gebhart/patrepeval huggingface dataset:
Heteroannelations with o-amino aldehyde and o-amino cyano of some pyrazole derivatives (2004)

The starting material 5-amino-1-phenyl-3-pyridin-4-yl-1H-pyrazolo-4-carbaldehyde (o-amino aldehyde) was prepared and subjected to reaction with some reagents as acetoacetic ester, malonic ester, acetylacetone, amides, urea, acetophenone and malononitrile under different reaction conditions to afford novel pyrazolopyridine and pyrazolo pyrimidine derivatives. The latter compound of these products is 6-amino-1-phenyl-3-pyridin-4-yl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (o-amino cyano) was also subjected to react with some different reagents such as guanidine hydrochloride, formamide, phenylisothiocyanate by 1:1 and 1:2 molar ratio, respectively and formic acid afforded an additional fused heterocyclic six-membered ring to the pyrazolo pyridine moiety.
A Quirk in Multiple Regression: The Whole Regression can be Greater Than the Sum of Its Parts (1988)

Philip V. Bertrand, Roger L. Holder, A Quirk in Multiple Regression: The Whole Regression can be Greater Than the Sum of Its Parts, Journal of the Royal Statistical Society. Series D (The Statistician), Vol. 37, No. 4/5 (1988), pp. 371-374
Effects of Allelochemicals on Seed Germination and Seedling Growth of Maize (2014)

The experiment studied the effects of four kinds of allelochemicals( ferulic acid,benzoic acid,Cinnamic acid and Syringic acid) on seed germination and seedling growth of maize. The concentration of four allelochemicals were used in four degrees: 50 mg /L,100 mg /L,200 mg /L and 500 mg /L. The results showed that the four allelochemicals had significant allelopathic effects on seed germination and seedling growth. The effects were significantly related to the allelochemicals and their concentrations. Four allelochemicals in concentration of 50 mg /L,100 mg /L significantly accelerated seed germination of maize,while the concentration was 200 mg /L and 500 mg /L,the inhibiting effect of allelochemicals appears. The four allelochemicals appeared to improve seedling growth at 50 mg /L,100 mg /L,200 mg /L,for instance,Syringic acid in concentration of 100 mg /L had a significant stimulating effect on fresh weight of the maize for promoting the lateral growth of the radicel. With the concentration of allelochemicals increased to 500 mg /L,four allelochemicals showed obvious inhibition effect of seedling growth.
Therapeutic effect of the anti-Fas antibody on arthritis in HTLV-1 tax transgenic mice. (1996)

We have recently demonstrated Fas-mediated apoptosis in the synovium, of patients with rheumatoid arthritis (RA) and suggested that it may be one factor responsible for the regression of RA. To examine whether the induction of apoptosis caused by anti-Fas mAb may play a potential role as a new therapeutic strategy for RA, we investigated the effect of anti-Fas mAb (RK-8) on synovitis in an animal model of RA, the human T cell leukemia virus type I (HTLV-1) tax transgenic mice. We report here that administration of anti-Fas mAb into mice intra-articularly improved the paw swelling and arthritis within 48 h. Immunohistochemical study and in vitro culture studies showed that 35% of synovial fibroblasts, 75% of mononuclear cells, and some of polymorphonuclear leukocytes infiltrating in synovium underwent apoptosis by anti-Fas mAb. In situ nick end labeling analysis and electron microscope analysis clearly showed that many cells in synovium were induced apoptosis by anti-Fas mAb administration. However, local administration of anti-Fas mAb did not produce systemic side effects. Results demonstrated that administration of anti-Fas mAb in arthritic joints of the HTLV-1 tax transgenic mice produced improvement of arthritis. These findings suggest that local administration of anti-Fas mAb may represent a useful therapeutic strategy for proliferative synovitis such as RA.
Neutrophil migration is defective during recombinant human granulocyte- macrophage colony-stimulating factor infusion after autologous bone marrow transplantation in humans (1988)

