gebhart/patrepeval huggingface dataset:
Abstract 727: Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a diaryl template (2010)

Abstract Designing single agents that act against multiple biological targets are of increasing interest and prominence. In recent years, an increasing volume of work has been published exemplifying the successful use of this strategy. Estrogen deprivation has been an effective therapeutic intervention for hormone-dependent breast cancer (HDBC). One established and clinically proven approach involves the inhibition of the aromatase enzyme, although the inhibition of steroid sulfatase (STS) is an emerging new strategy as demonstrated by the promising results of STX64 (BN83495),1 the first STS inhibitor that entered clinical trials. While both aromatase and STS are targets for treating HDBC, it is reasoned that estrogen deprivation may be more comprehensively achieved by dual inhibition of both enzymes. To this end, the reversible aromatase inhibitory pharmacophore, which is principally a heme-ligating nitrogen-containing heterocycle, was thus introduced into a known sulfamate-based STS inhibitor to give a series of dual aromatase-sulfatase inhibitors (DASIs). Several compounds were found to be good aromatase or STS inhibitors individually. However, two compounds show exceptional dual in vitro potency in JEG-3 cells, inhibiting aromatase with IC50 values of 0.5 and 2.0 nM, and STS with IC50 values of 5.5 and 35 nM. Both compounds share the common structural feature of having a sulfamate group on one aryl ring, and a heterocycle and a H-bond acceptor on the other. At 1 mg/kg p.o., both DASIs reduced plasma estradiol levels strongly and inhibited liver STS activity potently in vivo. One of the compounds was found to be non-estrogenic and potently inhibit human carbonic anhydrase II (hCAII IC50 = 86 nM). A complex of hCAII with the inhibitor was crystallized and solved by X-ray crystallography. This class of DASI should encourage further development towards multi-targeted therapeutic intervention in HDBC. Ref 1: a) Stanway, S. J. et al. Clin. Cancer Res. 2006, 12, 1585-1592. b) Stanway, S. J. et al. Oncologist 2007, 12, 370-374. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 2010 Apr 17-21; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2010;70(8 Suppl):Abstract nr 727.
Contribution of infill materials to the fire behavior of artificial grass (2019)

Artificial grass is mainly composed of organic polymers with a consequent potential fire hazard. However, the behavior of artificial grass in case of fire has been poorly studied and is thus misunderstood. The purpose of this study is thus to have a better understanding of the contribution of the different components of the artificial turf in the fire performances. In this work, the influence of the nature of the infill is more specifically investigated.
Childhood Atopic Asthma: Positive Association with a Polymorphism of IL-4 Receptor α Gene but Not with That of IL-4 Promoter or Fc ε Receptor I β Gene (2000)

We examined the relative contributions of three representative candidate genes for atopy (Fc ε receptor I β, IL-4, and IL-4 receptor α) to the development of atopic asthma. Four polymorphisms of the three candidate genes including Ile50Val and Gln551Arg of IL-4 receptor α, -590C/T of IL-4 promoter and Glu237Gly of Fc ε receptor I β were studied in 100 patients with atopic asthma and 100 nonatopic controls in the northern Kyushu area in Japan. Among the four polymorphisms of the three candidate genes, the Ile50 allele of the IL-4 receptor α chain gene demonstrated an association with atopic asthma subjects (p = 0.044), especially in patients with onset at 2 years of age or earlier (p = 0.034) and in patients with moderate to severe atopic asthma (p = 0.031). Gln551Arg of IL-4 receptor α, -590C/T of IL-4 promoter and Glu237Gly of Fc ε receptor I β showed no association with atopic asthma. A slight linkage disequilibrium between Ile50Val and Gln551Arg polymorphisms of the IL-4 receptor α chain gene was observed in both patients and nonatopic controls. The identification of additional atopy genes in areas with a certain genetic background is essential for genetic diagnosis and to establish new therapeutic modalities for atopic asthma.
A unique allosteric insulin receptor monoclonal antibody that prevents hypoglycemia in the SUR-1−/− mouse model of KATP hyperinsulinism (2018)

