gebhart/patrepeval huggingface dataset:
Mesoionic purinone analogs as inhibitors of cyclic-AMP phosphodiesterase: comparison of several ring systems (1981)

Several simple alkyl and aralkyl derivatives of mesoionic thiazolopyrimidines (1) and mesoionic 1,3,4-thiadiazolopyrimidines (2) were found to possess theophylline-like activity as inhibitors of cyclic-AMP phosphodiesterase (PDE). Reduction of the C2-C3 double bond of 1 or replacement of the sulfur atom of 1 or 2 with an N-methyl group nearly abolishes activity. Optimal activity appears to be associated with a hydrophobic substituent at the N8 position. The five-membered ring of 1 can be replaced by a pyridine or isoquinoline nucleus without untoward effects. Preliminary kinetic data suggest that the type of enzyme inhibition produced by the mesoionic derivatives is similar to that observed for theophylline. Thus, several novel mesoionic ring systems display activity as inhibitors of cyclic-AMP PDE and can serve as lead compounds for further investigation.
Lipid peroxidation in human spermatozoa as relatd to midpiece abnormalities and motility (1989)

The formation of malondialdehyde (MDA), a product of lipid peroxidation (LPO), was measured in human spermatozoa from 27 subjects with normal sperm characteristics. Peroxidation of lipids in washed spermatozoa was induced by catalytic amounts of ferrous ions and ascorbate and malondialdehyde determined by thiobarbituric method. MDA formation varied considerably from one sample to another. The studied population showed a strong correlation between lipid peroxidation potential (amount of MDA formed by 10(8) spermatozoa after 1 hour of incubation) and 1) initial motility r = -0.623, P = 0.001; and 2) morphologic abnormalities of the midpiece r = 0.405, P = 0.05. These results suggest that poor motility is linked with membrane fragility and that spermatozoa with midpiece abnormalities probably have membrane and/or cytoplasmic antiperoxidant system defects. Because LPO potential is related to the two most important characteristics of fertility, it seems possible that it has the potential to become a good biochemical index of semen quality.
Involvement of the rfp tripartite motif in protein-protein interactions and subcellular distribution (1997)

The ret finger protein (rfp) is a member of the B box zinc finger gene family which possesses a tripartite motif consisting of a RING finger, B box finger, and a coiled-coil domain. Rfp is expressed at specific stages of spermatogenesis and in various adult mouse and human tissues. It becomes oncogenic when the tripartite domain is recombined with the tyrosine kinase domain of the ret protooncogene. Many of the B box family proteins function as homodimers, although the role of the individual components of the tripartite motif in this process remains unclear. We demonstrate that rfp homomultimerization occurs through the coiled-coil domains; however, while the B box is not an interacting interface itself, its structural integrity is necessary for this interaction to occur. This is the first evidence that the B box zinc finger domain is involved in regulating protein-protein interactions. Interestingly, we find that mutations of the RING finger and B box affect the subcellular compartmentalization of rfp in various cell lines. These results demonstrate that the interactions of rfp with itself and its association with specific subcellular compartments is dependent upon the function of all of the components of the tripartite motif. It is likely that these domains play a crucial role in the function of the rfp protein in normal cell differentiation and in its transformation potential in the recombined state.
Band anticrossing in highly mismatched III V semiconductor alloys (2002)

In this paper we review the basic theoretical aspects as well as some important experimental results of the band anticrossing effects in highly electronegativity-mismatched semiconductor alloys, such as GaAs1−xNx and InyGa1−yAs1−xNx. The many-impurity Anderson model treated in the coherent potential approximation is applied to these semiconductor alloys, in which metallic anion atoms are partially substituted by a highly electronegative element at low concentrations. Analytical solutions of the Green's function provide dispersion relations and state broadenings for the restructured conduction bands. The solutions also lead to the physically intuitive and widely used two-level band anticrossing model. Significant experimental observations, including large bandgap reduction, great electron effective mass enhancement and unusual pressure behaviour of the bandgap, are compared with the predictions of the band anticrossing model. The band anticrossing model is extended over the entire Brillouin zone to explain the pressure behaviour of the lowest conduction band minimum in GaP1−xNx. Finally, we show that the band anticrossing can also account for the large bandgap bowing parameters observed in GaAsxSb1−x, InAsySb1−y and GaPxSb1−x alloys.
Bidder's strategy under group-buying auction on the internet (2002)

