gebhart/patrepeval huggingface dataset:
Synthesis and Anti‐Tumor Activities of a Novel Series of Tricyclic 1‐Anilino‐5H‐pyridazino[4,5‐b]indoles (2007)

A novel series of 1-anilino-5H-pyridazino[4,5-b]indoles was designed and synthesized in order to find novel potent anti-tumor compounds. Their structures were confirmed by MS, (1)H-NMR, and elemental analysis. All compounds were screened for their cytotoxic activity against two human cancer cell lines (Bel-7420, HT-1080). The compounds 8, 9, and 17 showed 50% growth inhibitory activity in low micromolar concentration (IC(50 )= 7.7 approximately 12.8 microM). Among them, compound 17 displayed the most potent anti-tumor activity with IC(50) values of 8.2 microM and 7.9 microM against Bel-7402 and HT-1080, respectively.
Increased density of ecto 5' nucleotidase antigen on leukemic T cells from patients with cutaneous T-cell lymphoma and adult T-cell leukemia/lymphoma (1989)

Malignant CD4+ T cells in adult T-cell leukemia/lymphoma (ATL) and cutaneous T-cell lymphoma (CTCL) express a number of cell surface molecules that are upregulated on normal T cells activated by foreign antigen. In this report we describe an interesting exception to the parallel phenotypic features of activated T cells and malignant CD4+ T cells. A monoclonal antibody (MoAb; termed 27.2) that was raised to HTLV-1+, CD4+25+ leukemic T cells stained weakly 25% of peripheral T cells, including approximately 50% of CD8+ T cells and 20% of CD4+ T cells. Flow cytometry analysis indicated that the surface density of the 27.2 antigen was unchanged or diminished when normal T cells were activated by antigen. However, 3/4 Sezary cases and 4/8 cases of ATL had relatively high densities of the 27.2 antigen. Immunoprecipitation and sodium dodecylsulfate polyacrylamide gel electrophoresis of the NP- 40-solubilized membranes of surface-iodinated ATL cells indicated that MoAb 27.2 reacted with a 75 Kd molecule. The size and distribution of the 27.2 antigen on T cell subsets suggested that it might be the enzyme ecto-5′ nucleotidase (NT), a phosphatidylinositol-linked enzyme that catalyzes dephosphorylation of monophosphate nucleotides to their respective nucleosides. This was confirmed by demonstrating that lymphocyte ecto-5′NT activity was blocked partially and inhibited completely by preincubating cells with MoAb 27.2 for 1 hour at 4 degrees C and 24 hours at 37 degrees C, respectively. When used with a second MoAb (27.1) to a novel T cell activation antigen found on all CTCL and ATL leukemias examined, 27.2 was found to discriminate between normal and leukemic T cells in two patients with ATL. These studies suggest that ecto-5′NT has diagnostic value in T cell malignancies and may be aberrantly expressed in some cases of ATL and CTCL.
Precise Spatial and Temporal Control of Oxygen within In Vitro Brain Slices via Microfluidic Gas Channels (2012)

The acute brain slice preparation is an excellent model for studying the details of how neurons and neuronal tissue respond to a variety of different physiological conditions. But open slice chambers ideal for electrophysiological and imaging access have not allowed the precise spatiotemporal control of oxygen in a way that might realistically model stroke conditions. To address this problem, we have developed a microfluidic add-on to a commercially available perfusion chamber that diffuses oxygen throughout a thin membrane and directly to the brain slice. A microchannel enables rapid and efficient control of oxygen and can be modified to allow different regions of the slice to experience different oxygen conditions. Using this novel device, we show that we can obtain a stable and homogeneous oxygen environment throughout the brain slice and rapidly alter the oxygen tension in a hippocampal slice. We also show that we can impose different oxygen tensions on different regions of the slice preparation and measure two independent responses, which is not easily obtainable with current techniques.
Expression of immune inhibitory receptor ILT3 in acute myeloid leukemia with monocytic differentiation (2012)

ILT3 is a highly sensitive and specific marker which distinguishes AML with monocytic differentiation from other types of AML. Testing of ILT3 expression should be incorporated into the initial diagnostic work-up and monitoring of patients with AML.
Nucleotide sequence of the gelatinase gene (gelE) from Enterococcus faecalis subsp. liquefaciens (1991)

