gebhart/patrepeval huggingface dataset:
Superparamagnetic iron oxide: pharmacokinetics and toxicity (1989)

The pharmacokinetics (distribution, metabolism, bioavailability, excretion) and toxicity (acute and subacute toxicity, mutagenicity) of a superparamagnetic iron oxide preparation (AMI-25), currently used in clinical trials, were evaluated by 59Fe radiotracer studies, measurements of relaxation times, the ability to reverse iron deficiency anemia, histologic examination, and laboratory parameters. One hour after administration of AMI-25 to rats (18 mumol Fe/kg; 1 mg Fe/kg), 82.6 +/- 0.3% of the administered dose was sequestered in the liver and 6.2 +/- 7.6% in the spleen. Peak concentrations of 59Fe were found in liver after 2 hr and in the spleen after 4 hr. 59Fe slowly cleared from liver (half-life, 3 days) and spleen (half-life, 4 days) and was incorporated into hemoglobin of erythrocytes in a time-dependent fashion. The half-time of the T2 effect on liver and spleen (24-48 hr) was shorter than the 59Fe clearance, indicating metabolism of AMI-25 into other forms of iron. IV administration of AMI-25 (30 mg Fe/kg) corrected iron-deficiency anemia and showed bioavailability similar to that of commercially available IV iron preparations within 7 days. No acute or subacute toxic effects were detected by histologic or serologic studies in rats or beagle dogs who received a total of 3000 mumol Fe/kg, 150 times the dose proposed for MR imaging of the liver. Our results indicate that AMI-25 is a fully biocompatible potential contrast agent for MR.
Peripheral neural serotonin receptors: identification and characterization with specific antagonists and agonists. (1986)

Serotonin (5-hydroxytryptamine, 5-HT) has been shown to be a neurotransmitter in the enteric nervous system (ENS). Although 5-HT is a mediator of slow excitatory postsynaptic potentials evoked by stimulation of interganglionic connectives, the precise role it plays in the physiology of the gut is unclear. Research has been hampered by an inadequate knowledge of the types of 5-HT receptor in the ENS and thus the lack of well-characterized antagonists. We now report the identification of two classes of enteric neural 5-HT receptor, the effects of activating these receptors on myenteric type II/AH neurons, and their characterization with specific agonists and antagonists. One class, which we propose to call 5-HT1P, is characterized by a high affinity for [3H]5-HT in radioligand binding assays. This class of receptor mediates a slow depolarization of myenteric type II/AH neurons associated with an increase in input resistance. Agonists at this receptor include, in addition to 5-HT (in order of potency), 5- and 6-hydroxyindalpine and 2-methyl-5-HT. 5-HT1P-mediated responses are specifically antagonized by 5-hydroxytryptophyl-5-hydroxytryptophan amide. The other class of 5-HT receptor, which we propose to call 5-HT2P, appears not to have a high affinity for [3H]5-HT. This receptor mediates a brief depolarization of myenteric II/AH neurons associated with a fall in input resistance. 2-Methyl-5-HT, at low concentrations, is a specific agonist at this receptor and ICS 205-930 is a specific antagonist. Binding of [3H]5-HT to enteric membranes is inhibited by 5-HT1P receptor agonists and antagonists but not by the 5-HT2P receptor antagonist ICS 205-930 or by MDL 72222, another compound reported to be an antagonist of 5-HT at peripheral receptors.
Drug Delivery of Antisense Molecules to the Brain for Treatment of Alzheimer’s Disease and Cerebral AIDS (1998)

