gebhart/patrepeval huggingface dataset:
Synthesis of 5-hydroxy-2,3,4,5-tetrahydro-[1H]-2-benzazepin-4-ones: selective antagonists of muscarinic (M3) receptors (2008)

Two approaches to tetrahydro-[1H]-2-benzazepin-4-ones of interest as potentially selective, muscarinic (M(3)) receptor antagonists have been developed. Base promoted addition of 2-(tert-butoxycarbonylamino)methyl-1,3-dithiane with 2-(tert-butyldimethylsiloxymethyl)benzyl chloride gave the corresponding 2,2-dialkylated 1,3-dithiane which was taken through to the dithiane derivative of the parent 2,3,4,5-tetrahydro-[1H]-2-benzazepin-4-one by desilylation, oxidation and cyclisation via a reductive amination. After conversion into the N-tert-butyloxycarbonyl, N-toluene p-sulfonyl and N-benzyl derivatives , hydrolysis of the dithiane gave the N-protected tetrahydro-[1H]-2-benzazepin-4-ones . However, preliminary attempts to convert these into 5-cycloalkyl-5-hydroxy derivatives were not successful. In the second approach, ring-closing metathesis was used to prepare 2,3-dihydro-[1H]-2-benzazepines which were hydroxylated and oxidized to give the required 5-hydroxy-2,3,4,5-tetrahydro-[1H]-2-benzazepin-4-ones. Following preliminary studies, ring-closing metathesis of the dienyl N-(2-nitrophenyl)sulfonamide gave the dihydrobenzazepine which was converted into the 2-butyl-5-cyclobutyl-5-hydroxytetrahydrobenzazepin-4-one by hydroxylation and N-deprotection followed by N-alkylation via reductive amination, and oxidation. This chemistry was then used to prepare the 2-[(N-arylmethyl)aminoalkyl analogues , , and . N-Acylation followed by amide reduction using the borane-tetrahydrofuran complex was also used to achieve N-alkylation of dihydrobenzazepines and this approach was used to prepare the 5-cyclopentyl-5-hydroxy-2,3,4,5-tetrahydro-[1H]-2-benzazepin-4-one and the 5-cyclobutyl-8-fluoro-5-hydroxy-2,3,4,5-tetrahydro-[1H]-2-benzazepin-4-one . The structures of 2-tert-butyloxycarbonyl-4,4-propylenedithio-2,3,4,5-tetrahydro-[1H]-2-benzazepine and (4RS,5SR)-2-butyl-5-cyclobutyl-4,5-dihydroxy-2,3,4,5-tetrahydro-[1H]-2-benzazepine were confirmed by X-ray diffraction. The racemic 5-cycloalkyl-5-hydroxy-2,3,4,5-tetrahydro-[1H]-2-benzazepin-4-ones were screened for muscarinic receptor antagonism. For M(3) receptors from guinea pig ileum, these compounds had log(10)K(B) values of up to 7.2 with selectivities over M(2) receptors from guinea pig left atria of approximately 40.
Update on Deep Brain Stimulation for Dyskinesia and Dystonia: A Literature Review (2016)

Deep brain stimulation (DBS) has been an established surgical treatment option for dyskinesia from Parkinson disease and for dystonia. The present article deals with the timing of surgical intervention, selecting an appropriate target, and minimizing adverse effects. We provide an overview of current evidences and issues for dyskinesia and dystonia as well as emerging DBS technology.
Efectos del cambio climático sobre la polinización y la producción agrícola en América tropical (2016)

Los organismos polinizadores desempe~nan un rol fundamental en la agricultura y consecuentemente en la seguridad alimentaria en America tropical. Debido a las alteraciones ambientales inducidas por el cambio climatico, una variedad de especies de polinizadores se encuentra actualmente en disminucion, lo cual tiene importantes implicaciones para los ecosistemas tanto naturales como agrcolas. Es probable que la \\crisis de los polinizadores" afecte a la produccion y los costos de ciertos cultivos contribuyendo con desequilibrios alimentarios y problemas de salud en los pases de la region. Ante esta problematica, es imprescindible llevar a cabo estudios que mejoren nuestra comprension sobre las relaciones planta{polinizador en cultivos agrcolas, ademas de implementar estrategias orientadas a revertir la declinacion de las poblaciones de polinizadores. De que manera el cambio climatico afectara la produccion agrcola y la seguridad alimentaria en America tropical dependera en gran medida de como las interacciones planta{polinizador se vean infuenciadas.
OPTIMIZATION OF PROTEIN ISOLATE PRODUCTION FROM SOY FLOUR USING INDUSTRIAL MEMBRANE SYSTEMS (1978)

