gebhart/patrepeval huggingface dataset:
Basis for Design and Development of Platinum(IV) Anticancer Complexes (2007)

ADVERTISEMENT RETURN TO ISSUEPerspectiveNEXTBasis for Design and Development of Platinum(IV) Anticancer ComplexesMatthew D. Hall, Howard R. Mellor, Richard Callaghan, and Trevor W. HambleyView Author Information Centre for Heavy Metals Research, School of Chemistry, The University of Sydney, New South Wales 2006, Australia, Laboratory of Cell Biology, National Cancer Institute, National Institutes of Health, 37 Convent Drive, Bethesda, Maryland 20893-4256, and Oxford Drug Resistance Group, Nuffield Department of Clinical Laboratory Sciences, John Radcliffe Hospital, University of Oxford, Oxford OX3 9DU, U.K. Cite this: J. Med. Chem. 2007, 50, 15, 3403–3411Publication Date (Web):June 28, 2007Publication History Received12 March 2007Published online28 June 2007Published inissue 1 July 2007https://pubs.acs.org/doi/10.1021/jm070280uhttps://doi.org/10.1021/jm070280ureview-articleACS PublicationsCopyright © 2007 American Chemical SocietyRequest reuse permissionsArticle Views5547Altmetric-Citations393LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose SUBJECTS:Antineoplastic agents,Cells,Ligands,Redox reactions,Toxicity Get e-Alerts
3D-DPE: A 3D high-bandwidth dot-product engine for high-performance neuromorphic computing (2017)

We present and experimentally validate 3D-DPE, a general-purpose dot-product engine, which is ideal for accelerating artificial neural networks (ANNs). 3D-DPE is based on a monolithically integrated 3D CMOS-memristor hybrid circuit and performs a high-dimensional dot-product operation (a recurrent and computationally expensive operation in ANNs) within a single step, using analog current-based computing. 3D-DPE is made up of two subsystems, namely a CMOS subsystem serving as the memory controller and an analog memory subsystem consisting of multiple layers of high-density memristive crossbar arrays fabricated on top of the CMOS subsystem. Their integration is based on a high-density area-distributed interface, resulting in much higher connectivity between the two subsystems, compared to the traditional interface of a 2D system or a 3D system integrated using through silicon vias. As a result, 3D-DPE's single-step dot-product operation is not limited by the memory bandwidth, and the input dimension of the operations scales well with the capacity of the 3D memristive arrays. To demonstrate the feasibility of 3D-DPE, we designed and fabricated a CMOS memory controller and monolitically integrated 2 layers of titanium-oxide memristive crossbars. Then we performed the analog dot-product operation under different input conditions in two scenarios: (1) with devices within the same crossbar layer and (2) with devices from different layers. In both cases, the devices exhibited low voltage operation and analog switching behavior with high tuning accuracy.
The development of live attenuated cold-adapted influenza virus vaccine for humans (1999)

A procedure to attenuate live influenza virus of type A and type B was developed using adaptation of the virus to grow at 25°C (cold adaptation; ca). Through a series of stepwise passages, two stable mutants were obtained and designated as ‘Master’ strains, one for type A influenza virus (A/Ann Arbor/6/60-H2N2) and one for type B influenza virus (B/Ann Arbor/1/66). These mutants were used in genetic reassortment using either the classical method or more recently described reverse genetics to update the relevant surface antigens of the circulating strains of influenza virus. The derivation is based on the concept of 6/2 where 6 signifies the six internal genes of the master strain and 2 refers to the two genes coding for the two surface glycoproteins HA and NA of the circulating influenza virus. The advantages of this vaccine were demonstrated to be (1) proper level of attentuation, (2) non-transmissibility, (3) genetic stability, (4) presence of the ca and ts markers and (5) immunogenicity involving both local and the cell-mediated immune responses. The clinical trials in infants, children, adults and elderly have provided the necessary data for eventual licensing of this vaccine. The ease of administration (intranasal) safety and high efficacy make this vaccine suitable to prevent influenza virus infection in all age groups. Copyright © 1999 John Wiley & Sons, Ltd.
A Phenytoin Assay Using Dried Blood Spot Samples Suitable for Domiciliary Therapeutic Drug Monitoring (1984)

