gebhart/patrepeval huggingface dataset:
FGF-1 - A Key Regulator Of Human Adipogenesis (2004)

The addition compound Cl(3)SiSiCl(3)·TMEDA was formed quantitatively by treatment of Cl(3)SiSiCl(3) with tetramethylethylenediamine (TMEDA) in pentane at room temperature. The crystal structure of Cl(3)SiSiCl(3)·TMEDA displays one tetrahedrally and one octahedrally bonded Si atom (monoclinic, P2(1)/n). (29)Si CP/MAS NMR spectroscopy confirms this structure. Density functional theory (DFT) calculations have shown that the structure of the meridional isomer of Cl(3)SiSiCl(3)·TMEDA is 6.3 kcal lower in energy than that of facial coordinate species. Dissolving of Cl(3)SiSiCl(3)·TMEDA in CH(2)Cl(2) resulted in an immediate reaction by which oligochlorosilanes Si(n)Cl(2n) (n = 4, 6, 8, 10; precipitate) and the Cl(-)-complexed dianions [Si(n)Cl(2n+2)](2-) (n = 6, 8, 10, 12; CH(2)Cl(2) extract) were formed. The constitutions of these compounds were confirmed by MALDI mass spectrometry. Additionally, single crystals of [Me(3)NCH(2)CH(2)NMe(2)](2)[Si(6)Cl(14)] and [Me(3)NCH(2)CH(2)NMe(2)](2)[Si(8)Cl(18)] were obtained from the CH(2)Cl(2) extract. We found that Cl(3)SiSiCl(3)·TMEDA reacts with MeCl, forming MeSiCl(3) and the products that had been formed in the reaction of Cl(3)SiSiCl(3)·TMEDA with CH(2)Cl(2). X-ray structure analysis indicates that the structures of [Me(3)NCH(2)CH(2)NMe(2)](2)[Si(6)Cl(14)] (monoclinic, P2(1)/n) and [Me(3)NCH(2)CH(2)NMe(2)](2)[Si(8)Cl(18)] (monoclinic, P2(1)/n) contain dianions adopting an "inverse sandwich" structure with inverse polarity and [Me(3)NCH(2)CH(2)NMe(2)](+) as countercations. Single crystals of SiCl(4)·TMEDA (monoclinic, Cc) could be isolated by thermolysis reaction of Cl(3)SiSiCl(3)·TMEDA (50 °C) in tetrahydrofuran (THF).
Three scrapie prion isolates exhibit different accumulation patterns of the prion protein scrapie isoform. (1993)

To investigate the molecular basis of prion diversity, we inoculated transgenic mice expressing the Syrian hamster prion protein (PrP) with three distinct prion isolates. We compared the three isolates designated Sc237, 139H, and Me7H in Tg(SHaPrP)7 mice with clinical signs of scrapie because the incubation times with these mice are considerably shorter than the times found with hamsters. Each prion isolate produced a distinctive pattern of the scrapie isoform of PrP (PrPSc) accumulation, as determined by histoblotting, a technique developed for the regional mapping of PrPSc deposition. The PrPSc pattern with the Me7H isolate was particularly interesting because it appeared to be confined to the hypothalamus and related structures--including the interstitial nucleus of the stria terminalis, the paraventricular nucleus of the thalamus, and periaqueductal grey. Additionally, the regions of PrPSc accumulation remained highly restricted, even though the incubation time for Me7H scrapie was significantly longer than with Sc237 and 139H isolates. Neuropathological changes characterized by neuronal vacuolation and astrocytic gliosis were confined to those regions where PrPSc accumulated. These findings argue that the cell-specific propagation of prion isolates may be responsible for different properties exhibited by each of the isolates.
Phase 1 study of interleukin-12 in combination with rituximab in patients with B-cell non-Hodgkin lymphoma (2002)

