gebhart/patrepeval huggingface dataset:
Tumor‐promoting activity of 2,4‐dinitrofluorobenzene (1995)

The aim of this study was to determine whether the skin-sensitizing agent 2,4-dinitrofluorobenzene (DNFB) would elicit the same morphological and biochemical events that are characteristic of 12-O-tetradecanoylphorbol-13-acetate (TPA). While single applications of 0.1% or 0.2% DNFB produced only mild epidermal hyperplasia, multiple applications produced pronounced hyperplasia. Compared with TPA, a single application of DNFB produced small increases in ODC activity, although a second DNFB treatment produced a greater response. Both DNFB and TPA caused marked induction of ODC, c-fos and c-jun mRNA. Vascular permeability increased significantly in response to DNFB, such that after 15 hr the response was quantitatively the same as for TPA. Repeated TPA produced the same response as a single application, but repeated DNFB resulted in a response that was half that of TPA. In contrast to TPA, DNFB failed to activate partially purified protein kinase C (PKC), although it did cause transient down-regulation of activity 15 hr after treatment. The ability of DNFB to induce ODC activity, however, was unaffected by prior down-regulation of PKC. DNFB was also shown to promote tumors in initiated SSIN mice. Twice-weekly applications of 0.1% or 0.2% DNFB resulted in approximately 65% and 85% of the mice developing an average of 2.0 or 3.2 tumors each, respectively. These results demonstrate that DNFB elicits many of the same changes as TPA and that it does so in a PKC-independent manner.
Input–output organization of jaw movement‐related areas in monkey frontal cortex (2005)

The brain mechanisms underlying mastication are not fully understood. To address this issue, we analyzed the distribution patterns of cortico-striatal and cortico-brainstem axon terminals and the origin of thalamocortical and intracortical fibers by injecting anterograde/retrograde tracers into physiologically and morphologically defined jaw movement-related cortical areas. Four areas were identified in the macaque monkey: the primary and supplementary orofacial motor areas (MIoro and SMAoro) and the principal and deep parts of the cortical masticatory area (CMaAp and CMaAd), where intracortical microstimulation produced single twitch-like or rhythmic jaw movements, respectively. Tracer injections into these areas labeled terminals in the ipsilateral putamen in a topographic fashion (MIoro vs. SMAoro and CMaAp vs. CMaAd), in the lateral reticular formation and trigeminal sensory nuclei contralaterally (MIoro and CMaAp) or bilaterally (SMAoro) in a complex manner of segregation vs. overlap, and in the medial parabranchial and Kölliker-Fuse nuclei contralaterally (CMaAd). The MIoro and CMaAp received thalamic projections from the ventrolateral and ventroposterolateral nuclei, the SMAoro from the ventroanterior and ventrolateral nuclei, and the CMaAd from the ventroposteromedial nucleus. The MIoro, SMAoro, CMaAp, and CMaAd received intracortical projections from the ventral premotor cortex and primary somatosensory cortex, the ventral premotor cortex and rostral cingulate motor area, the ventral premotor cortex and area 7b, and various sensory areas. In addition, the MIoro and CMaAp received projections from the three other jaw movement-related areas. Our results suggest that the four jaw movement-related cortical areas may play important roles in the formation of distinctive masticatory patterns.
Inhibition of Terminal Complement Complex Formation and Cell Lysis by Monoclonal Antibodies (1991)

Three monoclonal antibodies (mabs), two against C5 and one against C6, were identified and characterized. They inhibited the generation of the terminal complement complex (TCC) in serum to over 90% as assayed by a sensitive ELISA based on a neoepitope-specific mab, which recognized TCC-integrated C9. The haemolytic function of the TCC was markedly reduced by all three mabs implying that they are directed to epitopes on C5 and C6 which are essential for TCC formation in both the fluid phase and on erythrocyte membranes. Since the generation of C5a was also impaired by these mabs, they may serve as tools in investigations of the sequelae of the generation of C5a and of TCC.
High-Extraction-Efficiency Blue Light-Emitting Diode Using Extended-Pitch Photonic Crystal (2004)

