gebhart/patrepeval huggingface dataset:
3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation (1988)

3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural test these compounds were effective in reducing exudate volume and accumulation of white blood cells. This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin. The structural requirements for inhibiting the Arthus reactions were studied by systematic chemical modification of 1. These structure-activity relationship studies revealed that nitrogen 1' of the hydrazino group is essential for activity and must be electron rich, whereas chemical modifications of other sites of 1 had only a modest effect on activity.
Unraveling the biological significance of nitric oxide. (1990)

Independent investigations into the biochemical changes and cytostatic properties induced in immunostimulated macrophages and studies involving the identity and mechanism of action of endothelium-derived relaxing factor led to the finding of a new metabolic pathway which converts L-arginine to nitric oxide and citrulline. The pathway has since been reported in a number of additional cell types including cells in the central nervous system (CNS). In the endothelium and CNS nitric oxide is acting as a signaling agent with the evidence supporting activation of the enzyme guanylate cyclase in the target cell. Nitric oxide is toxic and evidence supports a cytostatic/cytotoxic function as the primary action of macrophage-derived nitric oxide.
Design Considerations of Silicon Nanowire Biosensors (2007)

Biosensors based on silicon nanowires (Si-NWs) promise highly sensitive dynamic label-free electrical detection of biomolecules. Despite the tremendous potential and promising experimental results, the fundamental mechanism of electrical sensing of biomolecules and the design considerations of NW sensors remain poorly understood. In this paper, we discuss the prospects and challenges of biomolecule detection using Si-NW biosensors as a function of device parameters, fluidic environment, charge polarity of biomolecules, etc., and refer to experimental results in literature to support the nonintuitive predictions wherever possible. Our results indicate that the design of Si nanobiosensor is nontrivial and as such, only careful optimization supported by numerical simulation would ensure optimal sensor performance.
Power-efficient software (2010)

Power-manageable hardware can help save energy, but what can software developers do to address the problem?
Enhancement of microwave tomography through the use of electrically conducting enclosures (2008)

We consider microwave tomography (MWT) where the imaging region is surrounded by an electrically conducting surface. This surface acts as both a shield from outside interference, holding tank for any possible matching media, and, in certain cases, serves to enhance the performance of electromagnetic (EM) inversion algorithms. For the 2D transverse magnetic (TM) case and where the surface consists of a perfect electrical conductor (PEC) in the shape of a circular cylinder, we formulate an appropriate Greens function which is amenable to implementation in the existing EM inversion codes. We utilize this Greens function in the multiplicative-regularized contrast source inversion (MR-CSI) method. Several different synthetic examples are used to test the performance of the inversion when the PEC surface is present and the results show that in many cases, the tomographic image is significantly improved. The reasons for the improved inversion results are an area of active research, but are likely to be due to the increased interrogation energy deposited into the imaging region. Results are also shown which demonstrate the problems which may arise if the unbounded domain Greens function is used in an MWT system that utilizes a matching medium of finite extent—a problem which is overcome by the inclusion of a PEC surface on the exterior of the MWT system.
CD14+CD16+ monocytes in coronary artery disease and their relationship to serum TNF-α levels (2004)

Monocytes play a central role in the inflammatory disease atherosclerosis. CD14+CD16+ monocytes are considered proinflammatory monocytes, as they have an increased capacity to produce proinflammatory cytokines, such as TNF-alpha, and are elevated in various inflammatory diseases. We hypothesized that patients with coronary artery disease (CAD) have increased levels of CD14+CD16+ monocytes, and that CD14+CD16+ monocytes are associated with inflammation markers. We investigated CD14+CD16+ monocytes in 247 patients with CAD and 61 control subjects using flow cytometry. In addition serum concentrations of TNF-alpha, IL-6, and Hs-CRP were assessed. Patients with CAD had higher levels of CD14+CD16+ monocytes than controls (13.6% versus 11.4%; p<0.001). Logistic regression analysis including quartiles of CD14+CD16+ monocytes showed that CD14+CD16+ monocytes were associated with prevalence of CAD (OR 4.9, 95% CI 2.5-19.1, for subjects in the fourth quartile in comparison to subjects in the first quartile). The association between CD14+CD16+ monocytes and CAD remained independently significant after adjustment for most potential confounders (OR 5.0, 95% CI 1.2-20.0). Serum concentrations of TNF-alpha were elevated in subjects within the highest quartiles of CD14+CD16+ monocytes (p=0.018). Our study showed that increased numbers of CD14+CD16+ monocytes are associated with coronary atherosclerosis and TNF-alpha. In accordance, recent animal studies suggest a possibly important role of these monocytes in the development of atherosclerosis.
Diversity and freedom: a fundamental tradeoff in multiple antenna channels (2003)

