gebhart/patrepeval huggingface dataset:
Asymmetric Synthesis of a New Helix‐Forming β‐Amino Acid: trans‐4‐Aminopiperidine‐3‐carboxylic Acid (2003)

Abstract We report a synthesis of a protected derivative of trans ‐4‐aminopiperidine‐3‐carboxylic acid (APiC). The route provides either enantiomer. All intermediates are purified by crystallization, and large‐scale preparation is therefore possible. An analogous route provides either enantiomer of trans ‐2‐aminocyclohexanecarboxylic acid (ACHC). We have previously shown that β‐peptide oligomers containing ACHC adopt a helical conformation defined by 14‐membered C=O( i ) ··· H−N( i − 2) hydrogen bonds (“14‐helix”). Here we show that APiC residues can be incorporated into the 14‐helix. (© Wiley‐VCH Verlag GmbH &amp; Co. KGaA, 69451 Weinheim, Germany, 2003)
Post-Irradiation Treatment with a Superoxide Dismutase Mimic, MnTnHex-2-PyP5+, Mitigates Radiation Injury in the Lungs of Non-Human Primates after Whole-Thorax Exposure to Ionizing Radiation (2018)

Radiation injury to the lung is the result of acute and chronic free radical formation, and there are currently few effective means of mitigating such injury. Studies in rodents indicate that superoxide dismutase mimetics may be effective in this regard; however, studies in humans or large animals are lacking. We hypothesized that post-exposure treatment with the lipophilic mitochondrial superoxide dismutase mimetic, MnTnHex-2-PyP<sup>5+</sup> (hexyl), would reduce radiation-induced pneumonitis and fibrosis in the lungs of nonhuman primates. Rhesus monkeys (<i>Macaca mulatta</i>) received 10 Gy whole thorax irradiation, 10 Gy + hexyl treatment, sham irradiation, or sham irradiation + hexyl. Hexyl was given twice daily, subcutaneously, at 0.05 mg/kg, for 2 months. Animals were monitored daily, and respiratory rates, pulse oximetry, hematology and serum chemistry panels were performed weekly. Computed tomography scans were performed at 0, 2, and 4 months after irradiation. Supportive fluid therapy, corticosteroids, analgesics, and antibiotics were given as needed. All animals were humanely euthanized 4.5 months after irradiation, and pathologic assessments were made. Multifocal, progressive lung lesions were seen at 2 and 4 months in both irradiated groups. Hexyl treatment delayed the onset of radiation-induced lung lesions, reduced elevations of respiratory rate, and reduced pathologic increases in lung weight. No adverse effects of hexyl treatment were found. These results demonstrate (1) development of a nonhuman primate model of radiation-induced lung injury, (2) a significant mitigating effect of hexyl treatment on lung pathology in this model, and (3) no evidence for toxicity of hexyl at the dose studied.
An Improved Methodology for the Synthesis of Enantiomerically Pure ( S )-2,3- O -Cyclohexylideneglyceraldehyde (2002)

An improved methodology to prepare (S)2,3-O-cyclohexylideneglyceraldehyde is described. Starting from the commercially available (L)-cyclohexylidene protected ascorbic acid the enantiomerically pure aldehyde was synthesized in only two steps in 41% overall yield.
Dandelion (2013)

Computer systems increasingly rely on heterogeneity to achieve greater performance, scalability and energy efficiency. Because heterogeneous systems typically comprise multiple execution contexts with different programming abstractions and runtimes, programming them remains extremely challenging.
Abstract 3905: Synthesis and structure activity relationship of substituted N,6-diphenyl-5,6-dihydrobenzo[h]quinazolin-2-amine as inhibitors of fibroblast growth factor receptors (FGFR) (2012)

Abstract Utilization of hydrophobic motifs present in auto-inhibited protein kinases has resulted in the identification of a series of 5,6-dihydrobenzo [h]quinazolin-2-amines with activity as fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors. Herein we describe the combination of a proprietary in silico design process, a new screening paradigm using an array of biochemical and biophysical technologies in conjunction with an established parallel chemistry process for the identification and optimization of a series of novel FGFR inhibitors. These potent FGFR inhibitors exhibit a preference for the inactive form of the kinase, are non-ATP competitive, and exhibit robust cellular pharmacodynamic inhibition as well as in vitro anti-proliferative effects in cells dependent on FGFR and significant anti-tumor activity in appropriate xenograft models in vivo. The design strategy, synthesis, structure activity relationships and in vitro and in vivo biology of selected inhibitors will be presented. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 3905. doi:1538-7445.AM2012-3905
Novel approach for evaluating detector-related uncertainties in a LArTPC using MicroBooNE data (2022)