Loss-of-function mutations of the ß-cell ATP-sensitive potassium channels (K<sub>ATP</sub>) cause the most common and severe form of congenital hyperinsulinism (K<sub>ATP</sub>HI), a disorder of ß-cell function characterized by severe hypoglycemia. Children with K<sub>ATP</sub>HI are typically unresponsive to medical therapy and require pancreatectomy for intractable hypoglycemia. We tested the hypothesis that inhibition of insulin receptor signaling may prevent hypoglycemia in K<sub>ATP</sub>HI. To test this hypothesis, we examined the effect of an antibody allosteric inhibitor of the insulin receptor, XMetD, on fasting plasma glucose in a mouse model of K<sub>ATP</sub>HI (SUR-1<sup>-</sup><sup>/</sup><sup>-</sup> mice). SUR-1<sup>-</sup><sup>/</sup><sup>-</sup> and wild-type mice received twice weekly intraperitoneal injections of either XMetD or control antibody for 8 wks. Treatment with XMetD significantly decreased insulin sensitivity, and increased hepatic glucose output and fasting plasma glucose. These findings support the potential use of insulin receptor antagonists as a therapeutic approach to control the hypoglycemia in congenital hyperinsulinism.
Metal–Organic Frameworks as Catalysts for Organic Reactions (2011)

This chapter contains sections titled: Introduction MOFs with Catalytically Active Metal Nodes in the Framework Catalytic Functionalization of Organic Framework Linkers Homochiral MOFs MOF-Encapsulated Catalytically Active Guests Mesoporous MOFs Conclusions References
Altered States of Telomere Deprotection and the Two-Stage Mechanism of Replicative Aging (2009)

The molecular distinctions between mortality stages 1 (M1; senescence) and 2 (M2; crisis) of human replicative aging are ill defined. We demonstrate a qualitative difference between telomeric end associations at M1 and the end fusions that produce dicentric chromosomes and breakage-fusion cycles. Knockdown of ligase IV sufficient to completely inhibit radiation-induced dicentric chromosome formation had no effect on the frequency of telomere associations (TAs), establishing that TAs are not covalent conventional nonhomologous end-joining (NHEJ) products. TAs preceded and were more numerous than dicentric chromosomes. Cells initially tolerated dicentric chromosomes without dying, but eventually, a combination of too many TAs and dicentrics/complex chromosomal rearrangements resulted in apoptosis. We propose a working model in which end associations represent abortive DNA repair intermediates when the number of telomeric repeats is too small to completely inhibit DNA damage signaling but is sufficient to prevent the final covalent ligation step of NHEJ and induces the M1 checkpoint arrest in normal human cells. Rather than being all-or-none, telomere deprotection would thus proceed first through TAs before additional shortening leads to dicentric chromosomes. M2/crisis involves both qualitative changes (a shift from TAs to TAs plus dicentric chromosomes) and quantitative changes (an increase in the number of dysfunctional telomeres).
Mechanisms of Action of Therapeutics in Idiopathic Thrombocytopenic Purpura (2003)

Idiopathic thrombocytopenic purpura (ITP) is a common immune disorder caused by platelet-reactive autoantibodies. Antibody-coated platelets are cleared more rapidly from the circulation, often in the spleen, than they can be replaced by compensatory stimulation of platelet production in the bone marrow. In some patients, platelet production is depressed as well. ITP in adults does not generally remit spontaneously, and most patients require treatment to prevent bleeding at one time or another. Therapy with corticosteroids, danazol, intravenous immune globulin, anti-D antibody, and several other agents inhibits clearance of the antibody-coated platelets but is rarely curative. Most patients will sustain a hemostatic response after splenectomy, although relapses may occur at any time. Patients may be more responsive to these same modalities after splenectomy, but treatment with an immunosuppressant that inhibits T- and B-cell function and cooperation, including azathioprine, cyclophosphamide, cyclosporine, mycophenolate mofetil, or anti-CD20, may be required. Antiviral therapy is useful in patients with HIV or hepatitis C infection, but no consensus has been reached as to the efficacy of antibiotics to eradicate Helicobacter pylori. Promising results have been seen in several patients treated with a modified thrombopoietin. It may be possible to design therapeutics that exploit the apparent restricted immunoglobulin gene usage by antiplatelet antibodies, perhaps in the form of engineered anti-idiotypic antibodies or other compounds that specifically target autoantibody-producing B cells. Rationale therapy awaits a more thorough understanding of autoantibody production.
Black Level Visibility as a Function of Ambient Illumination (2018)