Multiple antennas can be used for increasing the amount of diversity or the number of degrees of freedom in wireless communication systems. We propose the point of view to study the tradeoff between the two types of gains. In this paper, we present the complete results on the optimal tradeoff, and give a brief discussion on the techniques used to get the results.
Effects of Microrna-29 on Apoptosis, Tumorigenicity, and Prognosis of Hepatocellular Carcinoma (2009)

Our data highlight an important role of miR-29 in the regulation of apoptosis and in the molecular etiology of HCC, and implicate the potential application of miR-29 in prognosis prediction and in cancer therapy.
Substrate phosphorylation specificity of the human c-kit receptor tyrosine kinase. (1991)

The chimeric EK-receptor (EK-R), consisting of the epidermal growth factor receptor (EGF-R) extracellular binding domain and p145c-kit cytoplasmic signal-generating sequences, was fully functional in forming high and low affinity EGF binding sites and in ligand-regulated receptor and substrate phosphorylation activities. Relative to EGF-R, EK-R activation stimulated kit-characteristic phosphorylation of human 293 fibroblast substrate polypeptides. Transient coexpression of EK-R with candidate substrates resulted in ligand-induced phosphorylation of phospholipase C gamma and guanosine triphosphatase-activating polypeptide. The RAF-1 serine/threonine kinase was shown to be associated with activated EK-R, but no tyrosine phosphorylation could be detected. The faithfulness of EK-R substrate phosphorylation specificity was confirmed with stem cell factor-stimulated p145c-kit.
Chemokines and HIV-1 second receptors: The therapeutic connection (1998)

The discovery that HIV requires a chemokine co-receptor to invade host cells has prompted many investigations into therapeutic strategies that target these receptors in an attempt to block HIV entry. In this review, Scott Cairns and Patricia D'Souza discuss these potentially powerful approaches and how they complement existing antiretroviral drug therapy.
ChemInform Abstract: 1,3‐DICYCLOHEXYL‐5‐ALKYL‐5‐AMINOMETHYLBARBITURIC ACIDS AS POTENTIAL ANTIINFLAMMATORY AGENTS (1978)

The synthesis and the structure of 1,3-dicyclohexyl-5-alkyl-5-aminomethylbarbituric acids, obtained by the Mannich reaction, are described. Some of the obtained compounds showed a strong antiinflammatory activity in biological tests.
Gene expression pathways of high grade localized prostate cancer (2011)

In addition to androgen receptor signaling, growth factor, and cytokine mediated pathways are active in clinically localized high grade prostate cancer. The availability of therapeutics that selectively target these pathways encourages the development of clinical trials for their selective use in the neoadjuvant or adjuvant setting in men at high risk for disease progression.
In Situ Synthesis of Three-Dimensional Self-Assembled Metal Oxide–Reduced Graphene Oxide Architecture (2014)

The fabrication of self-assembled, three-dimensional (3-D) graphene structures is recognized as a powerful technique for integrating various nanostructured building blocks into macroscopic materials. In this way, nanoscale properties can be harnessed to provide innovative functionalities of macroscopic devices with hierarchical microstructures. To this end, we report on the fabrication of a three-dimensional (3-D) metal oxide (MO)–reduced graphene oxide (RGO) architecture by controlling the reduction conditions of graphene oxide. In this structure, SnO2 nanoparticles with dimensions of 2–3 nm are uniformly anchored and supported on a 3-D RGO structure. The resulting composite exhibits excellent rate capability as a binder-free electrode and shows great potential for use in Li-ion batteries. Furthermore, the proposed reduction synthesis can also be applied to the study of the synergetic properties of other 3-D MO–RGO architectures.
The Formation of Dimensionally Ordered Silicon Nanowires within Mesoporous Silica (2000)

ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTThe Formation of Dimensionally Ordered Silicon Nanowires within Mesoporous SilicaNicholas R. B. Coleman, M. A. Morris, Trevor R. Spalding, and Justin D. HolmesView Author Information Department of Chemistry and Supercritical Fluid Centre University College Cork, Cork, Ireland Cite this: J. Am. Chem. Soc. 2001, 123, 1, 187–188Publication Date (Web):December 8, 2000Publication History Received11 September 2000Published online8 December 2000Published inissue 1 January 2001https://pubs.acs.org/doi/10.1021/ja005598phttps://doi.org/10.1021/ja005598prapid-communicationACS PublicationsCopyright © 2001 American Chemical SocietyRequest reuse permissionsArticle Views1184Altmetric-Citations122LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose SUBJECTS:Nanowires,Physical and chemical processes,Porous materials,Silica,Silicon Get e-Alerts
The BH3-mimetic GX15-070 synergizes with bortezomib in mantle cell lymphoma by enhancing Noxa-mediated activation of Bak (2007)

