gebhart/patrepeval huggingface dataset:
3,7-Diazabicyclane. A new narcotic analgesic (1986)

The synthesis of a series of 9-phenyl-3,7-diazabicyclanes and 9-(m-hydroxyphenyl)-3,7-diazabicyclanes is described. Members of both series were tested for antinociception in rat tail withdrawal and mouse acetic acid writhing assays. Their affinities for opiate receptors in rat brain homogenate were also determined. The 9-phenyl compounds, 1a-c, were inactive. However, the 9-(m-hydroxyphenyl) analogues, 2a-c, were found to possess significant activity in the writhing assay, comparable to that of morphine. All activity was reversed by naloxone.
Engineering Hydrophobic Protein–Carbohydrate Interactions to Fine-Tune Monoclonal Antibodies (2013)

Biologically active conformations of the IgG1 Fc homodimer are maintained by multiple hydrophobic interactions between the protein surface and the N-glycan. The Fc glycan modulates biological effector functions, including antibody-dependent cellular cytotoxicity (ADCC) which is mediated in part through the activatory Fc receptor, FcγRIIIA. Consistent with previous reports, we found that site-directed mutations disrupting the protein-carbohydrate interface (F241A, F243A, V262E, and V264E) increased galactosylation and sialylation of the Fc and, concomitantly, reduced the affinity for FcγRIIIA. We rationalized this effect by crystallographic analysis of the IgG1 Fc F241A mutant, determined here to a resolution of 1.9 Å, which revealed localized destabilization of this glycan-protein interface. Given that sialylation of Fc glycans decreases ADCC, one explanation for the effect of these mutants on FcγRIIIA binding is their increased sialylation. However, a glycan-engineered IgG1 with hypergalactosylated and hypersialylated glycans exhibited unchanged binding affinity to FcγRIIIA. Moreover, when we expressed these mutants as a chemically uniform (Man5GlcNAc2) glycoform, the individual effect of each mutation on FcγRIIIA affinity was preserved. This effect was broadly recapitulated for other Fc receptors (FcγRI, FcγRIIA, FcγRIIB, and FcγRIIIB). These data indicate that destabilization of the glycan-protein interactions, rather than increased galactosylation and sialylation, modifies the Fc conformation(s) relevant for FcγR binding. Engineering of the protein-carbohydrate interface thus provides an independent parameter in the engineering of Fc effector functions and a route to the synthesis of new classes of Fc domain with novel combinations of affinities for activatory and inhibitory Fc receptors.
[Different expression of liver-specific insulin-like growth factor I gene in breast cancer; expression with mice]. (2008)

IGF-1 plays a role as a risk factor in the onset and development of breast cancer by affecting the expression of many differentially expressed genes.
Emil Kraepelin: ¿Un psiquiatra social?: Un comentario aclaratorio (2010)

El ensayo de Emil Kraepelin «Sobre el desarraigo» publicado en 1920, provoco en todos la sorpresa con su ultima frase. En ella Kraepelin expone la tesis de que el fenomeno del desarraigo es la clave para el desarrollo de una «psiquiatria social». La sorpresa que provoca hoy en dia esta declaracion, se basa principalmente en una cierta exclusividad de los intereses actuales de la psiquiatria. Hasta ahora casi no se ha pensado verdaderamente lo que Kraepelin quiso decir en realidad con el concepto de...
Neurotensin Regulates Growth of Human Pancreatic Cancer (1993)

NT stimulates growth of MIA PaCa-2 cells through stimulation of PI hydrolysis and mobilization of calcium. Stimulation of the cyclic AMP pathway by high concentrations of NT abolishes the growth-stimulatory effect of NT that is mediated through PI hydrolysis or calcium mobilization.
How To Unify Low-Shear-Rate Rheology and Gel Properties of Drilling Muds: A Transient Rheological and Structural Model for Complex Well Applications (2006)