ABSTRACT A new approach to the production of protein isolates from oilseed flours with industrial ultrafiltration and reverse osmosis membranes previously demonstrated has been further optimized for use with soy flour. The effects on membrane performance of prefiltering the flour extract feed to different degrees and processing the feed at different pH levels were examined. A wide range of industrial membrane systems embodying several configurations was tested. Prefiltration of feed to less than 100μ proved to be unnecessary for most systems. Feed at pH 7.0 processed at high permeation rates and yielded products with NSI values in excess of 90.
ITPKA expression is a novel prognostic factor in hepatocellular carcinoma (2015)

Our data indicated that ITPKA expression was significantly up-regulated in HCC and could serve as a potential novel prognostic biomarker for HCC patients after surgery.
Vasomotor Rhinitis Is Not a Wastebasket Diagnosis (2003)

The impact of chronic rhinitis on patients, health care systems, and resources is substantial, resulting in more than 25 million office visits per year and resulting in total indirect and direct costs of $6 billion annually. It is estimated that more than 10% of the population has chronic or recurrent nasal obstruction or congestion, rhinorrhea, sneezing, and pruritus. Approximately half of these patients are classified as having allergic rhinitis and half as having nonallergic rhinitis, including vasomotor rhinitis. These forms of chronic, noninfectious rhinitis represent a spectrum of nasal disorders that are best categorized as a hyperreactivity of the nasal mucosa to a variety of stimuli. Allergic rhinitis is diagnosed when specific antigens can be identified and is often subclassified as seasonal or perennial allergic rhinitis. When specific antigens are not identifiable, chronic rhinitis is often classified as vasomotor or nonallergic. These nonallergic forms of chronic rhinitis can be further evaluated by nasal cytology. Nasal scrapings of the inferior turbinate can yield epithelial lining, and detailed analysis of different cell types can be made. Patients with nonallergic rhinitis and abundant eosinophils on nasal cytology have the so-called nonallergic rhinitis with eosinophilia syndrome, which is sometimes associated with aspirin intolerance. Patients with nonallergic rhinitis and unremarkable nasal smear findings could have rhinitis medicamentosa, pregnancy, or hypothyroidism, but most are thought to have vasomotor rhinitis. Most of the literature concerning vasomotor rhinitis and its relationship to the autonomic nervous system came from investigations 50 years ago. These authors discuss the role of the autonomic nervous system in maintaining sinonasal health through the regulation of vascularity and mucosal gland function, and they speculate that the autonomic nervous system regulates the reactivity of the nasal and sinus mucous membranes and glands. They note that the inferior turbinate in particular contains mucous and serous glands, vascular channels, and autonomic nervous system branches that constitute a delicately sensitive and reactive organ. Vasomotor rhinitis was thought to represent either hyperfunction of the parasympathetic nervous system in the nose and paranasal sinuses or an imbalance between the parasympathetic nervous system and sympathetic nervous system. Does vasomotor rhinitis exist, and if so, what is its etiology? Is it a specific entity and part of a continuum of disease or is it a “wastebasket” diagnosis? This article hypothesizes the former.
DNA Complexing with Polyamidoamine Dendrimers:  Implications for Transfection (1999)

DNA and polyamidamine (PAMAM) dendrimers form complexes on the basis of the electrostatic interactions between negatively charged phosphate groups of the nucleic acid and protonated (positively charged) amino groups of the polymers. Charge neutralization of both components and subsequent increases of the net positive charge of the complex result in changes in the physicochemistry and biological properties of the complexes. The formation of soluble, low-density and insoluble, high-density complexes was analyzed using UV light absorption and measurements of radioactive labeled DNA. Formation of high molecular weight and high-density complexes depended mainly on the DNA concentration and was enhanced by increasing the dendrimer-DNA charge ratio. Electrostatic charge related effects (attraction or repulsion of charged particles) appeared to be modulated by the generation of dendrimer (size of the polymer). With the progressive increases in the dendrimer-DNA charge ratio (above 20), an increase in the amount of low-density, soluble complexes was observed. Functional analysis revealed that the great majority (>90%) of transfection is carried by low-density, soluble, complexes which only represent approximately 10-20% of total complexed DNA. The ability of the dendrimer to complex and form aggregates with DNA is crucial for efficient transfection and the function of the complexed DNA.
Development of a ciliary muscle–driven accommodating intraocular lens (2008)

