gebhart/patrepeval huggingface dataset:
Inhibitors of voltage-gated Sodium Channel Na v 1.7: Patent Applications Since 2010 (2014)

There has been intense interest in developing inhibitors of the sodium channel Nav1.7 because genetic studies have established very strong validation for the efficacy to alleviate both inflammatory and neuropathic pain. This review summarizes patent applications targeting Nav1.7 since 2010 until May, 2014. We have classified the patents into three categories as follows: small molecules with well-defined molecular selectivity among sodium channel isoforms; biologicals with well-defined molecular selectivity; and, small molecules that inhibit Nav1.7 with unknown molecular selectivity. Most of the review is dedicated to small molecule selective compounds.
First Observation of Raman Scattering Emission from Silicon High-Q Photonic Crystal Nanocavities (2011)

We report the first observation of spontaneous Raman scattering in silicon nanocavities with high quality factors. Stokes Raman scattering enhanced by the Q factor was spectrally measured under µW pumping.
Unconventional Alkoxylation of Pyrazino[2,3‐c][1,2,6]thiadiazine 2,2‐Dioxides Mediated by N‐Halosuccinimides. (2002)

Abstract For Abstract see ChemInform Abstract in Full Text.
Iron-57 NMR: relaxation mechanisms and chemical shifts (1984)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTIron-57 NMR: relaxation mechanisms and chemical shiftsLars Baltzer, Edwin D. Becker, B. A. Averill, J. M. Hutchinson, and Otto A. GansowCite this: J. Am. Chem. Soc. 1984, 106, 8, 2444–2446Publication Date (Print):April 1, 1984Publication History Published online1 May 2002Published inissue 1 April 1984https://pubs.acs.org/doi/10.1021/ja00320a042https://doi.org/10.1021/ja00320a042research-articleACS PublicationsRequest reuse permissionsArticle Views173Altmetric-Citations29LEARN 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 Get e-Alerts
MnAl and other novel permanent magnets in electrical machines - a review and simulation study (2020)

MnAl and other novel permanent magnets in electrical machines - a review and simulation study
Improvement of multiple pathophysiological phenotypes ofklotho (kl/kl) mice by adenovirus-mediated expression of theklotho gene (2000)

We showed that local expression of the klotho gene retards or partially improves pathological abnormalities in several organs of klotho mice after onset of the phenotypes. Therefore, the recombinant adenovirus vector will provide an important tool for investigating the molecular mechanism of the Klotho protein and give clues to understanding the individual disease mechanisms.
Supplementary Figure 2 from Chemogenetic Evaluation of the Mitotic Kinesin CENP-E Reveals a Critical Role in Triple-Negative Breast Cancer (2023)

&lt;p&gt;PDF - 165K, Comparison of the effect of PF-2771 and a Eg5/KSP inhibitor on the microtubule network.&lt;/p&gt;
5.5 kV normally-off low RonS 4H-SiC SEJFET (2002)

A normally-off type 5.5 kV 4H-SiC JFET with low specific on-resistance, called SEJFET (Static Expansion channel JFET), has been fabricated. Its normally-off operation was realized by a thin regrown epitaxial channel layer and using the buried p/sup +/ regions as a gate in addition to the top p/sup +/ regions. The achieved blocking voltage (BV) is the highest BV among the reported SiC switching devices. By the expansion of the channel region under the positive biases of both gates, specific on-resistance (R/sub on/S) can be reduced and 218 m/spl Omega/cm/sup 2/ achieved. Furthermore, a 4H-SiC SEJFET with a BV of 4.45 kV has been fabricated, which has the largest figure of merit BV/sup 2//RonS of 164 MW/cm/sup 2/.
Polymorphs and co-crystals of haloprogin: an antifungal agent (2014)

Haloprogin is a widely used antifungal agent. Here we report the first polymorphs and halogen-bonded co-crystals ever described.
Interconversion of Molybdenum or Tungsten d2 Styrene Complexes with d0 1-Phenethylidene Analogues (2021)