Antisense oligonucleotides (ODNs) and peptide nucleic acids (PNAs) are potential therapeutics for eradication of malignancies, viral infections, and other pathologies. However, ODNs and PNAs in general are unable to cross cellular membranes and blood-tissue barriers, such as the blood-brain barrier (BBB), which is only permeable to lipophilic molecules of molecular weight <600 Da. Cellular delivery systems based on conjugates of streptavidin (SA) and the OX26 monoclonal antibody directed to the transferrin receptor may be employed as a universal carrier for the transport of mono-biotinylated peptides, ODNs, or PNAs. 3'-Biotinylation of phosphodiester (PO)-ODN produces complete protection of ODN against serum and cellular 3'-exonucleases, facilitating the conjugation to avidin-based delivery systems and maintaining the activation of RNase H. These delivery systems markedly increased the cellular uptake and antisense efficacy of 3'-biotinylated ODNs in models of Alzheimer's disease and HIV-AIDS. In vivo brain delivery studies demonstrated that 3'-protected PO-ODNs and PO-phosphorothioate(PS)-ODN hybrids containing a single PO linkage are subjected to endonuclease degradation in vivo. On the contrary PS-ODNs, which were also protected at 3'-terminus by biotinylation, are metabolically stable in vivo and resistant to exo/endonuclease degradation. However, because of the strong binding of these oligomers to plasma protein, PS-ODNs are poorly transported into the brain through the BBB by the OX26-SA delivery vector following intravenous administration. PNAs are also resistant to exo/endonuclease and protease degradation, and these molecules biotinylated at the amino terminal group were transported into the brain by the OX26-SA delivery system with brain uptake levels comparable to that of morphine. Using the rev gene of HIV as a model target, RNase protection assays and cell-free translation arrest showed that the PNA-OX26-SA conjugate maintained active recognition and inactivation of target mRNA, respectively. The overall experimental evidence suggests that PNA-OX26-SA conjugates represent optimal antisense molecules for drug delivery to the brain.
Tofacitinib, an Oral Janus Kinase Inhibitor, in Active Ulcerative Colitis (2012)

Patients with moderately to severely active ulcerative colitis treated with tofacitinib were more likely to have clinical response and remission than those receiving placebo. (Funded by Pfizer; ClinicalTrials.gov number, NCT00787202.).
Temporal Trends in Coronary Heart Disease Mortality and Sudden Cardiac Death From 1950 to 1999 (2004)

The risks of SCD and nonsudden CHD mortality have decreased by 49% to 64% over the past 50 years. These trends were evident in subjects with and without heart disease, which suggests important contributions of primary and secondary prevention to the decreasing risk of CHD death and SCD.
Four New Metabolites of Aspergillus terreus. (1994)

Four new metabolites (1-4) were isolated from mycelium of Aspergillus terreus IFO 6123 producing asterriquinone (ARQ). The structures of 1 and 2 were shown to be 3,6-bis[1-(1,1-dimethyl-2-propenyl)-1H-indol-3-yl]-furo[3,2-b]furan- 2,5-dione (asterridinone) and 2,5-bis[1-(1,1-dimethyl-2-propenyl)-1H-indol-3- yl]-3-acetoxy-6-hydroxy-2,5-cyclohexadiene-1,4-dione (ARQ monoacetate), respectively, by the chemical and spectral data. Compounds 3 and 4 were identified with known asterriquinone isomers, 2-[1-(1,1-dimethyl-2-propenyl)-1H-indol-3-yl]-5-[2-(3-methyl-2-butenyl)- 1H-indol-3-yl]-3,6-dihydroxy-2,5-cyclohexadiene-1,4-dione (isoARQ) and 2,5-bis[2-(3-methyl-2-butenyl)-1H-indol-3-yl]-3,6-dihydroxy- 2,5-cyclohexadiene-1,4-dione (neoARQ), respectively.
Adversarial Examples in the Physical World (2018)