The group-buying auction is a new kind of dynamic pricing mechanism on the Internet. It is a variant of the sellers' price double auction, which makes the bidders as a group through Internet to get the volume discounts, i.e., the more bidders bid, the lower the price of the object being auctioned becomes. In this paper, we analyze the group-buying auction under some assumptions, such as that the independent private values (IPVs) model applies and bidders are risk neutral and symmetric, etc., and build an incomplete information dynamic game model to illustrate the bidders' bidding process. It proves that for the bidders there exists a weakly dominant strategy S, i.e., no matter when a bidder arrives at the auction and what the bidding history is, the highest permitted bid price that is no greater than his value to the object is always his optimal bid price but may not be the unique one.
Delta-1 enhances marrow and thymus repopulating ability of human CD34+CD38– cord blood cells (2002)

We investigated the effect of Notch signaling, a known regulator of cell fate in numerous developmental systems, on human hematopoietic precursors.We show that activation of endogenous Notch signaling in human CD34 + CD38 -cord blood precursors with immobilized Delta-1 in serum-free cultures containing fibronectin and hematopoietic growth factors inhibited myeloid differentiation and induced a 100-fold increase in the number of CD34 + cells compared with control cultures.Immobilized Delta-1 also induced a multifold expansion of cells with the phenotype of common lymphoid precursors (CD34 + CD7 + CD45RA + ) and promoted the development of cytoplasmic CD3 + T/NK cell precursors.IL-7 enhanced the promotion of T/NK cell differentiation by immobilized Delta-1, but granulocytic differentiation occurred when G-CSF was added.Transplantation into immunodeficient mice showed a substantial increase in myeloid and B cell engraftment in the marrow and also revealed thymic repopulation by CD3 + T cells due to cells being cultured for a longer period with immobilized Delta-1.These data suggest that Delta-1 can enhance myeloid and lymphoid marrow-repopulating ability and promote the generation of thymus-repopulating T cell precursors.
Human dendritic cells express a 95 kDa activation/differentiation antigen defined by CMRF‐56 (1999)

Despite the unique functions of dendritic cells (DC), only two cell surface antigens (CMRF-44 and CD83) with relatively restricted expression on human DC have been described to date. We describe a third mAb, CMRF-56, which recognizes another DC early activation/differentiation antigen with limited expression on other haemopoietic cell populations. Circulating blood leukocytes did not express the CMRF-56 antigen and, following either in vitro culture or activation of PBMC populations, CMRF-56 antigen expression was detected only on DC and a subpopulation of CD19+ lymphocytes. Circulating blood DC were CMRF-56 but induced expression within 6 h of in vitro culture. This, together with the finding that tonsil and synovial fluid DC upregulate the antigen following short-term in vitro culture, confirmed that CMRF-56 recognizes an early activation antigen on DC. Isolated Langerhan's cells, dermal DC, migratory dermal DC and monocyte derived DC (GM-CSF/IL-4/TNFalpha) also express the CMIRF-56 antigen. Antigen modulation studies demonstrated that the amount of cell surface bound CMRF-56 and CMRF-44 (but not CD83) mAb was dramatically reduced by short-term incubation at 37 degrees C. This effect was not due to internalization and the reduction in CMRF-56 binding was a reversible, temperature-dependent process. In contrast, the decrease in CMRF-44 binding was irreversible, suggesting that following ligation the CMRF-44 antigen undergoes an irreversible conformational change or shedding at 37 degrees C. Western blotting confirmed that CMRF-56 recognizes a previously undescribed 95 kDa activation antigen whose cellular distribution and expression kinetics overlaps with, but is clearly distinguishable from, that of the CD83 and CMRF-44 antigens. CMRF-56 therefore provides a useful additional marker for studies on human DC.
Bladder Inhibition by Penile Nerve Stimulation in Spinal Cord Injury Patients (1992)