We have previously reported that continuous intravenous (IV) administration of recombinant granulocyte-macrophage colony-stimulating factor (rHuGM-CSF) to humans following high-dose alkylating agent chemotherapy and autologous bone marrow support (ABMS) results in myeloid bone marrow maturation, accelerated granulocyte recovery, and reduced treatment-related toxicity. However, we found that leukocyte counts declined rapidly after discontinuation of rHuGM-CSF therapy, which suggests possible growth factor effects on leukocyte margination and migration. For these reasons we studied granulocyte margination by using 111In-labeled autologous granulocytes and found similar granulocyte margination before (21.5% +/- 13.4%) and during continuous IV rHuGM-CSF infusion (23.3% +/- 9.6%). Phagocytosis of Cryptococcus neoformans and granulocyte hydrogen peroxide production was similar before and during rHuGM-CSF infusion and similar to patients treated with the same high-dose chemotherapy and ABMS but not receiving growth factor. However, migration of granulocytes to a sterile inflammatory site was markedly reduced during continuous rHuGM-CSF infusion (1.2 +/- 0.9 WBCs/cm2, 24 hr) as compared with baseline (39.6 +/- 17.7 WBCs/cm2/24 hr; P less than .0008). These findings may be of relevance when extravascular granulocytes are required for host defense.
Automated security checking and patching using TestTalk (2000)

In many computer system security incidents, attackers successfully intruded computer systems by exploiting known weaknesses. Those computer systems remained vulnerable even after the vulnerabilities were known because it requires constant attention to stay on top of security updates. It is often both time-consuming and error-prone to manually apply security patches to deployed systems. To solve this problem, we propose to develop a framework for automated security checking and patching. The framework, named Securibot, provides a self-operating mechanism for security checking and patching. Securibot performs security testing using security profiles and security updates. It can also detect compromised systems using attack signatures. Most important, the Securibot framework allows system vendors to publish recently discovered security weaknesses and new patches in a machine-readable form so that the Securibot system running on deployed systems can automatically check out security updates and apply the patches.
Online learning for recency search ranking using real-time user feedback (2010)

Traditional machine-learned ranking algorithms for web search are trained in batch mode, which assume static relevance of documents for a given query. Although such a batch-learning framework has been tremendously successful in commercial search engines, in scenarios where relevance of documents to a query changes over time, such as ranking recent documents for a breaking news query, the batch-learned ranking functions do have limitations. Users' real-time click feedback becomes a better and timely proxy for the varying relevance of documents rather than the editorial judgments provided by human editors. In this paper, we propose an online learning algorithm that can quickly learn the best re-ranking of the top portion of the original ranked list based on real-time users' click feedback. In order to devise our algorithm and evaluate it accurately, we collected exploration bucket data that removes positional biases on clicks on the documents for recency-classified queries. Our initial experimental result shows that our scheme is more capable of quickly adjusting the ranking to track the varying relevance of documents reflected in the click feedback, compared to batch-trained ranking functions.
Xanthine metabolism in Bacillus subtilis: characterization of the xpt-pbuX operon and evidence for purine- and nitrogen-controlled expression of genes involved in xanthine salvage and catabolism (1997)

The xpt and pbuX genes from Bacillus subtilis were cloned, and their nucleotide sequences were determined. The xpt gene encodes a specific xanthine phosphoribosyltransferase, and the pbuX gene encodes a xanthine-specific purine permease. The genes have overlapping coding regions, and Northern (RNA) blot analysis indicated an operon organization. The translation of the second gene, pbuX, was strongly dependent on the translation of the first gene, xpt. Expression of the operon was repressed by purines, and the effector molecules appear to be hypoxanthine and guanine. When hypoxanthine and guanine were added together, a 160-fold repression was observed. The regulation of expression was at the level of transcription, and we propose that a transcription termination-antitermination control mechanism similar to the one suggested for the regulation of the purine biosynthesis operon exists. The expression of the xpt-pbuX operon was reduced when hypoxanthine served as the sole nitrogen source. Under these conditions, the level of the hypoxanthine- and xanthine-degrading enzyme, xanthine dehydrogenase, was induced more than 80-fold. The xanthine dehydrogenase level was completely derepressed in a glnA (glutamine synthetase) genetic background. Although the regulation of the expression of the xpt-pbuX operon was found to be affected by the nitrogen source, it was normal in a glnA mutant strain. This result suggests the existence of different signalling pathways for repression of the transcription of the xpt-pbuX operon and the induction of xanthine dehydrogenase.
Two DNA-binding factors recognize specific sequences at silencers, upstream activating sequences, autonomously replicating sequences, and telomeres in Saccharomyces cerevisiae. (1988)