Most existing machine learning classifiers are highly vulnerable to adversarial examples. An adversarial example is a sample of input data which has been modified very slightly in a way that is intended to cause a machine learning classifier to misclassify it. In many cases, these modifications can be so subtle that a human observer does not even notice the modification at all, yet the classifier still makes a mistake. Adversarial examples pose security concerns because they could be used to perform an attack on machine learning systems, even if the adversary has no access to the underlying model. Up to now, all previous work has assumed a threat model in which the adversary can feed data directly into the machine learning classifier. This is not always the case for systems operating in the physical world, for example those which are using signals from cameras and other sensors as input. This paper shows that even in such physical world scenarios, machine learning systems are vulnerable to adversarial examples. We demonstrate this by feeding adversarial images obtained from a cell-phone camera to an ImageNet Inception classifier and measuring the classification accuracy of the system. We find that a large fraction of adversarial examples are classified incorrectly even when perceived through the camera.
Complexation-mediated solubilization and processing of rigid-chain and ladder polymers in aprotic organic solvents (1990)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTComplexation-mediated solubilization and processing of rigid-chain and ladder polymers in aprotic organic solventsSamson A. Jenekhe and Paul O. JohnsonCite this: Macromolecules 1990, 23, 20, 4419–4429Publication Date (Print):October 1, 1990Publication History Published online1 May 2002Published inissue 1 October 1990https://pubs.acs.org/doi/10.1021/ma00222a015https://doi.org/10.1021/ma00222a015research-articleACS PublicationsRequest reuse permissionsArticle Views1276Altmetric-Citations141LEARN 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
Detector blinding attacks on counterfactual quantum key distribution (2020)

Counterfactual quantum key distribution protocols allow two sides to establish a common secret key using an insecure channel and authenticated public communication. As opposed to many other quantum key distribution protocols, part of the quantum state used to establish each bit never leaves the transmitting side, which hinders some attacks. We show how to adapt detector blinding attacks to this setting. In blinding attacks, gated avalanche photodiode detectors are disabled or forced to activate using bright light pulses. We present two attacks that use this ability to compromise the security of counterfactual quantum key distribution. The first is a general attack but technologically demanding (the attacker must be able to reduce the channel loss by half). The second attack could be deployed with easily accessible technology and works for implementations where single photon sources are approximated by attenuated coherent states. The attack is a combination of a photon number splitting attack and the first blinding attack which could be deployed with easily accessible technology. The proposed attacks show counterfactual quantum key distribution is vulnerable to detector blinding and that experimental implementations should include explicit countermeasures against it.
DNA-binding and trans-activation properties of Drosophila E2F and DP proteins. (1994)

The temporal activation of E2F transcriptional activity appears to be an important component of the mechanisms that prepare mammalian cells for DNA replication. Regulation of E2F activity appears to be a highly complex process, and the dissection of the E2F pathway will be greatly facilitated by the ability to use genetic approaches. We report the isolation of two Drosophila genes that can stimulate E2F-dependent transcription in Drosophila cells. One of these genes, dE2F, contains three domains that are highly conserved in the human homologs E2F-1, E2F-2, and E2F-3. Interestingly, one of these domains is highly homologous to the retinoblastoma protein (RB)-binding sequences of human E2F genes. The other gene, dDP, is closely related to the human DP-1 and DP-2 genes. We demonstrate that dDP and dE2F interact and cooperate to give sequence-specific DNA binding and optimal trans-activation. These features suggest that endogenous Drosophila E2F, like human E2F, may be composed of heterodimers and may be regulated by RB-like proteins. The isolation of these genes will provide important reagents for the genetic analysis of the E2F pathway.
Human esophageal carcinomas frequently express the tumor‐rejection antigens of MAGE genes (1995)

The human genes MAGE-1 and -3 encode melanoma peptide antigens that are recognized by autologous cytotoxic T lymphocytes. Tumors expressing MAGE genes are potential targets for cancer immunotherapy, because MAGE genes are expressed only in tumor tissue and not in any normal tissue except testis and placenta. However, little is known about MAGE gene expression in human esophageal carcinoma. The purpose of this study was therefore to analyze MAGE gene status in human esophageal carcinoma. We studied the expression status of these genes in 42 surgical samples and in 12 cell lines of human esophageal carcinoma using the reverse transcription polymerase chain reaction (RT-PCR). Various clinicopathological factors were also analyzed. No MAGE gene expression was seen in any of the 42 normal esophageal tissue specimens. In contrast, tumor tissue expressed MAGE-1, -2, and -3 in 26, 18 and 24 specimens, respectively. Thirty-three of 42 tumors expressed at least one MAGE gene. Significant clinicopathologic differences between the tumors were not observed, regardless of the presence or absence of MAGE gene expression. In cell lines, MAGE-1, -2, and -3 gene expression was recognized in 5, 4 and 4 cell lines, respectively. This study demonstrates that MAGE genes are frequently expressed in clinical samples as well as in cell lines of esophageal carcinoma. The identification of MAGE genes, therefore, may open up a new modality of treatment, namely specific immunotherapy, for patients with esophageal carcinoma.
Detection and analysis by dual‐laser flow cytometry of bacteriophage T4 DNA inside Escherichia coli (1991)

