gebhart/patrepeval huggingface dataset:
Novel 5-Alkyl Pyrrolidine Orexin Receptor Agonists for Treating Sleep Disorders (2020)

ADVERTISEMENT RETURN TO ISSUEPREVPatent HighlightNEXTNovel 5-Alkyl Pyrrolidine Orexin Receptor Agonists for Treating Sleep DisordersRam W. Sabnis*Ram W. SabnisSmith, Gambrell & Russell LLP, 1230 Peachtree Street NE, Suite 3100, Atlanta, Georgia 30309, United States*Email: [email protected]More by Ram W. Sabnishttp://orcid.org/0000-0001-7289-0581Cite this: ACS Med. Chem. Lett. 2020, 11, 11, 2085–2086Publication Date (Web):September 29, 2020Publication History Received14 September 2020Published online29 September 2020Published inissue 12 November 2020https://pubs.acs.org/doi/10.1021/acsmedchemlett.0c00501https://doi.org/10.1021/acsmedchemlett.0c00501editorialACS PublicationsCopyright © 2020 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 Views2058Altmetric-Citations1LEARN 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 (737 KB) Get e-AlertscloseSUBJECTS:Agonists,Alkyls,Peptides and proteins,Receptors,Substituents Get e-Alerts
Elevated temperature oxidation and etching of the Si(111) 7×7 surface observed with scanning tunneling microscopy (1993)

Scanning tunneling microscopy has been used to study the initial oxidation of the Si(111) 7×7 surface over the temperature range 400–600 °C. Oxygen-induced etching of the surface is observed for low O2 pressures (&lt;10−7 Torr) at temperatures between 500 and 600 °C, causing monolayer-deep holes in the surface and the retraction of step edges. The newly exposed surfaces often reconstruct into metastable 5×5 or 9×9 structures, as well as the stable 7×7 structure.
Penta-1,2,3,4,6-<i>O</i>-galloyl-β-<scp>d</scp>-glucose induces p53 and inhibits STAT3 in prostate cancer cells<i>in vitro</i>and suppresses prostate xenograft tumor growth<i>in vivo</i> (2008)

Penta-1,2,3,4,6-O-galloyl-beta-D-glucose (PGG) is a naturally occurring gallotannin from some Oriental herbs. Several cell culture studies suggested a potential for PGG as a novel agent for the chemoprevention and treatment of cancer. Here, we investigated the cell death signaling mechanisms induced by PGG in human prostate cancer cells of different p53 functional status. We observed the induction of G(1)- and S-phase arrests and caspase-mediated apoptosis in the androgen-dependent human LNCaP cells, which express wild-type p53, and in the androgen-independent, p53-mutant DU145 cells. In LNCaP cells, caspase-mediated apoptosis induction by PGG was associated with and mediated in major part by activation of p53 as established through small interfering RNA knockdown and dominant-negative mutant approaches. Intracellular reactive oxygen species production by PGG was found to be crucial for these molecular and cellular actions. In DU145 cells, which harbor constitutively active signal transducer and activator of transcription 3 (STAT3), caspase-mediated apoptosis induction by PGG was associated with an inhibition of STAT3 Tyr705 phosphorylation and the down-regulation of STAT3 transcriptional targets Bcl-XL and Mcl-1. Overexpression of Bcl-XL or knockdown of its binding partner Bak attenuated apoptosis induction. Furthermore, we provide, for the first time, in vivo data that PGG significantly inhibited DU145 xenograft growth in an athymic nude mouse model in association with an inhibition of pSTAT3. Our data support PGG as a multitargeting agent for chemoprevention and therapy of prostate cancer by activating the p53 tumor suppressor pathway and by inhibiting STAT3 oncogenic signaling.
Biotransformation of linoleic acid by <i>Clavibacter</i> sp. ALA2: Heterocyclic and heterobicyclic fatty acids (2000)