We have integrated the surface photonic crystal (PhC) on GaN-based blue light-emitting diodes (LEDs) for the first time in order to enhance the extraction efficiency of the LEDs. With the finite-difference time-domain method, we have calculated 3.6-fold enhancement in light output. The theoretical calculations have revealed that the optimum pitch of the PhC is much longer than the emission wavelength when the distance between the PhC and the active layer of LEDs is short. This design enables PhC formation on chemically stable GaN surfaces. In addition, an indium tin oxide (ITO)-based transparent electrode is formed directly on the surface of PhC to realize light emission from the whole area of the LED. The fabricated PhCs have increased the light output of blue LEDs by 1.5 times compared with the LEDs without PhC. We have demonstrated that PhC will realize highly efficient solid-state lighting with GaN-based LEDs.
P-glycoprotein and multidrug resistance-associated protein are involved in the regulation of extracellular levels of the major antiepileptic drug carbamazepine in the brain (2001)

Despite considerable advances in the pharmacotherapy of epilepsy, about 30% of epileptic patients are refractory to antiepileptic drugs (AEDs). In most cases, a patient who is resistant to one major AED is also refractory to other AEDs, although these drugs act by different mechanisms. The mechanisms that lead to drug resistance in epilepsy are not known. Recently, over-expression of multidrug transporters, such as P-glycoprotein (PGP) and multidrug resistance-associated protein (MRP), has been reported in surgically resected epileptogenic human brain tissue and suggested to contribute to the drug resistance of epilepsy. However, it is not known to what extent multidrug transporters such as PGP or MRP are involved in transport of AEDs. In the present study, we used in vivo microdialysis in rats to study whether the concentration of carbamazepine in the extracellular fluid of the cerebral cortex can be enhanced by inhibition of PGP or MRP, using the PGP inhibitor verapamil and the MRP inhibitor probenecid. Local perfusion with verapamil or probenecid via the microdialysis probe increased the extracellular concentration of carbamazepine. The data indicate that both PGP and MRP participate in the regulation of extracellular brain concentrations of the major AED carbamazepine.
Influence of coagulation factor, vitamin K epoxide reductase complex subunit 1, and cytochrome P450 2C9 gene polymorphisms on warfarin dose requirements (2006)

Polymorphisms in warfarin drug target and metabolizing enzyme genes, in addition to nongenetic factors, were important determinants of warfarin dose requirements.
Parameters for direct cortical electrical stimulation in the human: histopathologic confirmation (1990)

Safe parameters for electrical cortical stimulation in humans are difficult to estimate from the animal experimental literature. We therefore examined the light microscopic histology at a total of 11 sites of direct subdural electrical stimulation, taken as part of anterior temporal lobectomies in 3 patients. Stimulations had been done through 3.175 mm diameter electrodes, with 0.3 msec square wave pulses of alternating polarity at 50 pulses/sec. In 2 patients, one site each had been used as a common reference for stimulation, receiving over 251 stimulation trials, most of 2-5 sec duration, at currents of 12.5-15.0 mA, 1 day prior to resection. The maximum charge per phase was 4.0-4.4 microC; the maximum charge density was 52-57 microC per geometric cm2 per pulse at the electrode surfaces. Comparison of hematoxylin and eosin, periodic acid-Schiff, and cresyl violet-stained material from the electrode sites with that from other regions did not show any histologic abnormalities attributable to the electrical stimulation. The relatively brief and intermittent periods utilized for human stimulation testing do not appear to cause structural damage at the light microscopic level at charge densities that exceed the threshold for damage established in animal studies with more continuous, chronic stimulation schedules.
Visualizing Things in Construction Photos: Time, Spatial Coverage, and Content for Construction Management (2009)

