gebhart/patrepeval huggingface dataset:
The Nakada Synthesis of (+)-Ophiobolin A (2017)

Ophiobolin A 3 shows nanomolar toxicity toward a range of cancer cell lines. A central feature of this sesterterpene, isolated from the rice fungus Ophiobolus miyabeanus, is the highly-substituted eight-membered ring. A key step in the synthesis of 3 described (Chem. Eur. J. 2013, 19, 5476; Angew. Chem. Int. Ed. 2011, 50, 9452) by Masahisa Nakada of Waseda University was the acid-mediated cyclization of 1 to 2. The preparation of 1 began with the enantioselective hydrolysis of 4 to the mono­ester 5. Selective reduction followed by protection gave 6, that was carried on via 7 to 8. The ethoxyethyl group was selectively removed, and the alcohol was converted to an iodide (not illustrated) that was condensed with the lactone 9 to give 1. The cyclization of 1 could jeopardize the stereogenic center adjacent to the masked carbonyl, so eight diastereomers were possible. Careful optimization led to a prepar­atively useful yield of the desired product 2. Hydroboration gave 10, that was carried on to the aldehyde 11. The cyclopentanone 15 was prepared from the enantiomerically-enriched epox­ide 12. Opening with vinyl magnesium bromide followed by exposure to the second-generation Grubbs catalyst gave the diol 13, that was selectively protected, leading to 14. The derived bromohydrin was a mixture of regioisomers and diastereomers, from which, after oxidation, 15 dominated. Generation of the boron enolate from 15 in the presence of 11 gave the aldol product, that could be dehydrated with the Burgess rea­gent. Reduction with Raney nickel set the stereogenic center adjacent to the ketone, that was carried on to 16. Metathesis to close the eight-membered ring was not trivial. Finally, it was found that 17 could be induced to cyclize to 18 at an elevated temperature using the second-generation Hoyveda catalyst. Protecting group exchange gave 19. Routine functional group manipulation then completed the synthesis of (+)-ophiobolin 3. Some years ago, Neil E. Schore of the University of California, Davis showed (Tetrahedron Lett. 1994, 35, 1153) that the opening of Sharpless-derived epoxides such as 12 with vinyl nucleophiles was unexpectedly flexible. One set of conditions gave the expected inversion, but alternative conditions led to opening with clean retention (or double inversion) of absolute configuration.
A New Power Factor Improving Algorithm Under High-Line and Light-load Conditions (2022)

A new accurate computational method suitable for improving power factor of high-power AC-DC power supplies under high AC line voltage and light-load conditions is presented in this paper. The method is both adaptive and iterative and capable of maximizing power factor while total harmonic distortion is controlled within a pre-determined acceptable value. The algorithm can be embedded into a power supply micro-controller or digital signal processor to automatically adjust power factor iteratively under a given operating condition. A simulation model, which is highly correlated with the power factor correction converter stage of a 2kW power supply, is utilized to perform the study to demonstrate the effectiveness of the new algorithm.
Optimization of the Answering Method with Probability Conversion (2008)

The growth of the Internet has facilitated data collection on a large scale. User opinions and behavior are private information and need to be collected using a method that protects their confidentiality. In this paper, we develop a method of collecting information that employs probability conversion. We make clear the relations among the answer functions' variance, the number of respondents, confidence and accuracy. We also describe the answer functions that maximize anonymity.
Origin and phylogenetic status of the local Ashanti Dwarf pig (ADP) of Ghana based on evidence from mtDNA analysis, MC1R, and Y-chromosome haplotypes (2016)