Clavibacter sp. ALA2 transformed linoleic acid into a variety of oxylipins. In previous work, three novel fatty acids were identified, (9Z)-12, 13, 17-trihydroxy-9-octadecenoic acid and two tetrahydrofuran-(di)hydroxy fatty acids. In this report, we confirm the structures of the tetrahydrofuran-(di)hydroxy fatty acids by nuclear magnetic resonance as (9Z)-12-hydroxy-13,16-epoxy-9-octadecenoic acid and (9Z)-7,12-dihydroxy-13,16-epoxy-9-octadecenoic acid. Three other products of the biotransformation were identified as novel heterobicyclic fatty acids, (9Z)-12,17;13, 17-diepoxy-9-octadecenoic acid, (9Z)-7-hydroxy-12,17;13,17-diepoxy-9-octadecenoic acid, and (9Z)-12,17;13,17-diepoxy-16-hydroxy-9-octadecenoic acid. Thus, Clavibacter ALA2 effectively oxidized linoleic acid at C-7, -12, -13, -16, and/or -17.
An 8.4mW/Gb/s 4-lane 48Gb/s multi-standard-compliant transceiver in 40nm digital CMOS technology (2011)

The bandwidth limitation of existing backplanes has become an obstacle to meeting the increasing demand for high-data-rate wireline transmission. In order to compensate for this limitation, TX pre-emphasis, RX continuous-time linear equalizer (CTLE) and DFE are necessary [1,2]. This work presents a 4-lane transceiver implemented in 40nm CMOS technology that operates over a wide range of data rates from 1 to 12Gb/s (48Gb/s aggregated) using NRZ coding. The supply voltages are 0.9V and 1.8V. An algorithm is developed to adapt the CTLE and DFE to cancel the channel ISI. No inductors are used in the design and ring oscillators are used for both the TX and RX clock generation. This provides a wide frequency-tuning range, small layout area, and high design portability. With extensive use of digital programmability this transceiver is capable of meeting specifications of different standards, such as PCIe, SATA, and 1 to 10Gb/s Ethernet.
Preface to the third edition (2010)

Four things are required for plant growth: energy in the form of solar radiation; inorganic carbon in the form of carbon dioxide or bicarbonate ions; mineral nutrients; and water. Those plants which, in the course of evolution, have remained in, or have returned to, the aquatic environment have one major advantage over their terrestrial counterparts: namely, that water – lack of which so often limits productivity in the terrestrial biosphere – is for them present in abundance; but for this a price must be paid. The medium – air – in which terrestrial plants carry out photosynthesis offers, within the sort of depth that plant canopies occupy, no significant obstacle to the penetration of light. The medium – water – in which aquatic plants occur, in contrast, both absorbs and scatters light. For the phytoplankton and the macrophytes in lakes and rivers, coastal and oceanic waters, both the intensity and spectral quality of the light vary markedly with depth. In all but the shallowest waters, light availability is a limiting factor for primary production by the aquatic ecosystem. The aquatic plants must compete for solar radiation not only with each other (as terrestrial plants must also do), but also with all the other light-absorbing components of the aquatic medium. This has led, in the course of evolution, to the acquisition by each of the major groups of algae of characteristic arrays of light-harvesting pigments that are of great biochemical interest, and also of major significance for an understanding both of the adaptation of the algae to their ecological niche and of the phylogeny and taxonomy of the different algal groups. Nevertheless, in spite of the evolution of specialized light-harvesting systems, the aquatic medium removes so much of the incident light that aquatic ecosystems are, broadly speaking, less productive than terrestrial ones.
Numerical model for DNA loading in microdevices: Stacking and autogating effects (2006)

Many electrophoresis-based DNA sequencing and genotyping microdevices rely on field-driven effects to load and preconcentrate the sample. A quantitative model is developed for a broad class of electrophoresis-based microfabricated sample injectors. Quantitative predictions of DNA preconcentration are compared with experimental data and are shown to qualitatively reproduce the detailed time-evolving sample distribution in the injector. The model provides practical guidance on device and protocol design, in order to optimize this critical aspect of microfluidic devices.
Employing patterns and layers for early-stage design and prototyping of cross-device user interfaces (2008)

