gebhart/patrepeval huggingface dataset:
Prostaglandin E receptor subtypes in mouse osteoblastic cell line. (1996)

PGE2 is one of the key molecules in the osteoblast. It is the major prostanoid in the bone, and its production is under the control of both systemic and local factors. PGE2 has been reported to have multiple actions in the osteoblast, such as growth promotion and cell differentiation. To better understand the action of PGE2 in the osteoblast, we determined the PGE receptor subtypes in MC3T3-E1, an osteoblastic cell line derived from the normal mouse calvaria. Northern blot analysis revealed that EP1 and EP4 subtypes are expressed in MC3T3-E1. In contrast, EP3 subtype was not detected by either Northern blot analysis or RT-PCR. The contribution of each subtype was evaluated by studying the effects of subtype-specific analogs on osteoblastic function at confluency and 5 days after confluency. An EP1 agonist, 17-phenyl-omega-trinor PGE2, increased DNA synthesis and decreased alkaline phosphatase activity. 11-Deoxy-PGE1, and EP2 and EP4 agonist, decreased DNA synthesis and increased alkaline phosphatase activity at both stages. Butaprost, an EP2-selective agonist, showed effects similar to those of 11-deoxy-PGE1 only at confluency. Another and more differentiated osteoblastic marker, osteocalcin production, was detectable and was stimulated by 11-deoxy-PGE1 only 5 days after confluency. The exposure of these cells to EP1 agonist changed the cell shape to a more fibroblastic appearance. These results indicate that EP1, EP4, and probably EP2 are present in MC3T3-E1 cells; EP1 promotes cell growth, and EP2 and EP4 mediate differentiation of the osteoblast. Furthermore, the decreased response to EP2-specific agonist 5 days after confluency suggests that the expression of PGE receptor subtype is dependent on the stage of osteoblastic differentiation. This is the first report to determine PGE receptor subtypes in the bone.
Enantioselective Protonation of Catalytically Generated Chiral Enolates as an Approach to the Synthesis of α-Chloroesters (2005)

Treatment of alpha,alpha-dichloroaldehydes with various phenols in the presence of chiral triazolium salt catalysts and excess base results in the synthesis of alpha-chloro aryl esters in good yield and enantioselectivity. The reaction is tolerant of various functionality on the aldehyde as well as several electronically diverse phenols. The product chloroesters were further transformed into chloroacid, chlorohydrin, and azidoesters with nearly complete retention of enantioselectivity.
Calcium and Sodium Channel Antagonists for the Treatment of Pain (2000)

Several lines of evidence developed in preclinical models suggest that both spontaneous and evoked pain are mediated in part by voltage-sensitive sodium and calcium channels, which are in abundance in both the peripheral and the central nervous system. There is an abundance of research, both preclinical and clinical, on the effects of the sodium and calcium channel antagonists on nociceptive processing. Clinical studies on the efficacy of the sodium channel antagonists in the treatment of acute and chronic pain have had mixed results. Preliminary studies of the N-type calcium channel antagonists for the treatment of acute and chronic pain are promising but too early to enable researchers to make firm conclusions. This review summarizes the current literature on the effects of the sodium and calcium channel antagonists on acute nociceptive processing, facilitated pain, and neuropathic pain.
Naturally enhanced neutralizing breadth against SARS-CoV-2 one year after infection (2021)

