gebhart/patrepeval huggingface dataset:
Brain accumulation of sunitinib is restricted by P‐glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration (2011)

Sunitinib is an orally active, multitargeted tyrosine kinase inhibitor which has been used for the treatment of metastatic renal cell carcinoma and imatinib-resistant gastrointestinal stromal tumors. We aimed to investigate the in vivo roles of the ATP-binding cassette drug efflux transporters ABCB1 and ABCG2 in plasma pharmacokinetics and brain accumulation of oral sunitinib, and the feasibility of improving sunitinib kinetics using oral coadministration of the dual ABCB1/ABCG2 inhibitor elacridar. We used in vitro transport assays and Abcb1a/1b(-/-) , Abcg2(-/-) and Abcb1a/1b/Abcg2(-/-) mice to study the roles of ABCB1 and ABCG2 in sunitinib disposition. In vitro, sunitinib was a good substrate of murine (mu)ABCG2 and a moderate substrate of human (hu)ABCB1 and huABCG2. In vivo, the systemic exposure of sunitinib after oral dosing (10 mg kg(-1) ) was unchanged when muABCB1 and/or muABCG2 were absent. Brain accumulation of sunitinib was markedly (23-fold) increased in Abcb1a/b/Abcg2(-/-) mice, but only slightly (2.3-fold) in Abcb1a/b(-/-) mice, and not in Abcg2(-/-) mice. Importantly, a clinically realistic coadministration of oral elacridar and oral sunitinib to wild-type mice resulted in markedly increased sunitinib brain accumulation, equaling levels in Abcb1a/1b/Abcg2(-/-) mice. This indicates complete inhibition of the blood-brain barrier (BBB) transporters. High-dose intravenous sunitinib could saturate BBB muABCG2, but not muABCB1A, illustrating a dose-dependent relative impact of the BBB transporters. Brain accumulation of sunitinib is effectively restricted by both muABCB1 and muABCG2 activity. Complete inhibition of both transporters, leading to markedly increased brain accumulation of sunitinib, is feasible and safe with a clinically realistic oral elacridar/sunitinib coadministration.
Reduction of Conjugated Double Bonds with Sodium Borohydride (1966)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTReduction of Conjugated Double Bonds with Sodium BorohydrideSaul B. KadinCite this: J. Org. Chem. 1966, 31, 2, 620–622Publication Date (Print):February 1, 1966Publication History Published online1 May 2002Published inissue 1 February 1966https://pubs.acs.org/doi/10.1021/jo01340a523https://doi.org/10.1021/jo01340a523research-articleACS PublicationsRequest reuse permissionsArticle Views1688Altmetric-Citations63LEARN 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
New potential functions for mobile robot path planning (2000)

The paper first describes the problem of goals unreachable with obstacles nearby when using potential field methods for mobile robot path planning. Then, new repulsive potential functions are presented by taking the relative distance between the robot and the goal into consideration, which ensures that the goal position is the global minimum of the total potential.
“Recycling” Classical Drugs for Malaria (2014)

ADVERTISEMENT RETURN TO ISSUEPREVReviewNEXT"Recycling" Classical Drugs for MalariaCátia Teixeira*† ‡, Nuno Vale†, Bianca Pérez†, Ana Gomes†, José R. B. Gomes ‡, and Paula Gomes*†View Author Information† Centro de Investigação em Química da Universidade do Porto, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, P-4169-007 Porto, Portugal ‡ CICECO, Departamento de Química, Universidade de Aveiro, P-3810-193 Aveiro, Portugal*(C.T.) E-mail: [email protected]*(P.G.) E-mail: [email protected]Cite this: Chem. Rev. 2014, 114, 22, 11164–11220Publication Date (Web):October 20, 2014Publication History Received28 February 2014Published online20 October 2014Published inissue 26 November 2014https://pubs.acs.org/doi/10.1021/cr500123ghttps://doi.org/10.1021/cr500123greview-articleACS PublicationsCopyright © 2014 American Chemical SocietyRequest reuse permissionsArticle Views3482Altmetric-Citations107LEARN 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:Antimicrobial agents,Chemical structure,Parasites,Peptides and proteins,Reaction products Get e-Alerts
Catalytic fixation of molecular nitrogen by electrolytic and chemical reduction (1969)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTCatalytic fixation of molecular nitrogen by electrolytic and chemical reductionEugene E. Van Tamelen and Douglas A. SeeleyCite this: J. Am. Chem. Soc. 1969, 91, 18, 5194Publication Date (Print):August 1, 1969Publication History Published online1 May 2002Published inissue 1 August 1969https://pubs.acs.org/doi/10.1021/ja01046a063https://doi.org/10.1021/ja01046a063research-articleACS PublicationsRequest reuse permissionsArticle Views724Altmetric-Citations59LEARN 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
Italy: : AGCOM adopts new regulation on transfer of ownership and enforcement of concentration limits in the media sector (2014)