Bacteriophage T4 DNA was detected and analyzed inside E. coli by dual-laser flow cytometry using a dye combination of Hoechst 33258 (H33258) and chromomycin A3 (CA3) which bind to A-T- and G-C-rich regions of DNA, respectively. An exponentially-growing culture of E. coli ATCC 11303 was infected with T4 bacteriophage at a 1:1 multiplicity of infection. Samples were taken immediately and at 5 min intervals and placed on ice to interrupt viral replication. The samples were then centrifuged, ethanol-fixed, stained with H33258 and CA3, and analyzed by flow cytometry. Twenty-five minutes post-infection, a population of cells which contained T4 DNA began to appear on both a bivariate contour plot and a frequency histogram plot of the data. By 35 min, T4 DNA-containing cells could be distinguished from E. coli cells containing little or no T4 DNA. The ratio of CA3:H33258 fluorescence was then used to calculate the % G + C value for T4 DNA inside E. coli. A value of 35.6 +/- 0.2% was obtained, which agrees with % G + C values determined by traditional methods. These results demonstrate that dual-laser flow cytometry can be used to study viral DNA inside the bacterial host.
Trends and insight in heavy-duty vehicle electrification (2010)

This paper describes the results from Annex XII “Heavy-duty hybrid vehicles” of the International Energy Agency (IEA) Implementing Agreement on “Hybrid and Electric Vehicles” (IA-HEV). Since 1993, this Implementing Agreement has provided a platform to exchange knowledge, experience and strategies among the member states on the latest developments in hybrid and electric vehicles, mostly passenger cars. Because heavy-duty vehicles have specific technical requirements and economic boundary conditions compared to the passenger car market, a dedicated Annex was started in 2007 and has run for several years until the end of 2010. Six countries (Belgium, Canada, Finland, Switzerland, the Netherlands and the United States) have been participating to collect and share relevant information on the latest technical and market developments in “electrified” trucks, buses and mobile work machines. This information will broaden the insight in the existing applications of heavy-duty vehicles electrification and can provide essential information for future heavy-duty hybrid vehicle deployment projects.
PLU‐1 nuclear protein, which is upregulated in breast cancer, shows restricted expression in normal human adult tissues: A new cancer/testis antigen? (2002)

The PLU-1 gene is expressed at the level of message in breast cancers and breast cancer cell lines and shows restricted expression in normal adult tissues with the exception of testis. The predicted protein sequence contains several domains, including the PLU domain, which is shared by other proteins involved in transcription and/or development. We have developed a polyclonal antiserum to a C-terminal fragment of the PLU-1 protein, which shows little homology to other family members. Immunohistochemical analysis with the antiserum alpha-PLU-1C confirmed the nuclear localisation of PLU-1. alpha-PLU-1C also reacted with the mouse homologue of PLU-1 (mPlu-1) but not with the closest family member, RBP2. Using Western blot analysis, PLU-1 was shown to be well expressed in breast cancers and breast cancer cell lines, while it was not detected in a range of normal adult tissues. Our results suggest that the PLU-1 protein may belong to the class of testis/cancer antigens.
KATP channels and insulin secretion disorders (2002)