Abstract The Ashanti Dwarf Pig (ADP) of Ghana is an endangered pig breed with hardy and disease resistant traits. Characterisation of animal genetic resources provides relevant data for their conservation and sustainable use for food security and economic development. We investigated the origin and phylogenetic status of the local ADP of Ghana and their crosses with modern commercial breeds based on mtDNA, MC1R and Y-chromosome sequence polymorphisms, as well as genome-wide SNP genotyping. The study involved 164 local pigs sampled from the three agro-ecological zones of Ghana. Analyses of the mitochondrial D-loop region and Y-chromosome sequences revealed both European and Asian genetic signatures, with differences between the geographical zones. Black coat colour is the most predominant within the breed, with dominant black MC1R alleles of both Asian and European origin contributing. European alleles for spotting are present at a low frequency in the sample set, and may account for the occurrence of spotted piglets in some APD litters. PCA analysis of SNP data revealed a strong location and breed effect on clustering of local Ghanaian pigs. On a global level, Ghanaian local pigs cluster closely with European pigs of commercial origin, such as the Large White. The presence of both European and Asian contributions, with differences between geographical zones probably reflects trading and colonial influences.. Understanding the effects of admixture on important adaptive and economic traits of the ADP and other local breeds in Africa is critical for developing sustainable conservation programmes to prevent the decline of these genetic resources.
Kinetics and Mechanism of the Polyene Formation during Dehydrochlorination of Poly(Vinyl Chloride) in the Solid State (1992)

Abstract In investigating the thermal, photolytical and chemical dehydrochlorination of poly(vinyl chloride) (PVC) it is shown that the formation of polyenes proceeds independently of the kind of initiation in a fast zip reaction and by the same mechanism. The sequence length distribution of the formed polyenes depends mainly on the conformation of the PVC chains. A strong correlation between this distribution and the conformation equilibrium of the polymer chains as well as the physical structure of the polymer solid is demonstrated. Key Words: DehydrochlorinationPVCkineticsmechanism
High Selective Performance of Designed Antibacterial and Anticancer Peptide Amphiphiles (2015)

Short designed peptide amphiphiles are attractive at killing bacteria and inhibiting cancer cell growth, and the flexibility in their structural design offers a great potential for improving their potency and biocompatibility to mammalian host cells. Amino acid sequences such as G(IIKK)nI-NH2 (n≥3) have been shown to be membrane lytic, but terminal amino acid modifications could impose a huge influence on their performance. We report in this work how terminal amino acid modifications to G(IIKK)3I-NH2 influence its α-helical structure, membrane penetrating ability, and selective actions against different cell types. Deletion of an N-terminal Gly or a C-terminal Ile did not affect their antibacterial activity much, an observation consistent with their binding behavior to negatively charged membrane lipid monolayers. However, the cytotoxicity against mammalian cells was much worsened by the N-terminal Gly deletion, consistent with an increase in its helical content. Despite little impact on the antibacterial activity of G(IIKK)3I-NH2, deletion of both terminal amino acids greatly reduced its antitumor activity. Cholesterol present in tumor cell membrane-mimic was thought to constrain (IIKK)3-NH2 from penetrating into the cancerous membranes, evident from its lowest surface physical activity at penetrating model lipid membranes. On the other hand, its low toxicity to normal mammalian cells and high antibacterial activity in vitro and in vivo made it an attractive antibacterial agent. Thus, terminal modifications can help rebalance the different interactions involved and are highly effective at manipulating their selective membrane responses.
Full-reference and reduced-reference quality metrics based on SIFT (2014)

In the last decade, an important research effort has been dedicated to implement objective image quality assessment metrics that reflect effectively human perception. Therefore, the aim of this paper is to propose new objective metrics that fulfill the demands of the image quality assessment field. For this sake, we propose two main full-reference (FR) quality metrics, and then adapt them in such a way to constitute several new reduced-reference (RR) quality metrics, for the case where the complete reference image is not available. We evaluate the influence of five types of distortion such as JPEG, JPEG2000, Gaussian Blur, AWGN, and Contrast change, on the image quality. The proposed metrics are based on the number of Scale-Invariant Feature Transform (SIFT) points, the number of SIFT matches between the unpaired and distorted images, and the Structural Similarity index (SSIM). In order to validate our proposed metrics, we compute the correlation between our metrics' scores and the subjective evaluation results. The results show a high correlation and a better quality range compared to well-known metrics, as well as a good robustness to reduced-reference situations.
Function and Component (2004)

This chapter contains sections titled: Introduction, The ASSERT Statement, FUNCTION, PROCEDURE, FUNCTION versus PROCEDURE Summary, Overloading, VHDL 2008, Exercises
17β-Estradiol Inhibits Inflammatory Gene Expression by Controlling NF-κB Intracellular Localization (2005)