One of the key new attributes of HDR imaging and displays is the ability to present many stops of shadow detail, and with the best systems, a perceptually pure black. Displays perform at their best in a dark room as no ambient illumination impinges on the surface of the display, which would elevate the display's perceived black level. In addition, the viewer sees the most shadow detail when the region surrounding the display is also dark. In addition to applications where a display is viewed in a dark surround environment, there are also many viewing conditions where higher ambient light levels occur. Knowledgeable viewers prevent ambient illumination from reflecting from the display, but even for those viewers, surrounding luminance will be increased. To understand the impact of this surrounding ambient illumination on black level visibility and shadow detail, and to further guide ambient compensation algorithms, we performed a psychophysical study to assess the human visual system's ability to perceive detail when impacted by surround luminance. For the stimuli, we used a Gabor signal to probe the visual system's best capability. For the display, we used a Pulsar display with a large 1.0 neutral density filter placed over the display to enable black levels as low 0.0005 cd/m^2, relevant for OLED and cinema applications. The surround luminance levels ranged from fully dark up to 100 cd/m^ 2, and for each of these, shadow detail thresholds were measured as a function of display mean luminance levels from .001 to 400 cd/m^2. The results are useful for perceptual display performance assessment and tone-mapping applications, and PLUGE design. Further analysis found they are consistent with an existing surround effect visual model, which has basis in the cone photoreceptors.
TIPS-08 ACTION: A RANDOMIZED PHASE 3 STUDY OF DORDAVIPRONE (ONC201) IN PATIENTS WITH NEWLY DIAGNOSED H3 K27M-MUTANT DIFFUSE GLIOMA (2023)

Abstract BACKGROUND H3 K27M-mutant diffuse midline glioma is a universally fatal malignancy primarily affecting children and young adults. While radiotherapy (RT) provides transient benefit, no effective systemic therapy is currently available and current standard of care is RT followed by monitoring. Dordaviprone (ONC201), a first-in-class imipridone, is an oral, blood-brain barrier penetrating, selective small molecule antagonist of dopamine receptor D2/3 (DRD2) and agonist of the mitochondrial protease ClpP. An integrated pooled analysis of five open-label trials previously demonstrated efficacy in dordaviprone-treated patients with recurrent disease. This phase 3 trial will be the first randomized, controlled study evaluating ONC201 in patients with H3 K27M-mutant disease. METHODS ACTION (NCT05580562) is a randomized, double-blind, placebo-controlled, parallel-group, international Phase 3 study of ONC201 in patients with newly diagnosed H3 K27M-mutant diffuse glioma. Patients who have completed standard frontline radiotherapy will be randomized 1:1:1 to receive placebo, once-weekly dordaviprone, or twice-weekly dordaviprone on two consecutive days. Primary efficacy endpoints are overall survival (OS) and progression-free survival (PFS) in all participants; PFS will be assessed by response assessment in neuro-oncology-high grade glioma by blind independent central review. Other objectives include assessments of safety, additional efficacy endpoints, clinical benefit, quality of life, pharmacokinetics, biomarkers, and healthcare resource utilization. Eligible patients will have histologically confirmed H3 K27M-mutant diffuse glioma, a Karnofsky/Lansky performance status ≥70, and completed first-line radiotherapy. Eligibility will not be restricted based on age; however, patients must be ≥10 kg at time of randomization. Patients with a primary spinal tumor, diffuse intrinsic pontine glioma, leptomeningeal disease, or cerebrospinal fluid dissemination are not eligible. ACTION is currently enrolling in the United States, with international sites opening imminently.
Copper-Mediated Amidation of Heterocyclic and Aromatic C−H Bonds (2009)