Abstract Primary challenges for current and future precision neutrino experiments using liquid argon time projection chambers (LArTPCs) include understanding detector effects and quantifying the associated systematic uncertainties. This paper presents a novel technique for assessing and propagating LArTPC detector-related systematic uncertainties. The technique makes modifications to simulation waveforms based on a parameterization of observed differences in ionization signals from the TPC between data and simulation, while remaining insensitive to the details of the detector model. The modifications are then used to quantify the systematic differences in low- and high-level reconstructed quantities. This approach could be applied to future LArTPC detectors, such as those used in SBN and DUNE.
Characterization of DNA synthesis during the 2-cell stage and the production of tetraploid chimeric pig embryos (1996)

The DNA content of nuclei during the 2-cell stage as well as in presumptive tetraploid embryos was investigated. In vivo produced pig zygotes were cultured to the 2-cell stage and either monitored for cleavage to the 4-cell stage or mounted at various times post-cleavage and DNA content determined. The length of the 2-cell stage was 14.8 +/- 3.0 hr. There was a significant increase in the length of the 2-cell stage due to the time in vitro as a zygote (P < 0.001: R2 = 0.866). The DNA content increased (P < 0.05) each 2 hr postcleavage until 10 hr postcleavage. This suggested that there is a short G1 and G2 phase and a relatively long phase of DNA synthesis. Next, 2-cell stage embryos were pulsed with electricity to induce cell-to-cell fusion. Whereas only about half fused within 30 min (55%), most (96%) developed to the blastocyst stage. The DNA content of the nuclei of the embryos was consistent with them being tetraploid. A final experiment was designed to evaluate the ability of the tetraploid embryo to form a chimera with isolated inner cell mass (ICM) cells. Inner cell masses were isolated from d 6 embryos, cut into thirds, labeled with DiO (a membrane die) and injected into the perivitelline space of 4-cell-stage tetraploid embryos. Twelve of 17 formed blastocysts. In most (8/12), the ICM of the resulting blastocyst was labeled, whereas in one the only fluorescence was in the trophectoderm, and in two fluorescence was evenly distributed between the ICM and trophectoderm. These results suggest that it may be possible to create a fetus derived from ICM cells, or potentially stem cells, that has a tetraploid trophoblast.
Distinct Signal Codes Generate Dendritic Cell Functional Plasticity (2010)

Our adaptive immune system induces distinct responses to different pathogens because of the functional plasticity of dendritic cells (DCs); however, how DCs program unique responses remains unclear. Here, we found that the cytokine thymic stromal lymphopoietin (TSLP) potently transduced a unique T helper type 2 (T(H)2)-inducing compound signal in DCs. Whereas activation of nuclear factor kappaB (predominantly p50) drove DCs to produce OX40L to induce T(H)2 differentiation, the activation of signal transducer and activator of transcription 6 (STAT6) triggered DCs to secrete chemokines necessary for the recruitment of T(H)2 cells. In addition, TSLP signaling limited the activation of STAT4 and interferon regulatory factor 8 (IRF-8), which are essential factors for the production of the T(H)1-polarizing cytokine interleukin-12 (IL-12). By contrast, Toll-like receptor ligands and CD40 ligand did not activate STAT6 in myeloid DCs, but instead increased the abundance of STAT4 and IRF-8 to induce T(H)1 responses through the production of IL-12. Therefore, we propose that the functional plasticity of DCs relies on elaborate signal codes that are generated by different stimuli.
ChemInform Abstract: α‐Sulfinyl‐Substituted Radicals. Part 1. Stereoselective Radical Addition Reactions of Cyclic α‐Sulfinyl Radicals. (1991)

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.
Is global humeral head offset related to intramedullary canal width? A computer tomography morphometric study (2018)