The gene coding for gelatinase (also called metalloendopeptidase II; microbial proteinase, EC 3.4.24.4) of Enterococcus faecalis subsp. liquefaciens strain OG1-10 was cloned in an Escherichia coli-Enterococcus shuttle vector, and its nucleotide sequence was determined. The DNA sequence encodes one large open reading frame (ORF) with 509 amino acid residues. The ORF contains a signal sequence in its N-terminal region, whereas the N-terminal amino acid sequence determined from the purified extracellular proteinase starts at residue 192 deduced from the ORF. This implies that the gelatinase is synthesized as a prepropolypeptide or prezymogen. The mature gelatinase contains 318 amino acid residues (molecular weight, 34,582) and has significant homology with neutral proteinases from Bacillus species and elastase from Pseudomonas aeruginosa.
[Uterine cervix dysplasias. New therapeutic strategy based on virological data]. (1986)

There is no consistency in the treatment of dysplasias of the cervix of the uterus. It varies from team to team and there is no criterion that points with any certainty to how the lesion will develop--whether it will become worse, whether it will persist as it is or whether it will regress. For the first time there is an objective factor, namely typing of the papillomavirus by molecular hybridisation. The presence of HPV 16, 18 or 33 is prognostically bad. Active treatment should be instituted. In the other cases "armed surveillance" or destroying the lesions is sufficient. This is particularly important in young women who wish to have a family.
From HER2 to Herceptin (2001)

SUMMARYHER2 overexpression occurs in 25% of breast cancers and seems to correlate with poor prognosis. HER2 overexpression may predict tamoxifen failure and different response rates to chemotherapeutic agents such as the taxanes and anthracyclines. The detection of HER2 and its overexpression is performed using fluorescent in situ hybridisation (FISH) and/or immunohistochemistry (IHC).Trastuzumab [Herceptin (H)] is a humanised IgG monoclonal antibody specific for the growth factor receptor HER2. Pre-clinical trials using monoclonal antibodies have shown inhibition of breast tumour growth in athymic nude mice. Phase II and III clinical trials have evaluated the efficacy and safety of Herceptin in women with metastatic breast cancer in combination with other agents and as a single agent. Currently, Trastuzumab and paclitaxel is the only combination indicated for the treatment of patients with metastatic breast cancer whose tumours overexpress HER2. It is also indicated as a single agent in women with HER2-overexpressing metastatic breast cancer that has progressed after previous chemotherapy. Herceptin is a well-tolerated drug and the side-effects that are commonly seen with chemotherapy, such as neutropenia, alopecia and mucositis, are rarely observed.The main risk factors for cardiotoxicity are concurrent or previous anthracycline exposure The potential role of Herceptin in the adjuvant setting is currently being evaluated.
Wetting by Liquid Metals—Application in Materials Processing: The Contribution of the Grenoble Group (2015)

The wettability of ceramics by liquid metals is discussed from both the fundamental point of view and the point of view of applications. The role of interfacial reactions (simple dissolution of the solid in the liquid or formation of a layer of a new compound) is illustrated and analysed. Several results are presented in order to illustrate the role of wettability in materials processing, namely infiltration processing, joining dissimilar materials by brazing and selecting crucibles for crystallising liquid metals and semiconductors. The review includes results obtained during the last 15 years mainly, but not only, by the Grenoble group.
Lifetime correction of genetic deficiency in mice with a single injection of helper-dependent adenoviral vector (2001)

Ideally, somatic gene therapy should result in lifetime reversal of genetic deficiencies. However, to date, phenotypic correction of monogenic hyperlipidemia in mouse models by in vivo gene therapy has been short-lived and associated with substantial toxicity. We have developed a helper-dependent adenoviral vector (HD-Ad) containing the apolipoprotein (apo) E gene. A single i.v. injection of this vector completely and stably corrected the hypercholesterolemia in apoE-deficient mice, an effect that lasted the natural lifespan of the mice. At 2.5 years, control aorta was covered 100% by atherosclerotic lesion, whereas aorta of treated mice was essentially lesion-free. There was negligible toxicity associated with the treatment. We also developed a method for repeated HD-Ad vector administration that could be applied to organisms, e.g., humans, with life spans longer than 2-3 years. These studies indicate that HD-Ad is a promising system for liver-directed gene therapy of metabolic diseases.
Three-dimensional television system based on integral photography (2012)

