gebhart/patrepeval huggingface dataset:
In situ complexation directs the stereochemistry of N-glycosylation in the synthesis of thialanyl and dioxolanyl nucleoside analogs (1991)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTIn situ complexation directs the stereochemistry of N-glycosylation in the synthesis of thialanyl and dioxolanyl nucleoside analogsWoo Baeg Choi, Lawrence J. Wilson, Suresh Yeola, Dennis C. Liotta, and Raymond F. SchinaziCite this: J. Am. Chem. Soc. 1991, 113, 24, 9377–9379Publication Date (Print):November 1, 1991Publication History Published online1 May 2002Published inissue 1 November 1991https://pubs.acs.org/doi/10.1021/ja00024a058https://doi.org/10.1021/ja00024a058research-articleACS PublicationsRequest reuse permissionsArticle Views1148Altmetric-Citations121LEARN 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
Aerodynamic and Structural Design of a Small Nonplanar Wing UAV (2009)

The overall air vehicle performance of a multipl e lifting surface configuration has been studied with respect to both structural and aerodynamic considerations for a candidate mission similar to that of the AeroVironment Raven . The configuration studied is a biplane joined at the tips with endplates. M ore specifically , this study aims to determine if this particular nonplanar wing concept can meet the requirements of the mission for a small Reconnaissance, Surveillance and Target Acquisition UAV. The mission capabilities of small UAVs are constantly gro wing by implementing recent developments in miniature computers and peripherals, electronic sensors, and optical sensing equipment at affordable cost. The requirements for the mission profile of a small UAV using the aforementioned equipment are defined w ith an emphasis on the potential advantages that can be offered by the nonplanar concept wing under investigation. A structural analysis using the finite element software ADINA and an aerodynamic analysis based on wind tunnel experimental data and vortex p anel code results are performed. The results, compared under varying assumptions specific to an equivalent monoplane and a biplane, suggest potential efficiency gains for the new configuration may be possible using the nonplanar wing configuration under ex plicit conditions . The results also show structural characteristics and not aerodynamics alone are critical in determining the utility of this nonplanar concept.
STING Promotes the Growth of Tumors Characterized by Low Antigenicity via IDO Activation (2016)

Cytosolic DNA sensing is an important process during the innate immune response that activates the stimulator of interferon genes (STING) adaptor and induces IFN-I. STING incites spontaneous immunity during immunogenic tumor growth and accordingly, STING agonists induce regression of therapy-resistant tumors. However DNA, STING agonists, and apoptotic cells can also promote tolerogenic responses via STING by activating immunoregulatory mechanisms such as indoleamine 2,3 dioxygenase (IDO). Here, we show that IDO activity induced by STING activity in the tumor microenvironment (TME) promoted the growth of Lewis lung carcinoma (LLC). Although STING also induced IDO in tumor-draining lymph nodes (TDLN) during EL4 thymoma growth, this event was insufficient to promote tumorigenesis. In the LLC model, STING ablation enhanced CD8(+) T-cell infiltration and tumor cell killing while decreasing myeloid-derived suppressor cell infiltration and IL10 production in the TME. Depletion of CD8(+) T cells also eliminated the growth disadvantage of LLC tumors in STING-deficient mice, indicating that STING signaling attenuated CD8(+) T-cell effector functions during tumorigenesis. In contrast with native LLC tumors, STING signaling neither promoted growth of neoantigen-expressing LLC, nor did it induce IDO in TDLN. Similarly, STING failed to promote growth of B16 melanoma or to induce IDO activity in TDLN in this setting. Thus, our results show how STING-dependent DNA sensing can enhance tolerogenic states in tumors characterized by low antigenicity and how IDO inhibition can overcome this state by attenuating tumor tolerance. Furthermore, our results reveal a greater complexity in the role of STING signaling in cancer, underscoring how innate immune pathways in the TME modify tumorigenesis in distinct tumor settings, with implications for designing effective immunotherapy trials. Cancer Res; 76(8); 2076-81. ©2016 AACR.
The Yeast SLY Gene Products, Suppressors of Defects in the Essential GTP-Binding Ypt1 Protein, May Act in Endoplasmic Reticulum-to-Golgi Transport (1991)