Abstract Due to their complex formulations, Drilling Fluids and especially Oil base Muds exhibit very complex rheological properties. They are commonly described as thixotropic shear thinning fluids with a yield stress. A set of standards established by the American Petroleum Institute is available for the rheological characterization of these fluids and classical descriptions with non-Newtonian fluids such as yield power law models are typically employed. Although these descriptions and measurements are adequate for classical drilling situations, they reveal to be insufficient to describe more complex phenomena as barite sag, or pressure peak due to transient gel breaking on restart. In particular ultra low shear rate rheology has been early accepted as a key parameter for determining sag potential, and is poorly described by the classical models and measurements. On the other hand, time-dependent behavior (classically apprehended in static conditions through Gel 0 and Gel 10 measurements), which can be very significant even in dynamic conditions, is not quantitatively linked to the rheological description. This paper describes how a simple thixotropic and structural model is able to describe completely all the features of the rheological behavior of drilling muds. The parameters of the model can be simply deduced from on site measurement using Fann 35 rheometer. We show that mud viscosity results at any moment from the competition between aging and shear rejuvenation. As a consequence, viscosity bifurcation (abrupt transition towards complete stoppage or rapid shear) may appear at low shear, which might explain the occurrence of barite sag. Finally, it is shown how any transient phenomena like pressure peaks when starting a pump after circulation stoppage may be adequately predicted by using this model in hydraulic calculation.
The Structure of Sucrose Synthase-1 from Arabidopsis thaliana and Its Functional Implications (2011)

Sucrose transport is the central system for the allocation of carbon resources in vascular plants. During growth and development, plants control carbon distribution by coordinating sites of sucrose synthesis and cleavage in different plant organs and different cellular locations. Sucrose synthase, which reversibly catalyzes sucrose synthesis and cleavage, provides a direct and reversible means to regulate sucrose flux. Depending on the metabolic environment, sucrose synthase alters its cellular location to participate in cellulose, callose, and starch biosynthesis through its interactions with membranes, organelles, and cytoskeletal actin. The x-ray crystal structure of sucrose synthase isoform 1 from Arabidopsis thaliana (AtSus1) has been determined as a complex with UDP-glucose and as a complex with UDP and fructose, at 2.8- and 2.85-Å resolutions, respectively. The AtSus1 structure provides insights into sucrose catalysis and cleavage, as well as the regulation of sucrose synthase and its interactions with cellular targets.
Immunostimulatory activity of aminoalkyl glucosaminide 4-phosphates (AGPs): induction of protective innate immune responses by RC-524 and RC-529 (2002)

Earlier we showed that the structural requirements for adjuvanticity among the aminoalkyl glucosaminide 4-phosphate (AGP) class of synthetic immunostimulants may be less strict than those for other endotoxic activities, including the induction of nitric oxide synthase in murine macrophages and cytokine production in human whole blood. The known role of nitric oxide and pro-inflammatory cytokines in the activation of host defenses against infection prompted us to examine the ability of certain AGPs to enhance non-specific resistance in mice to Listeria monocytogenes and influenza infections as well as to stimulate the production of pro-inflammatory cytokines in mouse splenocytes, human PBMCs, and human U937 histiocytic lymphoma cells. Intranasal administration of RC-524 or RC-529 to mice 2 days prior to a lethal influenza challenge provided significant protection in each case. Similarly, the intravenous administration of these AGPs induced resistance to L. monocytogenes infection as measured by survival or reduction of bacteria in the spleen. Activation of the innate immune response by AGPs appears to involve activation of Toll-like receptor 4 (TLR4) because RC-524 failed to elicit a protective effect in C3H/HeJ mice which have a defect in TLR4 signaling or induce significant cytokine levels in C3H/HeJ splenocytes. Both AGPs also stimulated pro-inflammatory cytokine release in human cell cultures in a dose-dependent manner.
Electricity Generation in Microbial Fuel Cells Using Neutral Red as an Electronophore (2000)

