gebhart/patrepeval huggingface dataset:
New synthetic reactions. Sulfenylations and dehydrosulfenylations of esters and ketones (1976)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNew synthetic reactions. Sulfenylations and dehydrosulfenylations of esters and ketonesBarry M. Trost, Thomas N. Salzmann, and Kunio HiroiCite this: J. Am. Chem. Soc. 1976, 98, 16, 4887–4902Publication Date (Print):August 1, 1976Publication History Published online1 May 2002Published inissue 1 August 1976https://pubs.acs.org/doi/10.1021/ja00432a034https://doi.org/10.1021/ja00432a034research-articleACS PublicationsRequest reuse permissionsArticle Views3474Altmetric-Citations444LEARN 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
Ligand-induced polyubiquitination of the platelet-derived growth factor beta-receptor. (1992)

We have analyzed the nature of ligand-induced shift to higher molecular weight forms of the beta-receptor for platelet-derived growth factor expressed in porcine aortic endothelial cells. The modification of the beta-receptor was found to be due to polyubiquitination, as judged by immunoblotting using an anti-ubiquitin antiserum. A mutant beta-receptor made kinase negative by a point mutation (K634A mutant) did not undergo ubiquitination in response to ligand stimulation. A mutant in which carboxyl-terminal 98 amino acids were deleted (CT98 mutant) and which retained kinase activity was likewise not ubiquitinated. These data suggest that the kinase activity, as well as the carboxyl-terminal 98 amino acids, is required for ubiquitination of the beta-receptor. Ligand-induced degradation of the receptor-bound ligand, as well as of the receptor itself, was partially impaired in the CT98-receptor-expressing cells, suggesting that the ubiquitination is of importance for efficient degradation of the ligand-receptor complex.
Development of Multianalyte Flow-through and Lateral-Flow Assays Using Gold Particles and Horseradish Peroxidase as Tracers for the Rapid Determination of Carbaryl and Endosulfan in Agricultural Products (2006)

Membrane-based competitive immunoassays using gold particles and horseradish peroxidase (HRP) as tracers in flow-through and lateral-flow formats for multianalysis of carbaryl and endosulfan were developed. For gold-based immunoassay, membrane strips were coated with goat anti-rabbit IgG (control line) and carbaryl hapten-ovalbumin (OVA) and endosulfan hapten-OVA (test lines). The visual detection limits for carbaryl and endosulfan were 100 and 10 microg/L in gold-based assays, respectively. For immunoassay using HRP as tracer, anti-carbaryl and anti-endosulfan antibodies were separately coated on the membrane as test lines, and the visual detection limits were 10 microg/L for carbaryl and 1 microg/L for endosulfan. The developed assays used gold particles and HRP as labels, respectively; 10 times enhancement in the visual detection limit using HRP label was obtained in the study. Matrix interference was eliminated by appropriate dilution of sample extracts with buffer. For the validation of the multianalyte assay, the samples were screened by multianalyte gold-based assay and confirmed by HPLC for carbaryl determination and by GC for endosulfan determination. The results of multianalyte gold-based flow-through assay for the determination of carbaryl and endosulfan were in good agreement with the results of instrumental analysis (HPLC with ultraviolet detection and GC with electron capture detection). The developed multianalyte immunoassays for which the results were interpreted visually can be used as convenient qualitative tools for on-site rapid screening of carbaryl and endosulfan simultaneously in agricultural products.
The Groucho/Transducin-like Enhancer of split Transcriptional Repressors Interact with the Genetically Defined Amino-terminal Silencing Domain of Histone H3 (1997)