It has been shown previously that defects in the essential GTP-binding protein, Ypt1p, lead to a block in protein transport from the endoplasmic reticulum (ER) to the Golgi apparatus in the yeast Saccharomyces cerevisiae. Here we report that four newly discovered suppressors of YPT1 deletion (SLY1-20, SLY2, SLY12, and SLY41) to a varying degree restore ER-to-Golgi transport defects in cells lacking Ypt1p. These suppressors also partially complement the sec21-1 and sec22-3 mutants which lead to a defect early in the secretory pathway. Sly1p-depleted cells, as well as a conditional lethal sly2 null mutant at nonpermissive temperatures, accumulate ER membranes and core-glycosylated invertase and carboxypeptidase Y. The sly2 null mutant under restrictive conditions (37 degrees C) can be rescued by the multicopy suppressor SLY12 and the single-copy suppressor SLY1-20, indicating that these three SLY genes functionally interact. Sly2p is shown to be an integral membrane protein.
Bioinformatics (2006)

Abstract The past two decades have witnessed revolutionary changes in biomedical research and biotechnology and an explosive growth of biomedical data. High throughput technologies developed in automated DNA sequencing, functional genomics, proteomics, and metabolomics enable production of such high volume and complex data that the data analysis becomes a big challenge. Consequently, a promising new field, bioinformatics, has emerged and is growing rapidly. Combining biological studies with computer science, mathematics and statistics, bioinformatics develops methods, solutions, and software to discover patterns, generate models, and gain insight knowledge of complex biological systems. This chapter presents an introduction to this exciting new field.
Long-term protection of chimpanzees against high-dose HIV-1 challenge induced by immunization (1997)

A combination AIDS vaccine approach consisting of priming with adenovirus-HIV-1MN gp160 recombinants followed by boosting with HIV-1SF2 gp120 was evaluated in chimpanzees. Long-lasting protection, requiring only three immunizations, was achieved against a low-dose challenge with the SF2 strain of HIV-1 and a subsequent high-dose SF2 challenge administered 1 year later without an intervening boost. Notably, neutralizing antibody responses against both clinical and laboratory isolates developed in three chimpanzees and persisted until the time of high-dose challenge. The possibility that cytotoxic T-lymphocytes contribute to low-dose protection of a chimpanzee lacking neutralizing antibodies is suggested. Our results validate the live vector priming/subunit booster approach and should stimulate interest in assessing this combination vaccine approach in humans.
Fosphenytoin (Cerebyx) (1997)

Fosphenytoin is a phosphate ester prodrug of phenytoin developed as a replacement for standard injectable sodium phenytoin. After absorption, phenytoin is cleaved (conversion half-life 8-15 min) from fosphenytoin. Unlike phenytoin, fosphenytoin is freely soluble in aqueous solutions (including standard intravenous solutions) and rapidly absorbed by the intramuscular route. Fosphenytoin has been tested successfully for three indications in humans: intramuscular maintenance dosing, intramuscular loading dose administration, and intravenous treatment of status epilepticus. Local toxicity (pain, burning, itching) is less by the intramuscular or intravenous route for fosphenytoin than for standard injectable sodium phenytoin. Systemic toxicity is similar with both preparations except that hypotension is less common and paresthesias are more common with fosphenytoin.
Enantioselective Catalysis, XIII. Preparative and Structural Chemistry of Chiral 3‐(Diphenylphosphanyl)‐pyrrolidiens and Their Palladium(II) Complexes (1997)

Abstract The preparation of both enantiomers of 3‐diphenylphosphanulpyrrolidiine ( 2 ) and several N ‐substituted derivatives together with two Pd Ii complexes of this ligand is reported. Form L‐malic acid and L‐hydroxyproline both enantiomers of 3‐hydroxypyrrolidine are prepared without any problems due to epimerization. KPPh 2 in the presence of LiCl is shown to be the most effective reagent for the synthesis of 2 . The reported X‐ray structure determination sof Pdl 2 complexes show a rather rigid bicyclic hetero‐norbornane skeleton. The flexibility of the other parts of the molecules is obvious in several polymorphs revealed by this method. This polymorphism is additionally investigated by a 31 P‐CP‐MAS study. From solution 1 ‐, 13 C‐ and 31 P‐NMR studies it is concluded that the bicyclic hetero‐norbornane skeleton is retained in solution.
Inhibition of hepatitis B virus polymerase-activity by various agents. Transient expression of hepatitis B virus DNA in hepatoma cells as novel system for evaluation of antiviral drugs. (1990)