PhotoScope, a novel visualization, visualizes the spatiotemporal coverage of photos in a construction photo collection. It extends the standard photo browsing paradigm in two main ways: visualizing spatial coverage of photos on floor plans, and indexing photos by a combination of spatial coverage, time, and content specifications. This approach enables users to browse and search spaceand time-indexed photos more effectively. We designed PhotoScope specifically to address challenges in the construction management industry, where large photo collections are amassed to document project progress. These ideas may also apply to any photo collection that is spatially constrained and must be searched using spatial, temporal, and content criteria. Design choices made when developing PhotoScope are also described. Civil, mechanical and electrical engineers, and professionals from construction management validated the visualization mechanisms and functionalities of PhotoScope in a usability study. Empirical findings on the cognitive behaviors of participants are also discussed in this thesis.
Fatty acid synthase inhibition with Orlistat promotes apoptosis and reduces cell growth and lymph node metastasis in a mouse melanoma model (2008)

Fatty acid synthase (FASN) is the enzyme responsible for the endogenous synthesis of the saturated fatty acid palmitate. In contrast to most normal cells, malignant cells depend on FASN activity for growth and survival. In fact, FASN is overexpressed in a variety of human cancers including cutaneous melanoma, in which its levels of expression are associated with a poor prognosis and depth of invasion. Here, we show that the specific inhibition of FASN activity by the antiobesity drug Orlistat or siRNA is able to significantly reduce proliferation and promote apoptosis in the mouse metastatic melanoma cell line B16-F10. These results prompted us to verify the effect of FASN inhibition on the metastatic process in a model of spontaneous melanoma metastasis, in which B16-F10 cells injected in the peritoneal cavity of C57BL/6 mice metastasize to the mediastinal lymph nodes. We observed that mice treated with Orlistat 48 hr after the inoculation of B16-F10 cells exhibited a 52% reduction in the number of mediastinal lymph node metastases, in comparison with the control animals. These results suggest that FASN activity is essential for B16-F10 melanoma cell proliferation and survival while its inactivation by Orlistat significantly reduces their metastatic spread. The chemical inhibition of FASN activity could have a potential benefit in association with the current chemotherapy for melanoma.
Quantitative Measurement of Cell-Cell Adhesion Under Flow Conditions (2003)

Cell-cell and cell-matrix contacts play an important role in immunological processes and tissue organization. It has been shown that in many cases, cell adhesion is mediated by specialized adhesion receptors that are typically anchored in the cell membrane with mol wt ranging from 50 to 200 kDa. Binding of adhesion receptors anchored in the apposing cell membranes with their counterligands appears to be critical for many forms of cell-cell communication (1).
A novel, simple method for the preparation of hindered diphenyl ethers (1988)

The displacement of the nitro group from substituted nitrobenzenes is used for the synthesis of diphenyl ethers. 1,4-Dinitrobenzene has been converted into a variety of hindered diphenyl ethers using 2,6-disubstituted phenoxides and studies show that the mechanism of formation of the ether (5a) is radical in nature.
Therapeutics targeting signal transduction for patients with colorectal carcinoma (2002)

The cytotoxics developed for the treatment of patients with advanced colorectal cancer have yielded diminishing returns. Agents aimed at novel molecular targets are required to improve the prognosis of this disease. This review describes the most recent advances in the clinical development of therapies designed to block the function of several important signalling cellular proteins. Therapies discussed include agents targeting: (i) the epidermal growth factor receptor (EGFR) family; (ii) Ras via the inhibition of farnesyltransferase; (iii) Raf kinase; (iv) the mitogen-activated protein kinase pathway (MAPK, MEK, Erk); (v) Akt; and (vi) the apoptosis signalling pathways including NF-kappaB, Bcl-2 and the TRAIL receptor. The results of clinical trials of the first generation of such therapeutics to enter clinical evaluation in malignant diseases are presented. Potential advantages and disadvantages of these different therapeutic modalities are discussed and future challenges for the evaluation of these targeted agents in the clinic is presented.
Reaction of AcylketeneS,N-Acetals with Malonyl Chloride: Synthesis of Novel 1,5-Substituted 4-Hydroxy-6-methylthio-2 (1H)-pyridones and 6,8-Substituted 4-Hydroxy-7-methylthio-2,5-dioxo-5,6-dihydro-2H-pyrano [3,2-c] pyridines (1988)