More than one year after its inception, the coronavirus disease 2019 (COVID-19) pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) remains difficult to control despite the availability of several working vaccines. Progress in controlling the pandemic is slowed by the emergence of variants that appear to be more transmissible and more resistant to antibodies<sup>1,2</sup>. Here we report on a cohort of 63 individuals who have recovered from COVID-19 assessed at 1.3, 6.2 and 12 months after SARS-CoV-2 infection, 41% of whom also received mRNA vaccines<sup>3,4</sup>. In the absence of vaccination, antibody reactivity to the receptor binding domain (RBD) of SARS-CoV-2, neutralizing activity and the number of RBD-specific memory B cells remain relatively stable between 6 and 12 months after infection. Vaccination increases all components of the humoral response and, as expected, results in serum neutralizing activities against variants of concern similar to or greater than the neutralizing activity against the original Wuhan Hu-1 strain achieved by vaccination of naive individuals<sup>2,5-8</sup>. The mechanism underlying these broad-based responses involves ongoing antibody somatic mutation, memory B cell clonal turnover and development of monoclonal antibodies that are exceptionally resistant to SARS-CoV-2 RBD mutations, including those found in the variants of concern<sup>4,9</sup>. In addition, B cell clones expressing broad and potent antibodies are selectively retained in the repertoire over time and expand markedly after vaccination. The data suggest that immunity in convalescent individuals will be very long lasting and that convalescent individuals who receive available mRNA vaccines will produce antibodies and memory B cells that should be protective against circulating SARS-CoV-2 variants.
Stereoselective aldol condensations via boron enolates (1981)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStereoselective aldol condensations via boron enolatesD. A. Evans, J. V. Nelson, E. Vogel, and T. R. TaberCite this: J. Am. Chem. Soc. 1981, 103, 11, 3099–3111Publication Date (Print):June 1, 1981Publication History Published online1 May 2002Published inissue 1 June 1981https://pubs.acs.org/doi/10.1021/ja00401a031https://doi.org/10.1021/ja00401a031research-articleACS PublicationsRequest reuse permissionsArticle Views9070Altmetric-Citations482LEARN 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
Model Predictive Control and Optimization for Papermaking Processes (2011)

Brief description of papermaking processesIn general a paper machine can be divided into four sections: forming section, press section, drying section, and calendering section.In the forming section, the stock flow enters the headbox to be distributed evenly across a continuously running fabric felt called the wire.The newly formed sheet is carried by the wire along the Fourdrinier table, which has a set of drainage elements that promote water removal by various gravity and suction mechanisms.These elements include suction boxes, couch rolls, foils, etc.The solid consistency of the paper web can reach 20% by the time the web leaves the forming section and enters the press section.Figure 1 illustrates the configuration of a Fourdrinier-type paper machine.
BE-23372M, a novel protein tyrosine kinase inhibitor. II. Physico-chemical properties and structure elucidation. (1994)

BE-23372M, a new protein tyrosine kinase inhibitor, has been obtained as a reddish orange solid. The compound, C17H12O6, HRFAB-MS: m/z 312.0625 (M)+, is an acidic substance, showing UV (MeOH) lambda max (epsilon) 266 (8,800), 426 nm (20,400), and IR (KBr)vmax 1752(C = O) and 3298(OH) cm-1. The structure of BE-23372M, (E)-3-(3,4-dihydroxybenzylidene)-5-(3,4-dihydroxyphenyl)-2(3H)-fur anone, has been elucidated by 1H and 13C NMR studies.
Suppression of Rhizoctonia solani diseases of sugar beet by antagonistic and plant growth-promoting yeasts (2003)

Yeasts were shown to provide significant protection to sugar beet roots against R. solani, a serious soil-borne root pathogen. Yeasts also have the potential to be used as biological fertilizers.
Selective etching technology of in-situ P doped poly-Si (SEDOP) for high density DRAM capacitors (2002)

In order to keep a sufficient cell capacitance in a limited area, various kinds of three dimensional capacitor structures have been developed. However, fabrication procedure of those structures is very complicated, leading to a decrease in device yield and increase in manufacturing cost. Therefore, much effort has been focused on keeping the cell structure simple and manufacturable. Recently, surface enlargement methods such as hemispherical grained (HSG) Si and micro cavity have been developed, and by using these methods the surface could be enlarged as much as two times. However, these methods have a dielectric breakdown degradation characteristics and thickness dependence of NO capacitor dielectrics due to micro-grooves. Also the development of high dielectric films such as Ta/sub 2/O/sub 5/ and BaSrTiO/sub 3/ still have many problems in their application. In this work, we introduce a new technique called SEDOP (Selective Etching of in-situ P-Doped Poly-Si) for surface enlargement using large etch selectivity between phosphorus (P) in-situ doped poly-Si and undoped poly-Si. By using the SEDOP technique, a capacitor structure about 2 times larger in area and with a smooth surface can be formed with ease.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
The high threshold mechanotransducer: A status report (2005)