Neutral red (NR) was utilized as an electron mediator in microbial fuel cells consuming glucose to study both its efficiency during electricity generation and its role in altering anaerobic growth and metabolism of Escherichia coli and Actinobacillus succinogenes. A study of chemical fuel cells in which NADH, NR, and ferricyanide were the electron donor, the electronophore, and the electron acceptor, respectively, showed that electrical current produced from NADH was proportional to the concentration of NADH. Fourfold more current was produced from NADH in chemical fuel cells when NR was the electron mediator than when thionin was the electron mediator. In microbial fuel cells in which E. coli resting cells were used the amount of current produced from glucose when NR was the electron mediator (3.5 mA) was 10-fold more than the amount produced when thionin was the electron mediator (0.4 mA). The amount of electrical energy generated (expressed in joules per mole of substrate) and the amount of current produced from glucose (expressed in milliamperes) in NR-mediated microbial fuel cells containing either E. coli or A. succinogenes were about 10- and 2-fold greater, respectively, when resting cells were used than when growing cells were used. Cell growth was inhibited substantially when these microbial fuel cells were making current, and more oxidized end products were formed under these conditions. When sewage sludge (i.e., a mixed culture of anaerobic bacteria) was used in the fuel cell, stable (for 120 h) and equivalent levels of current were obtained with glucose, as observed in the pure-culture experiments. These results suggest that NR is better than other electron mediators used in microbial fuel cells and that sludge production can be decreased while electricity is produced in fuel cells. Our results are discussed in relation to factors that may improve the relatively low electrical efficiencies (1.2 kJ/mol) obtained with microbial fuel cells.
Putative hAPN receptor binding sites in SARS_CoV spike protein. (2003)

CD13 may be a possible receptor of the SARS-CoV S protein, which may be associated with the SARS infection. This study also provides a possible strategy for mapping the possible binding receptors of the proteins in a genome.
Short pulse high power fiber laser systems (2005)

We review the rapid recent progress in the development of short pulse high-power fiber laser and amplifier devices. Use of cladding pump technology now provides a route to compact and efficient laser and amplifier systems with high beam quality and high output powers. A new Yb-fiber CPA system incorporating a CFBG stretcher with both 2nd and 3rd order dispersion is presented for high pulse energy applications. In addition, a simplified Yb-fiber parabolic amplifier system is also shown to be suitable for producing higher average powers, here up to 25 W.
Trifluoromethanesulfonic Acid Efficiently Catalyzed the Intramolecular Glycosidation of 1-C-Alkyl-d-hexopyranoses to Form the Anhydroketopyranoses Having 6,8-Dioxabicyclo[3.2.1]octane Structures (2005)

The intramolecular glycosidation of the 1-C-alkyl-d-hexopyranose derivatives to form the anhydroketopyranoses having 6,8-dioxabicyclo[3.2.1]octane structures was investigated. We synthesized several 1-C-alkyl-2,3,4-tri-O-benzyl-d-hexopyranoses and found that only 5 mol% trifluoromethanesulfonic acid efficiently promoted the intramolecular glycosidation to afford the desired anhydroketopyranoses in good yields.
Synthesis and Reactions of 8-Hydrazinofuro[2',3':4,5]pyrrolo-[1,2-d][1,2,4]triazines (1997)

5-Ethyl-8-hydrazinofuro[2',3':4,5]pyrrolo[1,2- d ][1,2,4]triazine ( 4a ) and its 2-methyl derivative 4b were prepared from 4 H -furo[3,2- b ]pyrrole-5-carbohydrazides 1a and 1b, respectively. Compounds 1a and 1b reacted with triethyl orthopropionate to give 2a and 2b which afforded with phosphorus(V) sulfide corresponding thiones 3a and 3b . The title compounds 4a and 4b were made by treatment of 3a and 3b with hydrazine hydrate. By reactions of triethyl orthoesters with the title compounds and similar derivatives furo[2'3':4,5]pyrrolo[1,2- d ][1,2,4]triazolo[3,4- f ][1,2,4]triazines 5a-5j were prepared. Reactions of compounds 4 with some aldehydes and isocyanates led to hydrazones 6a-6c and semicarbazones 7a and 7b , respectively.
Pre-analytic saliva processing affect proteomic results and biomarker screening of head and neck squamous carcinoma (2007)

The objective of this study was to assess the effect of pre-analytical processing on proteomic analysis of saliva and to identify salivary biomarkers for potential clinical applications. Saliva samples from five healthy individuals and three head and neck squamous carcinoma (HNSC) patients were initially depleted of major protein constituents. Saliva from healthy subjects was divided and processed by three different methods prior to liquid chromatography and tandem mass spectrometry technique (LC-MS/MS) analysis. The results showed marked differences amongst the methods. The SDS-PAGE separation and in-gel digestion method yielded the highest number of proteins that included the majority of those identified by the other two methods. The in gel-digestion method was used in the LC-MS/MS analysis of saliva from three HNSC patients and the results were compared with those from healthy subjects. Our analysis identified two proteins, alpha-1-B-glycoprotein and complement factor B proteins, to be present in patients but not in normal specimens. Paradoxically, cystatin S, parotid secretory factor, and poly-4-hydrolase beta-subunit proteins were detected in most normal salivas but not in patient specimens. Subsequent analysis of complement factor B by Western blotting showed strong immunoreactive bands of complement factor B in HNSC patients' and negative or weakly positive in normal saliva samples. We conclude that: 1) initial saliva processing affects protein analysis, 2) in-gel digestion followed by LC-MS/MS detects the most saliva proteins, 3) certain proteins are differentially found in patient and normal salivas and 4) a small set of proteins can be targeted for future validation for clinical investigation.
PDBWiki: added value through community annotation of the Protein Data Bank (2010)