Upon addition of 5-15% PhNMe<sub>2</sub>H<sup>+</sup>X<sup>-</sup> (X = B(3,5-(CF<sub>3</sub>)<sub>2</sub>C<sub>6</sub>H<sub>3</sub>)<sub>4</sub> or B(C<sub>6</sub>F<sub>5</sub>)<sub>4</sub>) to Mo(NAr)(styrene)(OSiPh<sub>3</sub>)<sub>2</sub> (Ar = N-2,6-<i>i</i>-Pr<sub>2</sub>C<sub>6</sub>H<sub>3</sub>) in C<sub>6</sub>D<sub>6</sub> an equilibrium mixture of Mo(NAr)(styrene)(OSiPh<sub>3</sub>)<sub>2</sub> and Mo(NAr)(CMePh)(OSiPh<sub>3</sub>)<sub>2</sub> is formed over 36 h at 45 °C (<i>K</i><sub>eq</sub> = 0.36). A plausible intermediate in the interconversion of the styrene and 1-phenethylidene complexes is the 1-phenethyl cation, [Mo(NAr)(CHMePh)(OSiPh<sub>3</sub>)<sub>2</sub>]<sup>+</sup>, which can be generated using [(Et<sub>2</sub>O)<sub>2</sub>H][B(C<sub>6</sub>F<sub>5</sub>)<sub>4</sub>] as the acid. The interconversion can be modeled as two equilibria involving protonation of Mo(NAr)(styrene)(OSiPh<sub>3</sub>)<sub>2</sub> or Mo(NAr)(CMePh)(OSiPh<sub>3</sub>)<sub>2</sub> and deprotonation of the α or β phenethyl carbon atom in [Mo(NAr)(CHMePh)(OSiPh<sub>3</sub>)<sub>2</sub>]<sup>+</sup>. The ratio of the rate of deprotonation of [Mo(NAr)(CHMePh)(OSiPh<sub>3</sub>)<sub>2</sub>]<sup>+</sup> by PhNMe<sub>2</sub> in the α position versus the β position is ∼10, or ∼30 per H<sub>β</sub>. The slow step is protonation of Mo(NAr)(styrene)(OSiPh<sub>3</sub>)<sub>2</sub> (<i>k</i><sub>1</sub> = 0.158(4) L/(mol·min)). Proton sources such as (CF<sub>3</sub>)<sub>3</sub>COH or Ph<sub>3</sub>SiOH do not catalyze the interconversion of Mo(NAr)(styrene)(OSiPh<sub>3</sub>)<sub>2</sub> and Mo(NAr)(CMePh)(OSiPh<sub>3</sub>)<sub>2</sub>, while the reaction of Mo(NAr)(styrene)(OSiPh<sub>3</sub>)<sub>2</sub> with pyridinium salts generates only a trace (∼2%) of Mo(NAr)(CMePh)(OSiPh<sub>3</sub>)<sub>2</sub> and forms a monopyridine adduct, [Mo(NAr)(CHMePh)(OSiPh<sub>3</sub>)<sub>2</sub>(py)]<sup>+</sup> (two diastereomers). The structure of [Mo(NAr)(CHMePh)(OSiPh<sub>3</sub>)<sub>2</sub>]<sup>+</sup> has been confirmed in an X-ray study; there is no structural indication that a β proton is activated through a CH<sub>β</sub> interaction with the metal. W(NAr)(CMePh)(OSiPh<sub>3</sub>)<sub>2</sub> is also converted into a mixture of W(NAr)(CMePh)(OSiPh<sub>3</sub>)<sub>2</sub> and W(NAr)(styrene)(OSiPh<sub>3</sub>)<sub>2</sub> (<i>K</i><sub>eq</sub> = 0.47 at 45 °C in favor of the styrene complex) with 10% [PhNMe<sub>2</sub>H][B(C<sub>6</sub>F<sub>5</sub>)<sub>4</sub>] as the catalyst; the time required to reach equilibrium is approximately the same as in the Mo system.
Anti-Thrombotic Effects of Targeting Outside-in αIIbβ3 Signaling in Platelets (2008)