A copper-mediated aerobic coupling reaction enables direct amidation of heterocycles or aromatics having weakly acidic C-H bonds with a variety of nitrogen nucleophiles. These reactions provide efficient access to many biologically important skeletons, including ones with the potential to serve as inhibitors of HMTs.
Diethyl(di-tert-butylphosphino)borane and related compounds: the first stable monomeric tetraalkyl phosphinoborane (1993)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDiethyl(di-tert-butylphosphino)borane and related compounds: the first stable monomeric tetraalkyl phosphinoboraneThomas J. Groshens, Kelvin T. Higa, Robin Nissan, Raymond J. Butcher, and Alan J. FreyerCite this: Organometallics 1993, 12, 8, 2904–2910Publication Date (Print):August 1, 1993Publication History Published online1 May 2002Published inissue 1 August 1993https://doi.org/10.1021/om00032a011RIGHTS & PERMISSIONSArticle Views156Altmetric-Citations14LEARN 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 InReddit PDF (794 KB) Get e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
Supplementary Legend S1 from Identification of Novel Target Genes by an Epigenetic Reactivation Screen of Renal Cancer (2023)

Supplementary Legend S1 from Identification of Novel Target Genes by an Epigenetic Reactivation Screen of Renal Cancer
Optimizing systems for effective block-processing (1996)

Article Free Access Share on Optimizing systems for effective block-processing: the k-delay problem Authors: Kumar N. Lalgudi Department of Electrical Engineering, Yale University, New Haven, CT Department of Electrical Engineering, Yale University, New Haven, CTView Profile , Marios C. Papaefthymiou Department of Electrical Engineering, Yale University, New Haven, CT Department of Electrical Engineering, Yale University, New Haven, CTView Profile , Miodrag Potkonjak Department of Computer Science, University of California, Los Angeles, CA Department of Computer Science, University of California, Los Angeles, CAView Profile Authors Info & Claims DAC '96: Proceedings of the 33rd annual Design Automation ConferenceJune 1996 Pages 714–719https://doi.org/10.1145/240518.240653Online:01 June 1996Publication History 4citation242DownloadsMetricsTotal Citations4Total Downloads242Last 12 Months1Last 6 weeks0 Get Citation AlertsNew Citation Alert added!This alert has been successfully added and will be sent to:You will be notified whenever a record that you have chosen has been cited.To manage your alert preferences, click on the button below.Manage my AlertsNew Citation Alert!Please log in to your account Save to BinderSave to BinderCreate a New BinderNameCancelCreateExport CitationPublisher SiteeReaderPDF
Reactive Polymers: A Versatile Toolbox for the Immobilization of Functional Molecules on TiO2 Nanoparticles (2006)

Drei in einem: TiO2-Nanopartikel wurden mit reaktiven polymeren Liganden funktionalisiert, die drei Arten von Gruppen enthalten: chelatisierende Dopamin-Ankergruppen, eine Bindungsstelle für funktionale Moleküle wie Fluoreszenzfarbstoffe (siehe Bild) sowie Gruppen, die es ermöglichen, die Löslichkeit der anorganischen Nanokristalle in unterschiedlichen Lösungsmitteln einzustellen. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2001/2006/z502517_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
ChemInform Abstract: Synthesis of 2,7‐Disubstituted‐5,6‐dimethylpyrrolo(2,3‐d)‐1,3‐oxazin‐4‐ ones as Antifungal Agents. (1995)

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.
Characterization and analysis of the training effect of exchange bias in coupled NiFe∕IrMn bilayers (2007)

The training effect of the so-called exchange bias in coupled polycrystalline NiFe∕IrMn thin films has been experimentally and theoretically investigated. A different formula is used to describe the exchange bias dependence on the measurement cycle number. It can be understood to be a consequence of the antiferromagnetic domain dynamics based on the Kolmogorov-Avrami [Izv. Akad. Nauk, Ser. Math. 3, 355 (1937); J. Chem. Phys. 8, 212 (1940)] model, which describes the nucleation and growth of antiferromagnetic domains in the film structures.
Maximum entropy co-processor for computed tomography (2002)