A three-dimensional (3-D) television system based on integral photography, which is a spatial imaging method, is described. In our experimental setup, a video system has a resolution equivalent to 8000 scan lines and a lens array is configured with 400 lenses in the horizontal direction and 250 lenses in the vertical direction. It was confirmed that the 3D image reconstructed with the experimental setup changed smoothly in accordance with the position of the observer within a viewing area.
T cell responses to bacterial infection (1999)

Many exciting advances in our understanding of T cell mediated immunity to bacterial infection have occurred in the past several years. T cell responses have been more fully characterized, due in part to the development of MHC class I tetramers. The importance of cytokines and various effector molecules in defense against infection has come to light. Finally, intracellular bacteria are being exploited to deliver antigens and DNA in an effort to induce immunity to pathogens.
Changes in Human Cerebral Blood Flow and Cerebral Blood Volume during Hypercapnia and Hypocapnia Measured by Positron Emission Tomography (2003)

Hypercapnia induces cerebral vasodilation and increases cerebral blood flow (CBF), and hypocapnia induces cerebral vasoconstriction and decreases CBF. The relation between changes in CBF and cerebral blood volume (CBV) during hypercapnia and hypocapnia in humans, however, is not clear. Both CBF and CBV were measured at rest and during hypercapnia and hypocapnia in nine healthy subjects by positron emission tomography. The vascular responses to hypercapnia in terms of CBF and CBV were 6.0 +/- 2.6%/mm Hg and 1.8 +/- 1.3%/mm Hg, respectively, and those to hypocapnia were -3.5 +/- 0.6%/mm Hg and -1.3 +/- 1.0%/mm Hg, respectively. The relation between CBF and CBV was CBV = 1.09 CBF0.29. The increase in CBF was greater than that in CBV during hypercapnia, indicating an increase in vascular blood velocity. The degree of decrease in CBF during hypocapnia was greater than that in CBV, indicating a decrease in vascular blood velocity. The relation between changes in CBF and CBV during hypercapnia was similar to that during neural activation; however, the relation during hypocapnia was different from that during neural deactivation observed in crossed cerebellar diaschisis. This suggests that augmentation of CBF and CBV might be governed by a similar microcirculatory mechanism between neural activation and hypercapnia, but diminution of CBF and CBV might be governed by a different mechanism between neural deactivation and hypocapnia.
Oxalate synthesis in mammals: properties and subcellular distribution of serine:pyruvate/alanine:glyoxylate aminotransferase in the liver. (2000)

Primary hyperoxaluria Type 1 (PH1) is caused by a functional deficiency of a liver enzyme, serine:pyruvate/alanine:glyoxylate aminotransferase (SPT/AGT), which catalyzes transamination between L-serine or l-alanine as an amino acid substrate and glyoxylate or pyruvate as an alpha-keto acid substrate. A high affinity for glyoxylate is a notable feature of this enzyme, suggesting a role in glyoxylate metabolism in vivo. Another conspicuous feature of SPT/AGT is its species-specific and food habit-dependent subcellular distribution. Thus, the enzyme is located in peroxisomes in herbivores and man, largely in mitochondria in carnivores, and in both the organelles in rodents. The mechanism of the species-specific dual organelle localization of SPT/AGT is either transcription of the gene from two different start sites or loss of the upstream translation initiation ATG codon by mutations. It appears that the mitochondrial versus peroxisomal distribution of SPT/AGT in different animal species is indispensable in meeting the metabolic needs caused by their respective food habits. As for the peroxisomal localization, glycolate is contained in plants much more than in animal tissues, and when ingested, it is converted to glyoxylate, an immediate precursor of oxalate, in liver peroxisomes. Therefore, peroxisomal localization of SPT/AGT may be indispensable for herbivores to convert the glyoxylate formed in peroxisomes into glycine in situ rather than forming oxalate. On the other hand, our recent studies showed that SPT/AGT contributed substantially to serine metabolism in rabbit, human, and dog livers; i.e., irrespective of its mitochondrial or peroxisomal localization. Thus, the mitochondrial localization of SPT/AGT was not a prerequisite for the metabolism of L-serine. Another source of glyoxylate is the metabolism of L-hydroxyproline, and in this case, the enzyme responsible for the glyoxylate formation has been reported to be a mitochondrial matrix enzyme. Collagen accounts for about 30% of total animal proteins and contains about 13% (w/w) hydroxyproline. It is therefore possible that both mitochondrial and peroxisomal SPT/AGT contribute to the metabolism of glyoxylate and serine, but the subcellular site for glyoxylate metabolism is different in herbivores and carnivores.
Methylnaltrexone for Reversal of Constipation Due to Chronic Methadone Use (2000)

