gebhart/patrepeval huggingface dataset:
Synthetic Estrogens, Implantation Inhibitors, and Hypocholesterolemic Agents. I. Tetrahydronaphthalene Series (1967)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthetic Estrogens, Implantation Inhibitors, and Hypocholesterolemic Agents. I. Tetrahydronaphthalene SeriesW. L. Bencze, L. I. Barsky, R. W. J. Carney, A. A. Renzi, and George. deStevensCite this: J. Med. Chem. 1967, 10, 2, 138–144Publication Date (Print):March 1, 1967Publication History Published online1 May 2002Published inissue 1 March 1967https://pubs.acs.org/doi/10.1021/jm00314a002https://doi.org/10.1021/jm00314a002research-articleACS PublicationsRequest reuse permissionsArticle Views181Altmetric-Citations15LEARN 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
Highly efficient N‐Heterocyclic carbene–palladium complex‐catalyzed multicomponent carbonylative Suzuki reaction: novel practical synthesis of unsymmetric aryl ketones (2007)

Abstract Highly efficient and chemoselective N ‐heterocyclic carbene palladium complexes‐catalyzed multicomponent carbonyltive Suzuki reaction with sodium tetraphenylborate used as phenylating reagent has been demonstrated in this article. Both electron‐rich and electron‐deficient aryl iodides gave unsymmetric aryl ketones in excellent yields. Copyright © 2007 John Wiley &amp; Sons, Ltd.
Structure of human RNA N6-methyladenine demethylase ALKBH5 provides insights into its mechanisms of nucleic acid recognition and demethylation (2014)

ALKBH5 is a 2-oxoglutarate (2OG) and ferrous iron-dependent nucleic acid oxygenase (NAOX) that catalyzes the demethylation of N(6)-methyladenine in RNA. ALKBH5 is upregulated under hypoxia and plays a role in spermatogenesis. We describe a crystal structure of human ALKBH5 (residues 66-292) to 2.0 Å resolution. ALKBH5₆₆₋₂₉₂ has a double-stranded β-helix core fold as observed in other 2OG and iron-dependent oxygenase family members. The active site metal is octahedrally coordinated by an HXD…H motif (comprising residues His204, Asp206 and His266) and three water molecules. ALKBH5 shares a nucleotide recognition lid and conserved active site residues with other NAOXs. A large loop (βIV-V) in ALKBH5 occupies a similar region as the L1 loop of the fat mass and obesity-associated protein that is proposed to confer single-stranded RNA selectivity. Unexpectedly, a small molecule inhibitor, IOX3, was observed covalently attached to the side chain of Cys200 located outside of the active site. Modelling substrate into the active site based on other NAOX-nucleic acid complexes reveals conserved residues important for recognition and demethylation mechanisms. The structural insights will aid in the development of inhibitors selective for NAOXs, for use as functional probes and for therapeutic benefit.
Ultra-compact, high-yield intra-cavity contacts for GaAs/AlGaAs-based vertical-cavity surface-emitting lasers (2012)

A novel method of fabricating compact intra-cavity contacts with high yield for GaAs/AlGaAs-based vertical-cavity surface-emitting lasers is presented. By carefully tailoring the composition of high-aluminum content layer, a highly selective Al2O3 etch-stop layer can be formed simultaneously with the oxide aperture during wet thermal oxidation. With this technique, contact metals can be uniformly deposited on deeply embedded contact layers over large substrate areas. Utilizing this embedded etch-stop design, dual intra-cavity contacted three-terminal vertical-cavity surface-emitting lasers were fabricated, demonstrating submilliampere threshold currents, over 54% differential quantum efficiencies and over 9 mW output powers.
[New psychotropic agents. I. Synthesis and pharmacologic activity of derivatives of 5H-imidazo-[2,1-c][1,4]benzodiazepine]. (1985)

The synthesis of 5H-imidazo [2,1-c] [1,4] benzodiazepine derivatives is described. Hydroxymethylation of 1-(2-nitrobenzyl)imidazoles by reaction with formaldehyde in a sealed tube and subsequent oxidation of hydroxymethylimidazoles with activated manganese dioxide afforded 1-(2-nitrobenzyl)imidazole-2-carboxaldehydes. The latter compounds were treated with iron(II) sulphate to yield directly the expected tricyclic imidazobenzodiazepines by intramolecular cyclization of the intermediates aminoaldehydes. The tricyclic derivatives were subjected to pharmacological screening to evaluate the effects on the behavior of the animals and the interaction with some biogenic amines. Some of the tested compounds were comparable to chlordiazepoxide in sedative and muscle-relaxant activities. None of them showed antiserotonin, anticholinergic or adrenolytic activities.
Cisplatin and Vindesine Combination Chemotherapy for Advanced Carcinoma of the Lung: A Randomized Trial Investigating Two Dosage Schedules (1981)