The effect of three putative antiviral drugs--aciclovir (acyclovir, CAS 59277-89-3), zidovudine (azidothymidine, CAS 30516-87-1) and sorangicin B (a macrocyclic lactone, CAS 100415-25-6)--on replication and gene expression of hepatitis B virus (HBV) was studied in HepG2 cells. Transfection of these cells with cloned circular HBV DNA resulted in the production and secretion of virions into the medium. When antiviral drugs were added in increasing concentrations (aciclovir at 0.5 microgram/ml to 150 micrograms/ml, zidovudine 0.1 microgram/ml to 30 micrograms/ml, sorangicin B 1 micrograms/ml to 30 micrograms/ml), the activity of the viral polymerase decreased in a dose-dependent manner. Production of viral proteins as measured by the secretion of HBsAg and HBeAg into the medium was unaffected, suggesting interference of these drugs with viral DNA/RNA synthesis. It is concluded that aciclovir, zidovudine and sorangicin B inhibit the replication of HBV. Furthermore, the cell system used in our study appears to be suitable for the rapid testing of antiviral drugs and their evaluation for possible studies in vivo.
Focal Adhesion Motility Revealed in Stationary Fibroblasts (1999)

Focal adhesions (FAs) are clustered integrins and associated proteins that mediate cell adhesion and signaling. A green fluorescent protein-beta1 integrin chimera was used to label FAs in living cells. In stationary cells, FAs were highly motile, moving linearly for several plaque lengths toward the cell center. FA motility was independent of cell density and resulted from contraction of associated actin fibers. In migrating cells, FAs were stationary and only moved in the tail. FA motility in stationary cells suggests that cell movement may be regulated by a clutch-like mechanism by which the affinity of integrins to substrate may be altered in response to migratory cues.
Binding of Two Flaviolin Substrate Molecules, Oxidative Coupling, and Crystal Structure of Streptomyces coelicolor A3(2) Cytochrome P450 158A2 (2005)

Cytochrome P450 158A2 (CYP158A2) is encoded within a three-gene operon (sco1206-sco1208) in the prototypic soil bacterium Streptomyces coelicolor A3(2). This operon is widely conserved among streptomycetes. CYP158A2 has been suggested to produce polymers of flaviolin, a pigment that may protect microbes from UV radiation, in combination with the adjacent rppA gene, which encodes the type III polyketide synthase, 1,3,6,8-tetrahydroxynaphthalene synthase. Following cloning, expression, and purification of this cytochrome P450, we have shown that it can produce dimer and trimer products from the substrate flaviolin and that the structures of two of the dimeric products were established using mass spectrometry and multiple NMR methods. A comparison of the x-ray structures of ligand-free (1.75 angstroms) and flaviolin-bound (1.62 angstroms) forms of CYP158A2 demonstrates a major conformational change upon ligand binding that closes the entry into the active site, partly due to repositioning of the F and G helices. Particularly interesting is the presence of two molecules of flaviolin in the closed active site. The flaviolin molecules form a quasi-planar three-molecule stack including the heme of CYP158A2, suggesting that oxidative C-C coupling of these phenolic molecules leads to the production of flaviolin dimers.
Immunological effects of chimeric anti-GD3 monoclonal antibody KM871 in patients with metastatic melanoma. (2005)