Two DNA-binding factors from Saccharomyces cerevisiae have been characterized, GRFI (general regulatory factor I) and ABFI (ARS-binding factor I), that recognize specific sequences within diverse genetic elements. GRFI bound to sequences at the negative regulatory elements (silencers) of the silent mating type loci HML E and HMR E and to the upstream activating sequence (UAS) required for transcription of the MAT alpha genes. A putative conserved UAS located at genes involved in translation (RPG box) was also recognized by GRFI. In addition, GRFI bound with high affinity to sequences with the (C1-3A)-repeat region at yeast telomeres. Binding sites for GRFI with the highest affinity appeared to be of the form 5'-(A/G)(A/C)ACCCANNCA(T/C)(T/C)-3', where N is any nucleotide. ABFI-binding sites were located next to autonomously replicating sequences (ARSs) at controlling elements of the silent mating type loci HMR E, HMR I, and HML I and were associated with ARS1, ARS2, and the 2 micron plasmid ARS. Two tandem ABFI binding sites were found between the HIS3 and DED1 genes, several kilobase pairs from any ARS, indicating that ABFI-binding sites are not restricted to ARSs. The sequences recognized by ABFI showed partial dyad-symmetry and appeared to be variations of the consensus 5'-TATCATTNNNNACGA-3'. GRFI and ABFI were both abundant DNA-binding factors and did not appear to be encoded by the SIR genes, whose products are required for repression of the silent mating type loci. Together, these results indicate that both GRFI and ABFI play multiple roles within the cell.
Ultrasonic particle‐concentration for sheathless focusing of particles for analysis in a flow cytometer (2006)

The flow cell developed here uses acoustic focusing, which inherently concentrates the sample particles to the center of the sample stream. This method could eliminate the need for sheath fluid, and will enable increased interrogation times for enhanced sensitivity, while maintaining high particle-analysis rates. The concentration effect will also enable the analysis of extremely dilute samples on the order of several particles per liter, at analysis rates of a few particles per second. Such features offer the possibility of a truly versatile low-cost portable flow cytometer for field applications.
1,2‐Fused pyrimidines. III. Derivatives of 12H‐pyrido[1′,2′:1,2]pyrimido[4,5‐b]quinoline, a novel heterocyclic system (1987)

Abstract Reactivities of 2‐amino‐4 H ‐pyrido[1,2‐ a ]pyrimidin‐4‐ones and 4‐amino‐2 H ‐pyrido[1,2‐ a ]pyrimidin‐2‐ones, both N,N ‐dialkyl and ( N ‐alkyl, N ‐phenyl)substituted, when treated with the N,N ‐dimethylformamide/phosphorus oxychloride Vilsmeier‐Haack reagent XII were compared. Starting from 2‐[( N ‐alkyl, N ‐phenyl)amino] compounds IXa,b , the expected XVIa,b and XVIIa,b were obtained, which are derivatives of 12 H ‐pyrido[1′,2′:1,2]pyrimido[4,5‐ b ]quinoline, a novel heterocyclic system. When 2‐(phenylamino) compound IXc was used a mixture of 3‐formylderivative XVIII and 12 H ‐pyrido‐[1′,2′:1,2]pyrimido[4,5‐ b ]quinolin‐12‐one ( XIX ) resulted from the reaction. On the other hand, 2‐(dialkylamino)‐4 H ‐pyrido[1,2‐ a ]pyrimidin‐4‐ones IIIa‐c plainly afforded high yields of 3‐formylderivatives XIVa‐c. In contrast, no significant reaction occurred when 4‐(dialkylamino) and 4‐[( N ‐alkyl, N ‐phenyl)amino] compounds IIa‐c and VIIIa,b were treated with the reagent XII , under the same as well as more severe conditions. A clear difference in the nucleophilic reactivity of C‐3 position between these two classes of isomers is pointed out by the above summarized results.
An Integrated Genome-Wide Approach to Discover Tumor-Specific Antigens as Potential Immunologic and Clinical Targets in Cancer (2012)