On 17 July 2014, the Autorita per le garanzie nelle comunicazioni (Italian media regulation authority - AGCOM) adopted a new regulation concerning the notification of transfers of ownership, mergers, and agreements in the broadcasting sector, as well as the enforcement of the concentration limits set out in the Consolidated Law on Audiovisual and Radio Media Services (CLARMS). The regulation, which consists of six chapters, replaces and repeals an earlier regulation attached to AGCOM Decision no. 646/06/CONS.
Natural Enemies of Woolly Apple Aphid (Hemiptera: Aphididae) in Washington State (2012)

Woolly apple aphid, Eriosoma lanigerum (Hausmann), has become a pest of increasing importance in Washington apple orchards in the past decade. The increase in aphid outbreaks appears to be associated with changes in pesticide programs and disruption of biological control. We sampled woolly apple aphid colonies in central Washington apple orchards for natural enemies of this pest from 2006 to 2008. The most common predators encountered were Syrphidae (Syrphus opinator Osten Sacken, Eupeodes fumipennis Thomson, and Eupeodes americanus Wiedemann); Chrysopidae (Chrysopa nigricornis Burmeister); and Coccinellidae (Coccinella transversoguttata Brown and Hippodamia convergens Guérin-Méneville). The specialist syrphid Heringia calcarata Loew was recorded for the first time occurring in Washington apple orchards. The only parasitoid found in aerial colonies of woolly apple aphid was Aphelinus mali Haldeman; root colonies, however, were not parasitized. Identification of important natural enemies provides a better basis for conservation biological control of this pest.
Solid-Phase Synthesis of γ-AApeptides Using a Submonomeric Approach (2012)

The solid-phase synthesis of γ-AApeptides using a novel submonomeric approach that utilizes an allyl protection is reported. The strategy successfully circumvents the necessity of preparing γ-AApeptide building blocks in order to prepare γ-AApeptide sequences. This method will maximize the potential of developing chemically diverse γ-AApeptide libraries and thereby facilitate the biological applications of γ-AApeptides in the future.
The Mammalian Target of Rapamycin Regulates C2C12 Myogenesis via a Kinase-independent Mechanism (2001)

Rapamycin inhibits differentiation of mouse C2C12 myoblasts, a tissue culture model for skeletal muscle differentiation. The mechanism by which a rapamycin-sensitive signaling pathway regulates myogenesis is largely unknown. The mammalian target of rapamycin (mTOR) is a central regulator of cell growth and proliferation, but its role in myogenesis has not been examined directly. Here we report the investigation of the function of mTOR and its downstream effectors in muscle differentiation. Rapamycin exerts an inhibitory effect on C2C12 myogenesis at different stages, implying that a rapamycin-sensitive pathway may be required for multiple processes during muscle differentiation. The mTOR protein level increases 10-fold during differentiation, via a post-transcriptional mechanism. As the first direct demonstration of the essential role of mTOR in muscle differentiation, we show that a rapamycin-resistant mTOR, but not S6 kinase 1, can rescue rapamycin-inhibited myogenesis. Remarkably, the myogenic function of mTOR does not require its kinase activity. Two downstream effectors of the rapamycin-sensitive pathway, S6 kinase 1 and eIF4E-binding protein 1, undergo differential regulation during myogenesis, but neither protein is the relevant effector for the myogenic signaling of mTOR. Taken together, our observations suggest a novel mTOR signaling mechanism essential for skeletal muscle differentiation.
Dispersants for Cement and Salt Contaminated Manganese Tetraoxide High-Density Water-Based Drilling Fluids (2015)