Eighty-five patients with advanced squamous carcinoma or adenocarcinoma of the lung were randomly assigned to receive vindesine with either high dose (120 mg/m2 of body surface area) or low dose (60 mg/m2) cisplatin. All patients had measurable disease and had not previously received chemotherapy. The response rate was similar with both treatments (43% complete and partial remission rate), but the high dose cisplatin regimen was superior to the low dose in median duration of response (12 versus 5.5 months; p = 0.05) and in median survival for responding patients (21.7 versus 10 months; p = 0.02). Myelosuppression was generally not a treatment problem; peripheral neuropathy and moderate azotemia were the major dose-limiting toxicities. With improved survival and response rates over those reported for conventional regimens, this combination of new agents supports the approach of new drug investigation in patients with lung cancer and the importance of the incorporation of active new agents into initial chemotherapy regimens.
Control of an optimized converter for modular solar power generation (2002)

Important drawbacks of solar power generation are the DC-wiring and fusing needed for the serial and parallel connection of solar panels. These problems can be reduced to AC wiring and fusing by using a modular set up of panels together with integrated single phase DC-AC power converters on a power level of approximately 200 W. A general applicable model has been developed for the coupling of two single-phase systems by a voltage link with small storage capacitance. It allows the decoupling of the pulsating mains power from the panel. Based on this model, which avoids the need of large filters, a sophisticated control principle has been developed. The result is a power converter which allows the operation in the maximum power point without any power pulsation In the solar panel. The required reactive elements, and therefore the size of the power converter, are very small.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Recipient CD4+ T cells that survive irradiation regulate chronic graft-versus-host disease (2004)

Chronic graft-versus-host disease (cGVHD) is an increasingly common cause of morbidity and mortality in allogeneic stem cell transplantation (alloSCT). Relative to acute GVHD (aGVHD), much less is understood about cGVHD. Using the B10.D2 --> BALB/c murine cGVHD model, which shares critical pathologic features with human cGVHD, we find that radiation-resistant host T cells regulate cGVHD. We initially observed that recipients lacking all lymphocytes developed accelerated and more severe cGVHD. Using genetically deficient recipients, we determined that alphabeta+CD4+ T cells were required to regulate cGVHD. Increased cGVHD severity was not due to the absence of T cells per se. Rather, the potency of regulation was proportional to host T-cell receptor (TCR) diversity. Only CD4+CD25+, and not CD4+CD25-, host T cells ameliorated cGVHD when added back, indicating that host T cells acted not via host-versus-graft activity or by reducing homeostatic proliferation but by an undefined regulatory mechanism. Thus, preparative regimens that spare host CD4+CD25+ T cells may reduce cGVHD. Donor CD4+CD25+ T cells also reduced cGVHD. Depletion of CD4+CD25+ cells from the inoculum exacerbated disease, whereas transplantation of additional CD4+CD25+ cells protected against severe cGVHD. Additional CD4+CD25+ cells also promoted healing of established lesions, suggesting that their effects persist during the evolution of cGVHD.
A Placebo-Controlled, Double-blind, Randomized Trial of an Extract of Ginkgo Biloba for Dementia (1997)

<h3>Context.</h3> —EGb 761 is a particular extract of Ginkgo biloba used in Europe to alleviate symptoms associated with numerous cognitive disorders. Its use in dementias is based on positive results from only a few controlled clinical trials, most of which did not include standard assessments of cognition and behavior. <h3>Objective.</h3> —To assess the efficacy and safety of EGb in Alzheimer disease and multi-infarct dementia. <h3>Design.</h3> —A 52-week, randomized double-blind, placebo-controlled, parallelgroup, multicenter study. <h3>Patients.</h3> —Mildly to severely demented outpatients with Alzheimer disease or multi-infarct dementia, without other significant medical conditions. <h3>Intervention.</h3> —Patients assigned randomly to treatment with EGb (120 mg/d) or placebo. Safety, compliance, and drug dispensation were monitored every 3 months with complete outcome evaluation at 12, 26, and 52 weeks. <h3>Primary Outcome Measures.</h3> —Alzheimer's Disease Assessment Scale—Cognitive subscale (ADAS-Cog), Geriatric Evaluation by Relative's Rating Instrument (GERRI), and Clinical Global Impression of Change (CGIC). <h3>Results.</h3> —From 309 patients included in an intent-to-treat analysis, 202 provided evaluable data for the 52-week end point analysis. In the intent-to-treat analysis, the EGb group had an ADAS-Cog score 1.4 points betterthan the placebo group (<i>P</i>=.04) and a GERRI score 0.14 points better than the placebo group (<i>P</i>=.004). The same patterns were observed with the evaluable data set in which 27% of patients treated with EGb achieved at least a 4-point improvement on the ADAS-Cog, compared with 14% taking placebo (<i>P</i>=.005); on the GERRI, 37% were considered improved with EGb, compared with 23% taking placebo (<i>P</i>=.003). No difference was seen in the CGIC. Regarding the safety profile of EGb, no significant differences compared with placebo were observed in the number of patients reporting adverse events or in the incidence and severity of these events. <h3>Conclusions.</h3> —EGb was safe and appears capable of stabilizing and, in a substantial number of cases, improving the cognitive performance and the social functioning of demented patients for 6 months to 1 year. Although modest, the changes induced by EGb were objectively measured by the ADAS-Cog and were of sufficient magnitude to be recognized by the caregivers in the GERRI.
A Novel Epidermal Growth Factor Receptor Inhibitor Promotes Apoptosis in Non–Small Cell Lung Cancer Cells Resistant to Erlotinib (2007)

