gebhart/patrepeval huggingface dataset:
Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings (2021)

This work surveys a variety of diamino-heterocycles as an isosteric replacement for the piperazine substructure of our previously disclosed piperarinyl-tetrahydroisoquinoline containing CXCR4 antagonists. A late-stage Buchwald coupling route was developed for rapid access to final compounds from commercial building blocks. Among 13 analogs in this study, compound <b>31</b> embodying an aza-piperazine linkage was found to have the best overall profile with potent CXCR4 inhibitory activity and favorable in vitro absorption, distribution, metabolism, and excretion (ADME) properties. An analysis of the calculated physiochemical parameters (ROF, cLogD) and the experimental ADME attributes of the analogs lead to the selection of <b>31</b> for pharmacokinetic studies in mice. Compared with the clinical compound AMD11070, compound <b>31</b> has no CYP450 3A4 or 2D6 inhibition, higher metabolic stability and PAMPA permeability, greatly improved physiochemical parameters, and superior oral bioavailability (%<i>F</i> = 24). A binding rationale for <b>31</b> within CXCR4 was elucidated from docking and molecular simulation studies.
Serum IL-13 Predicts Response to Golimumab in Bio-Naïve Ulcerative Colitis (2022)

A certain number of patients with ulcerative colitis (UC) are refractory to anti-TNF-α antibodies; biomarkers are thus needed to predict treatment efficacy. This study aimed to evaluate whether serum biomarkers that were reported to be associated with UC or anti-TNF-α antibody could predict the response to golimumab, a human anti-TNF-α monoclonal antibody, in bio-naïve patients with UC. We prospectively enrolled 23 consecutive patients with UC who were treated with golimumab. Serum samples were collected before the first golimumab dose. Eleven molecules were measured by electrochemiluminescence (ECL) or enzyme-linked immunosorbent assay (ELISA) and their association with efficacy after 10 weeks of golimumab treatment. Among the serum biomarkers, IL-13 levels were significantly higher in the non-remission group than in the remission group (<i>p</i> = 0.014). IL-15 levels were significantly lower in the non-response group than in the response group (<i>p</i> = 0.04). For clinical remission at week 10, the IL-13 0.20 concentration of pg/mL was associated with a sensitivity and specificity of 82.4% and 83.3%, respectively. Serum IL-13 may be a biomarker to predict golimumab efficacy in biologic-naïve patients with UC, and thus may help to tailor personalized treatment strategies.
Decision making for symbolic probability (2004)

This paper proposes a decision theory for a symbolic generalization of probability theory (SP). Darwiche and Ginsberg [2, 3] proposed SP to relax the requirement of using numbers for uncertainty while preserving desirable patterns of Bayesian reasoning. SP represents uncertainty by symbolic supports that are ordered partially rather than completely as in the case of standard probability. We show that a preference relation on acts that satisfies a number of intuitive postulates is represented by a utility function whose domain is a set of pairs of supports. We argue that a subjective interpretation is as useful and appropriate for SP as it is for numerical probability. It is useful because the subjective interpretation provides a basis for uncertainty elicitation. It is appropriate because we can provide a decision theory that explains how preference on acts is based on support comparison.
Figure S2 from Genomic and Epigenomic Landscaping Defines New Therapeutic Targets for Adenosquamous Carcinoma of the Pancreas (2023)

&lt;p&gt;A-B) DNA content histograms and genomic profiles of flow sorted diploid only ASCP biopsies. A) female (two copies of chromosome X) and; B) male (one copy of chromosome X) diploid only ASCP biopsies. In both cases the 4.0N fractions were &lt;6% of the sample. C) DNA content histograms of ASCP PDX models. Each sample had a mouse host (green) and at least one tumor peak (red). All PDX samples were flow sorted prior to CNV, exome, and ATAC-seq analysis.&lt;/p&gt;
Design of a wide-bandwidth on-chip antenna for uncooled passive THz imaging (2013)

The design of a broadband on-chip antenna for passive THz imaging in the frequency range of 0.6 THz to 1.4 THz is reported. The antenna design has to fulfill the requirements of the IBM CMOS process and the MEMS post CMOS processing. The antenna is coupled directly to the sensor, a MOSFET bolometer. Because of this direct coupling and the need for real time imaging, only extremely physically small antennas are feasible. Hence, typical broadband antennas like the toothed log-periodic antenna are not useable for this application and new antenna approaches have to be examined.
Design and Characterization of Novel Wear Resistant Multilayer CVD Coatings with Improved Adhesion Between Al2O3 and Ti(C,N) (2010)