Rituximab is a chimeric murine/human monoclonal antibody that binds to CD20 on B lymphocytes. Although binding of the Fab domain may induce apoptosis, the Fc domain recruits immune effector functions to mediate cell lysis. Interleukin-12 (IL-12) facilitates cytolytic T-cell responses, enhances the lytic activity of natural killer (NK) cells, and induces the secretion of interferon gamma (IFN-gamma) by both T and NK cells. Therefore, the hypothesis was considered that combining IL-12 with rituximab would augment the immune-mediated cell lysis induced by rituximab. A phase 1 study of IL-12 in combination with rituximab was conducted in 43 adults with B-cell lymphoma to determine the optimal immunologic dose of this combination. Rituximab was administered at a dose of 375 mg/m(2) by intravenous infusion weekly for 4 weeks, and IL-12 was given subcutaneously twice weekly. The starting dose of IL-12 was 30 ng/kg and this was escalated to 500 ng/kg. Constitutional symptoms and liver enzyme elevations at 500 ng/kg of IL-12 were dose limiting. A greater than 20-fold increase in the serum levels of IFN-gamma and a 2.5- to 5-fold increase in inducible protein 10 (IP-10) levels was seen at IL-12 doses of 100 ng/kg or greater. Objective responses occurred in 29 of the 43 patients (69%), with 8 of 11 complete responses seen at IL-12 doses of 300 ng/kg or greater. The optimal immunologic dose of IL-12 in combination with rituximab was determined to be 300 ng/kg subcutaneously twice weekly starting on day 2. These data suggest that IL-12 and rituximab is an active combination and further studies of this combination in B-cell non-Hodgkin lymphoma are warranted.
Design and integration of a multi-channel fluorescence detector (2012)

In combination with fluidic systems, fluorescence detectors have a large variety of applications e.g. in biomedicine for ph-sensoring or the characterization of chemical reaction processes. Highly integrated and miniaturized optofluidic microsystems enable the handling of very small sample volumes in so-called segmented flow systems, which is beneficial for the practical application. A single-channel fluorescence sensor using planar integrated free space optical systems has been developed in the past. In order to increase the measuring flexibility and accuracy the extension to a multi-wavelength and multi-channel sensor system based on this concept is currently investigated. We present the concept, optical design and fabrication strategy of a highly integrated free space optical fluorescence detector for the application in a segmented-flow environment. The performance of the system is characterized and the application as a biochemical analysis system is discussed.
Microwave-assisted hydrolysis of phosphonate diesters: an efficient protocol for the preparation of phosphonic acids (2012)

A new highly efficient method for the hydrolysis of acyclic nucleoside phosphonate diesters (or generally of any organophosphonates) to the corresponding phosphonic acids has been developed. This novel methodology employs inexpensive hydrochloric acid in equimolar amounts to the number of ester groups present in the molecule and thus, avoids using trimethylsilyl halogenides, the standard reagents for these types of transformations. Moreover, simple and easy work-up of the reaction mixture affords very clean products in high yields (usually 77–93%). Another advantage of the described hydrolysis of phosphonate diesters is the fact that the course of the reaction can be instantly monitored through pressure changes in the reaction vessel. This ‘green’ method has also been successfully used for the preparation of otherwise synthetically difficult to access (phosphonomethoxy)ethyl (PME) derivatives of guanine (PMEG) and hypoxanthine (PMEHx), and furthermore, the method gains access to important novel acyclic nucleoside phosphonates derived from 2-chlorohypoxanthine and from xanthine (e.g. PMEX).
Histopathologic Examination and Enumeration of Polymorphonuclear Leukocytes in the Nasal Mucosa during Experimental Rhinovirus Colds (1984)

The histology of the nasal mucosa was examined by serial scrape and punch biopsies in 20 rhinovirus infected volunteers and 10 sham inoculated controls. No morphologic changes could be detected in the epithelial or subepithelial portions in the mucosa of specimens from infected volunteers. There was a significant increase in the number of polymorphonuclear leukocytes (PMNs) in the nasal epithelium of the infected subjects early in the course of the cold compared to their pre-infection baseline. However, trauma to the nasal mucosa from repeated sampling led to an outpouring of PMNs into nasal mucus, making evaluation of the results difficult. The number of mast cells seen in the mucosal specimens of the infected subjects did not differ from that seen in controls.
Functional Architecture of Chromosomal DNA Domains (1996)