The acylketene S,N-acetals 1 react with one equivalent of malonyl chloride in the presence of triethylamine to give novel 1,5-substituted 4-hydroxy-6-methylthio-2(1H)-pyridones 3 in good yields. However, in the presence of excess of malonyl chloride (three equivalents), the reaction proceeds further to give the corresponding pyrano[3,2-c] pyridones derivatives 4 in moderate yields.
Controlled Mechanical Stimulation in the Treatment of Tibial Fractures (1989)

Although it is known that the mechanical environment affects the fracture healing process, the optimal conditions for the different stages of healing have not been defined. In the present studies, the influence of applying a very short period of axial micromovement with defined characteristics to healing fractures has been studied both in simulated and clinical tibial fractures. The fracture healing process is seen to be acutely sensitive to small periods of daily strain applied axially within two weeks of fracture. There are boundaries of strain magnitude and force of application of applied movement that, if exceeded, inhibit the healing process. The application of appropriate applied strain to clinical tibial fractures at a time shortly after injury, when most patients would be very inactive, appears to enhance the healing process when using external skeletal fixation.
Proapoptotic effects of NARC 1 (= PCSK9), the gene encoding a novel serine proteinase (2006)

The mechanism by which NARC 1-EGFP over-expression induces cell death in cultured CGNs remains unclear. Mutation analysis established a positive correlation between the presence of the Narc 1 active site serine in the transiently expressed protein and induction of the BAF-sensitive component of the cell death phenotype. A caspase-independent component proved sufficiently complex to map discretely within the Narc 1 protein.
Purification and Characterization of an Inducible s -Triazine Hydrolase from Rhodococcus corallinus NRRL B-15444R (1994)

The widespread use and relative persistence of s-triazine compounds such as atrazine and simazine have led to increasing concern about environmental contamination by these compounds. Few microbial isolates capable of transforming substituted s-triazines have been identified. Rhodococcus corallinus NRRL B-15444 has previously been shown to possess a hydrolase activity that is responsible for the dechlorination of the triazine compounds deethylsimazine (6-chloro-N-ethyl-1,3,5-triazine-2,4-diamine) (CEAT) and deethylatrazine (6-chloro-N-isopropyl-1,3,5-triazine-2,4-diamine) (CIAT). The enzyme responsible for this activity was purified and shown to be composed of four identical subunits of 54,000 Da. Kinetic experiments revealed that the purified enzyme is also capable of deaminating the structurally related s-triazine compounds melamine (2,4,6-triamino-1,3,5-triazine) (AAAT) and CAAT (2-chloro-4,6-diamino-1,3,5-triazine), as well as the pyrimidine compounds 2,4,6-triaminopyrimidine (AAAP) and 4-chloro-2,6-diaminopyrimidine (CAAP). The triazine herbicides atrazine and simazine inhibit the hydrolytic activities of the enzyme but are not substrates. Induction experiments demonstrate that triazine hydrolytic activity is inducible and that this activity rises approximately 20-fold during induction.
Evidence that Thienamycin Biosynthesis Proceeds via C‐5 Epimerization: ThnE Catalyzes the Formation of (2S,5S)‐trans‐Carboxymethylproline (2008)

Unusual antibiotic biosynthesis enzymes: The observation that formation of trans-carboxymethylproline (t-CMP) and 6-methyl-t-CMP is catalyzed by ThnE from Streptomyces cattleya using glutamate semi-aldehyde and malonyl- or methylmalonyl-CoA implies the need for a C-5 epimerization step in the biosynthesis of thienamycin and reveals the possibility that a methyl group at C-6 might be introduced at an early stage. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
Distribution of ice nucleation-active bacteria on plants in nature (1978)