Abstract Multilayer CVD coatings for high speed cutting applications were designed to achieve high wear and heat resistance during machining of steel alloys. In this work the microstructure and cutting performance of these novel multilayer CVD coatings are investigated and compared with standard CVD multilayer coatings. 3D‐FIB tomography is used to characterize the microstructure of the layers, especially the transition between the Ti(C,N) and the Al 2 O 3 layer. The 3D reconstruction of the surface of the Ti(C,N) layer shows the formation of protruded Ti(C,N) grains with a very particular architecture, which penetrate into the Al 2 O 3 top‐layer, providing a mechanical anchoring between both layers. Cemented carbides coated with the novel CVD multilayer present reduced crater and flank wear as well as improved adherence between the Al 2 O 3 top‐layer and the Ti(C,N) layer leading to a dramatic improvement of cutting performance.
Correction to Effect of Water Content on Sodium Chloride Sorption in Cross-Linked Cation Exchange Membranes (2019)

ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to Effect of Water Content on Sodium Chloride Sorption in Cross-Linked Cation Exchange MembranesEui-Soung JangEui-Soung JangMore by Eui-Soung Janghttp://orcid.org/0000-0001-5515-9789, Jovan KamcevJovan KamcevMore by Jovan Kamcev, Kentaro KobayashiKentaro KobayashiMore by Kentaro Kobayashi, Ni YanNi YanMore by Ni Yan, Rahul SujananiRahul SujananiMore by Rahul Sujanani, Samantha J. TalleySamantha J. TalleyMore by Samantha J. Talley, Robert B. MooreRobert B. MooreMore by Robert B. Moorehttp://orcid.org/0000-0001-9057-7695, Donald R. PaulDonald R. PaulMore by Donald R. Paul, and Benny D. Freeman*Benny D. FreemanMore by Benny D. Freemanhttp://orcid.org/0000-0003-2779-7788Cite this: Macromolecules 2019, 52, 9, 3573Publication Date (Web):April 26, 2019Publication History Published online26 April 2019Published inissue 14 May 2019https://pubs.acs.org/doi/10.1021/acs.macromol.9b00737https://doi.org/10.1021/acs.macromol.9b00737correctionACS PublicationsCopyright © 2019 American Chemical Society. This publication is available under these Terms of Use. Request reuse permissions This publication is free to access through this site. Learn MoreArticle Views896Altmetric-Citations-LEARN 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 PDF (235 KB) Get e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
The experimental study of a miniature high-speed gas-bearing expansion turbine (2011)

The miniature high-speed gas-bearing turbomachinery is one of the research focuses in the fields of energy and cryogenic engineering in recent years. In this article, a new miniature static gas-bearing expansion turbine with a shaft diameter of 6 mm, turbine impeller diameter of 9 mm, and designed rotational speed of 300 000 r/min was developed. The developed prototype of this miniature expansion turbine is comprehensively introduced and the structure characteristics are presented. Then the preliminary mechanical and thermodynamic performances for the developed prototype are experimentally measured. Research results show that this developed expansion turbine has some noticeable features, such as stable operation with small vibration. It can reach 15 per cent over-speed and provide a quick temperature drop. Experimental verification demonstrates that both mechanical and thermodynamic performances agree with expected requirements. Hence, a strong base has been established in China to further develop miniature high-speed gas-bearing expansion turbines.
Imaging the collapse of electron wave-functions: the relation to plasmonic losses (2019)

We show how free-electron interaction with plasmons in electron microscopes leads to electron-plasmon entanglement, connecting electron decoherence with plasmonic losses. We utilize this connection to propose a new method to probe plasmonic lifetimes. © 2019 The Author(s)
Self-accelerating self-trapped nonlinear beams of Maxwell's equations (2012)

We present shape-preserving self-accelerating beams of Maxwell's equations with optical nonlinearities. Such beams are exact solutions to Maxwell's equations with Kerr or saturable nonlinearity. The nonlinearity contributes to self-trapping and causes backscattering. Those effects, together with diffraction effects, work to maintain shape-preserving acceleration of the beam on a circular trajectory. The backscattered beam is found to be a key issue in the dynamics of such highly non-paraxial nonlinear beams. To study that, we develop two new techniques: projection operator separating the forward and backward waves, and reverse simulation. Finally, we discuss the possibility that such beams would reflect themselves through the nonlinear effect, to complete a 'U' shaped trajectory.
High-Efficiency Operating Modes for Isolated Piezoelectric-Transformer-Based DC-DC Converters (2020)