A commercially available substrate-labelled fluorescent immunoassay procedure has been modified to create a simple rapid method for the determination of capillary phenytoin concentration in dried filter paper blood spots of patients on phenytoin therapy. The specimens are collected and dispatched to the laboratory by the patient, thus domiciliary monitoring of phenytoin therapy can take place. The technique was validated by comparing the phenytoin results of simultaneously collected capillary dried blood spots and conventional plasma samples. The technique offers a convenient method for overcoming many of the practical problems of monitoring phenytoin therapy in epilepsy.
On the use of electrical precompensation of dispersion in optical single-sideband transmission systems (2006)

The use of electrical predistortion in optical single-sideband (OSSB) transmission systems is proposed to extend the tolerance to fiber dispersion impairment. Due to the spectral properties of OSSB signals, a simple electrical dispersive line can be used to mitigate the fiber dispersion, reducing the complexity of electrical predistortion methods proposed recently for optical modulations other than OSSB. Carrier-suppressed and carrier-unsuppressed optical modulations can be compensated by such technique, extending the range compared to previously reported works on fiber dispersion mitigation after direct detection using OSSB signals, where only carrier-unsuppressed modulations can be effectively compensated. The use of electrical precompensation is investigated for three signaling formats: Nonreturn to zero, return to zero, and alternate mark inversion (AMI). Due to distortion occurring in the sideband suppression process, signaling formats with reduced duty cycles present improved performance as a consequence of enhanced tolerance to intersymbol interference. Using such formats with electrical predistortion, the reach limitation arises not from fiber dispersion but from nonlinear impairments and optical noise accumulation. Using AMI and ideal electrical predistortion, distances greater than 1200 km of standard single mode fiber are achieved at 10 Gb/s with bit error ratio (BER) lower than 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">-12 </sup> , without using optical dispersion compensation. Introducing accurate models for the electrical dispersive lines, the transmission distance is reduced to 720 km for BER lower than 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">-12</sup>
Pre-emptive intrathecal administration of an NMDA receptor antagonist (AP-5) prevents hyper-reflexia in a model of persistent visceral pain (1994)

Dorsal horn sensitization following somatic noxious stimuli is partly mediated by the N-methyl-D-aspartate (NMDA) sub-type of glutamate receptor. This phenomenon has been comparatively sparsely investigated in the area of visceral pain. We have therefore investigated the role of spinal NMDA receptors in central sensitization in an animal model of persistent visceral pain. In anaesthetized rats the lumbosacral spinal cord was exposed by laminectomy and the pre-emptive effect of intrathecal AP-5 upon the hyper-reflexia associated with chemical inflammation of the bladder was investigated. The effect of intrathecal AP-5 (an NMDA receptor antagonist) upon the normal cystometrogram (CMG) was also measured. AP-5 (125-1000 micrograms) prevented the hyper-flexia associated with bladder inflammation in a dose-dependant fashion. In general, within the dose range 62.5-1000 micrograms, AP-5 had no significant effect upon the normal micturition reflex. However, at the top of this dose range a minor non-significant depression of this reflex was noted. NMDA receptors do not appear to mediate the micturition reflex at a spinal cord level. However, they are involved in the induction of hyper-reflexia following urinary bladder inflammation, this hyper-reflexia can be prevented by pre-emptive intrathecal administration of AP-5.
LOCUS a network transparent, high reliability distributed system (1981)

LOCUS is a distributed operating system that provides a very high degree of network transparency while at the same time supporting high performance and automatic replication of storage. By network transparency we mean that at the system call interface there is no need to mention anything network related. Knowledge of the network and code to interact with foreign sites is below this interface and is thus hidden from both users and programs under normal conditions. LOCUS is application code compatible with Unix 2 , and performance compares favorably with standard, single system Unix. LOCUS runs on a high bandwidth, low delay local network. It is designed to permit both a significant degree of local autonomy for each site in the network while still providing a network-wide, location independent name structure. Atomic file operations and extensive synchronization are supported. Small, slow sites without local mass store can coexist in the same network with much larger and more powerful machines without larger machines being slowed down through forced interaction with slower ones. Graceful operation during network topology changes is supported.
Influenza virus infection of desialylated cells (2000)