The present study revealed that humeral offset is not correlated with intramedullary canal width. Implant manufacturers and shoulder surgeons should be aware of the subtle morphologic features, to enhance humeral stem design and restore native anatomy.
Is Histone a Solitary Vile Sepsis-Inducing Agent or Just "a Member of the Gang"? (2017)

In this communication we argue that it is improbable that the main cause of death in sepsis is that, upon release of extracellular traps from neutrophils adhering to endothelial cells, highly cationic toxic histones uniquely cause endothelial dysregulation, organ failure and death. Activation of neutrophils is always accompanied by a plethora of pro-inflammatory agents, which may act in synergy with histones to injure cells. Furthermore, many recent articles have shown a steep rise of circulating histones in many clinical disorders unrelated to sepsis. We argue therefore that histones do not act as unique alarmins with an outsized role, but are probably another marker of cell damage.
Better performance for shunt active power filters (2011)

This paper proposes a time domain harmonic detection technique which is an improved a-b-c reference frame formula based upon the p-q theory with a positive sequence detector to solve the problem of bad performance of shunt active power filters (SAPF) under non-ideal mains. The improved formula needs fewer calculations than the conventional p-q theory. Moreover, it is very easy to implement this algorithm in a digital signal processor (DSP). Also the proposed method is compared to three detection algorithms which are the instantaneous reactive power theory (IRPT), synchronous reference frame (SRF), and synchronous detection method (SDM). The simulation results show better performance of the shunt active power filter with the proposed algorithm.
A Robust Temporal Alignment Technique for Infrared and Visible-Light Video Sequences (2013)

Traditional temporal video alignment techniques depend on the existence of a sufficient number of mutual scene characteristics to perform temporal synchronization. However, for video sequences originating from different spectral modalities such information may fail to exist, subsequently leading to unreliable alignment results. In this work, a novel, practical approach for the temporal alignment of infrared (IR) and visiblelight video sequences is introduced. Utilizing a planar alignment device consisting of an array of miniature light bulbs, we propose to increase the number of mutual feature points within the frames of a temporally misaligned IR/visible-light video sequence pair. Thereby, we provide an abundant number of mutual scene characteristics which can subsequently be used to determine the time-shift between the two sequences. Tests with five different IR/visible-light sequence pairs suggest that our technique is able to estimate the temporal offset with a very high confidence level. Furthermore, due to the simplicity of the construction of the alignment board, the proposed framework can be seamlessly integrated within a stereo camera calibration scheme.
Biomimetic cellulose-based superabsorbent hydrogels for treating obesity (2021)

In the treatment of obesity, nutritional and behavioral modifications are difficult to implement and maintain. Since vegetable consumption is a fundamental part of many dietary interventions and daily nutrient requirements, we developed a novel cellulose-based superabsorbent hydrogel (CB-SAH) platform, inspired by the composition and mechanical properties of raw vegetables, as a mechanobiological therapy. The CB-SAHs properties were studied in a simulated gastrointestinal environment, while their impact on gut tissue was investigated by an ex vivo organ culture (EVOC) model. Functional fibers and raw vegetables were used as reference. CB-SAHs demonstrated orders of magnitude higher elasticity in comparison to the tested functional fibers, however performed similar to the tested raw vegetables. Notably, the biomimetic CB-SAHs with elasticity levels similar to raw vegetables showed benefits in preserving and regulating the gut tissue in the EVOC model. Non-systemic oral mechanotherapeutics based on this technology were advanced through clinical studies, with a first product cleared as an aid for weight management in the US and Europe.
Detecting Irregular Curvilinear Structures in Gray Scale and Color Imagery Using Multi-directional Oriented Flux (2013)

We propose a new approach to detecting irregular curvilinear structures in noisy image stacks. In contrast to earlier approaches that rely on circular models of the cross-sections, ours allows for the arbitrarily-shaped ones that are prevalent in biological imagery. This is achieved by maximizing the image gradient flux along multiple directions and radii, instead of only two with a unique radius as is usually done. This yields a more complex optimization problem for which we propose a computationally efficient solution. We demonstrate the effectiveness of our approach on a wide range of challenging gray scale and color datasets and show that it outperforms existing techniques, especially on very irregular structures.
Pneumatic Displacement of Subretinal Hemorrhage Without Tissue Plasminogen Activator (1999)