Detrusor hyperreflexia causing voiding dysfunction in spinal cord injury patients is a difficult problem and is not always treated effectively by anticholinergic agents. We have been investigating electrical stimulation methods to inhibit hyperreflexia and dorsal penile nerve stimulation is the most promising. Six chronic suprasacral spinal cord injury men (average age 36 years) underwent stimulation testing with water cystometry before, during and after stimulation. Dorsal penile stimulation was done with carbon rubber butterfly electrodes (Medtronic) with parameters of 5 pulses per second, 0.35 msec. pulse duration, and current at a level above the threshold for pelvic twitching activity and adjusted for optimal bladder effect (range 25 to 70 mamp.). In all 6 patients the cystometrogram during stimulation showed an increase in bladder volume over the prestimulation cystometrogram (range 27 to 150%). In 2 patients there was no detrusor activity after filling to 500 cc. Stimulation was then stopped and a spontaneous contraction occurred. The cystometrogram conducted after the stimulus also had less volume than that performed during stimulation but it was larger than the prestimulation volume. Penile nerve stimulation was painless with no side effects. Penile nerve electrical stimulation is effective for inhibiting bladder hyperreflexia and should be easily adaptable for chronic home use as an alternative to current therapy.
Stromal Cell–Derived Factor-1 Effects on Ex Vivo Expanded Endothelial Progenitor Cell Recruitment for Ischemic Neovascularization (2003)

These findings indicate that locally delivered SDF-1 augments vasculogenesis and subsequently contributes to ischemic neovascularization in vivo by augmenting EPC recruitment in ischemic tissues.
The Zimbabwean Human Rights Crisis: A Collaborative Approach to International Advocacy (2004)

Over the past several years, a serious human rights crisis has\ndeveloped in Zimbabwe, where President Robert Mugabe\nemploys repressive measures to cling to power. Civil society and\nhuman rights groups in Zimbabwe are among those who have\ncome under attack by the government, and they face an\nextremely difficult challenge in bringing about positive change\nin the country. This article describes the development of the\ncurrent crisis in Zimbabwe, focusing on the problems faced by\nlocal activists and organizations that seek to promote greater\nrespect for human rights. It further discusses one recent\ninitiative launched by the U.S.-based organization Human\nRights First, which organized a consultative meeting of regional\ncivil society groups in August 2003. The article addresses the\nrole that can and should be played by international civil society\norganizations, which must be sensitive to the contextual\ndynamics particular to the Zimbabwean crisis and to the region.\nIf they are to be in any way effective, such organizations must\nact in support of local actors and stronger regional networks.
Pharmacokinetics and Side Effects of Perfluorocarbon-Based Blood Substitutes (1994)

Perfluorochemicals are fluorine-saturated carbon-based molecules which demonstrate utility in the areas of imaging and oxygen delivery. In general, these molecules are biologically inert and, therefore, do not pose toxicologic risk from metabolic degradation. Intravenous (i.v.) perfluorocarbon (PFC) emulsions are cleared from the blood through a process involving phagocytosis of emulsion particles by reticuloendothelial macrophages (RES) and ultimate elimination through the lung in expired air. RES phagocytosis of PFC emulsion particles leads to characteristic, predictable, and reversible biological effects that are a consequence of a normal host-defense mechanism. This mechanism is characterized by dose-related stimulation of macrophages and subsequent release of intracellular products (particularly metabolites of the arachidonic acid cascade and cytokines) which are responsible for most of the biological effects associated with i.v. PFC emulsions (i.e., cutaneous flushing and fever at lower doses, and macrophage hypertrophy and recruitment at higher doses). These biological effects are reversible, and do not result in any permanent tissue alteration, even with prolonged exposure at relatively high doses. The rate of PFC elimination from the RES is proportional to the vapor pressure of the PFC, inversely proportional to molecular weight and positively influenced by lipophilicity. This dose-dependent respiratory excretion occurs with no evidence of metabolic products. Repeated administration of high doses of PFC emulsion may lead to a saturation of the RES-mediated clearance capacity, resulting in a redistribution of PFC to non-RES tissues and ingestion by resident or mobile macrophages. This condition is benign with respect to the integrity of the surrounding parenchyma, as well as to the macrophages themselves. Increased pulmonary residual volume (IPRV) due to pulmonary gas (air) trapping, a reversible side effect, has been observed with i.v. doses of PFC emulsion in some animal species. The gross morphological change associated with IPRV is not accompanied by any histological alteration other than the appearance of vacuolated macrophages (characteristic of the normal clearance mechanism) and some minor, increased interalveolar cellularity. Animal lungs affected by IPRV have a normal, pale pink appearance with no visible lesions or signs of edema. The degree of IPRV is dependent on species, PFC dose, and type of PFC administered; PFCs with higher vapor pressures produce the most severe cases of IPRV in sensitive species. Species sensitivity depends upon physiological and morphological characteristics. There is no evidence indicating that IPRV occurs in humans. Although i.v. PFC emulsions may elicit minor untoward effects, these effects are reversible and, at clinically relevant doses, do not pose a toxicologic risk.
Profound Inhibition of Antigen-Specific T-Cell Effector Functions by Dasatinib (2008)