We conducted an open label dose-escalation phase I trial of chimeric anti-GD3 mAb KM871 in patients with metastatic melanoma. Patients were entered into one of five dose levels (1, 5, 10, 20, and 40 mg/m2) and received three infusions of KM871 at 2-wk intervals. A metastatic melanoma site was biopsied at day 7-10. Pharmacokinetics, immune function, and mechanism of action of KM871 were analysed. A total of 17 patients were entered into the trial; 15 were evaluable. KM871 had a serum half-life (T1/2-beta) based on ELISA of 10.39 +/- 1.12 d (mean +/- SD). Trough levels >1.0 microg/mL KM871 at 2 wk postinfusion were seen with the 10 mg/m2 and higher dose levels. There were no significant changes in white blood cell subsets or serum complement levels during KM871 treatment. KM871 was stable in vivo and maintained binding affinity and complement-dependent cytotoxicity (CDC) function up to 2 wk postinfusion. No significant trends in CDC or antibody-dependent cellular-cytotoxicity (ADCC) activity in patients were observed during treatment. Analysis of tumour biopsies demonstrated a significant increase in CD4+ T cell infiltrates compared to control patient tumours (P = 0.010), and in patients with either stable disease (2 patients) or a clinical partial response (1 patient) at restaging, a significant increase in CD3 and CD4 infiltrates in tumour over nonresponding patients was observed. The favourable immune properties of KM871, combined with this preliminary clinical data, indicate that KM871 has potential for the treatment of metastatic melanoma.
KLIFS: a structural kinase-ligand interaction database (2015)

Protein kinases play a crucial role in cell signaling and are important drug targets in several therapeutic areas. The KLIFS database contains detailed structural kinase-ligand interaction information derived from all (>2900) structures of catalytic domains of human and mouse protein kinases deposited in the Protein Data Bank in order to provide insights into the structural determinants of kinase-ligand binding and selectivity. The kinase structures have been processed in a consistent manner by systematically analyzing the structural features and molecular interaction fingerprints (IFPs) of a predefined set of 85 binding site residues with bound ligands. KLIFS has been completely rebuilt and extended (>65% more structures) since its first release as a data set, including: novel automated annotation methods for (i) the assessment of ligand-targeted subpockets and the analysis of (ii) DFG and (iii) αC-helix conformations; improved and automated protocols for (iv) the generation of sequence/structure alignments, (v) the curation of ligand atom and bond typing for accurate IFP analysis and (vi) weekly database updates. KLIFS is now accessible via a website (http://klifs.vu-compmedchem.nl) that provides a comprehensive visual presentation of different types of chemical, biological and structural chemogenomics data, and allows the user to easily access, compare, search and download the data.
Brass Bands: Tradition, Change, and the Mass Media in Indian Wedding Music (1990)

A distinctive feature of most Indian weddings is the barCt, the procession from the groom's house to the home of the bride. This procession is frequently accompanied by lights, fireworks, music, and dance. In urban India, the most common musical accompaniment for the barat is the brass band.1 For ethnomusicologists, these multicultural ensembles pose a number of intriguing questions that are both specific to the Indian band world and relevant to wider areas of cultural change and interaction. These questions concern adaptation and maintenance of traditional social and professional patterns of behavior and organization, music activity as a means of increasing social mobility and economic opportunity, rural-urban migration, the historical roots of enculturation, and the effects of the mass entertainment media on musical activities and folk traditions. My research into these questions suggests that patterns of folk music activity, in an urban setting, have combined with features of a popular, mass-mediated music repertoire to create a unique sociomusical entity, the Indian brass band.
Phase 1 Clinical Experience Using Intravenous Administration of PV701, an Oncolytic Newcastle Disease Virus (2007)