Growth Factors and Regeneration Group, Max-Delbrück Center for Molecular Medicine and Charité Universitätsmedizin Berlin, Robert-Rössle-Str. 10, Berlin-Buch D-13092, Germany *Corresponding author. Tel.: +49 30 9406 2430. E-mail address:[email protected] Submitted and accepted November 15, 2005.
The Complete Nucleotide Sequence of the Human Immunoglobulin Heavy Chain Variable Region Locus (1998)

The complete nucleotide sequence of the 957-kb DNA of the human immunoglobulin heavy chain variable (VH) region locus was determined and 43 novel VH segments were identified. The region contains 123 VH segments classifiable into seven different families, of which 79 are pseudogenes. Of the 44 VH segments with an open reading frame, 39 are expressed as heavy chain proteins and 1 as mRNA, while the remaining 4 are not found in immunoglobulin cDNAs. Combinatorial diversity of VH region was calculated to be approximately 6,000. Conservation of the promoter and recombination signal sequences was observed to be higher in functional VH segments than in pseudogenes. Phylogenetic analysis of 114 VH segments clearly showed clustering of the VH segments of each family. However, an independent branch in the tree contained a single VH, V4-44.1P, sharing similar levels of homology to human VH families and to those of other vertebrates. Comparison between different copies of homologous units that appear repeatedly across the locus clearly demonstrates that dynamic DNA reorganization of the locus took place at least eight times between 133 and 10 million years ago. One nonimmunoglobulin gene of unknown function was identified in the intergenic region.
Relaxin as a Cardiovascular Hormone: Physiology, Pathophysiology and Therapeutic Promises (2007)

Relaxin is a hormone belonging to the so-called relaxin superfamily, which also includes insulin-like peptides. Relaxin is best known for its effects on the female reproductive system, which primarily include lengthening of the pubic symphysis and softening of the tissues of the birth canal, stimulating mammary and endometrial development, and maintenance of myometrial quiescence. In recent years, evidence has been accumulating that relaxin can have multiple and diverse effects on both reproductive and nonreproductive organs, tissues and cells, thus acting as a sort of 'manager' hormone to optimize the many physiological changes taking place during pregnancy. Among the specific relaxin targets, there are the blood vessels and the heart. In fact, relaxin is a potent vasodilatator of the systemic and coronary circulation, by a mechanism of action involving nitric oxide, and can influence cardiac beating rate. Identification of the numerous possible roles of relaxin in the pathophysiology of cardiovascular diseases, not to mention the possible therapeutical applications of relaxin, remains a difficult task. Based on the known biological effects of relaxin, it is becoming increasingly evident that the potential fields of clinical investigation of human relaxin as a cardiovascular drug could be in ischemic heart disease (acute and chronic myocardial infarction), in cardiac fibrosis, in cell transplantation for cardiac repair, and in obliterative peripheral arterial disease. Availability of the homologous human peptide, knowledge of its pharmacological, pharmacokinetic and pharmacodynamic profiles, and increasing interest of clinicians and pharmaceutical companies should synergistically act to transfer relaxin from the laboratory bench to the bedside.
The assumed assimilation of cholesterol by Lactobacilli and Bifidobacterium bifidum is due to their bile salt-deconjugating activity (1993)

To study the mechanism of the propsed assimilation of cholesterol, we cultured various strains of Lactobacillus acidophilus and a Bifidobacterium sp. in the presence of cholesterol and oxgall. During culturing, both cholesterol and bile salts were precipitated. Because of bacterial bile salt deconjugation, no conjugated bile salts were observed in either the culture fluids or the pellets. During incubation, the cell count and optical density decreased. The degree of precipitation of bile salts and of cholesterol was dependent on the culture conditions. If L. acidophilus RP32 was cultured under acidifying conditions, the degree of precipitation of deconjugated bile salts was higher than if the pH was maintained at 6.0. Under acidifying conditions, cholesterol was coprecipitated with the bile salts, whereas in pH-controlled cultures, no coprecipitation of cholesterol was observed. From control experiments with different mixtures of bile salts, it appeared that coprecipitation of cholesterol during culturing was a result of formation of deconjugated bile salts, which have a decreased solubility at pH values lower than 6.0. It is concluded that the removal of cholesterol from the culture medium by L. acidophilus RP32 and other species is not due to bacterial uptake of cholesterol, but results from bacterial bile salt-deconjugating activity.
The future for direct retailing of travel and tourism products: the influence of information technology (1998)