These findings indicate that caution is warranted with use of this drug in the clinical setting and provide a rationale to explore the potential of dasatinib as an immunosuppressant in the fields of transplantation and T-cell-driven autoimmune diseases.
A Novel Anti-HIV Macrocyclic Peptide from Palicourea condensata (2001)

A 37 amino acid cyclic polypeptide has been isolated from the organic extract of the tropical tree Palicourea condensata. Palicourein (1) is the largest of a growing family of plant peptides that contain a cyclized amino acid backbone cross-linked via three internal disulfide bridges. Palicourein inhibits the in vitro cytopathic effects of HIV-1RF infection of CEM-SS cells with an EC50 value of 0.1 microM and an IC50 value of 1.5 microM.
Update: Systemic Radiotherapy Can Cure Lymphoma: A Paradigm for Other Malignancies? (2008)

The cytocidal potency of a molecule can be augmented by conjugating a radionuclide for molecular targeted radionuclide therapy (MTRT) for cancer. Radioimmunotherapy (RIT) should be incorporated into the management of patients with B-cell non-Hodgkin's lymphoma (NHL) soon after the patients have proven incurable. Better drugs, strategies, and combinations with other drugs seem certain to make RIT integral to the management of patients with NHL and likely to lead to a cure of the currently incurable NHL. These improved drugs, strategies, and combinations thereof also offer opportunities for RIT to become part of the management of solid malignancies, including epithelial cancers. Smaller radionuclide carriers, such as those used for pretargeted strategies, provide dose intensification. The potential of pretargeted RIT to improve patient outcomes is striking.
A New General Pressure-Analysis Procedure for Slug Tests (1993)

Summary A new analysis procedure for determining formation flow capacity and skin factor from slug-test data is presented. The procedure arises from exact deconvolution equations that convert measured slug-test pressure data into equivalent pressure and pressure-derivative responses that would be obtained if the well were produced at a constant surface flow rate. The converted data then can be analyzed by use of existing wellbore-storage and skin type curves for the particular reservoir or well model represented by the field data. For cases where the slug test is short, we show that flow rate convolution can be incorporated to improve analysis reliability. The analysis procedures do not require direct knowledge of the sandface flow rate.
Practical Batch-Updatable External Hashing with Sorting (2013)

This paper presents a practical external hashing scheme that supports fast lookup (7 microseconds) for large datasets (millions to billions of items) with a small memory footprint (2.5 bits/item) and fast index construction (151 K items/s for 1-KiB key-value pairs). Our scheme combines three key techniques: (1) a new index data structure (Entropy-Coded Tries); (2) the use of sorting as the main data manipulation method; and (3) support for incremental index construction for dynamic datasets. We evaluate our scheme by building an external dictionary on flash-based drives and demonstrate our scheme's high performance, compactness, and practicality.
Cloning and DNA sequencing of the dextranase inhibitor gene (dei) from Streptococcus sobrinus (1994)

Some dextranase-deficient (Dex-) mutants of Streptococcus sobrinus UAB66 (serotype g) synthesize a substance which inhibits dextranase activity (S.-Y. Wanda, A. Camilli, H. M. Murchison, and R. Curtiss III, J. Bacteriol. 176:7206-7212, 1994). This substance produced by the Dex- mutant UAB108 was designated dextranase inhibitor (Dei) and identified as a protein. The Dei gene (dei) from UAB108 has been cloned into pACYC184 to yield pYA2651, which was then used to generate several subclones (pYA2653 to pYA2657). The DNA sequence of dei was determined by using Tn5seq1 transposon mutagenesis of pYA2653. The open reading frame of dei is 990 bp long. It encodes a signal peptide of 38 amino acids and a mature Dei protein of 292 amino acids with a molecular weight of 31,372. The deduced amino acid sequence of Dei shows various degrees of similarity with glucosyltransferases and glucan-binding protein and contains A and C repeating units probably involved in glucan binding. Southern hybridization results showed that the dei probe from UAB108 hybridized to the same-size fragment in S. sobrinus (serotype d and g) DNA, to a different-size fragment in S. downei (serotype h) and S. cricetus (serotype a), and not at all to DNAs from other mutans group of streptococci.
The hub and spoke paradigm for CSR evaluation (1994)