Objective To assess the efficacy and complications of intravitreal injection of perfluoropropane gas for displacement of subretinal hemorrhage (SRH), without the use of tissue plasminogen activator. Patients and Methods Pure perfluoropropane gas (0.4-0.5 mL) was injected into the vitreous cavity in 5 patients with SRH involving the fovea because of age-related macular degeneration (4 eyes) or ruptured retinal arterial macroaneurysm (1 eye). The patients were instructed to maintain a prone position. Results Visual acuity ranged from 20/300 to 20/2000 before gas injection. On the day after gas injection, SRH was dramatically displaced in 3 eyes and slightly displaced with a reduction in the thickness of subfoveal hemorrhage in the remaining 2 eyes. Final visual acuity improved in all cases, ranging from 20/15 to 20/220. Three eyes had a final visual acuity of 20/50 or better. Vitreous hemorrhage caused by migration of SRH into the vitreous cavity and retinal detachment each occurred in 1 eye, and both complications were successfully treated by vitrectomy. Conclusions Gas injected into the vitreous cavity can displace SRH without the use of tissue plasminogen activator in some cases. Visual acuity after gas injection may be improved, making this treatment an alternative to evacuation of SRH with vitrectomy.
Automated Drilling Systems for MPD—The Reality (2012)

Abstract Managed pressure drilling (MPD) has heralded an era of accurate and precise downhole pressure control. Not only can today’s MPD systems operate in tight operational envelopes, but they, more importantly, provide dynamic real-time well control while drilling. This dynamic precision has directly enabled access to assets that were previously considered virtually “undrillable.” But, how can MPD boast such success? One of the major reasons is automation. Automation can provide levels of functional control that are difficult, if not impossible, for human operators to achieve and maintain. MPD’s inherent closed-loop setup, coupled with conventional methodology, naturally lends to automated applications. Furthermore, despite all the advancements in MPD automation within the past few years, there is a common misconception that current MPD systems can provide fully automatic control (“cruise control”) of the entire drilling process. This is far from reality, as MPD systems today provide “supervised automation.” Though there is a lot of material pertaining to the benefits and functionality of MPD automated drilling systems, there is very little technical information on how the systems actually function. The primary focus of this paper is to fill this disparate gap by examining the internals of such a system and, in turn, detailing how it actually works. The paper will start by developing a generic framework, which is common to all MPD automated drilling systems (independent of the company). The components, technology, and architecture will all be presented in detail, which will be augmented by tracing the information flow through the system to clearly illustrate how the MPD process is actually carried out. Having established the technologies, capabilities, and limitations will become apparent. This will then be followed by examples of concrete implementations.
TFP5, a Peptide Derived from Cdk5 Activator p35, Protects Pancreatic β-cells from Glucose Toxicity (2022)

Abstract Type 2 diabetes mellitus (T2DM) is worldwide epidemic, which challenges the health of the public. The pathological hyperactivity of cyclin-dependent kinase 5 (Cdk5) contributes to the pathogenesis of T2DM. P5, a peptide derived from the Cdk5 activator p35, shows excellent performance as a Cdk5 activity inhibitor. However, its inhibitory effect and functional regulation on Cdk5 activity needs to be confirmed. In this study, we conjugated P5 with a fluorescein isothiocyanate (FITC) tag at the N-terminus and a TAT protein transduction domain, an 11-amino acid peptide, at the C-terminus to synthesize TFP5, which was used to inhibits Cdk5 activity. We then evaluated the efficiency of TFP5 in treating T2DM. We demonstrated that TFP5 effectively penetrated pancreatic β-cells, inhibited the pathological hyperactivity of Cdk5, enhanced insulin secretion, and protected penetrated pancreatic β-cells (MIN6 cells) from apoptosis in pancreatic tissues of db/db mice (type II diabetes mice). Furthermore, we found that TFP5 reduced inflammation in pancreatic islets by reducing the expression of inflammatory cytokines, including TGF-β1, TNF-α, and IL-1β. These data indicates that the TFP5 peptide is a promising candidate for T2DM treatment.
Verfahren zur Losgrößenermittlung in Teilenetzen / Methods of lot sitze scheduling in parts networks (1972)