Designing UIs that run across multiple devices is increasingly important. To address this, we have created a prototyping tool called Damask, which targets web UIs that run on PCs and mobile phones, and prompt-and-response style voice UIs. In Damask, designers sketch out their design for one device while using design patterns to specify higher-level concepts within their design. Damask's patterns include pre-built UI fragments that are already optimized for each device. Designers also use layers to specify which UI parts are common across devices and which are specific to one device. Damask uses the sketches and patterns to generate designs for the other devices, which the designers can refine. A study performed with 12 professional UI designers found that, in the early stages, designers using patterns and layers in Damask created cross-device UIs that are rated at least as good as those created without patterns and layers, without more time.
The endothelium during cuff-induced neointima formation in the rabbit carotid artery. (1993)

Intimal thickening in human arteries is considered as a site of predilection for atherosclerosis. The placement of a flexible, physically nonconstrictive, silicone cuff around the rabbit carotid artery induced a neointima composed of smooth muscle cells (SMCs) within 14 days. To investigate possible alterations of the endothelial cells (ECs) during neointima formation, their morphology was examined with scanning electron microscopy (SEM), transmission electron microscopy (TEM), and confocal microscopy. In the early postoperative period (6 hours), both cuffed and sham-operated arteries demonstrated small foci (5 to 200 microns) of denudation, presumably as a consequence of the manipulation. Within 24 hours the luminal surface of the cuffed and sham-operated arteries was completely covered with endothelium, which remained continuous throughout the study. However, after 1 week the ECs of the cuffed arteries contained a pronounced rough endoplasmic reticulum. From 6 hours until 3 days, polymorphonuclear leukocytes infiltrated the cuffed but not the sham-operated arteries from the lumen. Subendothelial SMC accumulation in the cuffed arteries began after this time period. At day 14 a full-blown neointima composed of longitudinally oriented SMCs had formed in the cuffed arteries. The sham-operated arteries did not develop a neointima. During neointima formation immunoreactivity for von Willebrand factor (vWf) increased in the ECs, and vWf was deposited in the extracellular spaces of the neointima. At day 14 the area of vWf deposits correlated positively with the area of the neointima (r = .73, P < .001). In subsequent weeks, the intimal area did not increase, and vWf deposits vanished from the neointimal matrix. The endothelium of the sham-operated arteries showed no change in vWf immunoreactivity compared with untreated arteries throughout the study. The altered ultrastructural morphology of the ECs and the concurrent vWf deposition in cuffed but not in sham-operated arteries point to alterations in EC function during the development of the neointima. The vWf secretion could possibly lead to increased adhesiveness of the extracellular matrix for the ECs as well as modulate neointima formation.
Todayʼs Management Methods: A Guide for the Health Care Executive (1999)

American Hospital Publishing, Inc., 737 N. Michigan Avenue, Chicago, IL 6061 1, 800/2422626,1996,313 pages, $69 (nonmembers), $55 (TTETXY), ISBN 1-55648-153-5
A cross layer routing protocol for cognitive radio networks using channel activity tracking (2012)

We propose a cross-layer routing protocol for cognitive radio (CR) networks, where spectrum sensing, medium access control (MAC) and routing are done simultaneously at each node. First, we propose a sensing scheme using sequential Bayesian estimation where each sensor computes the posterior probability of channel availability for each frequency band. Then, we design a reward metric based on the posterior probability of channel availability and achievable channel capacity. Using this reward metric, the MAC layer selects the channel on which the link between two SUs is established. Finally, in the network layer, we adopt a Best-first-search routing algorithm which selects the node in the direction of the destination to forward the packet. The performance of the proposed scheme is evaluated by calculating the number of successful packet transmissions between a given source - destination pair and the number of collisions with the primary users.
Thrust Vectoring Nozzle for Modern Military Aircraft (2000)

This paper describes the technical features of the Thrust Vectoring Nozzle (TVN) developed by ITP and its advantages for modem military aircraft. It is presented in Conjunction with two other papers by DASA (Thrust Vectoring for Advanced Fighter Aircraft High Angle of Attack Intake Investigations) and MTU-Muenchen (Integrated Thrust Vector Jet Engine Control) respectively.
Hardware design of PMSM control system based on DSP (2021)