Groucho is a transcriptional repressor implicated in Notch signaling and involved in neural development and segmentation in Drosophila. We are investigating the molecular mechanisms underlying the functions of Groucho and its mammalian homologs, the transducin-like Enhancer of split (TLE) proteins. We report that Groucho/TLEs are associated with chromatin in live cells and that they co-purify with isolated histones. Affinity chromatography and far Western blotting studies show further that native Groucho/TLE proteins interact specifically with histone H3 and not with other core histones. This interaction is mediated by the H3 amino-terminal domain previously shown by genetic analysis in yeast to be essential for the role of H3 in transcriptional silencing. We also demonstrate that Groucho/TLEs form oligomeric structures in vivo. These combined findings suggest that transcription complexes containing Groucho/TLEs may associate with chromatin through interactions with the amino terminus of histone H3 and that these interactions may be propagated along the chromosome due to the ability of Groucho/TLEs to participate in higher order structures.
Effects of size, capping agent, and concentration of CdSe and CdTequantum dots doped into a nematic liquid crystal on the optical and electro-optic properties of the final colloidal liquid crystal mixture (2009)

To investigate size and capping agent-dependent alignment and electro-optic effects of quantum dots (QDs) in nematic LCs, mixtures of a nematic phenylpyrimidine LC (LC1) doped with hexadecylamine-capped CdSe and thioglycolic acid-capped CdTe QDs were prepared and investigated by polarized optical microscopy between plain, untreated glass slides and in ITO-coated glass cells with rubbed polyimide alignment layers as well as by electro-optic analysis. The five investigated CdSe QDs, varying in size from 2.5 to 5.2 nm, show fluorescence emission maxima ranging from 480 to 610 nm, and the four CdTe QDs, varying in size from 3.2 to 4.0 nm, emit light from 530 to 610 nm depending on their size. The CdSe QDs favoring homeotropic anchoring of the nematic LC induce vertical alignment at 1 and 2 wt% in LC1 between plain glass slides and only at 1 wt% in the planar cells, except for CdSe QD emitting at 590 nm (CdSe590), which induces vertical alignment independent of the substrate only at 1 wt%. Concentrations above 2 wt% of the CdSe QDs in LC1 show planar alignment mainly due to aggregation of the QDs in LC1 at these higher concentrations. On the contrary, the CdTe QDs favoring planar anchoring of the nematic LC induce homeotropic alignment of LC1 at concentrations above 2 wt% between plain glass slides. All QDs are effective in reducing the threshold voltage (Vth) and the splay elastic constant (K11). The most drastic reduction over the entire temperature range, however, was observed for the smallest CdSe480 QDs, which showed the least tendency of all investigated QDs to aggregate in LC1.
Abolition by omeprazole of aspirin induced gastric mucosal injury in man. (1990)

This study investigates whether aspirin injury to the human gastric mucosa can be prevented by profound acid suppression with omeprazole, in a randomised, double blind, crossover design according to latin square. It was concluded that profound acid suppression can prevent aspirin induced gastric mucosal injury in normal subjects. This approach may prevent the development of peptic ulcers and their complications in patients taking aspirin and other non-steroidal anti-inflammatory drugs.
Expression of hepatitis B surface antigen in transgenic plants. (1992)

Tobacco plants were genetically transformed with the gene encoding hepatitis B surface antigen (HBsAg) linked to a nominally constitutive promoter. Enzyme-linked immunoassays using a monoclonal antibody directed against human serum-derived HBsAg revealed the presence of HBsAg in extracts of transformed leaves at levels that correlated with mRNA abundance. This suggests that there were no major inherent limitations of transcription or translation of this foreign gene in plants. Recombinant HBsAg was purified from transgenic plants by immunoaffinity chromatography and examined by electron microscopy. Spherical particles with an average diameter of 22 nm were observed in negatively stained preparations. Sedimentation of transgenic plant extracts in sucrose and cesium chloride density gradients showed that the recombinant HBsAg and human serum-derived HBsAg had similar physical properties. Because the HBsAg produced in transgenic plants is antigenically and physically similar to the HBsAg particles derived from human serum and recombinant yeast, which are used as vaccines, we conclude that transgenic plants hold promise as low-cost vaccine production systems.
Trait stacking via targeted genome editing (2013)

