi.nlm.nih.gov/32296068/
The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug (2022)

Chronic myeloid leukemia (CML) is driven by the constitutive activity of the BCR-ABL1 fusion oncoprotein. Despite the great success of drugs that target the BCR-ABL1 ATP-binding site in transforming CML into a manageable disease, emerging resistance point mutations impair inhibitor binding, thereby limiting the effectiveness of these drugs. Recently, allosteric inhibitors that interact with the ABL1 myristate-binding site have been shown to awaken an endogenous regulatory mechanism and reset full-length BCR-ABL1 into an inactive assembled state. The discovery and development of these allosteric inhibitors demonstrates an in-depth understanding of the fundamental regulatory mechanisms of kinases. In this review, we illustrate the structural basis of c-ABL1's dynamic regulation of autoinhibition and activation, discuss the discovery of allosteric inhibitors and the characterization of their mechanism of action, present the therapeutic potential of dual binding to delay the development of mutation-driven acquired resistance, and suggest key lessons learned from this program.
Simple Frequency Characteristic Evaluation of Shaped-Beam Design for Reflectarray Antenna (2018)

The analysis of the reflectarray antenna's frequency characteristics is a time consuming task. This is owing to the design of the size of the phasing elements, and the analysis of the reflection phase of the phasing elements. We propose a method for estimating the frequency characteristics of a reflectarray antenna by introducing aberration theory. The frequency characteristics can be estimated without the design consideration to phasing element size, and by the analysis of the reflection phase of phasing elements by the conditions of aberration theory. Therefore, in this paper, we propose a simple method to estimate the frequency characteristics of the reflectarray antenna that does not require element design estimates the frequency characteristics by using the desired reflection phase of our proposed design frequency.
Abstract 17473: Obesity is Associated With Impaired Left Atrial Function in Young Patients With Recent Onset Atrial Fibrillation (2015)

Introduction: Obesity is a risk factor for atrial fibrillation (AF), and reduction of weight has been shown to reduce the burden of AF. However, the exact underlying pathogenesis is unknown. Hypothesis: We hypothesize that obesity is related with impaired left atrial function, measured with echocardiographic strain analysis, in young patients (&lt;60 years) with recent onset AF (AF history&lt; 3 years). Methods: We studied 94 patients of the Phenotyping young-onset AF patients study, all with sinus rhythm during echocardiography. Detailed clinical and echocardiographic information was collected. Three strain-patterns (reservoir, activation, and conduit strain) representing left atrial functional phases were measured. Results: Of the 94 patients, 32 were obese and 62 were non-obese (34±3 kg/m2 vs. 25±2 kg/m2, p&lt;0.001). Mean age was 50±9 years and 34% were women. No significant differences in cardiovascular conditions and risk factors were found, except for diabetes mellitus (13% vs. 2%, p=0.026), and metabolic syndrome (56% vs. 8%, p&lt;0.001), both more common in obese patients. Left atrial volume index (mean 30±8ml/m2), and left ventricular mass index and ejection fraction were not significantly different between both groups. However, the left atrial reservoir (27±8 vs. 33±10%, p=0.008) and conduit strain (16±6 vs. 20±8%, p=0.011) were significantly reduced in obese patients, the left atrial activation strain was not (p=0.118). Using linear regression analysis adjusting for significant baseline differences, the association between reservoir strain (beta=-0.304, p=0.013), and conduit strain (beta=-0.246, p=0.045) and obesity remained significant. The correlation between BMI and left atrial function are shown in the figure. Conclusions: In young patients with recent onset AF, obesity is associated with impaired left atrial function, in absence of dilatation. Left atrial dysfunction may be the first sign of atrial remodeling in obese AF patients.
Materials in Space: Exploring the Effect of Low Earth Orbit on Thin Film Solid Lubricants (2014)

Abstract This article considers the effect of atomic oxygen exposure in low earth orbit on thin film solid lubricants of molybdenum disulphide and diamond-like carbon nanocomposites, a silica-containing diamond-like carbon film. Advances in deposition methods over the past few decades enable dense films to be created that are more resistant to oxidative degradation and the effects of adsorbed moisture than their predecessors. Further, incorporating additional phases improves the tribological performance of the films in a range of atmospheres.
The anatomical basis of intestinal immunity (1997)

The lymphoid tissues associated with the intestine are exposed continuously to antigen and are the largest part of the immune system. Many lymphocytes are found in organised tissues such as the Peyer's patches and mesenteric lymph nodes, as well as scattered throughout the lamina propria and epithelium of the mucosa itself. These lymphocyte populations have several unusual characteristics and the intestinal immune system is functionally and anatomically distinct from other, peripheral compartments of the immune system. This review explores the anatomical and molecular basis of these differences, with particular emphasis on the factors which determine how the intestinal lymphoid tissues discriminate between harmful pathogens and antigens which are beneficial, such as food proteins or commensal bacteria. These latter antigens normally provoke immunological tolerance, and inappropriate responses to them are responsible for immunopathologies such as food hypersensitivity and inflammatory bowel disease. We describe how interactions between local immune cells, epithelial tissues and antigen-presenting cells may be critical for the induction of tolerance and the expression of active mucosal immunity. In addition, the possibility that the intestine may act as an extrathymic site for T-cell differentiation is discussed. Finally, we propose that, under physiological conditions, immune responses to food antigens and commensal bacteria are prevented by common regulatory mechanisms, in which transforming growth factor beta plays a critical role.