Abstract Compared with traditional motor, permanent magnet synchronous motor has the characteristics of strong anti-interference ability, high starting torque and power density, and good speed regulation performance.Permanent magnet synchronous motor servo system has become a research hotspot in the field of servo drive.In this paper, with DSP28335 as the main control chip to give a permanent magnet synchronous motor AC servo control hardware system design scheme, the paper introduces in detail the system core control circuit, main power circuit, detection circuit design and the choice of main components.The hardware system designed has been applied to engineering practice, and has achieved good control effect.
FPAA-based mho distance relay considering CVT transient supervision (2009)

Present-day numerical relays provide remarkable capabilities such as monitoring, recording and communication. These capabilities are considered as secondary priority whereas speed and reliability are the two most important characteristics of a protective relay. Even though present-day numerical relays have provided considerable capabilities and advantages, they have not improved speed of operation in comparison to their solid-state counterparts. The idea of applying mixed signals processing using advanced analogue and digital technology in several applications has started. Use of advanced programmable analogue technology, which is known as field programmable analogue arrays (FPAAs), seems to have the potential to be used in protective relays. Hybrid hardware using both digital signal processor (DSP) and FPAAs is proposed to implement mho distance relay considering capacitor voltage transformer (CVT) transient supervision for low and high system impedance ratio (SIR) systems. Test results are reported and compared with a commercial relay test results.
<i>In vivo</i> Color-Coded Imaging of the Interaction of Colon Cancer Cells and Splenocytes in the Formation of Liver Metastases (2006)

The role of host cells in tumor progression and metastasis is critical. Intrasplenic injection of tumor cells has long been known as an effective method of developing liver metastases in nude mice, whereas portal vein (PV) injection of tumor cells can result in rapid death of the tumor cells. Host cells were thought to play a role in these phenomena. We report here that after splenic injection of tumor cells, splenocytes cotraffic with the tumor cells to the liver and facilitate metastatic colony formation. Human colon cancer cells that express green fluorescent protein (GFP) linked to histone H2B in the nucleus and red fluorescent protein (RFP) in the cytoplasm (HCT-116-GFP-RFP) were injected in either the PV or spleen of nude mice and imaged at the subcellular level in vivo. Extensive clasmocytosis (destruction of the cytoplasm) of the cancer cells occurred within 6 hours after PV injection and essentially all the cancer cells died. In contrast, splenic injection of these tumor cells resulted in the aggressive formation of liver and distant metastasis. GFP spleen cells were found in the liver metastases that resulted from intrasplenic injection of the tumor cells in transgenic nude mice ubiquitously expressing GFP. When GFP spleen cells and the RFP cancer cells were coinjected in the PV, liver metastasis resulted that contained GFP spleen cells. These results suggest a novel tumor-host interaction that enables efficient formation of liver metastasis via intrasplenic injection.
Purification and characterisation of TOL plasmid‐encoded benzyl alcohol dehydrogenase and benzaldehyde dehydrogenase of <i>Pseudomonas putida</i> (1990)

Benzyl alcohol dehydrogenase and benzaldehyde dehydrogenase, two enzymes of the xylene degradative pathway encoded by the plasmid TOL of a Gram-negative bacterium Pseudomonas putida, were purified and characterized. Benzyl alcohol dehydrogenase catalyses the oxidation of benzyl alcohol to benzaldehyde with the concomitant reduction of NAD+; the reaction is reversible. Benzaldehyde dehydrogenase catalyses the oxidation of benzaldehyde to benzoic acid with the concomitant reduction of NAD+; the reaction is irreversible. Benzyl alcohol dehydrogenase and benzaldehyde dehydrogenase also catalyse the oxidation of many substituted benzyl alcohols and benzaldehydes, respectively, though they were not capable of oxidizing aliphatic alcohols and aldehydes. The apparent Km value of benzyl alcohol dehydrogenase for benzyl alcohol was 220 microM, while that of benzaldehyde dehydrogenase for benzaldehyde was 460 microM. Neither enzyme contained a prosthetic group such as FAD or FMN, and both enzymes were inactivated by SH-blocking agents such as N-ethylmaleimide. Both enzymes were dimers of identical subunits; the monomer of benzyl alcohol dehydrogenase has a mass of 42 kDa whereas that of the monomer of benzaldehyde dehydrogenase was 57 kDa. Both enzymes transfer hydride to the pro-R side of the prochiral C4 of the pyridine ring of NAD+.
Integrated Project Views: Decision Support Platform for Drug Discovery Project Teams (2012)