Modern agriculture demands crops carrying multiple traits. The current paradigm of randomly integrating and sorting independently segregating transgenes creates severe downstream breeding challenges. A versatile, generally applicable solution is hereby provided: the combination of high-efficiency targeted genome editing driven by engineered zinc finger nucleases (ZFNs) with modular 'trait landing pads' (TLPs) that allow 'mix-and-match', on-demand transgene integration and trait stacking in crop plants. We illustrate the utility of nuclease-driven TLP technology by applying it to the stacking of herbicide resistance traits. We first integrated into the maize genome an herbicide resistance gene, pat, flanked with a TLP (ZFN target sites and sequences homologous to incoming DNA) using WHISKERS™-mediated transformation of embryogenic suspension cultures. We established a method for targeted transgene integration based on microparticle bombardment of immature embryos and used it to deliver a second trait precisely into the TLP via cotransformation with a donor DNA containing a second herbicide resistance gene, aad1, flanked by sequences homologous to the integrated TLP along with a corresponding ZFN expression construct. Remarkably, up to 5% of the embryo-derived transgenic events integrated the aad1 transgene precisely at the TLP, that is, directly adjacent to the pat transgene. Importantly and consistent with the juxtaposition achieved via nuclease-driven TLP technology, both herbicide resistance traits cosegregated in subsequent generations, thereby demonstrating linkage of the two independently transformed transgenes. Because ZFN-mediated targeted transgene integration is becoming applicable across an increasing number of crop species, this work exemplifies a simple, facile and rapid approach to trait stacking.
Phase I and pharmacokinetic study of ecteinascidin 743 administered as a 72-hour continuous intravenous infusion in patients with solid malignancies. (2001)

Ecteinascidin 743 (ET-743) is a cytotoxic tetrahydroisoquinoline alkaloid that covalently binds to DNA in the minor groove. The in vitro chemosensitivity of cancer cells to ET-743 is markedly enhanced by prolonging the duration of exposure to the drug. A Phase I study of ET-743 given as a 72-h continuous i.v. infusion every 21 days was performed. Characteristics of the 21 adult patients with refractory solid tumors enrolled in the study were as follows: (a) 12 men; (b) 9 women; (c) median age, 59 years; (d) Eastern Cooperative Oncology Group performance status < or = 1, 20 patients; and (e) two prior regimens of chemotherapy, 7 patients. Dose limiting toxicity (DLT) was defined by typical criteria, except that grade 3 transaminitis did not constitute a DLT. There were no DLTs in the six patients evaluated at the first two dose levels of 600 and 900 microg/m2. Reversible grade 4 transaminitis occurred in two of nine patients after treatment with the first cycle of therapy at the third dose level of 1200 microg/m2. Another patient experienced grade 4 rhabdomyolysis, renal failure requiring hemodialysis, grade 4 neutropenia, and grade 3 thrombocytopenia during the second cycle of therapy with this dose. The maximum tolerated dose was 1200 microg/m2, and an additional six patients were enrolled at an intermediate dose level of 1050 microg/m2. This well-tolerated dose was established as the recommended Phase II dose. The disposition of ET-743 was distinctly biexponential, and a departure from linear pharmacokinetic behavior was evident at the 1200-microg/m2 dose level. Pharmacokinetic parameters determined at 1050 microg/m2 were (mean +/- SD): maximum plasma concentration, 318 +/- 147 pg/ml; initial disposition phase half-life, 9.0 +/- 10.3 min; terminal phase half-life, 69.0 +/- 56.7 h; and total plasma clearance, 28.4 +/- 22.5 liters/h/m2. Prolonged systemic exposure to concentrations of the agent that are cytotoxic in vitro were achieved. Toxicity of the drug is clearly schedule-dependent, because increasing the duration of infusion from 3 or 24 h to 72 h results in decreased myelosuppression and comparable hepatotoxicity. Although there were no objective responses to therapy, clear evidence of antitumor activity was observed in a patient with epithelioid mesothelioma, as confirmed by positron emission tomography studies. A Phase II trial to assess the efficacy of ET-743 against this highly refractory neoplasm has been initiated on the basis of this observation. The therapeutically optimal administration schedule remains to be established, inasmuch as there have been indications of activity against a variety of tumors during Phase I studies when the drug was infused over times ranging from 1 to 72 h. Characterizing the pharmacokinetics of ET-743 during the course of Phase II trials and Phase I combination studies is recommended to assure that this promising new anticancer drug can be used with an acceptable margin of safety.
Preclinical Characterization of the Antiglioma Activity of a Tropism-Enhanced Adenovirus Targeted to the Retinoblastoma Pathway (2003)