Tumor-specific antigens (TSA) are central elements in the immune control of cancers. To systematically explore the TSA genome, we developed a computational technology called heterogeneous expression profile analysis (HEPA), which can identify genes relatively uniquely expressed in cancer cells in contrast to normal somatic tissues. Rating human genes by their HEPA score enriched for clinically useful TSA genes, nominating candidate targets whose tumor-specific expression was verified by reverse transcription PCR (RT-PCR). Coupled with HEPA, we designed a novel assay termed protein A/G-based reverse serological evaluation (PARSE) for quick detection of serum autoantibodies against an array of putative TSA genes. Remarkably, highly tumor-specific autoantibody responses against seven candidate targets were detected in 4% to 11% of patients, resulting in distinctive autoantibody signatures in lung and stomach cancers. Interrogation of a larger cohort of 149 patients and 123 healthy individuals validated the predictive value of the autoantibody signature for lung cancer. Together, our results establish an integrated technology to uncover a cancer-specific antigen genome offering a reservoir of novel immunologic and clinical targets.
Serum containing tumor necrosis factor is cytotoxic for the human malaria parasite Plasmodium falciparum (1983)

Sera (BCG-lipopolysaccharide [LPS] serum) were obtained from mice infected with Mycobacterium bovis BCG 2 h after intravenous administration of bacterial endotoxin (LPS). Varying concentrations of sera were added to cultures of Plasmodium falciparum-infected human erythrocytes; parasite viability was assessed by hypoxanthine incorporation after 4 days in culture. At concentrations of 1 to 3%, cultures treated with BCG-LPS serum showed a two- to threefold increase in hypoxanthine incorporation; at higher concentrations (4 to 8%), hypoxanthine incorporation fell to 2 to 5% of that in control cultures. Concurrent assays with control sera (from untreated mice or mice treated with BCG or LPS alone) caused some stimulation but no inhibition at up to 8% concentration. Examination of cultures treated with BCG-LPS serum showed morphological, deterioration of parasites within erythrocytes. The presence of tumor necrosis factor in the BCG-LPS serum was confirmed by using a standard L-cell cytotoxicity assay. In addition, rabbit antiserum against partially purified tumor necrosis factor protected intraerythrocytic forms of P. falciparum from the toxic effects of BCG-LPS serum. These data suggest that the factor in BCG-LPS serum that is toxic to P. falciparum in human erythrocytes is antigenically similar or identical to tumor necrosis factor. This nonantibody mediator of killing may play a role in human malaria.
Species and size compositions and reproductive biology of rays (Chondrichthyes, Batoidea) caught in target and non‐target fisheries in eastern Indonesia (2007)

Extensive surveys of various fish landing sites in eastern Indonesia, conducted between April 2001 and March 2006, recorded a total of 54 species of batoid rays belonging to 12 families. The Dasyatidae was by far the most speciose family, comprising half of the recorded species, and was also the most abundant, contributing 89 and 44% to the total numbers and total estimated biomass of batoids, respectively. The size and sex compositions of 23 species of rays are described and an accurate size at maturity of males, i.e. with 95% CI, was determined for 13 of these species. The sex ratios were found to be close to parity in the majority of species, however, the landings of the whitespotted guitarfish Rhynchobatus australiae consisted of significantly more females than males, a situation also recorded for this species in the by‐catch of the northern Australian prawn fishery. Data on aspects of the reproductive biology of three dasyatid species ( Dasyatis cf. kuhlii , Dasyatis zugei and Himantura walga ), which form a substantial component of the by‐catch of the bottom trawl fisheries in the region, were collected on most sampling occasions. These small rays, i.e. maximum sizes 243–379 mm disc width, were found to have no distinct seasonal reproductive cycle and small litter sizes, i.e. less than four embryos. Opportunistic reproductive data, e.g. litter size and embryo sizes, were also collected from various other species. The litter sizes of the rhynchobatid and rhinobatid species examined were found to be larger than those of the gymnurid and dasyatid species examined, i.e. seven to 19 and two to 13 v. one to four, respectively. The data presented in this paper for the numerous species of rays which are landed by target and non‐target fisheries in Indonesia represent the first such data for the vast majority of these species.
Identification of Synthetic Endothelial Cell-Specific Promoters by Use of a High-Throughput Screen (2004)