Our data demonstrate that intravenous methylnaltrexone can induce laxation and reverse slowing of oral cecal-transit time in subjects taking high opioid dosages. Low-dosage methylnaltrexone may have clinical utility in managing opioid-induced constipation.
Methods of prophylaxis in stress ulcer disease (1981)

Abstract Although infrequent, acute upper gastrointestinal bleeding is potentially life‐threatening for critically ill patients. Gastric erosions can be detected endoscopically in almost all seriously ill patients. Although gastric acid plays a key role in the pathogenesis of acute gastric erosions, mucosal integrity is very much dependent on mucosal permeability, gastric blood flow, the secretory state of the mucosa, and acid‐base balance. Various agents that affect any of these physiological processes such as vitamin A, carbenoxolone, gastrin, vasoactive agents, sodium bicarbonate, and anticholinergic drugs have been used experimentally or clinically in the prevention of stress ulcerations. However, no controlled clinical trials are available. The effectiveness of antacids in the prevention of acute stress ulceration in critically ill patients has been documented in controlled, prospective trials. The effectiveness of the histamine H 2 ‐receptor antagonist cimetidine remains controversial; it is less effective in critically ill patients of the type usually encountered in a respiratory‐surgical intensive care unit but it may be effective in selected groups of patients with head and thermal injury. Prostaglandins have been evaluated increasingly for their cytoprotective effects on the gastric mucosa. Clinical trials are needed to evaluate their effectiveness in the prevention of stress ulcers.
Pathfinding by neuronal growth cones in grasshopper embryos. IV. The effects of ablating the A and P axons upon the behavior of the G growth cone (1984)

In the companion paper (Bastiani, M. J., J. A. Raper, and C. S. Goodman (1984) J. Neurosci. 4: 2311-2328), we show that as the G growth cone reaches its choice point and turns anteriorly on the A/P fascicle, its filopodia demonstrate selective affinity for the A/P fascicle as compared to the other approximately 25 longitudinal axon fascicles, and within the A/P fascicle itself, G's filopodia selectively contact the P axons as compared to the A axons. These results support the hypothesis that the A/P fascicle, and, moreover, subsets of axons within it (Ps versus As), are specifically labeled and that the G growth cone is determined to follow a particular labeled pathway. We tested the "labeled pathways" hypothesis by specifically ablating these axons and examining the subsequent behavior of the G growth cone in embryos grown in culture. Ablation of the A and P axons prevents G from growing more than a short distance anteriorly, although the G growth cone is within grasp of many other longitudinal axon fascicles. Ablation of only the P axons has a similar effect; the G growth cone behaves normally if only the A axons are ablated. Transmission electron micrograph semiserial section reconstructions of experimental embryos further indicate that G's growth cone behaves abnormally when the A and P axons, or only the P axons, are ablated. The G growth cone branches extensively in the lateral and ventral neuropil without it or its filopodia showing a high affinity for any other axon fascicle. These results indicate that the G growth cone is able to distinguish the A/P fascicle from the other longitudinal axon fascicles in the developing neuropil. Moreover, the results suggest that within the A/P fascicle the G growth cone is able to distinguish the P axons from the A axons.
Interactions of ?Ultra-Low? Doses of Naltrexone and Morphine in Mature and Young Male and Female Rats (2004)