In this paper, we introduce the new paradigm used in the most recent ARPA-sponsored Continuous Speech Recognition (CSR) evaluation and then discuss the important features of the test design.The 1993 CSR evaluation was organized in a novel fashion in an attempt to accomodate research over a broad variety of important problems in CSR while maintaining a clear program-wide research focus. Furthermore, each test component in the evaluation was designed as an experiment to extract as much information as possible from the results.The evaluation was centered around a large vocabulary speaker-independent (SI) baseline test, which was required of every participating site. This test was dubbed the 'Hub' since it was common to all sites and formed the basis for controlled inter-system comparisons.The Hub test was augmented with a variety of problem-specific optional tests designed to explore a variety of important problems in CSR, mostly involving some kind of mismatch between the training and test conditions. These tests were known as the 'Spokes' since they all could be informatively compared to the Hub, but were otherwise independent.In the first trial of this evaluation paradigm in November, 1993, 11 research groups participated, yielding a rich array of comparative and contrastive results, all calibrated to the current state of the art in large vocabulary CSR.
Crucial roles of binding sites for NF-κB and C/EBPs in IκB-ζ-mediated transcriptional activation (2007)

IkappaB-zeta [inhibitor of NF-kappaB (nuclear factor kappaB) zeta] is a nuclear protein that is induced upon stimulation of TLRs (Toll-like receptors) and IL (interleukin)-1 receptor. IkappaB-zeta harbours C-terminal ankyrin repeats that interact with NF-kappaB. Our recent studies have shown that, upon stimulation, IkappaB-zeta is essential for the induction of a subset of inflammatory genes, represented by IL-6, whereas it inhibits the expression of TNF (tumour necrosis factor)-alpha. In the present study, we investigated mechanisms that determine the different functions of IkappaB-zeta. We found that co-expression of IkappaB-zeta and the NF-kappaB subunits synergistically activates transcription of the hBD-2 (human beta-defensin 2) and NGAL (neutrophil gelatinase-associated lipocalin) genes, whereas it inhibits transcription of E-selectin. Reporter analyses indicated that, in addition to an NF-kappaB-binding site, a flanking C/EBP (CCAAT/enhancer-binding protein)-binding site in the promoters is essential for the IkappaB-zeta-mediated transcriptional activation. Using an artificial promoter consisting of the NF-kappaB- and C/EBP-binding sites, transcriptional activation was observed upon co-transfection with IkappaB-zeta and NF-kappaB, indicating that these sequences are minimal elements that confer the IkappaB-zeta-mediated transcriptional activation. Chromatin immunoprecipitation assays and knockdown experiments showed that both IkappaB-zeta and the NF-kappaB subunits were recruited to the NGAL promoter and were essential for the transcriptional activation of the hBD-2 and NGAL promoters on stimulation with IL-1beta. The activation of the NGAL promoter by transfection of IkappaB-zeta and NF-kappaB was suppressed in C/EBPbeta-depleted cells. Thus IkappaB-zeta acts as an essential transcriptional activator by forming a complex with NF-kappaB on promoters harbouring the NF-kappaB- and C/EBP-binding sites, upon stimulation of TLRs or IL-1 receptor.
Software defined networking and virtualization for broadband satellite networks (2015)

Satellite networks have traditionally been considered for specific purposes. Recently, new satellite technologies have been pushed to the market enabling high-performance satellite access networks. On the other hand, network architectures are taking advantage of emerging technologies such as software-defined networking (SDN), network virtualization and network functions virtualization (NFV). Therefore, benefiting communications services over satellite networks from these new technologies at first, and their seamless integration with terrestrial networks at second, are of great interest and importance. In this paper, and through comprehensive use cases, the advantages of introducing network programmability and virtualization using SDN and/or NFV in satellite networks are investigated. The requirements to be fulfilled in each use case are also discussed.