Abstract Platelet activation by agonists stimulates high affinity binding of adhesive ligands, such as fibrinogen, to integrin αIIbβ3. In turn, ligand binding initiates Src kinase-dependent outside-in signaling, platelet spreading on sub-endothelial matrices, and platelet aggregation. Short-term integrin blockade by parenteral αIIbβ3 antagonists is effectively anti-thrombotic in certain clinical situations, but long-term blockade by oral αIIbβ3 antagonists has been problematic. As an alternative approach, we evaluated the feasibility of disrupting outside-in αIIbβ3 signaling in vivo. A “β3(Δ760-762)” knock-in mouse was generated that lacked the three C-terminal β3 amino acid residues (RGT) necessary for αIIbβ3-dependent c-Src signaling, but retained β3 residues necessary for agonist- and talin-dependent fibrinogen binding. β3(Δ760-762) mice were compared with wild-type β3+/+ littermates, β3+/− heterozygotes, and “β3/β1(EGK)” knock-in mice where β3 RGT was replaced by three C-terminal residues in β1 (EGK) to potentially enable outside-in integrin signaling by certain Src kinases other than c-Src. Whereas β3+/+, β3+/− and β3/β1(EGK) platelets spread and underwent tyrosine phosphorylation normally on fibrinogen, β3(Δ760-762) platelets spread poorly and exhibited reduced tyrosine phosphorylation of c-Src substrates, including the β3 cytoplasmic domain itself (Tyr-747). Furthermore, unlike the three groups of control mice, all of the β3(Δ760-762) mice tested were protected from carotid artery occlusive thrombosis following vessel injury with FeCl3. The median tail bleeding time for the β3(Δ760-762) mice was approximately two-fold longer than that of the control mice. However, β3(Δ760-762) mice did not exhibit spontaneous bleeding, excess bleeding after surgical exposure of the carotid artery, fecal blood loss or anemia. Fibrinogen binding to β3(Δ760-762) platelets was normal in response to saturating concentrations of agonists to the PAR4 thrombin receptor or the GP VI collagen receptor; however, responses to ADP were impaired. These studies establish that deletion of β3 RGT disrupts outside-in αIIbβ3 signaling and confers protection from arterial thrombosis in vivo. Currently available anti-platelet drugs either inhibit agonist-induced activation of αIIbβ3 or block fibrinogen binding to the integrin. The studies reported here suggest that targeting outside-in αIIbβ3 signaling may represent an alternative anti-thrombotic strategy.
The Printing Dress (2011)

You are probably familiar with the old saying, “You are what you eat” but how about, “You are what you tweet?” What if this concept were incorporated into garments of the future? Would you censor yourself, knowing you would reveal your statements to the world around you? The “Printing Dress” is an artistic piece that explores the notion of wearable text and its potential impact on the future of fashion, as well as our social identity. Built almost entirely of paper, the dress enables the wearer to enter “thoughts” on to its fabric and wear them as public art. By selecting materials and technologies that draw on the past, present, and future of communication media, we encourage viewers to reflect on the path that has brought us to ubiquitous digital communication and to contemplate its forward evolution. “Best in Show” ISWC 2011 Design Exhibition “Best Concept” ISWC 2011 Design Exhibition
Thermally nucleated magnetic reversal in CoFeB/MgO nanodots (2017)