Sex and age influence morphine analgesia in humans and animals. Mature rats show greater morphine analgesia in males than in females. Ultra-low doses of naltrexone enhance morphine analgesia. In mature rats (18-22 weeks), naltrexone (0.002-2.0 mg/kg)-morphine (2 mg/kg) cotreatment enhanced morphine analgesia in females, an effect inversely related to naltrexone dose. Conversely, in mature male rats, naltrexone tended to decrease morphine analgesia with increasing dose. In young rats (8-10 weeks), morphine analgesia was unrelated to sex and in both sexes the naltrexone-morphine interaction was negligible. These data show that dose, age, and sex alter the naltrexone-morphine interaction in rats.
A Europium-Ion-Based Luminescent Sensing Probe for Hydrogen Peroxide (2002)

A bright idea: A 15-fold increase in fluorescence intensity occurs when the complex formed between Eu3+ and the antibiotic tetracycline binds to hydrogen peroxide at neutral pH. The complex can be used in the determination of the concentration of H2O2, the activity of oxidases, the concentration of glucose, and also in an optical sensor for H2O2.
Brain-on-a-chip model enables analysis of human neuronal differentiation and chemotaxis (2016)

Migration of neural progenitors in the complex tissue environment of the central nervous system is not well understood. Progress in this area has the potential to drive breakthroughs in neuroregenerative therapies, brain cancer treatments, and neurodevelopmental studies. To a large extent, advances have been limited due to a lack of controlled environments recapitulating characteristics of the central nervous system milieu. Reductionist cell culture models are frequently too simplistic, and physiologically more relevant approaches such as ex vivo brain slices or in situ experiments provide little control and make information extraction difficult. Here, we present a brain-on-chip model that bridges the gap between cell culture and ex vivo/in vivo conditions through recapitulation of self-organized neural differentiation. We use a new multi-layer silicone elastomer device, over the course of four weeks to differentiate pluripotent human (NTERA2) cells into neuronal clusters interconnected with thick axonal bundles and interspersed with astrocytes, resembling the brain parenchyma. Neurons within the device express the neurofilament heavy (NF200) mature axonal marker and the microtubule-associated protein (MAP2ab) mature dendritic marker, demonstrating that the devices are sufficiently biocompatible to allow neuronal maturation. This neuronal-glial environment is interfaced with a layer of human brain microvascular endothelial cells showing characteristics of the blood-brain barrier including the expression of zonula occludens (ZO1) tight junctions and increased trans-endothelial electrical resistance. We used this device to model migration of human neural progenitors in response to chemotactic cues within a brain-tissue setting. We show that in the presence of an environment mimicking brain conditions, neural progenitor cells show a significantly enhanced chemotactic response towards shallow gradients of CXCL12, a key chemokine expressed during embryonic brain development and in pathological tissue regions of the central nervous system. Our brain-on-chip model thus provides a convenient and scalable model of neural differentiation and maturation extensible to analysis of complex cell and tissue behaviors.
Steroid derivatives of cysteamine and cysteine (1969)

A number of androstenone, estrone, and pregnenone derivatives of cysteamine have been prepared by reacting the steroid amines with ethylene monothiolcarbonate. The amides of androstenone carboxylic acid with mercaptoethylamine and cysteine have also been prepared.
Compound strategies of coding, equalization, and space diversity for wide-band TDMA indoor wireless channels (1992)

Compound strategies of equalization and space diversity in the form of an optimum baseband combiner are attractive for wideband time division multiple access (TDMA) portable communication radio links in order to combat dispersive fading and cochannel interference. The authors investigate the performance of such a scheme in conjunction with convolutional coding and soft-decision Viterbi decoding via a semianalytical technique based on the method of moments. Such an approach avoids a Gaussian characterization of interference and yields results for both ideal interleaving and no interleaving. With dual space diversity, three taps per forward filter, and a data rate of 10 Mb/s, it is shown that, although a third space diversity branch remains preferable in terms of performance, channel coding can be a viable alternative, particularly in terms of outage rate, to increasing the space diversity order, even in the absence of interleaving, provided the signal-to-interference ratio is sufficiently high.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>