PV701 is a naturally-attenuated, non-recombinant, oncolytic strain of Newcastle disease virus that displays preclinical intravenous (IV) efficacy. PV701 is selective at killing human cancer cells versus normal human cells based on tumor specific defects in the interferon (IFN)-mediated antiviral response. This oncolytic virus displays a broad spectrum of antitumor activity in vitro and in vivo. Preclinical models successfully predicted key clinical parameters including the mechanism of toxicity, two complementary strategies (desensitization and slow infusion) to reduce toxicity, and the starting dose for phase 1 trials. In three phase 1 trials of 114 patients using IV administration of PV701, Wellstat Biologics Corporation has evaluated the effects of dose, schedule, and infusion rate for PV701. Three general classes of side effects were seen: flu-like symptoms; tumor-site-specific adverse events (AEs); and infusion reactions. The first PV701 dose desensitized the patient to the side effects of further doses, allowing a marked increase in the maximum tolerated dose for subsequent doses compared to the first dose. Tumor responses were first noted at the higher doses achieved using desensitization. In the most recent phase 1 trial of 19 patients at Hamilton, Ontario, that employed desensitization, high repeat doses, and a slower infusion rate (Hamilton Regimen), there were six responses (4 major; 2 minor) and a total of six patients with survival for at least 2 years. In addition, patient tolerability improved using the Hamilton Regimen compared to IV bolus dosing used previously. Phase 2 studies of this novel biologic agent are about to begin.
Landscape of the SOX2 protein–protein interactome (2011)

SOX2 is a key gene implicated in maintaining the stemness of embryonic and adult stem cells that appears to re-activate in several human cancers including glioblastoma multiforme. Using immunoprecipitation (IP)/MS/MS, we identified 144 proteins that are putative SOX2 interacting proteins. Of note, SOX2 was found to interact with several heterogeneous nuclear ribonucleoprotein family proteins, including HNRNPA2B1, HNRNPA3, HNRNPC, HNRNPK, HNRNPL, HNRNPM, HNRNPR, HNRNPU, as well as other ribonucleoproteins, DNA repair proteins and helicases. Gene ontology (GO) analysis revealed that the SOX2 interactome was enriched for GO terms GO:0030529 ribonucleoprotein complex and GO:0004386 helicase activity. These findings indicate that SOX2 associates with the heterogeneous nuclear ribonucleoprotein complex, suggesting a possible role for SOX2 in post-transcriptional regulation in addition to its function as a transcription factor.
Orthogonal frequency division multiplex synchronisation techniques for wireless local area networks (2002)

A range of frequency acquisition, frequency tracking, symbol synchronisation and frame synchronisation techniques are proposed and evaluated for employment in 155 Mbit/s, 60 GHz local area networks. The algorithms are based on two correlation functions, exhibit a moderate implementational complexity and high robustness against channel noise.
Effect of Dietary Level of Phytic Acid on Hepatic and Serum Lipid Status in Rats Fed a High-sucrose Diet (2004)

The effect of dietary 0.02-10% sodium phytate on the hepatic and serum lipid status of rats fed a high-sucrose diet for 14 d was investigated. Hepatic levels of triglyceride and cholesterol and lipogenic enzymes activity were reduced with increasing dietary phytate level. The addition of 10% sodium phytate drastically depressed growth, food intake, and serum triglyceride and cholesterol levels.
Deposition of Gold Nanoparticles on Silica Spheres:  A Sonochemical Approach (2003)

Gold nanoparticles with an average size of ∼5 nm were deposited on the surface of preformed silica submicrospheres with the aid of power ultrasound. The sonochemical reduction was carried out by ultrasonic irradiation in an argon atmosphere at room temperature. Ultrasonic irradiation of a slurry of silica submicrospheres, chloroauric acid (HAuCl4), and ammonia in an aqueous medium for 45 min yielded a gold−silica nanocomposite. By controlling reaction conditions, we could achieve the deposition of metallic gold on the surface of the silica spheres. A unique crystallization process of the silica particles is observed. The crystallization process is assisted by the gold nanoparticles yielding the cristobalite phase of silica at a relatively low temperature. The resulting gold-deposited silica submicrosphere samples were characterized with XRD, EDAX, TEM, TGA, DSC, HR-SEM, and FT-IR, photoacoustic, and UV−visible spectroscopy.
A 80 MFLOPS 64-bit microprocessor for parallel computer (2002)

A 80-MFLOPS 64-bit microprocessor is described that employs superscalar architecture to execute two instructions, including the combination of 64-bit floating-point add and multiply instructions, in one 25-ns cycle simultaneously. The processor, implemented in a 0.8- mu m CMOS technology, contains 1300 K transistors. The processor also employs a RISC (reduced instruction set computer) architecture and Harvard-style bus organization. Division is accomplished every 200 ns. A typical performance is 64 MFLOPS.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>