The drive to miniaturize power electronics motivates investigation into alternative converter energy storage technologies such as piezoelectrics, which offer fundamentally higher power density and efficiency capabilities compared to magnetics. Piezoelectric transformers (PTs) have seen utilization in dc-dc converter designs, but typically alongside magnetics or with limited/unreported efficiency. In this work, we systematically enumerate isolated dc-dc converter operating modes and topologies that utilize PTs as their only energy storage components. The proposed operating modes leverage simple converter topologies to maintain high-efficiency behaviors (e.g., zero voltage switching (ZVS) and all-positive instantaneous power transfer) across wide operating regions. We present techniques for deriving these operating modes' ZVS regions, estimating PT efficiency, mapping switching sequence combinations to the PT's resonant cycle, and solving for periodic steady state and switching times; these offer insights for comparing and implementing design options. We then illustrate an example design and verify our analyses using LTspice simulations, which attest to the high potential capabilities of dc-dc converters based on strategically-utilized PTs.
Preparation of (3S)-N,N-1,7-Bis-tert- butoxycarbonyl-3-hydroxyspermidine in High Enantiomeric Purity (1999)

ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTPreparation of (3S)-N,N-1,7-Bis-tert- butoxycarbonyl-3-hydroxyspermidine in High Enantiomeric PurityD. Scott Coffey, Andrew I. McDonald, and Larry E. OvermanView Author Information Department of Chemistry, 516 Rowland Hall, University of California, Irvine, California 92697-2025 Cite this: J. Org. Chem. 1999, 64, 23, 8741–8742Publication Date (Web):October 16, 1999Publication History Received1 July 1999Published online16 October 1999Published inissue 1 November 1999https://pubs.acs.org/doi/10.1021/jo991061mhttps://doi.org/10.1021/jo991061mbrief-reportACS PublicationsCopyright © 1999 American Chemical SocietyRequest reuse permissionsArticle Views295Altmetric-Citations11LEARN 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 SUBJECTS:Aromatic compounds,Inorganic carbon compounds,Nitrogen compounds,Pharmaceuticals,Reaction products Get e-Alerts
Prevalence of increased body weight and hypertension in the population of Croatian mainland and Adriatic Islands--are islanders really healthier? (2009)

The aim of this study was to compare the prevalence of the hypertension and the increased body weight (BMI) between Croatian mainland and Adriatic island population. The data from the Croatian Adult Health Survey (N = 9,070) served as an estimate for the mainland Croatian population, while the data from "1001 Dalmatian study" (N = 1,001) were collected from four Adriatic islands; Rab, Vis, Lastovo and Mljet. The prevalence of increased body weight and hypertension was calculated for the four age groups and analyzed using chi-square test. The results indicate that men from the islands less frequently had normal body mass index (P < 0.001), and were more frequently overweight (P < 0.001). The prevalence of overweight and obesity were similar between the island and mainland women. The percent of normotensive respondents in men was significantly lower in islands (P < 0.001), while the prevalence of newly diagnosed hypertension was significantly higher among islanders in both genders (P < 0.001). Despite the traditionally prevalent Mediterranean diet and overall more favorable lifestyle islanders may not be as healthy as previously studies suggested, in terms of cardiovascular risk factors prevalence. This might be related to the poor access to health care and preventive measures or low interest for health care especially among men on the islands, reflected in the higher prevalence of newly diagnosed hypertension. These findings suggest that island populations represent good candidates for disease awareness programs and health promotion interventions.
Analytical thermal model for HEMTs with complex epitaxial structures (2014)

Although wide bandgap solid state devices are one of the most promising technologies for high power, high frequency applications, high device temperatures often lead to degraded performance and reliability. Thus, accurately predicting and maintaining device temperature at an acceptable level is a key to realizing the full potential of wide bandgap electronics. In this work, we present a closed-form analytical solution to the steady-state heat equation applicable to compound semiconductor high electronic mobility transistors (HEMTs), such as those based on gallium nitride (GaN). While numerical techniques are widely used to predict device temperature, our analytical solution is more computationally-efficient and can account for complex multi-layer structures, internal heat sources, and a variety of thermal interface conditions. Through a Fourier series-based solution and recursive relations for the Fourier coefficients in adjacent layers, we report manageable expressions for the Fourier coefficients. We also demonstrate that these solutions are two orders of magnitude more efficient than state of the art semi-analytical techniques for complex 3D structures. In addition, we have validated the model with high spatial resolution micro-Raman thermography measurements on GaN device structures.
Hematopoietic stem cell and progenitor defects in Sca-1/Ly-6A–null mice (2002)