The antitumor activity of Delta-24-RGD suggests that it has the potential to be an effective agent in the treatment of gliomas.
Cyclic‐diGMP signal transduction systems in Vibrio cholerae: modulation of rugosity and biofilm formation (2006)

Cyclic di-guanylic acid (c-diGMP) is a second messenger that modulates the cell surface properties of several microorganisms. Concentrations of c-diGMP in the cell are controlled by the opposing activities of diguanylate cyclases and phosphodiesterases, which are carried out by proteins harbouring GGDEF and EAL domains respectively. In this study, we report that the cellular levels of c-diGMP are higher in the Vibrio cholerae rugose variant compared with the smooth variant. Modulation of cellular c-diGMP levels by overexpressing proteins with GGDEF or EAL domains increased or decreased colony rugosity respectively. Several genes encoding proteins with either GGDEF or EAL domains are differentially expressed between the two V. cholerae variants. The generation and characterization of null mutants of these genes (cdgA-E, rocS and mbaA) revealed that rugose colony formation, exopolysaccharide production, motility and biofilm formation are controlled by their action. Furthermore, epistasis analysis suggested that cdgC, rocS and mbaA act in convergent pathways to regulate the phenotypic properties of the rugose and smooth variants, and are part of the VpsR, VpsT and HapR signal transduction pathway.
A complex mutant of TEM-1 beta-lactamase with mutations encountered in both IRT-4 and extended-spectrum TEM-15, produced by an Escherichia coli clinical isolate (1997)

Escherichia coli GR102 was isolated from feces of a leukemic patient. It expressed different levels of resistance to amoxicillin or ticarcillin plus clavulanate and to the various cephalosporins tested. The double-disk synergy test was weakly positive. Production of a beta-lactamase with a pI of 5.6 was transferred to E. coli HB101 by conjugation. The nucleotide sequence was determined by direct sequencing of the amplification products obtained by PCR performed with TEM gene primers. This enzyme differed from TEM-1 (blaT-1B gene) by four amino acid substitutions: Met-->Leu-69, Glu-->Lys-104, Gly-->Ser-238 and Asn-->Asp-276. The amino acid susbstitutions Leu-69 and Asp-276 are known to be responsible for inhibitor resistance of the IRT-4 mutant, as are Lys-104 and Ser-238 substitutions for hydrolytic activity of the extended-spectrum beta-lactamases TEM-15, TEM-4, and TEM-3. These combined mutations led to a mutant enzyme which conferred a level of resistance to coamoxiclav (MIC, 64 microg/ml) much lower than that conferred by IRT-4 (MIC, 2,048 microg/ml) but higher than that conferred by TEM-15 or TEM-1 (MIC, 16 microg/ml). In addition, the MIC of ceftazidime for E. coli transconjugant GR202 (1 microg/ml) was lower than that for E. coli TEM-15 (16 microg/ml) and higher than that for E. coli IRT-4 or TEM-1 (0.06 microg/ml). The MICs observed for this TEM-type enzyme were related to the kinetic constants Km and k(cat) and the 50% inhibitory concentration, which were intermediate between those observed for IRT-4 and TEM-15. In conclusion, this new type of complex mutant derived from TEM-1 (CMT-1) is able to confer resistance at a very low level to inhibitors and at a low level to extended-spectrum cephalosporins. CMT-1 received the designation TEM-50.
Oligonucleotide Ligation Assay for Detection of Mutations Associated with Reverse Transcriptase and Protease Inhibitor Resistance in Non-B Subtypes and Recombinant Forms of Human Immunodeficiency Virus Type 1 (2005)