In this paper, we present a neural net co-processor capable of performing computed tomographic image reconstruction. The circuit performs the Radon transformation using a cost function gradient descent method. The unique aspect of this co-processor is the incorporation of informational entropy as a regularizer in the optimization problem. A 10 pixel/spl times/10 pixel array was designed and fabricated in 2 /spl mu/m CMOS technology. Convergence time of the array was less than 5 /spl mu/s. Issues relating to scaling the array to larger sizes are discussed in this paper.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Control system design using H [infinity] optimization (1988)

Thesis (M.S.)--Massachusetts Institute of Technology, Dept. of Aeronautics and Astronautics, 1988.
Evaluation of different operational strategies for lithium ion battery systems connected to a wind turbine for primary frequency regulation and wind power forecast accuracy improvement (2012)

High penetration levels of variable wind energy sources can cause problems with their grid integration. Energy storage systems connected to wind turbine/wind power plants can improve predictability of the wind power production and provide ancillary services to the grid. This paper investigates economics of different operational strategies for Li-ion systems connected to wind turbines for wind power forecast accuracy improvement and primary frequency regulation.
Characterisation of Lean Burn Module Air Blast Pilot Injector With Laser Techniques (2013)

For lean burn combustor development in low emission aero-engines, the pilot stage of the fuel injector plays a key role with respect to stability, operability, NOx emissions, and smoke production. Therefore it is of considerable interest to characterize the pilot module in terms of pilot zone mixing, fuel placement, flow field and interaction with the main stage. This contribution focusses on the investigation of soot formation during pilot-only operation. Optical test methods were applied in an optically accessible single sector rig at engine idle conditions. Using planar laser-induced incandescence (LII), the distribution of soot and its dependence on air/fuel ratio, as well as geometric injector parameters, was studied. The data shows that below a certain air/fuel ratio, an increase of soot production occurs. This is in agreement with smoke number measurements in a standard single sector flame tube rig without optical access. Reaction zones were identified using chemiluminescence of OH radicals. In addition, the injector flow field was investigated with PIV. A hypothesis regarding the mechanism of pilot smoke formation was made based on these findings. This along with further investigations will form the basis for developing strategies for smoke improvement at elevated pilot only conditions.
High-Performance Spectroscopy using Virtual Slit Optics (2013)

The High Throughput Virtual Slit (HTVS™) is a novel spectroscopic technology which simultaneously maximizes spectral resolution and throughput. We describe the advantages of HTVS spectrometers for Raman measurements and hyperspectral imaging.
Steroid Profiles in Ovarian Follicular Fluid from Regularly Menstruating Women and Women after Ovarian Stimulation (2009)

The data provide the first MS-based concentration values for 13 steroids in ovarian FF from RM women, from estrogen- and androgen-dominant follicles, and from women after ovarian stimulation for IVF.
Exploiting Wireless Channel State Information Structures Beyond Linear Correlations: A Deep Learning Approach (2019)

Knowledge of information about the propagation channel in which a wireless system operates enables better, more efficient approaches for signal transmissions. Therefore, channel state information (CSI) plays a pivotal role in the system performance. The importance of CSI is in fact growing in the upcoming 5G and beyond systems, for example, for the implementation of massive multiple-input multiple-output (MIMO). However, the acquisition of timely and accurate CSI has long been considered a major issue, and becomes increasingly challenging due to the need for obtaining CSI of many antenna elements in massive MIMO systems. To cope with this challenge, existing works mainly focus on exploiting linear structures of CSI, such as CSI correlations in the spatial domain, to achieve dimensionality reduction. In this article, we first systematically review the state of the art on CSI structure exploitation. We then extend to seek deeper structures that enable remote CSI inference wherein a data-driven deep neural network (DNN) approach is necessary due to model inadequacy. We develop specific DNN designs suitable for CSI data. Case studies are provided to demonstrate great potential in this direction for future performance enhancement.