Sialic acid has long been considered to be the sole receptor for influenza virus. The viral hemagglutinin (HA) is known to bind cell surface sialic acid, and sialic acids on viral glyco-proteins are cleaved by the viral neuraminidase (NA) to promote efficient release of progeny virus particles. However, NWS-Mvi, a mutant virus completely lacking NA, grows well in MDCK cells continuously treated with exogenous neuraminidase (sialidase). Exogenous sialidase quantitatively releases all sialic acids from purified glycoproteins and glycolipids of MDCK cells and efficiently removes surface sialic acid from intact cells. Binding of NWS-Mvi and parent influenza viruses to MDCK cells is indistinguishable, and is only partially reduced by sialidase treatment of the cells. Both mutant and wild-type viruses enter enzymatically desialylated cells and initiate transcription. The ability of influenza A reassortant viruses to infect desialylated cells is shared by recent H3N2 clinical isolates, suggesting that this may be a general property of influenza A viruses. We propose that influenza virus infection can result from sialic acid-independent receptors, either directly or in a multistage process. When sialic acid is present, it may act to enhance virus binding to the cell surface to increase interaction with secondary receptors to mediate entry. Understanding virus entry will be critical to further efforts in infection control and prevention.
Human Articular Chondrocytes – Plasticity and Differentiation Potential (2006)

Articular cartilage has no or very low ability of self-repair, and untreated lesions may lead to the development of osteoarthritis. One method which has been proven to result in long-term repair of isolated lesions is autologous chondrocyte transplantation. In this method, culture-expanded chondrocytes isolated from full-thickness biopsies, taken from a non-weight-bearing area at the supromedial edge of the femoral condyle, are transplanted back to the patient under a cover of periosteum. The treatment is able to regenerate hyaline cartilage with long-term durability. Although the repair mechanism behind this treatment has not been fully elucidated, emerging data generated by microarray technologies reveal an interesting regeneration process involving cellular and molecular mechanisms found during fetal development. In hyaline cartilage, the human chondrocyte population is generally considered a homogenous cell population, but recently several investigators have demonstrated that cells isolated from human articular cartilage have stem cell properties and that the superficial layer contains such cells. This paper will discuss these recent data and their implications for future treatment strategies aiming to induce regeneration in articular cartilage surfaces.
Heat Shock Protein 96 Is Elevated in Rheumatoid Arthritis and Activates Macrophages Primarily via TLR2 Signaling (2009)

Macrophages are important mediators of chronic inflammation and are prominent in the synovial lining and sublining of patients with rheumatoid arthritis (RA). Recently, we demonstrated increased TLR2 and TLR4 expression and increased response to microbial TLR2 and TLR4 ligands in macrophages from the joints of RA. The current study characterized the expression of the 96-kDa heat shock glycoprotein (gp96) in the joints of RA and its role as an endogenous TLR ligand to promote innate immunity in RA. gp96 was increased in RA compared with osteoarthritis and arthritis-free control synovial tissues. The expression of gp96 strongly correlated with inflammation and synovial lining thickness. gp96 was increased in synovial fluid from the joints of RA compared with disease controls. Recombinant gp96 was a potent activator of macrophages and the activation was mediated primarily through TLR2 signaling. The cellular response to gp96 was significantly stronger with RA synovial macrophages compared with peripheral blood monocytes from RA or healthy controls. The transcription of TLR2, TNF-alpha, and IL-8, but not TLR4, was significantly induced by gp96, and the induction was significantly greater in purified RA synovial macrophages. The expression of TLR2, but not TLR4, on synovial fluid macrophages strongly correlated with the level of gp96 in the synovial fluid. The present study documents the potential role of gp96 as an endogenous TLR2 ligand in RA and provides insight into the mechanism by which gp96 promotes the chronic inflammation of RA, identifying gp96 as a potential new therapeutic target.
Monoclonal antibody to human endothelial cell surface internalization and liposome delivery in cell culture (1988)