Despite its wide use as a marker for hematopoietic stem cells (HSCs), the function of stem cell antigen-1 (Sca-1) (also known as lymphocyte activation protein-6A [Ly-6A]) in hematopoiesis remains poorly defined. We have previously established that Sca-1(-/-) T cells develop normally, although they are hyperresponsive to antigen. Here, we report detailed analysis of hematopoiesis in Sca-1-deficient animals. The differentiation potential of Sca-1-null bone marrow was determined from examination of the most mature precursors (culture colony-forming units [CFU-Cs]) to less committed progenitors (spleen CFUs [CFU-Ss]) to long-term repopulating HSCs. Sca-1-null mice are mildly thrombocytopenic with a concomitant decrease in megakaryocytes and their precursors. Bone marrow cells derived from Sca-1(-/-) mice also have decreased multipotential granulocyte, erythroid, macrophage, and megakaryocyte CFU (GEMM-CFU) and CFU-S progenitor activity. Competitive repopulation assays demonstrated that Sca-1(-/-) HSCs are at a competitive disadvantage compared with wild-type HSCs. To further analyze the potential of Sca-1(-/-) HSCs, serial transplantations were performed. While secondary repopulations using wild-type bone marrow completely repopulated Sca-1(-/-) mice, Sca-1(-/-) bone marrow failed to rescue one third of lethally irradiated wild-type mice receiving secondary bone marrow transplants from irradiation-induced anemia and contributed poorly to the surviving transplant recipients. These data strongly suggest that Sca-1 is required for regulating HSC self-renewal and the development of committed progenitor cells, megakaryocytes, and platelets. Thus, our studies conclusively demonstrate that Sca-1, in addition to being a marker of HSCs, regulates the developmental program of HSCs and specific progenitor populations.
Digital Calibration Methodology Applied to a Sensor Microsystem (2006)

This paper presents the application of a complete digital calibration methodology to the improvement of a Hall sensor-based current measurement microsystem. It is a step-by-step illustration of how generic calibration techniques and circuits can be used on a practical example. At system-level, the microsystem is analyzed and its imperfections identified. The circuit is designed so that for each imperfection to be cancelled, detection and compensation nodes are identified. To these nodes, generic digital calibration circuits are connected to perform continuous background calibration. In the presented current measurement microsystem, the use of this methodology reduced the sensitivity drift down to 50 ppm/degC, which is 10 times less than the state of the art
Progress in BazookaSPECT: high-resolution dynamic scintigraphy with large-area imagers (2012)

We present recent progress in BazookaSPECT, a high-resolution, photon-counting gamma-ray detector. It is a new class of scintillation detector that combines columnar scintillators, image intensifiers, and CCD (charge-coupled device) or CMOS (complementary metal-oxide semiconductors) sensors for high-resolution imaging. A key feature of the BazookaSPECT paradigm is the capability to easily design custom detectors in terms of the desired intrinsic detector resolution and event detection rate. This capability is possible because scintillation light is optically amplified by the image intensifier prior to being imaging onto the CCD/CMOS sensor, thereby allowing practically any consumer-grade CCD/CMOS sensor to be used for gamma-ray imaging. Recent efforts have been made to increase the detector area by incorporating fiber-optic tapers between the scintillator and image intensifier, resulting in a 16× increase in detector area. These large-area BazookaSPECT detectors can be used for full-body imaging and we present preliminary results of their use as dynamic scintigraphy imagers for mice and rats. Also, we discuss ongoing and future developments in BazookaSPECT and the improved event-detection rate capability that is achieved using Graphics Processing Units (GPUs), multi-core processors, and new high-speed, USB 3.0 CMOS cameras.
Sucrose absorption by the rat small intestine in vivo and in vitro (1977)

1. The absorption of glucose and fructose derived from sucrose has been studied using in vitro and in vivo loops of the rat jejunum. 2. At low sucrose concentrations (1 and 10 m M ) glucose appeared in the serosal compartment of the in vitro preparation at a faster rate than fructose, but at high sucrose concentrations (50 and 100 m M ) the rates of serosal transfer of the two sugars were similar. Glucose and fructose appeared in the mucosal compartment, with the rate of fructose appearance exceeding that of glucose, at all the sucrose concentrations studied. 3. Phlorizin (5 × 10 −5 M ) added to the mucosal medium of the in vitro preparation abolished the serosal transfer of glucose derived from 50 m M sucrose, and reduced that of fructose by 75%. 4. In the absence of sodium ions, the in vitro preparation failed to transfer glucose and fructose derived from 50 m M sucrose, into the serosal compartment. 5. Glucose was actively accumulated in the whole gut wall of the in vivo preparation to concentrations higher than those in the plasma at 50 and 100 m M , but not at 10 m M sucrose concentrations. Fructose was also actively accumulated to about half the extent of glucose, but reached tissue concentrations greater than those in the plasma, at each sucrose concentration. 6. The whole wall concentrations of glucose and fructose derived from sucrose added to the lumen continued to rise when the blood supply to the in vivo preparation was terminated. 7. No increase in the in vivo whole wall concentrations of glucose and fructose were detected when sucrose was added to the lumen together with concentrations of glucose sufficient to saturate the monosaccharide transport systems. 8. The results favour the view that disaccharide hydrolysis and resulting hexose transfer are sequential, separate events.