Power consumption is the main limitation in the development of new high performance random access memory for portable electronic devices. Magnetic RAM (MRAM) with CoFeB/MgO based magnetic tunnel junctions (MTJs) is a promising candidate for reducing the power consumption given its non-volatile nature while achieving high performance. The dynamic properties and switching mechanisms of MTJs are critical to understanding device operation and to enable scaling of devices below 30 nm in diameter. Here we show that the magnetic reversal mechanism is incoherent and that the switching is thermally nucleated at device operating temperatures. Moreover, we find an intrinsic thermal switching field distribution arising on the sub-nanosecond time-scale even in the absence of size and anisotropy distributions or material defects. These features represent the characteristic signature of the dynamic properties in MTJs and give an intrinsic limit to reversal reliability in small magnetic nanodevices.
Laparoscopic-Assisted Transversus Abdominis Plane Block to Decrease Postoperative Opioid Use in Laparoscopic Sleeve Gastrectomy Patients (2018)

Margulies, Ilana G. MS; Eskin, Yulia MSN, CRNP; Nana, Ninna; Emamhosseini, Ali MD; Cook, Tuesday FA. MD, FACS, FASMBS; Greene, Barry S. MD, FACS, FASMBS Author Information
Interferometric Acousto-Optic Receiver (1989)

This paper reports the progress on the development of an interferometric acousto-optic receiver. The receiver is designed to receive radio frequency (RF) signals as input and generate digital words as output which includes frequency, pulse amplitude, pulse width and time of arrival (TOA). The system consists of the following basic building blocks: the optical bench, the RF reference, the IF portion and the digital encoder. This paper presents alternative designs and corresponding receiver performance. This paper also describes some of the problems and suggests possible solutions to improve the performance.
Paramagnetic relaxivity of delocalized long-lived states of protons in chains of CH 2 groups (2022)

Abstract. Long-lived states (LLS) have lifetimes TLLS that can be much longer than longitudinal relaxation times T1. In molecules containing several geminal pairs of protons in neighbouring CH2 groups, it has been shown that delocalized long-lived states can be excited by converting magnetization into imbalances between the populations of singlet and triplet states of each pair. Since the yield of conversion of observable magnetization into LLS and back are on the order of 10 % or less if one uses spin-locked induced crossing (SLIC), it would be desirable to boost the sensitivity by dissolution dynamic nuclear polarization (d-DNP). To enhance the magnetization of nuclear spins by d-DNP, the analytes must be mixed with radicals such as 4-hydroxy-2,2,6,6-tetramethylpiperidin-1-oxyl (TEMPOL) prior to freezing at low temperatures in the vicinity of 1 K. After dissolution, these radicals lead to an undesirable paramagnetic relaxation enhancement (PRE) which shortens not only the longitudinal relaxation times T1 but also the lifetimes TLLS of long-lived states. It is confirmed in this work that PRE by TEMPOL is less deleterious for LLS than for longitudinal magnetization for four different molecules: 2,2-dimethyl-2-silapentane-5-sulfonate (DSS), homotaurine, taurine, and acetylcholine. The relaxivities (i.e., the slopes of relaxation rates as a function of the radical concentration) of LLS rLLS are 3 to 5 times smaller than the relaxivities of longitudinal magnetization r1. Partial delocalization of the LLS across neighbouring CH2 groups may decrease this advantage, but in practice, this effect was observed to be minor when comparing taurine containing two CH2 groups and homotaurine with three CH2 groups. Regardless of whether the LLS are delocalized or not, it is shown that PRE should not be a major problem for experiments combining d DNP and LLS, provided the concentration of paramagnetic species after dissolution does not exceed 1 mM, a condition that is readily fulfilled in typical d-DNP experiments. In bullet d-DNP experiments, however, it may be necessary to reduce TEMPOL by adding ascorbate or using lower concentrations of TEMPOL.
Chronic GVHD and Pretransplantation Abnormalities in Pulmonary Function Are the Main Determinants Predicting Worsening Pulmonary Function in Long-term Survivors after Stem Cell Transplantation (2006)