A monoclonal antibody (mAb), E25, is described that binds to the surface of cultured human endothelial cells. Upon binding E25 is rapidly internalized and digested intracellularly. Selective liposome targeting to the surface of the cells is performed using a biotinylated E25 antibody and an avidin-biotin system. Up to 30% of the cell-adherent liposomal lipid is internalized.
A study on direct antitumor activity of bropirimine (oral interferon inducer) for renal cell carcinoma. (1994)

Aryl pyrimidinones, including bropirimine, exert anti-tumor activity through the induction of interferon (IFN)-alpha. Herein, the direct anti-tumor effect of bropirimine on 17 renal cell carcinoma (RCC) surgically obtained was examined using an organ culture system closely resembling the in vivo state, and also using the heterotransplanted nude mouse system. The findings obtained using the organ culture system showed that bropirimine inhibited 3H-thymidine uptake significantly in 15 of the 17 RCC (88.2%) compared with the control. Furthermore, the 3H-thymidine uptake was dose-dependently inhibited in 3 of the 17 tumors (17.6%). The oral administration of bropirimine against RCC heterotransplanted in nude mice (JRC 901: an erythropoietin-producing strain) tended to inhibit tumor growth dose-dependently, but not significantly (mean tumor weight ratio: T/C ratio: over 43%, degeneration degree of tumor: incomplete). However, the production of erythropoietin from the JRC 901 was significantly inhibited. These findings suggest that bropirimine has a direct anti-tumor activity, without the mediation of IFN-alpha induction, against human renal cell carcinoma.
Stereocontrolled Solid-Phase Synthesis of Phosphorothioate Oligoribonucleotides Using 2′-O-(2-Cyanoethoxymethyl)-nucleoside 3′-O-Oxazaphospholidine Monomers (2012)

A method for the synthesis of P-stereodefined phosphorothioate oligoribonucleotides (PS-ORNs) was developed. PS-ORNs of mixed sequence (up to 12mers) were successfully synthesized by this method with sufficient coupling efficiency (94-99%) and diastereoselectivity (≥98:2). The coupling efficiency was greatly improved by the use of 2-cyanoethoxymethyl (CEM) groups in place of the conventional TBS groups for the 2'-O-protection of nucleoside 3'-O-oxazaphospholidine monomers. The resultant diastereopure PS-ORNs allowed us to clearly demonstrate that an ORN containing an all-(Rp)-PS-backbone stabilizes its duplex with the complementary ORN, whereas its all-(Sp)-counterpart has a destabilizing effect.
Molecular recognition of B-DNA by Hoechst 33258 (1985)

The binding sites of Hoechst 33258, netropsin and distamycin on three DNA restriction fragments from plasmid pBR322 were compared by footprinting with methidiumpropyl-EDTA X Fe(II) [MPE X Fe(II)]. Hoechst, netropsin and distamycin share common binding sites that are five +/- one bp in size and rich in A X T DNA base pairs. The five base pair protection patterns for Hoechst may result from a central three base pair recognition site bound by two bisbenzimidazole NHs forming a bridge on the floor of the minor groove between adjacent adenine N3 and thymine O2 atoms on opposite helix strands. Hydrophobic interaction of the flanking phenol and N-methylpiperazine rings would afford a steric blockade of one additional base pair on each side.
Digital video libraries and the Internet (1999)

Digital video libraries are positioned to be a major driving application for the Next Generation Internet Initiative. Likewise, the advancements in the communications infrastructure will be of great benefit to digital video libraries. This report investigates some of the recent technologies for handling video in digital video libraries and reviews the NGII's planned advancements in network communications technologies in order to examine their impact on deploying digital video libraries on the Internet.
HLA class I antigen and transporter associated with antigen processing downregulation in metastatic lesions of head and neck squamous cell carcinoma as a marker of poor prognosis (2010)