The success of community projects such as Wikipedia has recently prompted a discussion about the applicability of such tools in the life sciences. Currently, there are several such 'science-wikis' that aim to collect specialist knowledge from the community into centralized resources. However, there is no consensus about how to achieve this goal. For example, it is not clear how to best integrate data from established, centralized databases with that provided by 'community annotation'. We created PDBWiki, a scientific wiki for the community annotation of protein structures. The wiki consists of one structured page for each entry in the the Protein Data Bank (PDB) and allows the user to attach categorized comments to the entries. Additionally, each page includes a user editable list of cross-references to external resources. As in a database, it is possible to produce tabular reports and 'structure galleries' based on user-defined queries or lists of entries. PDBWiki runs in parallel to the PDB, separating original database content from user annotations. PDBWiki demonstrates how collaboration features can be integrated with primary data from a biological database. It can be used as a system for better understanding how to capture community knowledge in the biological sciences. For users of the PDB, PDBWiki provides a bug-tracker, discussion forum and community annotation system. To date, user participation has been modest, but is increasing. The user editable cross-references section has proven popular, with the number of linked resources more than doubling from 17 originally to 39 today. Database URL: http://www.pdbwiki.org.
Pharmacological Management of Neurological and Psychiatric Disorders (1998)

This practical, user-friendly guide assists diagnosis and therapeutic of neurological and psychiatric disorders. An introductory chapter covers basic neuroscience and pharmacology as they pertain to the treatment of central nervous system disorders. Subsequent chapters cover the full spectrum of major psychiatric and neurological conditions including schizophrenia, ADD and developmental disorders, obsessive-compulsive behavior, disorders of sleep, neuromuscular disorders, delirium and dementia, and much more. Special chapters address drug addiction and substance abuse, brain ischemia, headache, and pain. Chapter organization for each condition features a clinical description (presenting symptoms), diagnostic criteria (pathophysiology), pharmacotherapeutics, and recommended management and treatment regimens. Throughout, tables and figures illustrate important concepts and treatment algorithms guide therapeutic decision making.
High in vivo expression of interleukin‐17 receptor in synovial endothelial cells and chondrocytes from arthritis patients (2001)

IL-17-positive cells are found exclusively in RA. On the other hand, synovial endothelial cells and chondrocytes expressing IL-17R are found in the majority of patients with different types of arthritis. This finding suggests a role for a second ligand for IL-17R, which could be either a different cytokine or a different isoform of IL-17.
Principles Of Cmos Vlsi Design A Systems Perspective (1985)

Introduction to CMOS Circuits. Introduction. MOS Transistors. MOS Transistor Switches. CMOS Logic. Circuit Representations. CMOS Summary. MOS Transistor Theory. Introduction. MOS Device Design Equation. The Complemenatry CMOS Inverter-DC Characteristics. Alternate CMOS Inverters. The Differential Stage. The Transmission Gate. Bipolar Devices. CMOS Processing Technology. Silicon Semiconductor Technology: An Overview. CMOS Technologies. Layout Design Rules. CAD Issues. Circuit Characterization and Performance Estimation. Introduction. Resistance Estimation. Capacitance Estimation. Inductance. Switching Characteristics. CMOS Gate Transistor Sizing. Power Consumption. Determination of Conductor Size. Charge Sharing. Design Margining. Yield. Scaling of MOS Transistor Dimensions. CMOS Circuit and Logic Design. Introduction. CMOS Logic Structures. Basic Physical Design of Simple Logic Gates. Clocking Strategies. Physical and Electrical Design of Logic Gates. 10 Structures. Structured Design Strategies. Introduction. Design Economics. Design Strategies. Design Methods. CMOS Chip Design Options. Design Capture Tools. Design Verification Tools. CMOS Test Methodolgies. Introduction. Fault Models. Design for Testability. Automatic Test Pattern Generation. Design for Manufacturability. CMOS Subsystem Design. Introduction. Adders and Related Functions. Binary Counters. Multipliers and Filter Structures. Random Access and Serial Memory. Datapaths. FIR and IIR Filters. Finite State Machines. Programmable Logic Arrays. Random Control Logic.
Determination of 25-Hydroxyvitamin D in Human Plasma Using High-Performance Liquid Chromatography−Tandem Mass Spectrometry (2005)