Evaluation of an accommodating IOL that meets the requirements for a spectacle-independent solution to presbyopia showed that the mechanical and optical designs must be further optimized to improve optical quality and functionality.
Fabrication of Arrays of Metal and Metal Oxide Nanotubes by Shadow Evaporation (2008)

This paper describes a simple technique for fabricating uniform arrays of metal and metal oxide nanotubes with controlled heights and diameters. The technique involves depositing material onto an anodized aluminum oxide (AAO) membrane template using a collimated electron beam evaporation source. The evaporating material enters the porous openings of the AAO membrane and deposits onto the walls of the pores. The membrane is tilted with respect to the column of evaporating material, so the shadows cast by the openings of the pores onto the inside walls of the pores define the geometry of the tubes. Rotation of the membrane during evaporation ensures uniform deposition inside the pores. After evaporation, dissolution of the AAO in base easily removes the template to yield an array of nanotubes connected by a thin backing of the same metal or metal oxide. The diameter of the pores dictates the diameter of the tubes, and the incident angle of evaporation determines the height of the tubes. Tubes up to approximately 1.5 mum in height and 20-200 nm in diameter were fabricated. This method is adaptable to any material that can be vapor-deposited, including indium-tin oxide (ITO), a conductive, transparent material that is useful for many opto-electronic applications. An array of gold nanotubes produced by this technique served as a substrate for surface-enhanced Raman spectroscopy: the Raman signal (per molecule) from a monolayer of benzenethiolate was a factor of approximately 5 x 10(5) greater than that obtained using bulk liquid benzenethiol.
Regulation of glycerol metabolism in Pseudomonas aeruginosa: characterization of the glpR repressor gene (1996)

The operons of the glp regulon encoding the glycerol metabolic enzymes of Pseudomonas aeruginosa were hitherto believed to be positively regulated by the product of the glpR regulatory gene. During nucleotide sequence analysis of the region located upstream of the previously characterized glpD gene, encoding sn-glycerol-3-phosphate dehydrogenase, an open reading frame (glpR) was identified which encodes a protein of 251 amino acids that is 59% identical to the Glp repressor from Escherichia coli and could be expressed as a 28-kDa protein in a T7 expression system. Inactivation of chromosomal glpR by gene replacement resulted in constitutive expression of glycerol transport activity and glpD activity. These activities were strongly repressed after introduction of a multicopy plasmid containing the glpR gene; the same plasmid also efficiently repressed expression of a glpT-lacZ+ transcriptional fusion in an E. coli glpR mutant. Analysis of the glpD and glpF upstream region identified conserved palindromic sequences which were 70% identical to the E. coli glp operator consensus sequence. The results suggest that the operons of the glp regulon in P. aeruginosa are negatively regulated by the action of a glp repressor.
Activation of ras Oncogenes Preceding the Onset of Neoplasia (1990)

The identification of ras oncogenes in human and animal cancers including precancerous lesions indicates that these genes participate in the early stages of neoplastic development. Yet, these observations do not define the timing of ras oncogene activation in the multistep process of carcinogenesis. To ascertain the timing of ras oncogene activation, an animal model system was devised that involves the induction of mammary carcinomas in rats exposed at birth to the carcinogen nitrosomethylurea. High-resolution restriction fragment length polymorphism analysis of polymerase chain reaction-amplified ras sequences revealed the presence of both H-ras and K-ras oncogenes in normal mammary glands 2 weeks after carcinogen treatment and at least 2 months before the onset of neoplasia. These ras oncogenes can remain latent within the mammary gland until exposure to estrogens, demonstrating that activation of ras oncogenes can precede the onset of neoplasia and suggesting that normal physiological proliferative processes such as estrogen-induced mammary gland development may lead to neoplasia if the targeted cells harbor latent ras oncogenes.
Developmental regulation of a complete 70-kb human beta-globin locus in transgenic mice. (1992)