Pulmonary function (PF) was studied in 69 consecutive patients with hematologic diseases, with a minimum 5-year (range, 5-13 years) follow-up after allogeneic stem cell transplantation from an HLA-matched sibling. Fifty-six patients (81%) received total body irradiation based myeloablative stem cell transplantation (MT) and 13 (19%) underwent nonmyeloablative stem cell transplantation (NST). Thirty-one patients (45%) developed a late decrease in PF from baseline, 25 with a restrictive and 6 with an obstructive pattern PF abnormality. Twelve patients (17%) were symptomatic, 8 with a severe restrictive PF defect, but none required supplemental oxygen. The incidence of developing a late PF abnormality was comparable in MT (24 of 56) and NST (5 of 13; P = .51). In multivariate analysis, chronic graft-versus-host disease (relative risk, 16) and pretransplantation diffusion capacity for carbon monoxide or forced expiratory volume in the first second <80% predicted were independently associated with a late decrease in PF from baseline (relative risk, 7). Our results indicate that late PF abnormality is common after MT and NST. Patients with a low pretransplantation diffusion capacity for carbon monoxide of or forced expiratory volume in the first second who developed chronic graft-versus-host disease were most severely affected. Longer follow-up is needed to determine whether PF will continue to decrease or reach a plateau and whether more patients with PF abnormality will eventually become symptomatic.
Spatial aspects of oncogenic signalling determine the response to combination therapy in slice explants from Kras‐driven lung tumours (2018)

A key question in precision medicine is how functional heterogeneity in solid tumours informs therapeutic sensitivity. We demonstrate that spatial characteristics of oncogenic signalling and therapy response can be modelled in precision-cut slices from Kras-driven non-small-cell lung cancer with varying histopathologies. Unexpectedly, profiling of in situ tumours demonstrated that signalling stratifies mostly according to histopathology, showing enhanced AKT and SRC activity in adenosquamous carcinoma, and mitogen-activated protein kinase (MAPK) activity in adenocarcinoma. In addition, high intertumour and intratumour variability was detected, particularly of MAPK and mammalian target of rapamycin (mTOR) complex 1 activity. Using short-term treatment of slice explants, we showed that cytotoxic responses to combination MAPK and phosphoinositide 3-kinase-mTOR inhibition correlate with the spatially defined activities of both pathways. Thus, whereas genetic drivers determine histopathology spectra, histopathology-associated and spatially variable signalling activities determine drug sensitivity. Our study is in support of spatial aspects of signalling heterogeneity being considered in clinical diagnostic settings, particularly to guide the selection of drug combinations. © 2018 The Authors. The Journal of Pathology published by John Wiley & Sons Ltd on behalf of Pathological Society of Great Britain and Ireland.
Assessment of frequency drift on CEST MRI and dynamic correction: application to gagCEST at 7 T (2018)

Prospective or retrospective correction of the frequency drift of the MRI scanner is essential for reproducible gagCEST measurements. The proposed retrospective correction method fulfills this requirement without the need of additional measurements.
Mobility-Lifetime Products in N-Carbazolyl-Substituted Polysilanes (2000)

Mobility-lifetime products, µτ, of N -carbazolyl-substituted silane co- and homopolymers have been studied by means of photo-induced discharge measurements. With increasing concentration of N -carbazolyl groups, the µτ product is abruptly decreased at a certain concentration of N -carbazolyl groups. The result is consistent with our earlier finding that the hole transit was unobservable above the concentration in the time-of-flight measurements. The origin of the decrease in the µτ product is discussed.
First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study (2017)