The steady improvement in the quantity of information which can be delivered to a remote computer terminal and in the sophistication with which it can be manipulated, together with the continued drop in cost of information technology, may have dramatic effects on the way business is conducted in the travel and tourism industries (including hospitality). Today, direct purchase of travel by electronic means is a practical possibility. The research reported here explores the prospects for direct retailing by electronic means, and the implications for the industry of this. It includes the results of a survey of senior people in the UK travel and tourism industry and its suppliers, carried out in 1995. The paper concludes that the most rapid changes will be in the business travel market, followed by the market for single components of travel (e.g. an airfare or a hotel booking). Changes in other markets will be slower. These changes represent both threats and opportunities for the industry. The number of high-street travel agents can be expected to fall, but there will remain an important role for those who can provide a high-quality service to business and leisure consumers. © 1998 John Wiley & Sons, Ltd.
5-Lipoxygenase, but Not 12/15-Lipoxygenase, Contributes to Degeneration of Retinal Capillaries in a Mouse Model of Diabetic Retinopathy (2008)

5-Lipoxygenase represents a novel pathway for therapeutic intervention of diabetic retinopathy.
The aspartic proteases (1992)

The Aspartic proteases (EC 3.4.23) are a group of proteolytic enzymes that share the same catalytic apparatus. Members of the aspartic protease family can be found in different organisms, ranging from humans to plants and retroviruses. The best known sources of aspartic proteases are the stomach of mammals, yeast and fungi, with porcine pepsin as the proto type. The aim of this review is to summarize some of the characteristics of the aspartic protease family.
Antitumor effect of adriamycin entrapped in liposomes conjugated with anti-human alpha-fetoprotein monoclonal antibody. (1987)

The monoclonal antibody, 19-F-12 (IgG2b), against human alpha-fetoprotein was conjugated to liposomes containing Adriamycin, and the therapeutic effects of the conjugate were experimentally studied using the alpha-fetoprotein-producing human hepatoma strain, Li-7, maintained in BALB/c nu/nu male mice. Three i.v. injections of liposomes containing Adriamycin (7.5 mg/kg) into tumor-bearing mice significantly inhibited the tumor growth, and the therapeutic effect of the antibody-conjugated liposomes was greater than that of unconjugated liposomes, as judged from the tumor weights and histological findings. Furthermore, the experiments were repeated with Adriamycin (4-5 mg/kg) in free form, since administration of Adriamycin (7.5 mg/kg) in free form was highly toxic for the mice. The results still indicated that the therapeutic effect of Adriamycin in 19-F-12 conjugated liposomes was superior to that of free Adriamycin or Adriamycin in unconjugated liposomes. In contrast to the treatment for Li-7 in nude mice, the therapeutic effect of Adriamycin in 19-F-12 conjugated liposomes was not much different from that of Adriamycin in normal mouse IgG (IgG2b fraction) conjugated liposomes against alpha-fetoprotein-negative human breast cancer strain MX1. Tissue distribution studies after i.v. injection of Adriamycin in various forms into mice revealed that preferential delivery of Adriamycin to tumors occurred to some extent with antibody-conjugated liposomes as compared to the unconjugated liposomes. In addition, reduction of the distribution of Adriamycin to the heart was achieved by administering the drug in the liposome-entrapped form, and this enabled the use of a higher dose (7.5 mg/kg) of Adriamycin without toxic side effect.
Cerebral Mast Cells Participate In Postoperative Cognitive Dysfunction by Promoting Astrocyte Activation (2016)

These findings indicate that activated MCs could trigger astrocyte activation, be involved in neuroinflammation and possibly contribute to POCD. Interactions between MCs and astrocytes could provide potential therapeutic targets for POCD.
An interleaved porous laminate composed of reduced graphene oxide sheets and carbon black spacers by in situ electrophoretic deposition (2013)