We have used a linker-based ligation strategy to combine two 35-kb cosmid inserts from the human beta-globin locus into one linear fragment containing the entire locus. This 70-kb fragment was introduced into transgenic mice by microinjection of fertilized eggs. Southern blot analysis showed that a single complete transgene locus can be introduced into the germ line with high efficiency. Analysis of the expression patterns of the locus during development shows that the epsilon-globin gene behaves as a purely embryonic gene, the gamma-globin gene as an embryonic and early fetal gene, and the beta-globin gene as a fetal adult gene. Quantitation of expression showed that the levels of transcription of the epsilon- and gamma-globin genes are reversed relative to their mouse homologs but that the total output of the human and mouse loci is constant during development. These results suggest that multiple changes in DNA sequences and transcription factor balance must have occurred for the human gamma-globin gene to have evolved into a fetal gene.
Tetracyclines in Biology, Chemistry and Medicine (2001)

The tetracyclines have an illustrious history as therapeutic agents which dates back over half a century. Initially discovered as an antibiotic in 1947, the four ringed molecule has captured the fancy
Endothelial Progenitor Cells Are Decreased in Blood of Cardiac Allograft Patients With Vasculopathy and Endothelial Cells of Noncardiac Origin Are Enriched in Transplant Atherosclerosis (2003)

These data suggest that the human cardiac transplant arteriopathy is associated with reduction in circulating endothelial precursors and with seeding of recipient-derived endothelial cells at the site of plaque development.
Use of a Human Minichromosome as a Cloning and Expression Vector for Mammalian Cells (1999)

A natural human minichromosome (MC1) derived from human chromosome 1 was shown to be linear and to have a size of 5.5 Mb. Human IL-2 cDNA and the neo gene were co-transfected into a MC1-containing human-CHO hybrid cell line. Integration of the foreign genes was directed to the pericentromeric region of MC1 by co-transfection of chromosome 1-specific satellite 2 DNA. A number of G418-resistant transfectants were obtained and expression of IL-2 was determined. FISH analysis demonstrated co-localization in the minichromosome of the IL-2 gene and of the satellite 2 DNA. An IL-2-producing clone was used in cell fusion experiments with IL-2-dependent murine CTLL cells to generate CTLL-human hybrids containing the modified minichromosome (MC1-IL2). The hybrids were able to grow in medium lacking IL-2 for 17 mean population doublings (MPD), indicating that expression of the cytokine was sufficient to relieve the IL-2 dependence of CTLL proliferation. Endogenous IL-2 production delayed the onset of apoptosis in the IL-2-dependent CTLL cells. Mitotic stability was shown to be 100% in the human-CHO hybrids and 97% per MPD in CTLL cells. These results demonstrate that a natural human minichromosome can be utilized as a cloning and expression vector for mammalian cells and that the MC1 minichromosome can be engineered to deliver IL-2 to two types of cells, fibroblasts and lymphocytes.
Rolling Bearing Fault Diagnosis and Prediction Method Based on Gray Support Vector Machine Model (2015)

The article put forward a method based on GM (1, 1)-SVM for rolling bearing fault, prediction and diagnosis. Firstly, the method extract, time and frequency domain feature values, of vibration, signal of rolling bearing under, all kinds of, fault, and, normal condition. Then the method select important characteristic, parameters to build a grey model and carry on multi, step prediction, Lastly, the method use all kinds of fault and normal condition eigen value to train binary tree support vector machine and construct the decision tree of rolling bearing to classify the, fault type.
Nutrition in the nineties: policy issues (1995)

This study presents a discussion of the major policy issues with regard to nutrition and development which have been evolving over the last decade. The major issues for the 1990s were decided by members of the IUNS Committee on Nutrition and Development. The book highlights the need for education in general, and for nutrition and health education in particular, in developing countries. It also demonstrates the need for more research to establish the ideal diet in different cultures and ecological environments. Many of the chapters are the product of major nutritional studies.
Current concepts and treatment options in eosinophilic esophagitis. (2006)

Eosinophilic esophagitis (EE) is an inflammatory disorder of the esophagus that affects both children and adults, and is different from gastro-esophageal reflux disease. The immunopathogenesis of EE involves an allergic response to environmental and food allergens, and the proinflammatory cytokines IL-5 and IL-13. EE may be associated with atopic disorders and peripheral eosinophilia, and may be familial in distribution. The most common presentation is dysphagia and food impaction in adults, with additional manifestations of epigastric pain, emesis, weight loss and failure to thrive in children. Typical endoscopic findings include ringed esophagus, linear furrows, strictures and narrow esophagus. Diagnosis is confirmed by the presence of 20 or more eosinophils per high power field in the esophagus. The available treatment options include elemental diet, avoidance of specific food allergens, topical and systemic corticosteroids, and humanized monoclonal antibodies against IL-5. This review summarizes the etiopathogenesis, clinical, endoscopic and histopathological findings in EE, and describes current available treatment options.
On the attribution and additivity of binding energies (1981)