Abstract The flocculation of aqueous-based drilling fluid, particularly at high temperature or in a high-salinity environment, is a common problem. The aggregation and settling of solid particles (e.g. manganese tetraoxide) causes operational problems, such as stuck pipe, well control, false bit gain, and scale problems. The flocculation of manganese tetraoxide particles becomes more severe at high density with the presence of clays such as bentonite and common fluid contaminants, such as cement and divalent salts. This affects the rheological behavior and sagging tendency of the drilling fluid adversely. Dispersants called deflocculants, thinner or dispersing agents, are used in drilling fluids to prevent solid flocculation. To minimize such flocculation problems, a thorough study was undertaken to identify aggregation of Mn3O4 particles and appropriate dispersants for water–based fluids weighted with Mn3O4. The dispersion of Mn3O4 particles in aqueous solutions was evaluated through visual transparency testing and a PC-2200 Spectrek laser particle analyzer. A Mastersizer 2000 was used to obtain the particle size distribution and specific surface area of Mn3O4 particles. A TGA was used to assess the thermal stability. The compatibility of over 50 dispersants with aqueous solutions was examined using a variable speed mixer. Viscosity and sagging tendency were evaluated using a Fan 35A viscometer and density variation measurements. The effect of CaCl2 was considered in the experimental study. The drilling fluids were aged using a hot rolling oven up to 400°F. Linear and other structures of particle aggregations were identified in Mn3O4-based filter cake. Dispersants examined were categorized into groups A, B, and C. Groups A and B dispersants showed settling times of 24 hours and 1–3 hours, respectively. More than 25 dispersants were assigned to groups A and B. Laser particle analysis showed that aggregation of particles was reduced in the presence of a lignosulfonate-based dispersant. Lignosulfonate and acrylate-based dispersants were compatible with water-based fluids and thermally stable up to 400°F and in the presence of CaCl2. Both dispersants reduced the sag factor and fluid loss for the drilling fluids in the presence of cement contamination. The shear stress/rate relationship and viscosity measurements showed that the rheological behavior of drilling fluids dispersed with either dispersants was improved. The dispersants chosen were non-toxic to aquatic organisms and biodegradable. The examined drilling fluids were high-density fluids up to 20 lbm/gal appropriate for deep drilling.
Identification of a Mobile Endogenous Transposon in <i>Arabidopsis thaliana</i> (1993)

A mobile endogenous transposable element, Tag1, has been identified in the plant Arabidopsis thaliana. Tag1 was found in the nitrate transporter gene, CHL1, of a chlorate-resistant mutant present in a population of plants containing an active maize Ac transposon. Tag1 excises from the chl1 gene producing chlorate-sensitive revertants with Tag1 or Tag1-related elements at different loci. Tag1 and related elements are present in the Landsberg but not Columbia or Wassilewskija ecotypes of Arabidopsis. Thus, Tag1 provides a tool for the insertional mutagenesis of plant genes essential for biological processes of agronomic importance.
Treating inflammation and infection in the 21st century: new hints from decoding resolution mediators and mechanisms (2017)

Practitioners of ancient societies from the time of Hippocrates and earlier recognized and treated the signs of inflammation, heat, redness, swelling, and pain with agents that block or inhibit proinflammatory chemical mediators. More selective drugs are available today, but this therapeutic concept has not changed. Because the acute inflammatory response is host protective to contain foreign invaders, much of today's pharmacopeia can cause serious unwanted side effects, such as immune suppression. Uncontrolled inflammation is now considered pathophysiologic and is associated with many widely occurring diseases such as cardiovascular disease, neurodegenerative diseases, diabetes, obesity, and asthma, as well as classic inflammatory diseases (<i>e.g.</i>, arthritis and periodontal diseases). The inflammatory response, when self-limited, produces a superfamily of chemical mediators that stimulate resolution of the response. Specialized proresolving mediators (SPMs), identified in recent years, are endogenous mediators that include the n-3-derived families resolvins, protectins, and maresins, as well as arachidonic acid-derived (n-6) lipoxins, which promote resolution of inflammation, clearance of microbes, reduction of pain, and promotion of tissue regeneration <i>via</i> novel mechanisms. Aspirin and statins have a positive impact on these resolution pathways, producing epimeric forms of specific SPMs, whereas other drugs can disrupt timely resolution. In this article, evidence from recent human and preclinical animal studies is reviewed, indicating that SPMs are physiologic mediators and pharmacologic agonists that stimulate resolution of inflammation and infection. The findings suggest that it is time to challenge current treatment practices-namely, using inhibitors and antagonists alone-and to develop immunoresolvents as agonists to test resolution pharmacology and their role in catabasis for their therapeutic potential.-Serhan, C. N. Treating inflammation and infection in the 21st century: new hints from decoding resolution mediators and mechanisms.
Use of RADFETs for Quality Assurance of Radiation Cancer Treatments (2006)

The paper presents recent developments in quality assurance of radiation cancer treatments involving RADFETs (MOSFET dosimeters) developed and manufactured at Tyndall National Institute. Construction of a RADFET linear array for intracavitary in-vivo dosimetry is described in detail
CREM: A master-switch regulating the balance between differentiation and apoptosis in male germ cells (2000)