Estrogen is an immunoregulatory agent, in that hormone deprivation increases while 17beta-estradiol (E2) administration blocks the inflammatory response; however, the underlying mechanism is still unknown. The transcription factor p65/relA, a member of the nuclear factor kappaB (NF-kappaB) family, plays a major role in inflammation and drives the expression of proinflammatory mediators. Here we report a novel mechanism of action of E2 in inflammation. We observe that in macrophages E2 blocks lipopolysaccharide-induced DNA binding and transcriptional activity of p65 by preventing its nuclear translocation. This effect is selectively activated in macrophages to prevent p65 activation by inflammatory agents and extends to other members of the NF-kappaB family, including c-Rel and p50. We observe that E2 activates a rapid and persistent response that involves the activation of phosphatidylinositol 3-kinase, without requiring de novo protein synthesis or modifying Ikappa-Balpha degradation and mitogen-activated protein kinase activation. Using a time course experiment and the microtubule-disrupting agent nocodazole, we observe that the hormone inhibits p65 intracellular transport to the nucleus. This activity is selectively mediated by estrogen receptor alpha (ERalpha) and not ERbeta and is not shared by conventional anti-inflammatory drugs. These results unravel a novel and unique mechanism for E2 anti-inflammatory activity, which may be useful for identifying more selective ligands for the prevention of the inflammatory response.
A study on the stereoscopic codecs for non-real-time 3DTV services (2011)

This paper presents a study on the stereoscopic 3D codec for non-real-time 3DTV services. Delivering stereoscopic 3DTV contents via broadcast networks can be based on either real-time or non-real-time scenarios. For a digital television system where its bandwidth is somewhat limited to accommodate the full 3D HD quality video, a complementary enabler is the non-real-time delivery in which 3D video component is downloaded in advance. In the case of ATSC system, MPEG-2, H.264/AVC and any other codec can be used for stereoscopic video based on Non- Real-Time services. In order to put in the best performance, the analysis on the stereoscopic codec, scenarios and preliminary considerations are required. In this paper, the NRT 3D codec scenarios and preliminary considerations are addressed to develop the prerequisites required for the analysis on NRT 3D codec. The experimentation of both independent and inter-view coding are covered to investigate the codec combination for NRT 3D video services based on considerations and scenarios.
ChemInform Abstract: A SAFER DIAZOTRANSFER REAGENT (1982)

Abstract Unter den Aspekten von synthetischer Brauchbarkeit, thermischer Stabilität, einfacher Handhabung, Sicherheit und Preis schneidet von den untersuchten Diazotransfer‐Reagenzien (I)‐(V) das p‐Dodecyl‐lvenzolsulfonylazid (V) am besten ab.
Measurement of sound pressure levels at low frequencies in rooms. Comparison of available methods and standards with respectto microphone positions (1999)

Measurement of sound pressure levels at low frequencies in rooms. Comparison of available methods and standards with respect
to microphone positions
Controlled introduction of mass calibrant into a highresolution mass spectrometer (1967)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTControlled introduction of mass calibrant into a highresolution mass spectrometerL. A. Shadoff and L. B. WestoverCite this: Anal. Chem. 1967, 39, 8, 1048Publication Date (Print):July 1, 1967Publication History Published online1 May 2002Published inissue 1 July 1967https://pubs.acs.org/doi/10.1021/ac60252a011https://doi.org/10.1021/ac60252a011research-articleACS PublicationsRequest reuse permissionsArticle Views30Altmetric-Citations2LEARN 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
Vertical Breast Reduction (2004)

The vertical approach to breast reduction surgery has achieved increasing popularity. The learning curve can be a problem for surgeons starting to incorporate vertical techniques into their practices; the medial pedicle approach is outlined in detail. Designing and creating the medial pedicle is straightforward and rotating it into position is easy. An elegant curve to the lower pole of the reduced breast can thus be created. Current concepts related to the skin brassiere, breast sutures, and the longevity of results are reviewed. It is important for the surgeon to understand that the skin resection pattern and the pedicle design are separate issues when discussing breast reduction surgery.
What's Not There: Odd Lots and Market Data (2014)