HLA class I antigen processing machinery plays a crucial role in the generation of peptides from endogeneously synthesized proteins and in their presentation to cytotoxic T lymphocytes. The purpose of this study was to analyze the downregulation of HLA class I antigen, transporter associated with antigen processing (TAP) and tapasin in primary and metastatic lesions of head and neck squamous cell carcinoma (HNSCC) and to compare TAP, tapasin and HLA class I antigen downregulation in metastatic lesions with that of primary lesions. We analyzed expression levels of TAP1, TAP2, tapasin and HLA class I antigen in 25 primary and autologous metastatic lesions by staining formalin-fixed, paraffin-embedded tissue sections in the immunoperoxidase reaction. We identified the expression levels of TAP1, TAP2, tapasin and HLA class I antigen were coordinately downregulated in both primary and metastatic lesions and were significantly lower in metastatic lesions than in autologous primary lesions tested. HLA class I antigen downregulation in metastatic lesion was significantly associated with reduced disease-free survival of patients (P<0.05). Multivariate Cox proportional hazards model analysis identified negativity of HLA class I antigen as an independent prognostic marker. HLA class I antigen and TAP are likely to be downregulated in metastatic lesions compared with primary lesions in HNSCC. The higher frequency of HLA class I antigen and TAP down-regulation in metastases play a role in the clinical course of the disease.
Some Recent Developments in RAFT Polymerization (2012)

This paper reviews some recent developments in RAFT Polymerization at CSIRO. We report the successful use of switchable RAFT agents for controlling the polymerization of N,N-dimethylacrylamide in aqueous media and the dependence of RAFT agent activity on acid type and acid strength. For best results a stoichiometric amount of a strong acid should be used. We describe new RAFT agents (N-aryl-N-(4-pyridinyl) dithiocarbamates, aryl trithiocarbonates). We assess the for scope for RAFT single unit monomer insertion and describe its application in the synthesis of block copolymers containing organic semiconductor segments. Finally we briefly summarize methods of transforming RAFT synthesized polymers and disclose a potential click process based on successive 1,3-doplar addition steps for quantitatively transforming RAFT end groups.
Four out of eight genes in a mouse chromosome 7 congenic donor region are candidate obesity genes (2011)

We previously identified a region of mouse chromosome 7 that influences body fat mass in F2 littermates of congenic × background intercrosses. Current analyses revealed that alleles in the donor region of the subcongenic B6.C-D7Mit318 (318) promoted a twofold increase in adiposity in homozygous lines of 318 compared with background C57BL/6ByJ (B6By) mice. Parent-of-origin effects were discounted through cross-fostering studies and an F1 reciprocal cross. Mapping of the donor region revealed that it has a maximal size of 2.8 Mb (minimum 1.8 Mb) and contains a maximum of eight protein coding genes. Quantitative PCR in whole brain, liver, and gonadal white adipose tissue (GWAT) revealed differential expression between genotypes for three genes in females and two genes in males. Alpha-2,8-sialyltransferase 8B (St8sia2) showed reduced 318 mRNA levels in brain for females and males and in GWAT for females only. Both sexes of 318 mice had reduced Repulsive guidance molecule-a (Rgma) expression in GWAT. In brain, Family with sequence similarity 174 member b (Fam174b) had increased expression in 318 females, whereas Chromodomain helicase DNA binding protein 2 (Chd2-2) had reduced expression in 318 males. No donor region genes were differentially expressed in liver. Sequence analysis of coding exons for all genes in the 318 donor region revealed only one single nucleotide polymorphism that produced a nonsynonymous missense mutation, Gln7Pro, in Fam174b. Our findings highlight the difficulty of using expression and sequence to identify quantitative trait genes underlying obesity even in small genomic regions.
High Birefringence Phenylacetylene Liquid Crystals with Low Viscosity (2001)

Abstract We have synthesized new high Δ n 3-ring phenylacetylene(3PA) liquid crystals which have substituent groups with core center phenyl ring and investigated the effects of substitution on physical properties. Nematic range and viscosity were improved remarkably with keeping high Δ n by introducing trifluoromrthoxy group. The Δ n of 3PAs were also descussed with relationship of polarizability and order parameter.