The oligonucleotide ligation assay is a genotypic assay for the detection of resistance-associated mutations to reverse transcriptase and protease inhibitors in human immunodeficiency virus type 1 subtype B. This assay has been modified and developed for non-B subtypes and recombinant strains and has been evaluated with sequencing, resulting in a more sensitive assay than sequencing for non-B subtypes.
Design of Biodegradable Polymer Systems for Controlled Release of Bioactive Agents (1993)

Major advances in therapeutic regimens are now possible with biodegradable polymer systems for controlled delivery of bioactive agents. Therapies involving peptide and protein drugs will be most applicable in the future; however, these types of therapies are limited in use due to their low oral absorption potential and relatively short half-lives. Parenteral (subcutaneous or intramuscular) administration of a "depot" preparation of a peptide/protein drug in a controlled release polymer matrix can provide very effective continuous therapy. Many of these delivery systems use microspheres composed of biodegradable homo- and copolymers of lactic and glycolic acid. Extensive experience with these materials has established their safety, biocompatibility, and subsequent biodegradation to non-toxic products. Short-term therapeutic regimens can be designed based on the selection and optimization of a number of drug/polymer variables. This paper examines the technology involved in the design of a controlled release injectable product for peptides and proteins, with particular emphasis on the pharmaceutical aspects of quality control and regulatory compliance.
Long‐term Compliance of Laryngectomized Patients With a Specialized Pulmonary Rehabilitation Device (1998)

Previous studies have demonstrated the positive effect of a heat and moisture exchanger (HME) on the respiratory system in patients after laryngectomy. However, patient compliance with these devices was reduced by device-related problems and troublesome combination with a voice prosthesis. Recently a more specialized device has become available. This is an HME combined with a valve for easy digital occlusion of the stoma (Provox Stomafilter; Hörby, Sweden). In the authors' initial study of this revised device, a clear improvement in short-term compliance was demonstrated. To investigate long-term compliance, 69 consecutive patients were interviewed by means of a structured questionnaire. The results show that all patients expressed their satisfaction with the valve used for digital occlusion of the stoma. Sixty-three percent of the patients reported that voicing was facilitated. Subjective intelligibility improved in 55% of the patients. Previous problems with other devices (e.g., plaster adherence, skin irritation, and handling) were clearly diminished, increasing the long-term compliance of the patients to 78%. This new HME can be considered as a beneficial pulmonary rehabilitation tool for laryngectomized patients.
Advanced animation and rendering techniques : theory and practice (1992)

Part I Basics 1. Rendering polygonal objects Part II Theoretical Foundations 2. The theory and practice of light/object interaction 3. The theory and practice of parametric representation techniques 4. The theory and practice of anti-aliasing techniques Part III Advanced Rendering Techniques: Approaches, Applications and Algorithms 5. Shadow generation techniques 6. Mapping techniques: texture and environment mapping 7. Procedural texture mapping and modelling 8. Ray tracing I: basic recursive ray tracing 9. Ray tracing II: practical ray tracing 10. Ray tracing III: advanced ray tracing models 11. Radiosity methods 12. Global illumination models 13. Volume rendering techniques 14. Advanced rendering interfaces: shading languages and RenderMan Part IV Advanced Animation 15. Overview and low-level motion specification 16. Animating articulated structures 17. Soft object animation 18. Procedural animation Reference Index
Synthesis and Screening of Linear and Cyclic Oligocarbamate Libraries. Discovery of High Affinity Ligands for GPIIb/IIIa (1998)

Synthetic methodology has been developed for the generation of large, diverse libraries of “unnatural” carbamate oligomers using the “one bead, one peptide” method. Using a pool of 27 structurally and functionally diverse monomers, one acyclic and two cyclic libraries were synthesized and screened for binding to the integrin GPIIb/IIIa. Several classes of oligocarbamate ligands for GPIIb/IIIa were discovered, and two cyclic ligands have activities that are within a factor of 3 of kistrin, a snake venom protein that effectively inhibits platelet aggregation. Preliminary pharmacokinetic characterization was performed on a linear oligocarbamate ligand, which was cleared from plasma with a half-life of 3.6 min.