ATP-sensitive potassium (K(ATP)) channels are inhibited by intracellular ATP and activated by ADP. Nutrient oxidation in beta-cells leads to a rise in [ATP]-to-[ADP] ratios, which in turn leads to reduced K(ATP) channel activity, depolarization, voltage-dependent Ca(2+) channel activation, Ca(2+) entry, and exocytosis. Persistent hyperinsulinemic hypoglycemia of infancy (HI) is a genetic disorder characterized by dysregulated insulin secretion and, although rare, causes severe mental retardation and epilepsy if left untreated. The last five or six years have seen rapid advance in understanding the molecular basis of K(ATP) channel activity and the molecular genetics of HI. In the majority of cases for which a genotype has been uncovered, causal HI mutations are found in one or the other of the two genes, SUR1 and Kir6.2, that encode the K(ATP) channel. This article will review studies that have defined the link between channel activity and defective insulin release and will consider implications for future understanding of the mechanisms of control of insulin secretion in normal and diseased states.
Open Tubular Capillary LC (1980)

Journal Article Open Tubular Capillary LC Get access Daido Ishii, Daido Ishii Department of Applied Chemistry, Faculty of Engineering, Nagoya University, Chikusa-ku, Nagoya-shi, 464, Japan Search for other works by this author on: Oxford Academic PubMed Google Scholar Toyohide Takeuchi Toyohide Takeuchi Department of Applied Chemistry, Faculty of Engineering, Nagoya University, Chikusa-ku, Nagoya-shi, 464, Japan Search for other works by this author on: Oxford Academic PubMed Google Scholar Journal of Chromatographic Science, Volume 18, Issue 9, September 1980, Pages 462–472, https://doi.org/10.1093/chromsci/18.9.462 Published: 01 September 1980
Preparation and Spectroscopic Studies of Cobalt(II)-Stellacyanin (1974)

The cobalt(II) derivative of the "blue" copper protein stellacyanin has been prepared, and its visible-ultraviolet spectrum is reported. Tryptophan fluorescence quenching and p-mercuribenzoate titration results strongly suggest that Co(II) and Cu(II) compete for the same stellacyanin binding site and that a cysteine sulfur atom is coordinated in both cases. This interpretation is supported by the finding of an intense band at 355 nm in Co(II)-stellacyanin attributable to a charge transfer transition of the RS(-) --> Co(II) type. The visible absorption spectrum of Co(II)-stellacyanin exhibits band maxima at 540, 625, and 655 nm. These bands are attributable to d-d transitions originating in a high-spin Co(II) center. It is suggested that a correspondence exists between charge transfer bands observed at 355 and 300 nm in the Co(II) derivative to those found at 604 and 450 nm in the native protein. It is concluded that the intense 604-nm peak in Cu(II)-stellacyanin is attributable to a cys-S --> Cu(II) charge transfer transition.
Changes in stress and coercivity after annealing of amorphous Co(Zr, Nb) thin films deposited by RF sputtering (1988)

The variations of the coercivity and the stress of low-magnetostriction Co(Zr, Nb) thin films are investigated, for various values of the sputtering gas pressure, P/sub Ar/, before and after annealing at 300 degrees C. The origin of the stresses and their implications for the coercivity and the anisotropy are discussed on the basis of inert gas incorporation, morphological features, and relaxation effects.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Future potential and status of selective sodium channel blockers for the treatment of pain. (2009)

Voltage-gated sodium (NaV1) channels in the peripheral nervous system and CNS play a critical role in pain signaling. Nociceptive neurons express several NaV1 channel subtypes that may contribute to the hyperexcitability characteristic of chronic pain states. The non-subtype selective, state-dependent NaV1 channel blockers lidocaine and carbamazepine are efficacious in the treatment of neuropathic pain; however, the target-driven development of novel sodium channel blocking analgesics has been generally unsuccessful. Recent human genetic data indicate an important role for the NaV1.7 channel subtype in pain signaling, and significant preclinical data identifies the NaV1.8 channel as a promising analgesic target, suggesting that the selective blockade of these subtypes may improve on the therapeutic index of sodium channel modulators. However, few subtype-selective small-molecule sodium channel blockers have been described. This review provides an overview of the NaV1 channel subtypes that are preferentially expressed in nociceptive neurons, the assay technologies used to develop NaV1 channel blockers, and a summary of recent advances in the development of subtype-selective and novel state-dependent NaV1 channel blockers.