Mantle cell lymphoma (MCL) is an aggressive B-cell lymphoma resistant to conventional chemotherapy. The Bcl-2 pathway is deregulated in these tumors and may represent an interesting target for new therapeutic strategies. The new small-molecule pan-Bcl-2 inhibitor GX15-070 mimics BH3-only proteins by binding to multiple antiapoptotic Bcl-2 members. Here we show that GX15-070 induced apoptosis in vitro in MCL cell lines and primary cells from patients with MCL by releasing Bak from Mcl-1 and Bcl-X(L) at short incubation times and low micromolar doses. GX15-070 was effective in cells bearing defective DNA damage-sensor genes or cell-cycle regulators, inducing Bax and Bak conformational changes, mitochondrial depolarization, phosphatidylserine exposure, and caspase-3 activation. Furthermore, GX15-070 synergized with bortezomib, sensitizing MCL cells to low doses of this proteasome inhibitor, by neutralizing bortezomib-induced Mcl-1 accumulation and cooperating with Noxa to induce Bak displacement from this protein. These events led to an increased activation of the mitochondrial apoptotic pathway. Importantly, GX15-070 alone or in combination with bortezomib showed no significant cytotoxic effect in peripheral blood mononuclear cells from healthy donors. All these findings suggest that GX15-070 alone or in combination with bortezomib represents a new attractive therapeutic approach for MCL treatment.
Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 1. 2-[2-(1-Imidazolyl)alkyl]-1(2H)-phthalazinones (1993)

A number of 4-substituted 2-[omega-(1-imidazolyl)alkyl]-1(2H)-phthalazinones were synthesized in order to develop agents possessing both thromboxane A2 synthetase inhibitory and bronchodilatory activities. The pharmacological evaluation of these compounds disclosed that they have both activities to various extents. Both activities were slightly dependent on the length of the 2-substituents and largely affected by the nature of the 4-substituents. Compounds bearing phenyl and thienyl groups exhibited relatively high and well-rounded activities. Among these compounds, 12j and 15f were found to be the most effective agents having well-rounded activities in vitro and in vivo. Introduction of a carboxyl group reduced both activities contrary to our expectation. 4-(3-Pyridyl)phthalazinone 18b was of particular interest because of unexpectedly high in vivo activities in spite of an absence of significant in vitro activities.
Mutation of Phosphoserine 389 Affects p53 Function in Vivo (1996)

To study the importance of phosphorylation for p53 transactivation function, we generated mutations at each of its known phosphorylated serine amino acids. Mutations of murine p53 serine residues individually to either alanine or glutamic acid at positions 7, 9, 12, 18, 37, 312, and 389 resulted in equivalent levels of transcriptional activation in standard transient transfection experiments. However, when p53 transcriptional activity was measured in cells that attain G1 arrest upon contact inhibition, wild-type p53 was inactive, and only alteration at serine 389 to glutamic acid resulted in a functional p53 protein. This Ser --> Glu mutant also has an increased ability to bind DNA. Elimination of the phosphorylation site by substitution of an alanine amino acid resulted in loss of transcriptional activity. We also demonstrated that specific phosphorylation of p53 at serine 389 is induced by cyclin E overexpression in high-density cells. Our data establish for the first time that phosphorylation of p53 at serine 389 is important in activating its function in vivo.
Ultrasound-induced acoustophoretic motion of microparticles in three dimensions (2013)

We derive analytical expressions for the three-dimensional (3D) acoustophoretic motion of spherical microparticles in rectangular microchannels. The motion is generated by the acoustic radiation force and the acoustic streaming-induced drag force. In contrast to the classical theory of Rayleigh streaming in shallow, infinite, parallel-plate channels, our theory does include the effect of the microchannel side walls. The resulting predictions agree well with numerics and experimental measurements of the acoustophoretic motion of polystyrene spheres with nominal diameters of 0.537 and 5.33 μm. The 3D particle motion was recorded using astigmatism particle tracking velocimetry under controlled thermal and acoustic conditions in a long, straight, rectangular microchannel actuated in one of its transverse standing ultrasound-wave resonance modes with one or two half-wavelengths. The acoustic energy density is calibrated in situ based on measurements of the radiation dominated motion of large 5-μm-diameter particles, allowing for quantitative comparison between theoretical predictions and measurements of the streaming-induced motion of small 0.5-μm-diameter particles.
Contribution of adenosine A2 receptors and cyclic adenosine monophosphate to protective ischemic preconditioning of sinusoidal endothelial cells against storage/reperfusion injury in rat livers (2000)