Cyclic AMP-responsive element modulator (CREM) is a transcription factor highly expressed in the post-meiotic germ cells of the testis. Its pivotal role is to regulate the expression of several germ cell-specific genes, a crucial function as demonstrated by the severe phenotype of mice whose CREM gene was mutated by homologous recombination. CREM-deficient male animals are sterile and display a ten-fold increase in the apoptosis of germ cells. Recent results have shown that CREM needs a tissue-specific co-activator, ACT (activator of CREM in testis) to elicit its regulatory function in testis.
Human pregnancy serum inhibits interleukin-2 production. (1984)

Cell-mediated immunity may be depressed during pregnancy. We used the two way mixed lymphocyte reaction as an in vitro model of cell mediated immunity and studied the effect of pregnancy sera on this system by the amount of tritiated thymidine taken up by activated lymphocytes. We found that: (1) pregnancy sera contain a factor inhibiting the mixed lymphocyte reaction; (2) the inhibition of the mixed lymphocyte reaction induced by sera could be reversed by the addition of the supernatant from allogeneic mixed lymphocyte reaction; (3) pure interleukin-1 could not reverse the inhibitory effect and (4) recombinant interleukin-2 (IL-2) completely reversed the inhibitory effect of pregnancy sera on the mixed lymphocyte reaction. We conclude that a factor (or factors) present in serum from pregnant women is capable of inhibiting the generation of IL-2 during lymphocyte activation.
Inter-Injection-Locked Oscillators with Applications to Spatial Power Combining and Phased Arrays (2005)

Although the principle of injection locking has been applied to single- and multiple-device oscillators at microwave through millimeter wavelengths, the technique has not found many uses in hybrid or monolithic microwave integrated circuits. We present here a novel circuit topology which leads to the inter-injection-locking of a set of interconnected oscillators. Since each oscillator is coupled only to its two nearest neighbors, the scheme is very well adapted to integrated planar construction. Furthermore, phase control of only one injection power source can control the phases of all oscillators in the system in a manner suitable for driving a phased antenna array. A summary of the theory is followed by a description of results from an experimental VHF three-oscillator system. We conclude with a discussion of some proposed applications of inter-injection-locked systems.
Photoinitiated anionic coordination polymerization of epoxides, a novel polymerization process (1987)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPhotoinitiated anionic coordination polymerization of epoxides, a novel polymerization processYoshihisa Fukuchi, Tamotsu Takahashi, Hiromichi Noguchi, Masahiko Saburi, and Yasuzo UchidaCite this: Macromolecules 1987, 20, 9, 2316–2317Publication Date (Print):September 1, 1987Publication History Published online1 May 2002Published inissue 1 September 1987https://pubs.acs.org/doi/10.1021/ma00175a047https://doi.org/10.1021/ma00175a047research-articleACS PublicationsRequest reuse permissionsArticle Views199Altmetric-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-Alertsclose Get e-Alerts
Graphene-based CO<sub>2</sub> sensing and its cross-sensitivity with humidity (2017)

We present graphene-based CO<sub>2</sub> sensing and analyze its cross-sensitivity with humidity.
Plastid-Expressed <i>Betaine Aldehyde Dehydrogenase</i> Gene in Carrot Cultured Cells, Roots, and Leaves Confers Enhanced Salt Tolerance (2004)

Salinity is one of the major factors that limits geographical distribution of plants and adversely affects crop productivity and quality. We report here high-level expression of betaine aldehyde dehydrogenase (BADH) in cultured cells, roots, and leaves of carrot (Daucus carota) via plastid genetic engineering. Homoplasmic transgenic plants exhibiting high levels of salt tolerance were regenerated from bombarded cell cultures via somatic embryogenesis. Transformation efficiency of carrot somatic embryos was very high, with one transgenic event per approximately seven bombarded plates under optimal conditions. In vitro transgenic carrot cells transformed with the badh transgene were visually green in color when compared to untransformed carrot cells, and this offered a visual selection for transgenic lines. BADH enzyme activity was enhanced 8-fold in transgenic carrot cell cultures, grew 7-fold more, and accumulated 50- to 54-fold more betaine (93-101 micromol g(-1) dry weight of beta-Ala betaine and Gly betaine) than untransformed cells grown in liquid medium containing 100 mm NaCl. Transgenic carrot plants expressing BADH grew in the presence of high concentrations of NaCl (up to 400 mm), the highest level of salt tolerance reported so far among genetically modified crop plants. BADH expression was 74.8% in non-green edible parts (carrots) containing chromoplasts, and 53% in proplastids of cultured cells when compared to chloroplasts (100%) in leaves. Demonstration of plastid transformation via somatic embryogenesis utilizing non-green tissues as recipients of foreign DNA for the first time overcomes two of the major obstacles in extending this technology to important crop plants.