It can be useful to describe the Gibbs free energy changes for the binding to a protein of a molecule, A-B, and of its component parts, A and B, in terms of the "intrinsic binding energies" of A and B, DeltaG(A) (i) and DeltaG(B) (i), and a "connection Gibbs energy," DeltaG(s) that is derived largely from changes in translational and rotational entropy. This empirical approach avoids the difficult or insoluble problem of interpreting observed DeltaH and TDeltaS values for aqueous solutions. The DeltaG(i) and DeltaG(s) terms can be large for binding to enzymes and other proteins.
RELATIONSHIP BETWEEN HEPATITIS C GENOTYPE AND SEVERITY OF RECURRENT HEPATITIS C AFTER LIVER TRANSPLANTATION1,2 (1997)

(1) Histologic evidence of recurrent hepatitis C is seen in 90% of liver allografts; (2) Histologic hepatitis C recurs with similar frequency in genotype 1b and non-1b recipients; (3) Genotype 1b is associated with more severe histologic disease recurrence than non-1b genotypes; (4) Genotype 1b appears to be associated with a higher degree of posttransplant fibrosis and cirrhosis than non-1b genotypes.
A Retrospective Case Series Review of the Peroxisome Proliferator-Activated Receptor Ligand Rosiglitazone in the Treatment of Atopic Dermatitis (2008)

Peroxisome proliferator-activated receptors (PPARs) are nuclear hormone receptors that are expressed in a variety of cells, including keratinocytes and cells of the immune system. The gamma subtype, activated by the antidiabetic thiazolidinediones, was originally identified as a regulator of adipogenesis and glucose homeostasis. Recent data, however, have linked PPAR-gamma to several genes involved in inflammation. Among others, these pathways reduce certain inflammatory mediators in the skin and regulate epidermal barrier homeostasis, alterations of which contribute to the inflammation associated with atopic dermatitis (AD). To our knowledge, the addition of rosiglitazone maleate to the standard treatment of AD has not been evaluated.Severe adverse events were not observed, although 1 patient experienced weight gain. All patients responded to rosiglitazone therapy with decreased total body surface area involvement, severity of lesions, and number of flares.Rosiglitazone, a drug that has an excellent safety profile, may offer a well tolerated systemic treatment option for AD. However, its role should be further assessed in controlled trials to establish its efficacy and safety in this disease.
Dp140: a novel 140 kDa CNS transcript from the dystrophin locus (1995)

We have identified a 7.5 kb transcript from the dystrophin locus which encodes a novel 140 kDa protein (Dp140). Based on immunoblotting Dp140 consists of the distal rod domain and C-terminus of 427 kDa dystrophin and is found throughout the CNS. This protein is transcribed from an alternative promoter in the dystrophin locus upstream to exon 45. The unique 5' first exon is conserved between rat and human. The transcript has a 1 kb 5' untranslated region, and the first methionine initiation codon occurs in exon 51, predicting a protein of 140 kDa. Several studies report that Duchenne dystrophy patients with deletions in the exon 45-52 region have an increased incidence of cognitive impairment. Such deletions would affect expression of 427 kDa dystrophin and this shorter 140 kDa isoform but not the recently described small distal transcripts Dp116 or Dp71, suggesting particular importance to CNS function.
Integrate Internet solutions into your energy management network (2002)

The rapid increase in use of the Internet has brought not only a global network and means of communication into homes but also all kinds of new areas of functionality. Major advantages with Internet include the possibility to execute software in a Web-browser independent of the platform used, and the speed and the way development of new techniques and possibilities is done. By simply addressing a web-address, a connection may be established into your energy network. Java-applets will run on the client computer and enable complete presentation and control of equipment, or current status of equipment is simply presented by use of HTML-documents. This paper explains the basic concepts of the Internet (including Intranets) and concepts for management in general. It also explains how Internet techniques can be used to implement Web-based management for energy equipment in some alternative ways, as well as giving a brief introduction to some of the more important techniques such as http, HTML, JavaScript and Java.