Ulixertinib (BVD-523) is an ERK1/2 kinase inhibitor with potent preclinical activity in BRAF- and RAS-mutant cell lines. In this multicenter phase I trial (NCT01781429), 135 patients were enrolled to an accelerated 3 + 3 dose-escalation cohort and six distinct dose-expansion cohorts. Dose escalation included 27 patients, dosed from 10 to 900 mg twice daily and established the recommended phase II dose (RP2D) of 600 mg twice daily. Ulixertinib exposure was dose proportional to the RP2D, which provided near-complete inhibition of ERK activity in whole blood. In the 108-patient expansion cohort, 32% of patients required dose reduction. The most common treatment-related adverse events were diarrhea (48%), fatigue (42%), nausea (41%), and dermatitis acneiform (31%). Partial responses were seen in 3 of 18 (17%) patients dosed at or above maximum tolerated dose and in 11 of 81 (14%) evaluable patients in dose expansion. Responses occurred in patients with <i>NRAS</i>-, <i>BRAF</i> V600-, and non-V600 <i>BRAF</i>-mutant solid tumors.<b>Significance:</b> Here, we describe the first-in-human dose-escalation study of an ERK1/2 inhibitor for the treatment of patients with advanced solid tumors. Ulixertinib has an acceptable safety profile with favorable pharmacokinetics and has shown early evidence of clinical activity in <i>NRAS</i>- and <i>BRAF</i> V600- and non-V600-mutant solid-tumor malignancies. <i>Cancer Discov; 8(2); 184-95. ©2017 AACR.</i><i>See related commentary by Smalley and Smalley, p. 140</i><i>This article is highlighted in the In This Issue feature, p. 127</i>.
Supplementary Figure 3 from Impaired IFN-α Production by Plasmacytoid Dendritic Cells Favors Regulatory T-cell Expansion That May Contribute to Breast Cancer Progression (2023)

&lt;p&gt;PDF file, 64K, Breast TUMSN, but not BCCSN, inhibit IFN-α production by CpGA- or Flu-activated pDC in a dose-dependent manner.&lt;/p&gt;
Characterization of Sr‐Doped LaMnO3 and LaCoO3 as Cathode Materials for a Doped LaGaO3 Ceramic Fuel Cell (1996)

Energy dispersive spectrometry line scan and ac impedance spectroscopy were used in this study to investigate the chemical reactions between two cathode materials, La0.84Sr0.16MnO3 (LSM), La0.5Sr0.5CoO3-δ (LSC), and the electrolyte La0.9Sr0.1Ga0.8Mg0.2O2.85 (LSGM). Significant interdiffusions of Co into LSGM and Ga into LSC were found at an LSC/LSGM interface even at relatively low fabrication temperatures. In contrast, only small interdiffusions of Mn into LSGM and Ga into LSM were detected at the LSM/LSGM interface even though it was fired at 1470°C. The ac impedance spectra of the electrolyte LSGM with LSM, LSC, and Pt electrodes indicate a grain‐boundary contribution to the total conductivity in the intermediate frequency range and a diffusion‐controlled impedance in the low‐frequency range. Irrespective of chemical reactions and a larger thermal expansion coefficient, LSC has the lowest dc resistance of all three electrodes investigated. Considering both the small interdiffusion reactions between LSM and LSGM and their similar thermal expansion coefficients, LSM could be an appropriate cathode material for LSGM‐based fuel cells.
Probing the Consequences of Cubic Particle Shape and Applied Field on Colloidal Crystal Engineering with DNA (2020)

Abstract In a magnetic field, cubic Fe 3 O 4 nanoparticles exhibit assembly behavior that is a consequence of a competition between magnetic dipole–dipole and ligand interactions. In most cases, the interactions between short hydrophobic ligands dominate and dictate assembly outcome. To better tune the face‐to‐face interactions, cubic Fe 3 O 4 nanoparticles were functionalized with DNA. Their assembly behaviors were investigated both with and without an applied magnetic field. Upon application of a field, the tilted orientation of cubes, enabled by the flexible DNA ligand shell, led to an unexpected crystallographic alignment of the entire superlattice, as opposed to just the individual particles, along the field direction as revealed by small and wide‐angle X‐ray scattering. This observation is dependent upon DNA length and sequence and cube dimensions. Taken together, these studies show how combining physical and chemical control can expand the possibilities of crystal engineering with DNA.