Article Verfahren zur Losgrößenermittlung in Teilenetzen / Methods of lot sitze scheduling in parts networks was published on December 1, 1972 in the journal it - Information Technology (volume 14, issue 1-6).
Evaluation of chemokine-ligand pathways in pretreatment tumor biopsies as predictive biomarker of response to adoptive therapy in metastatic melanoma patients. (2012)

8576 Background: Adoptive therapy with tumor infiltrating lymphocytes (TILs) induces objective responses (OR) in approximately 50% of patients with metastatic melanoma. The recruitment of TILs through CXCR3/CCR5-ligand chemokines is believed critical for immune-mediated rejection. Here, we investigated the predictive role of a gene-signature based on CXCR3/CCR5-ligand chemokine transcripts in pre-treatment melanoma biopsies, its biological role and its relation with CCR5-Δ32 polymorphism, which encodes a protein not expressed on cell surface. Methods: Expression of CXCR3/CXCR3-ligand transcripts (i.e CXCL9, 10, 11) and CCR5/CCR5-ligand transcripts (i.e. CCL3, 4, 5) were assessed in 113 pre-treatment tumor biopsies from patients enrolled in adoptive therapy trials: 24 patients achieved a complete remission (CR), 34 a partial remission (PR), and 55 did not respond (NR). Copy number variation and gene expression profile of these target genes were assessed in 15 biopsy-derived cell lines. CCR5-Δ32 was assessed by sequencing germinal DNA. Results: CXCL9, 10 and 11 and CCL5 clustered together and were selected for hierarchical clustering analysis based on the mean-centered gene expression values. A signature characterized by the over-expression of these genes was associated with the likelihood to achieve a clinical response (OR rate: PR+CR: 65% vs 38%, High vs Low, respectively, P=0.015). Neither correlation between the copy number variation and the gene-expression of the corresponding genes, nor correlation between the transcripts of the investigated genes between tumor biopsies and the matched cell lines was detected. Transcript expression of the target genes did not differ between CCR5-Δ32 (n =20) and wild type patients (n=93). Conclusions: Coordinate over-expression of CXCR3/CCR5 ligands in pre-treatment tumor samples was associated with responsiveness to treatment. However, the lack of correlation between in vivo and ex vivo data suggest the inflammatory status characterized by the up-regulation of these inflammatory chemokine genes is an in vivo multifactorial phenomenon.
A functional Notch–survivin gene signature in basal breast cancer (2008)

A Notch-1-survivin functional gene signature is a hallmark of basal breast cancer, and may contribute to disease pathogenesis. Antagonists of Notch and survivin currently in the clinic may be tested as novel molecular therapy for these recurrence-prone patients.
Impact of Substitution Registry on the Receptor‐Activation Profiles of Backbone‐Modified Glucagon‐like Peptide‐1 Analogues (2019)

Family B G protein-coupled receptors play important physiological roles and possess large extracellular domains (ECDs) that aid in binding the long polypeptide hormones that are their natural agonists. We have previously shown that agonist analogues in which subsets of native α-amino acid residues are replaced with β-amino acid residues can retain activity while avoiding proteolytic degradation. This study focuses on eight new α/β analogues of glucagon-like peptide 1 (GLP-1) that each contain five α-to-β replacements in the C-terminal half of the peptide. This portion of GLP-1 is known to adopt an α-helical conformation and contact the ECD. All four registries of the αααβ backbone pattern were evaluated; previous work has shown that the αααβ pattern supports adoption of an α-helix-like conformation. Two α-to-β replacement formats were employed, one involving β<sup>3</sup> homologues of the native residues replaced and the other involving a cyclic β residue. GLP-1R response was characterized in terms of stimulation of cAMP production and β-arrestin recruitment. Some of the backbone-modified GLP-1 analogues display biased agonism of the GLP-1R. This study helps to establish the scope of the α→β backbone modification strategy.
Large χ(3) of squarylium dye J aggregates measured using the Z-scan technique (2001)

Third-order nonlinear optical coefficients χ(3) were measured for the J aggregates of two types of squarylium dye derivatives at resonant and near-resonant wavelengths by using the Z-scan technique. The maximum χ(3) value evaluated at one-photon resonance was 2.9×10−6 e.s.u., which was greater than that of phthalocyanines by 4 orders of magnitude. χ(3) for one squarylium derivative was approximately two times as large as that of the other. This can be attributed to the difference of the number of molecules contributing to a coherent state in each J aggregate.