A replica plating method for rapid quantitation of ice nucleation-active (INA) bacteria was developed. Leaf washings of plant samples from California, Colorado, Florida, Louisiana, and Wisconsin were tested for the presence of INA bacteria. Of the 95 plant species sampled, 74 were found to harbor INA bacteria. Only the conifers were, as a group, unlikely to harbor INA bacteria. All of the INA bacteria isolated resembled either Pseudomonas syringae or Erwinia herbicola. Sufficient numbers of INA bacteria were present on the samples to account for the ice nuclei associated with leaves that are necessary for freezing injury to occur. Numbers of INA bacteria were large enough to suggest that plant surfaces may constitute a significant source of atmospheric ice nuclei.
Distinct neuropsychological profiles within ADHD: a latent class analysis of cognitive control, reward sensitivity and timing (2014)

Our findings support multiple pathway models of ADHD, as we were able to define separable subgroups with differing cognitive profiles. Furthermore, we found both quantitative and qualitative differences from controls, suggesting that ADHD may represent both categorical and dimensional differences. These results show that by addressing heterogeneity in ADHD, we can identify more homogeneous subsets of individuals to further investigate.
"And Hold the Bondman Still": Biogeography and Utopia in Slave and Serf Narratives (2002)

This article reads the contrasting topographies structuring autobiographical narratives by US slaves and Russian serfs as constitutive of specific imaginings of freedom and constraints on freedom. It argues for seeing the classic "passage" of the bondsman from slavery to freedom as a kind of "passing" involving the manipulation of categories provided by dominant racial (US) or state (Russia) ideologies. The final inability of the bondsman to "pass" into a space of true freedom forces us to posit a fourth space, beyond those of bondage, liberty, or exile. This (non-)space is utopia, perceived largely though the way the putative goal of the escaping slave falls short of being a true "land of liberty."
C-Glycosylated Diphenylmethanes and Benzophenones: The Stille Coupling Reaction ofC-Glycosylated Aryl Tins with Benzyl Bromides and Acid Chlorides (1999)

ABSTRACT C-glycosylated diphenylmethanes and C-glycosylated benzophenones were prepared by the palladium-catalyzed cross-coupling reaction of C-glycosylated aryl tins with various benzyl bromides or acid chlorides to provide physiologically stable glycomimetics of miscellaneous glycoepitopes.
Monoclonal Antibody Pharmacokinetics and Pharmacodynamics (2008)

More than 20 monoclonal antibodies have been approved as therapeutic drugs by the US Food and Drug Administration, and it is quite likely that the number of approved antibodies will double in the next 7-10 years. Antibody drugs show several desirable characteristics, including good solubility and stability, long persistence in the body, high selectivity and specificity, and low risk for bioconversion to toxic metabolites. However, many antibody drugs demonstrate attributes that complicate drug development, including very poor oral bioavailability, incomplete absorption following intramuscular or subcutaneous administration, nonlinear distribution, and nonlinear elimination. In addition, antibody administration often leads to an endogenous antibody response, which may alter the pharmacokinetics and efficacy of the therapeutic antibody. Antibodies have been developed for a wide range of disease conditions, with effects produced through a complex array of mechanisms. This article attempts to provide a brief overview of the main determinants of antibody pharmacokinetics and pharmacodynamics. Clinical Pharmacology & Therapeutics (2008); 84, 5, 548-558 doi:10.1038/clpt.2008.170.
In Vitro Mutagenesis Protocols (2010)

In the post-genomic era, in vitro mutagenesis has emerged as a critically important tool for establishing the functions of components of the proteome. The third edition of In Vitro Mutagenesis Protoco
Dynamic network reconfiguration support for mobile computers (1997)

Hot swapping technology combined with pervasive heterogeneous networks empowers mobile laptop users to select the best network device for their current environment. Unfortunately, the majority of systemsoftwareremains'%ustomized"foraparticularnehvorkconfiguration, and assumes that many characteristics associated with the network environment remain invariant over the runtime of the software. Mobility causes changes in the environment and nullifies many of these assumptions. This leads to severeloss in system functionality when resources are lost, and failure to benefit when resources are gained.