More than 20 years ago, it was found that chromosomal DNA in eukaryotic cell nuclei was organized into large loops by periodic attachment to the high salt-insoluble proteinous nuclear (chromosomal) matrix. The specificity of genomic DNA partitioning into loops has been studied intensively trying to find out whether loops may constitute quasiindependent structural-functional units of the genome. These studies have resulted in conflicting findings and, consequently, in conflicting conclusions. Recently, we have developed a conceptually new approach for analysis of specificity of the DNA loop organization by topoisomerase II-mediated excision of individual loops and their oligomers. Using this approach we have obtained new data supporting the supposition that loops may constitute the basic units of genome organization and evolution. In the present article we critically analyze all existing data on specificity and functional significance of chromosomal DNA organization into loops. The goals of this analysis are: 1. To evaluate the available experimental data and try to understand the reasons of the conflicting results obtained by different experimental approaches. 2. Try to answer the long-standing question about a possible correlation between the functional organization of the genome and the mode of its packaging within the nuclei.
Relationship Between Interleukin 6 and Mortality in Patients With Unstable Coronary Artery Disease (2001)

Circulating IL-6 is a strong independent marker of increased mortality in unstable CAD and identifies patients who benefit most from a strategy of early invasive management.
Reversible tumorigenesis in mice by conditional expression of the HER2/c-erbB2 receptor tyrosine kinase. (1996)

In the present study we describe the reversible transformation of NIH3T3 fibroblasts by overexpression of the HER2/c-erbB2 receptor tyrosine kinase. Cell lines expressing HER2 under control of a tetracycline-responsive promoter were isolated. Induction of HER2 expression resulted in cellular transformation in vitro as depicted by growth in soft agar and focus formation in tissue culture. Subsequent treatment of these cells with the effector anhydrotetracyline switched-off HER2 expression and induced morphological and functional changes characteristic for non-transformed cells. Subcutaneous transplantation of cells in nude mice resulted in the formation of solid tumors. Interestingly tumor formation was completely suppressed by treatment of the animals with anhydrotetracyline. Our findings indicate that overexpression of HER2 induces the transformed phenotype of NIH3T3 cells and is required for tumor formation and progression in nude mice. By linking the expression of the marker gene secreted placental alkaline phosphatase to the expression of HER2, a sensitive monitoring of tumor development in nude mice was feasible.
Intratumoral injection of dendritic cells after treatment of anticancer drugs induces tumor‐specific antitumor effect in vivo (2002)

We investigated the in vivo antitumor effects of intratumoral (i.t.) administration of dendritic cells (DC) after low-dose chemotherapy using cisplatin + 5-FU. Combination of i.t. injection of DC and systemic chemotherapy induced complete rejection of the treated tumor, MC38 murine adenocarcinoma. Furthermore, the antitumor effects were also observed on a distant tumor inoculated in the contralateral flank of the animal. When 10x the number of tumor cells were inoculated, the antitumor effect of the combination of DC after chemotherapy was also confirmed and in comparison to that of DC or chemotherapy alone, thereafter contributed to a greater prolongation of survival. To analyze the mechanisms of the systemic antitumor effect generated in this system, we assessed the cytolytic activity against inoculated tumors. The cytolytic activity of effector cells from treated animals was shown to be tumor-specific and was mainly CD8 and MHC Class-I (p < 0.01) restricted. CD4 and MHC Class-II treatment marginally inhibited the cytolytic activity but not significantly (p = 0.07, 0.08 respectively). The cytolysis of effector cells was enhanced more significantly by the treatment of both DC and chemotherapy, than that of either DC or chemotherapy alone. Our study suggests that the strategy of i.t. injection of DC after low-dose chemotherapy could be a powerful weapon to treat patients with cancer in the clinical settings.
Small atrial natriuretic peptide analogs: design, synthesis, and structural requirements for guanylate cyclase activation (1992)