Transcriptional targeting is a desirable property for many gene transfer applications. Because endothelial cells line most blood vessels, they are attractive candidates for the introduction of therapeutic gene products. As a proof-of-concept study, we attempted to identify a synthetic, endothelial cell-specific promoter by use of a high-throughput screen involving self-inactivating (SIN) human immunodeficiency virus type 1 (HIV-1)-based vectors. Select duplex oligodeoxynucleotides recognized by transcription factors and located 5' of endothelial cell-specific mRNA transcripts were randomly ligated and cloned upstream of a minimal ICAM-2 promoter driving enhanced green fluorescent protein (eGFP) in a SIN HIV-1-based vector. Vesicular stomatitis virus G protein-pseudotyped particles were prepared from a library of >10(6) vector recombinants and used to transduce an endothelial cell line. The highest eGFP expressers were repeatedly sorted, and the synthetic promoters were recovered and retested by a luciferase reporter. Several promoters were active and specific to endothelial cells of varied species, with high selectivity indexes and inducibility under hypoxia-mimetic conditions. One in particular was then introduced back into a SIN HIV-1-based vector to confirm its endothelial cell activity and specificity. This study suggests that SIN vectors may be used in a high-throughput manner to identify tissue-specific promoters of high activity, with potential applications for both transcriptional targeting and gene transfer.
Protein kinase C and mammary cell differentiation: involvement of protein kinase C alpha in the induction of beta-casein expression. (1994)

Treatment of HC11 mouse mammary epithelial cells with the lactogenic hormones dexamethasone, insulin, and prolactin (DIP) leads to cellular differentiation and production of the milk protein beta-casein. The following experimental evidence suggests the involvement of protein kinase C (PKC) in DIP induced signal transduction. Down-regulation of PKC by 12-O-tetradecanoylphorbol-13-acetate or addition of CGP 41251, a selective inhibitor of PKC, inhibited beta-casein protein expression induced by DIP in HC11 cells. This inhibition occurs at the level of transcription, since the DIP mediated activation of a beta-casein promoter-luciferase reporter construct or of mammary gland specific factor (MGF), an essential transcription factor for beta-casein promoter activity, was also inhibited by CGP 41251. Inhibition or down-regulation of PKC reduced the activation of MGF by prolactin as well. PKC-alpha, the only conventional PKC isoform expressed in HC11 cells, is most likely involved in the DIP induced beta-casein expression. (a) Only PKC-alpha and PKC-epsilon are down-regulated by 12-O-tetradecanoylphorbol-13-acetate whereas PKC-delta and PKC-zeta are not. (b) Of the PKC isoforms expressed in HC11 cells, CGP 41251 inhibits PKC-alpha more potently than PKC-delta, PKC-epsilon, and PKC-zeta. The IC50 for the inhibition of beta-casein synthesis, MGF activation, and beta-casein promoter activity by CGP 41251 correlated well with the IC50 of PKC-alpha inhibition. (c) Finally, only PKC-alpha translocated to membrane fractions after DIP or prolactin treatment. Taken together, these data indicate that PKC-alpha plays an important role in the signaling pathway activated by prolactin during beta-casein induction.
Aminolysis of activated esters of indole-3-acetic acid in acetonitrile (1993)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAminolysis of activated esters of indole-3-acetic acid in acetonitrileMichael J. Pfeiffer and Samir B. HannaCite this: J. Org. Chem. 1993, 58, 3, 735–740Publication Date (Print):January 1, 1993Publication History Published online1 May 2002Published inissue 1 January 1993https://pubs.acs.org/doi/10.1021/jo00055a031https://doi.org/10.1021/jo00055a031research-articleACS PublicationsRequest reuse permissionsArticle Views819Altmetric-Citations18LEARN 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