Drug discovery teams continuously have to decide which compounds to progress and which experiments to perform next, but the data required to make informed decisions is often scattered, inaccessible, or inconsistent. In particular, data tend to be stored and represented in a compound-centric or assay-centric manner rather than project-centric as often needed for effective use in drug discovery teams. The Integrated Project Views (IPV) system has been created to fill this gap; it integrates and consolidates data from various sources in a project-oriented manner. Its automatic gathering and updating of project data not only ensures that the information is comprehensive and available on a timely basis, but also improves the data consistency. Due to the lack of suitable off-the-shelf solutions, we were prompted to develop custom functionality and algorithms geared specifically to our drug discovery decision making process. In 10 years of usage, the resulting IPV application has become very well-accepted and appreciated, which is perhaps best evidenced by the observation that standalone Excel spreadsheets are largely eliminated from project team meetings.
THE APPLICATION OF GAS-CHROMATOGRAPHY TO THE IDENTIFICATION OF WAXES (1978)

The sources and chemistry of waxes likely to be encountered in art objects are briefly reviewed and their gas-chromatograms are illustrated. Examples of the identification of waxes and wax-mixtures in a variety of objects are described, and the advantages for this purpose of gas-chromatography over infrared spectroscopy are indicated.
Actively quenched single-photon avalanche diode for high repetition rate time-gated photon counting (1996)

This paper reports an experimental characterization of the EG&G SPCM-AQ single-photon avalanche diode module with an active quenching bias circuit that gives a dead time of ∼35 ns for use in high count rate, fast timing applications. A quantum efficiency of ≳70% and an optimal timing jitter with a full width at one-thousandth maximum of 1.5 ns is obtained if the light is tightly focused to a spot of &lt;25 μm in the center of the active region, if the signal from the diode before the active quenching circuitry is used as input to the timing electronics, and if an external dead time of ∼55 ns is imposed. Under these conditions, the total probability of obtaining an afterpulse is found to be ∼2×10−3. Limitations of existing time-correlated single-photon counting instrumentation for count rates exceeding 106 s−1 are discussed.
Blockade of Myeloid-Derived Suppressor Cells after Induction of Lymphopenia Improves Adoptive T Cell Therapy in a Murine Model of Melanoma (2012)

Administration of nonmyeloablative chemotherapeutic agents or total body irradiation (TBI) prior to adoptive transfer of tumor-specific T cells may reduce or eliminate immunosuppressive populations such as T regulatory cells (Tregs) and myeloid-derived suppressor cells (MDSC). Little is known about these populations during immune reconstitution. This study was designed to understand the reconstitution rate and function of these populations post TBI in melanoma tumor-bearing mice. Reconstitution rate and suppressive activity of CD4(+)CD25(+)Foxp3(+) Tregs and CD11b(+)Gr1(+) MDSC following TBI-induced lymphopenia was measured in B16 melanoma tumor-bearing mice. To ablate the rapid reconstitution of suppressive populations, we treated mice with docetaxel, a known chemotherapeutic agent that targets MDSC, in combination with adoptive T cell transfer and dendritic cell immunotherapy. Both Treg and MDSC populations exhibited rapid reconstitution after TBI-induced lymphopenia. Although reconstituted Tregs were just as suppressive as Tregs from untreated mice, MDSC demonstrated enhanced suppressive activity of CD8(+) T cell proliferation compared with endogenous MDSC from tumor-bearing mice. TBI-induced lymphopenia followed by docetaxel treatment improved the efficacy of adoptive T cell transfer and dendritic cell immunotherapy in melanoma-bearing mice, inducing a significant reduction in tumor growth and enhancing survival. Tumor regression correlated with increased CTL activity and persistence of adoptively transferred T cells. Overall, these findings suggest that TBI-induced MDSC are highly immunosuppressive and blocking their rapid reconstitution may improve the efficacy of vaccination strategies and adoptive immunotherapy.