ABSTRACT We investigate odd‐lot trades in equity markets. Odd lots are increasingly used in algorithmic and high‐frequency trading, but are not reported to the consolidated tape or in databases such as TAQ. In our sample, the median number of odd‐lot trades is 24% but in some stocks odd lots are 60% or more of trading. Odd‐lot trades contribute 35% of price discovery, consistent with informed traders using odd lots to avoid detection. Omitting odd‐lot trades leads to inaccuracies in order imbalance measures and makes sentiment measures unreliable. Excluding odd lots from the consolidated tape raises important regulatory issues.
Phytochemicals and bioactive analysis of different sweet tea ( Lithocarpus litseifolius [Hance] Chun ) varieties (2020)

This paper aims to investigate the constituent phytochemicals and biological activities of six Lithocarpus litseifolius (Hance) Chun (L. litseifolius) cultivars. Processed by UPLC-MS/MS and untargeted metabolomics analysis software (MS-DIAL and MS-FINDER), components of different L. litseifolius cultivars were analyzed qualitatively and quantitatively. By conducting a comprehensive analysis of spectra, MS/MS fragmentation, and retention time, 40 compounds (including 6 phenolic glycosides and 34 flavonoids) were identified rapidly and accurately. Moreover, the total phenolic content (TPC), total flavonoid content (TFC), antioxidant, antimicrobial effects, and pheochromocytoma (PC12) cell viability of different L. litseifolius varieties were evaluated. Purple small leaf (PSL) was found to be the most superior variety with the highest antioxidant activities (8.27, 10.09, and 10.80 mg TE/g for DPPH, ABTS, and FRAP assays, respectively), broad-spectrum antimicrobial activity, and lowest cell cytotoxicity. The results showed that these bioactivities were closely related to phytochemicals among the six cultivars. PRACTICAL APPLICATIONS: L. litseifolius is well known as an important folk drink in the Southern China folklore for its specific efficacy in preventing diabetes. However, there is still a paucity of information on L. litseifolius, as other active components and bioactivities of it remain to be investigated. The wide range of flavonoids discovered in L. litseifolius provides abundant natural health-promoting agents for further applications in medicine and functional food.
A phase I study of cisplatin, etoposide, and paclitaxel in small cell lung cancer. (1997)

This phase I study was designed to determine the maximum tolerated dose of paclitaxel (Taxol; Bristol-Myers Squibb Company, Princeton, NJ) with standard doses of cisplatin and etoposide for patients with untreated, extensive-stage small cell lung cancer. Secondary objectives were to determine the toxicities, response rate, response duration, and overall survival in this cohort. Twenty-four patients were enrolled into four dose levels. All patients received a fixed dose of cisplatin at 80 mg/m2 intravenously (IV) on day 1. The first group received etoposide 50 mg/m2 IV on day 1 and 100 mg orally on days 2 and 3, while all subsequent groups received etoposide 80 mg/m2 IV on day 1 and 160 mg/m2 orally on days 2 and 3. The paclitaxel starting dose was 135 mg/m2 IV over 3 hours and escalated to 175 mg/m2 and 200 mg/m2. Cycles were repeated every 21 days for a maximum of six cycles. Granulocyte colony-stimulating factor was not given prophylactically, but was allowed in subsequent cycles according to American Society of Clinical Oncology guidelines. Nineteen patients were evaluable for toxicity and 18 patients were evaluable for response. Myelosuppression was the major toxicity, with grade 4 neutropenia occurring in 18 of 19 patients (95%), but febrile neutropenia was uncommon and developed in four of 19 patients (21%). Dose-limiting peripheral neuropathy was observed at a paclitaxel dose of 200 mg/m2. Grade 4 nausea/vomiting and diarrhea were also noted at this dose level. Four patients had complete responses (22%) and 13 patients had partial responses (72%). The overall response rate was 94%, with a median survival of 11 months and a 2-year survival rate of 19%. This three-drug combination of paclitaxel with cisplatin and etoposide is highly active with acceptable toxicity. Neurotoxicity was dose limiting at 200 mg/m2 paclitaxel. Neutropenia was frequent but was not associated with significant morbidity. The recommended doses for future clinical trials are paclitaxel 175 mg/m2 IV over 3 hours on day 1 with cisplatin 80 mg/m2 IV on day 1 and etoposide 80/160 mg/m2 IV on day 1 and orally on days 2 and 3. Growth factor support should be used according to American Society of Clinical Oncology guidelines.
Efficient Hydroliquefaction of Sawdust over a Novel Silica-Supported Monoclinic Molybdenum Dioxide Catalyst (2016)