We report here the development of a precise and sensitive method to determine 25-hydroxyvitamin D (25-OH-D(2)/ -D(3)) in human plasma using high-performance liquid chromatography-tandem mass-mass spectrometry with atmospheric pressure chemical ionization (LC-APCI-MS/MS). The method involves the use of deuterated 25-OH-D(3) as an internal standard compound for 25-OH-D(2)/-D(3), which was synthesized in our laboratory, and the selection of a precursor and product ion with a MS/MS multiple reaction monitoring method. The average intraassay and interassay variation values (relative standard deviation) were 5.7 and 2.5%, respectively, for 25-OH-D(3) and 4.5 and 5.1%, respectively, for 25-OH-D(2). The average spiked recoveries from authentic compounds added to normal human plasma samples for 25-OH-D(3) and 25-OH-D(2) were 103.8 and 98.8%, respectively. Mean plasma concentrations of 25-OH-D(3) and 25-OH-D(2) in healthy subjects were 20.5 and 0.4 ng/mL, respectively. We conclude that this novel LC-APCI-MS/MS method would be useful for the evaluation of the vitamin D status in postmenopausal women and elderly subjects and provide useful information in the diagnosis of vitamin D insufficiency/deficiency, as well as for the treatment and prevention of osteoporosis with vitamin D.
Analysis of Human Immunodeficiency Virus Type 1 Gene Expression in Latently Infected Resting CD4 + T Lymphocytes In Vivo (2003)

In individuals with human immunodeficiency virus type 1 (HIV-1) infection, a small reservoir of resting memory CD4(+) T lymphocytes carrying latent, integrated provirus persists even in patients treated for prolonged periods with highly active antiretroviral therapy (HAART). This reservoir greatly complicates the prospects for eradicating HIV-1 infection with antiretroviral drugs. Therefore, it is critical to understand how HIV-1 latency is established and maintained. In particular, it is important to determine whether transcriptional or posttranscriptional mechanisms are involved. Therefore, HIV-1 DNA and mRNAs were measured in highly purified populations of resting CD4(+) T lymphocytes from the peripheral blood of patients on long-term HAART. In such patients, the predominant form of persistent HIV-1 is latent integrated provirus. Typically, 100 HIV-1 DNA molecules were detected per 10(6) resting CD4(+) T cells. Only very low levels of unspliced HIV-1 RNA ( approximately 50 copies/10(6) resting CD4(+) T cells) were detected using a reverse transcriptase PCR assay capable of detecting a single molecule of RNA standard. Levels of multiply spliced HIV-1 RNA were below the limit of detection (<50 copies/10(6) cells). Only 1% of the HIV-1 DNA-positive lymphocytes in this compartment could be induced to up-regulate HIV-1 mRNAs after cellular activation, indicating that most of the proviral DNA in resting CD4(+) T cells either carries intrinsic defects precluding transcription or is subjected to transcriptional control mechanisms that preclude high-level production of multiply spliced mRNAs. Nevertheless, by inducing T-cell activation, it is possible to isolate replication-competent virus from resting CD4(+) T lymphocytes of all infected individuals, including those on prolonged HAART. Thus, a subset of integrated proviruses (1%) remains competent for high-level mRNA production after cellular activation, and a subset of these can produce infectious virus. Measurements of steady-state levels of multiply spliced and unspliced HIV-1 RNA prior to cellular activation suggest that infected resting CD4(+) T lymphocytes in blood synthesize very little viral RNA and are unlikely to be capable of producing virus. In these cells, latency appears to reflect regulation at the level of mRNA production rather than at the level of splicing or nuclear export of viral mRNAs.