A brief period of liver ischemia decreases sinusoidal endothelial cell killing after cold liver storage and improves graft survival after liver transplantation, a phenomenon called ischemic preconditioning. In this study, we investigated the mechanism of sinusoidal endothelial cell protection after ischemic preconditioning. Livers were preconditioned by 5 minutes of ischemia and 5 minutes of reperfusion. Subsequently, livers were stored for 30 hours in cold University of Wisconsin (UW) solution and reperfused briefly with physiological buffer containing Trypan blue. Ischemic preconditioning decreased sinusoidal endothelial cell killing after storage/reperfusion, as assessed by Trypan blue staining of nonparenchymal cells. Adenosine A(2) receptor blockade prevented the protective effect of ischemic preconditioning. By contrast, adenosine A(1) receptor blockade did not prevent protective ischemic preconditioning. Other rat livers were treated with adenosine A(1) and A(2) receptor agonists or dibutyryl-cyclic adenosine monophosphate (DB-cAMP) before storage. The adenosine A(2) receptor agonist, CGS-21680, and DB-cAMP decreased sinusoidal endothelial cell killing to the same extent as ischemic preconditioning, but the adenosine A(1) receptor agonist, 2-chloro-N(6)-cyclopentyladenosine (CCPA), had no effect. The adenosine A(2) agonist and prostaglandin E(2), another agent that preconditions sinusoidal endothelial cells against storage/reperfusion injury, but not the adenosine A(1) agonist, increased cAMP levels in cultured sinusoidal endothelial cells. In conclusion, an adenosine A(2) receptor pathway coupled to increased cAMP mediates sinusoidal endothelial cell protection by ischemic preconditioning.
Potential Purine Antagonists. VI. Synthesis of 1-Alkyl- and 1-Aryl-4-substituted Pyrazolo[3,4-d]pyrimidines1,2 (1956)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPotential Purine Antagonists. VI. Synthesis of 1-Alkyl- and 1-Aryl-4-substituted Pyrazolo[3,4-d]pyrimidines1,2C. C. CHENG and ROLAND K. ROBINSCite this: J. Org. Chem. 1956, 21, 11, 1240–1256Publication Date (Print):November 1, 1956Publication History Published online1 May 2002Published inissue 1 November 1956https://pubs.acs.org/doi/10.1021/jo01117a010https://doi.org/10.1021/jo01117a010research-articleACS PublicationsRequest reuse permissionsArticle Views1260Altmetric-Citations154LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Binuclear complexes of nickel bridged by hydrocarbon ligands. Isocyanide insertion chemistry and amide formation by intramolecular coupling of acyl and imidoyl functionalities (1992)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTBinuclear complexes of nickel bridged by hydrocarbon ligands. Isocyanide insertion chemistry and amide formation by intramolecular coupling of acyl and imidoyl functionalitiesJuan Campora, Ernesto Carmona, Enrique Gutierrez, Pilar Palma, Manuel L. Poveda, and Caridad RuizCite this: Organometallics 1992, 11, 1, 11–13Publication Date (Print):January 1, 1992Publication History Published online1 May 2002Published inissue 1 January 1992https://pubs.acs.org/doi/10.1021/om00037a006https://doi.org/10.1021/om00037a006research-articleACS PublicationsRequest reuse permissionsArticle Views143Altmetric-Citations22LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
High-speed fiber–based polarization-sensitive optical coherence tomography of in vivo human skin (2000)

A high-speed single-mode fiber-based polarization-sensitive optical coherence tomography (PS OCT) system was developed. With a polarization modulator, Stokes parameters of reflected flight for four input polarization states are measured as a function of depth. A phase modulator in the reference arm of a Michelson interferometer permits independent control of the axial scan rate and carrier frequency. In vivo PS OCT images of human skin are presented, showing subsurface structures that are not discernible in conventional OCT images. A phase retardation image in tissue is calculated based on the reflected Stokes parameters of the four input polarization states.
Preferential potentiation of topoisomerase I poison cytotoxicity by PARP inhibition in S phase (2014)

Rucaparib preferentially sensitises S-phase cells by increasing the frequency of collapsed replication forks.