Although the graphene-based materials have a great potential to be used for various energy storage devices, the expected performance of graphene has not been achieved yet seemingly due to the lack of interconnected porosity and actively-exposed surface area that should be developed in the re-stacked graphene electrodes. Herein we used an electrophoretic deposition (EPD) method to fabricate a binder-free porous supercapacitor electrode composed of reduced graphene oxide (RGO) sheets and conductive carbon black (CB) particles. Applying EPD for an electrostatically-stabilized aqueous mixture of RGO and CB nanoparticles, the electrophoretic squeezing force in EPD induced the RGO sheets to align in the in-plane direction along with the CB particles placed in the interlayers of RGO. The developed ladder-like interleaved composite structure allowed a desirable porosity network and conductive path for a facile movement of ions and electrons. Controlling the ratios of concentrations (Cs,RGO/Cs,CB) and/or zeta potentials (ξRGO/ξCB) of the RGO and CB nanoparticles in aqueous mixtures, different nanostructures of the interleaved RGO/CB laminates could be fabricated. Thoroughly tested as a supercapacitor electrode in an organic electrolyte (TEA BF4), the developed RGO/CB electrodes provided excellent performance of the specific capacitance of 218 F g−1 at a scan rate of 1 mV s−1 (133.3 F g−1 at a current density of 2 A g−1), energy density of 43.6 W h kg−1 and power density of 71.3 kW kg−1. It is believed that an ideal performance of intrinsic graphene properties could be exerted by the unique nanostructure of binder-free interleaved graphene laminates as developed by the scalable in situ EPD process for large-volume production.
Synthesis of 6-anilino-2-thiouracils and their inhibition of human placenta iodothyronine deiodinase (1985)

Several 6-anilino-2-thiouracils were synthesized and tested for their ability to inhibit the inner-ring iodothyronine deiodinase from human placenta. The p-ethyl and p-n-butyl analogues were strongly inhibitory to the enzyme and were much more effective than the standard deiodinase inhibitor, 6-propyl-2-thiouracil. The degree of inhibition caused by 6-(p-n-butylanilino)-2-thiouracil was, moreover, unaffected by high concentrations of reducing agent in the enzyme assay. Attempts to prepare 3-alkyl derivatives via S-debenzylation of 2-benzylthio intermediates led to rearrangement to, for example, 3-methyl-5-benzyl-6-amino-2-thiouracil. This compound also strongly inhibited the deiodinase reaction. Preliminary results suggest that these compounds are useful to study in vitro and in vivo metabolism of thyroid hormones and may be clinically useful to enhance the availability of active thyroid hormones to certain organs.
Flexibility in the donor substrate specificity of β 1,4-galactosyltransferase: application in the synthesis of complex carbohydrates (1991)

Biosynthetically, bovine N-acetylglucosamine beta 1,4-galactosyltransferase (GalT) catalyses the transfer of galactosyl residues from UDP-Gal to the 4-position of GlcNAc units, resulting in the production of N-acetyllactosamine sequences. UDP-Glc and UDP-GalNAc were also found to act as donors for this enzyme, allowing the preparation of beta Glc(1----4)-beta GlcNAc and beta GalNAc(1----4) beta GlcNAc terminating structures on the milligram scale. GalT could thus be used to add beta GalNAc to beta GlcNAc(1----2) alpha Man terminating structures, converting them to the beta GalNAc(1----4) beta GlcNAc(1----2) alpha Man sequences found on glycoprotein hormones. GalT did not transfer GlcNAc residues from UDP-GlcNAc, but it could utilize UDP-GlcNH2 as a donor. Synthesis of beta GlcNAc(1----4) beta GlcNAc sequences could therefore be accomplished by transfer of GlcNH2 from its UDP derivative, followed by N-acetylation of the product amino-disaccharide using acetic anhydride in methanol. The products of the enzymatic reactions were characterized by 1H-NMR-spectroscopy and fast-atom bombardment mass spectrometry. This work expands the scope of the combined chemical-enzymatic synthesis of complex carbohydrates, using glycosyltransferases, to the production of oligosaccharides different from those for which these enzymes were designed. These unnatural reactions should find application in glycoprotein and glycolipid remodelling.