A novel synthesis method was developed to prepare a silica-supported monoclinic molybdenum dioxide (MoO2/SiO2) catalyst via calcination of molybdenum disulfide (MoS2)/SiO2 in N2 flow with 0.1 vol % O2. MoO2/SiO2 was employed as a catalyst for sawdust hydroliquefaction in ethanol at 320 °C under an initial H2 pressure (IHP) of 2–6 MPa, and the bio-oil yield as high as 72.3% was obtained under an IHP of 6 MPa. The high catalytic activity of MoO2/SiO2 should be attributed to the efficient cleavage of H2 on the surface of highly dispersed MoO2, which shows an unusual metallic characteristic. The obtained bio-oil was analyzed with gas chromatography/mass spectrometry (GC/MS), and the main organic compounds detected by GC/MS were phenolics and ethyl esters.
Co-delivery of PLGA encapsulated invariant NKT cell agonist with antigenic protein induce strong T cell-mediated antitumor immune responses (2015)

Antitumor immunity can be enhanced by the coordinated release and delivery of antigens and immune-stimulating agents to antigen-presenting cells via biodegradable vaccine carriers. So far, encapsulation of TLR ligands and tumor-associated antigens augmented cytotoxic T cell (CTLs) responses. Here, we compared the efficacy of the invariant NKT (iNKT) cell agonist α-galactosylceramide (α-GalCer) and TLR ligands (R848 and poly I:C) as an adjuvant for the full length ovalbumin (OVA) in PLGA nanoparticles. We observed that OVA+α-GalCer nanoparticles (NP) are superior over OVA+TLR-L NP in generating and stimulating antigen-specific cytotoxic T lymphocytes without the need for CD4<sup>+</sup> T cell help. Not only a 4-fold higher induction of antigen-specific T cells was observed, but also a more profound IFN-γ secretion was obtained by the addition α-GalCer. Surprisingly, we observed that mixtures of OVA containing NP with α-GalCer were ineffective, demonstrating that co-encapsulation of both α-GalCer and antigen within the same nanoparticle is essential for the observed T cell responses. Moreover, a single immunization with OVA+α-GalCer NP provided substantial protection from tumor formation and even delayed the growth of already established tumors, which coincided with a prominent and enhanced antigen-specific CD8<sup>+</sup> T cell infiltration. The provided evidence on the advantage of antigen and α-GalCer coencapsulation should be considered in the design of future nanoparticle vaccines for therapeutic purposes.
Supplementary Data 3 from NR0B1 Is Required for the Oncogenic Phenotype Mediated by EWS/FLI in Ewing's Sarcoma (2023)

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Rapid Optimization of a Peptide Inhibitor of Malaria Parasite Invasion by Comprehensive N-Methyl Scanning (2009)

Apical membrane antigen 1 (AMA1) of the malaria parasite Plasmodium falciparum has been implicated in the invasion of host erythrocytes and is an important vaccine candidate. We have previously described a 20-residue peptide, R1, that binds to AMA1 and subsequently blocks parasite invasion. Because this peptide appears to target a site critical for AMA1 function, it represents an important lead compound for anti-malarial drug development. However, the effectiveness of this peptide inhibitor was limited to a subset of parasite isolates, indicating a requirement for broader strain specificity. Furthermore, a barrier to the utility of any peptide as a potential therapeutic is its susceptibility to rapid proteolytic degradation. In this study, we sought to improve the proteolytic stability and AMA1 binding properties of the R1 peptide by systematic methylation of backbone amides (N-methylation). The inclusion of a single N-methyl group in the R1 peptide backbone dramatically increased AMA1 affinity, bioactivity, and proteolytic stability without introducing global structural alterations. In addition, N-methylation of multiple R1 residues further improved these properties. Therefore, we have shown that modifications to a biologically active peptide can dramatically enhance activity. This approach could be applied to many lead peptides or peptide therapeutics to simultaneously optimize a number of parameters.