Structure/activity studies on atrial natriuretic peptide ANP (1-28) have highlighted three portions of the native molecule as necessary for its biological responses. We have linked these three regions and excised the remaining segments to produce a family of small analogues (less than half the size of the parent) which demonstrate the full range of ANP's actions. Importantly, these compounds act at both major types of ANP receptor. Two critical modifications lead to more potent analogues; both involve expanding the cyclic portion of the molecule. Further optimization of one of these modified structures leads to A68828, a full ANP agonist which shows promise as a preventative agent against acute renal failure.
A new method for the synthesis of N-phenyl-uracil and -pyrimidine nucleosides (1995)

Reaction of uracil or pyrimidine nucleosides with iodobenzene in the presence of cuprous oxide in 2,4,6-trimethylpyridine for 20 h gave N1,N3-diphenyluracil 1 or N3-phenylpyrimidine nucleosides 4, 7. The identity of these products were confirmed by comparison of their physical and spectroscopic data with those of 2,4-diphenoxypyrimidine 2 or 4-phenoxypyrimidin-2(1H)-one nucleoside 5b.
Preparation and properties of quaternary ammonium and phosphonium permanganates (1984)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPreparation and properties of quaternary ammonium and phosphonium permanganatesHasan Karaman, Richard J. Barton, Beverly E. Robertson, and Donald G. LeeCite this: J. Org. Chem. 1984, 49, 23, 4509–4516Publication Date (Print):November 1, 1984Publication History Published online1 May 2002Published inissue 1 November 1984https://pubs.acs.org/doi/10.1021/jo00197a037https://doi.org/10.1021/jo00197a037research-articleACS PublicationsRequest reuse permissionsArticle Views837Altmetric-Citations50LEARN 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
Purification and characterization of endoglucanase C of Cellulomonas fimi, cloning of the gene, and analysis of in vivo transcripts of the gene (1989)

Two nonglycosylated endoglucanases which bind to Sephadex were purified from culture supernatants of Cellulomonas fimi grown on microcrystalline cellulose. Their Mrs were 120,000 and 130,000. The N-terminal amino acid sequences of the enzymes were identical, suggesting that the enzymes were related. A DNA fragment encoding this N-terminal sequence was cloned in Escherichia coli. The nucleotide sequence corresponding to the N-terminal amino acid sequence was preceded by a sequence encoding a typical leader peptide. Transcripts hybridizing to the cloned fragment were detected in total RNA isolated from C. fimi cells grown on carboxymethyl cellulose but not from cells grown on glycerol or glucose. Transcription started at a cluster of sites 53 to 59 nucleotides upstream of a GUG translation initiation codon and terminated at either of two closely spaced C residues immediately downstream of a region of potential secondary structure. The size of the transcript was approximately 3.5 kilobases, sufficient to encode a polypeptide of 130 kilodaltons. The 130-kilodalton polypeptide is designated endoglucanase C (CenC), and the gene encoding it is designated cenC.
Synthesis of carbon‐14 labeled clomiphene (1985)

Abstract Clomiphene, 2‐[4‐(2‐chloro‐1,2‐diphenylethenyl)phenoxy]‐N, N‐diethylethanamine, an antiestrogen, is a nonsteroidal triphenylethylene derivative. For the successful synthesis of carbon‐14 labeled clomiphene it is essential to have a free radical inhibitor in the reaction medium.
Dipeptidyl Peptidase IV Inhibitors: The Next Generation of New Promising Therapies for the Management of Type 2 Diabetes (2007)

Type 2 diabetes is a chronic metabolic disease characterized by the presence of both fasting and postprandial hyperglycemia which is a result of pancreas beta-cell dysfunction, deficiency in insulin secretion, insulin resistance and/or increased hepatic glucose production. More recently, the role of other glucoregulatory hormones, including glucagon, amylin, and the gut peptide glucagon-like peptide (GLP)-1, and an increase in the rate of postmeal carbohydrate absorption have also been included as important pathophysiologic defects. Existing anti-diabetes medications are often unefficient at achieving sustained glycemic control because they predominantly address only a single underlying defect. A number of alternative therapies for type 2 diabetes are currently under development that take advantage of the actions of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide on the pancreatic beta-cell. One such approach is based on the inhibition of dipeptidyl peptidase IV (DPP-IV), the major enzyme responsible for degrading the incretins in vivo. DPP-IV exhibits characteristics that have allowed the development of specific inhibitors with proven efficacy in improving glucose tolerance in animal models of diabetes and type 2 diabetic patients. While enhancement of insulin secretion, resulting from blockade of incretin degradation, has been proposed to be the major mode of inhibitor action, there is also evidence that inhibition of gastric emptying, reduction in glucagon secretion, peripheral insulin sensitization and important effects on beta-cell differentiation and survival can potentially preserve beta-cell mass, and improve insulin secretory function and glucose handling in diabetic patients. The present article focuses on the preclinical and clinical data of DPP-IV inhibitors that make it unique therapeutic agents representing the next generation of antidiabetes drugs.
Recent developments for the efficient crystallographic refinement of macromolecular structures (1998)

Macromolecular crystallographic refinement has recently been made more efficient by the use of cross-validated maximum likelihood targets and torsion-angle molecular dynamics simulated annealing. In combination with automated model building methods, the amount of manual intervention required to complete and refine a structure is greatly reduced.
Amniotic membrane graft for primary pterygium: comparison with conjunctival autograft and topical mitomycin C treatment (2000)

This study showed that amniotic membrane graft was as effective as conjunctival autograft and mitomycin C in preventing pterygium recurrence, and can be considered as a preferred grafting procedure for primary pterygium.
The Vinyl Homopolymerization of Norbornene (2001)

A full literature and patent account (about 100 references) is given on work describing vinyl polymerization to form the homopolymer poly(norbornene). The interest in vinyl-poly(norbornene) is driven by its dielectric and mechanical properties for the technical application as an interlevel dielectric in microelectronics applications. For comparison, the norbornene/olefin copolymerization is discussed also. The metal catalysts are introduced and important polymer product properties are emphasized. The six possible isomers for stereoregular poly(norbornene) are presented.
HPV E6 induces eIF4E transcription to promote the proliferation and migration of cervical cancer (2013)

Increasing evidence has placed eukaryotic translation initiation factor 4E (eIF4E) at the hub of tumor development and progression. Several studies have reported that eIF4E is over-expressed in cervical cancer; however, the mechanism remains elusive. The results of this study further confirm over-expression of eIF4E in cervical cancer tumors and cell lines, and we have discovered that the transcription of eIF4E is induced by protein E6 of the human papillomavirus (HPV). Moreover, regulation of eIF4E by E6 significantly influences cell proliferation, the cell cycle, migration, and apoptosis. Therefore, eIF4E emerges as a key player in tumor development and progression and a potential target for CC treatment and prevention.
Biosynthesis of natural products. Part 1. Incorporations of ent-kaur-16-ene and ent-kaur-16-en-15-one into enmein and oridonin (1976)

Incorporations of ent-kaur-16-ene (7a) and ent-kaur-16-en-15-one (14a) into enmein (1a) and oridonin (6a) by Isodon japonicus Hara have been demonstrated by tracer experiments with seven labelled ent-kaurene derivatives. Furthermore, evidence has been obtained that functionalisation of ent-kaur-16-ene at the allylic position C–15 proceeds through direct oxygenation.
A Synthetic Adjuvant to Enhance and Expand Immune Responses to Influenza Vaccines (2010)

Safe, effective adjuvants that enhance vaccine potency, including induction of neutralizing Abs against a broad range of variant strains, is an important strategy for the development of seasonal influenza vaccines which can provide optimal protection, even during seasons when available vaccines are not well matched to circulating viruses. We investigated the safety and ability of Glucopyranosyl Lipid Adjuvant-Stable Emulsion (GLA-SE), a synthetic Toll-like receptor (TLR)4 agonist formulation, to adjuvant Fluzone® in mice and non-human primates. The GLA-SE adjuvanted Fluzone vaccine caused no adverse reactions, increased the induction of T helper type 1 (T(H)1)-biased cytokines such as IFNγ, TNF and IL-2, and broadened serological responses against drifted A/H1N1 and A/H3N2 influenza variants. These results suggest that synthetic TLR4 adjuvants can enhance the magnitude and quality of protective immunity induced by influenza vaccines.