Non-small cell lung cancer (NSCLC) with activating mutations in the epidermal growth factor receptor (EGFR) responds to EGFR tyrosine kinase inhibitors such as erlotinib. However, secondary somatic EGFR mutations (e.g., T790M) confer resistance to erlotinib. BMS-690514, a novel panHER/vascular endothelial growth factor receptor (VEGFR) inhibitor described here, exerted antiproliferative and proapoptotic effects on NSCLC cell lines, with prominent efficacy on H1975 cells expressing the T790M mutation. In this model, BMS-690514 induced a G(1) cell cycle arrest, as well as ultrastructural hallmarks of apoptosis, mitochondrial release of cytochrome c, and activation of caspases involved in the intrinsic (e.g., caspase-2, caspase-3, caspase-7, and caspase-9), but not in the extrinsic (e.g., caspase-8), pathway. Caspase inhibition conferred partial protection against BMS-690514 cytotoxicity, pointing to the involvement of both caspase-dependent and caspase-independent effector mechanisms. Transcriptome analyses revealed the up-regulation of proapoptotic (e.g., Bim, Puma) and cell cycle inhibitory (e.g., p27(Kip1), p57(Kip2)) factors, as well as the down-regulation of antiapoptotic (e.g., Mcl1), heat shock (e.g., HSP40, HSP70, HSP90), and cell cycle promoting [e.g., cyclins B1, D1, and D3; cyclin-dependent kinase 1 (CDK1); MCM family proteins; proliferating cell nuclear antigen (PCNA)] proteins. BMS-690514-induced death of H1975 cells was modified in a unique fashion by a panel of small interfering RNAs targeting apoptosis modulators. Down-regulation of components of the nuclear factor-kappaB survival pathway (e.g., p65, Nemo/IKK gamma, TAB2) sensitized cells to BMS-690514, whereas knockdown of proapoptotic factors (e.g., Puma, Bax, Bak, caspase-2, etc.) and DNA damage-related proteins (e.g., ERCC1, hTERT) exerted cytoprotective effects. BMS-690514 is a new pan-HER/VEGFR inhibitor that may become an alternative to erlotinib for the treatment of NSCLC.
Energy coupling efficiency of a hydrogen microwave plasma reactor (2001)

Zero-dimensional and two-dimensional plasma models and optical emission spectroscopy are used in tandem to investigate the power coupling efficiency for a pure hydrogen microwave plasma. The zero-dimensional model accounts for the vibrational kinetics of H2, the chemistry of H2 and H excited states, and the kinetics of ground-state species. The set of species conservation equations are then coupled to the electron Boltzmann equation (to account for the non-Maxwellian electron energy distribution function) and the total energy equation for solution. The two-dimensional model makes use of a simpler thermochemical description of the plasma. The chemistry is described with nine species and thirty chemical reactions. Three energy modes are considered to describe the plasma’s thermal nonequilibrium, and Maxwellian distribution functions for kinetic and vibrational modes are assumed. The non-Maxwellian nature of the electron energy distribution function is separately accounted for. Experimentally, the absolute line emission intensity is utilized to obtain number densities of up to five hydrogen excited states using the following transitions: Hα (6563 Å), Hβ (4861 Å), Hγ (4340 Å), Hδ (4102 Å), and Hε (3970 Å). The first three transitions were used for a 38 Torr, 1000 W hydrogen discharge, and all five transitions were used for a 121 Torr, 4000 W hydrogen discharge. The absolute continuum emission from the plasma was compared to numerical predictions. The comparison of the numerical and experimental data indicates that 90%–100% of the input power is deposited in the plasma and that both the line and continuum emission match within a factor of 3, with the exception of the high energy excited states for the 4000 W plasma. A control volume heat transfer analysis validates the energy coupling.
Hen egg-white lysozyme-specific T cells elicited in hen egg-white lysozyme-transgenic mice retain an imprint of self-tolerance. (1993)

The characteristics of T cell self-tolerance were examined in hen egg-white lysozyme (HEL)-transgenic (Tg) mice that were tolerant to a dose of HEL that was immunogenic in non-Tg littermates. HEL-specific T cells were identified in the periphery of the Tg mice after immunization with 100-times more HEL than was required to achieve a response in normal littermates. The Tg T cells were functional in vivo as they were capable of providing help to generate a HEL-specific antibody response. Selective deletion of T cells specific for the dominant T cell determinant of the native protein was not the primary mechanism of T cell tolerance in the HEL-Tg mice because, similar to non-Tg littermates, the majority of lymph node (LN) and T cell clones from HEL-Tg mice were specific for the dominant T cell determinant of HEL. Rather, our findings support the idea that the HEL-reactive T cells were anergic in vivo, but could be partially activated with a strong stimulus to the immune system (i.e., 20 nmol HEL and CFA). This conclusion is based on three observations: 1) proliferation in vitro to HEL by Tg LN T cells was subnormal (25% of control) and required 2 log more Ag to proliferate when compared with proliferation of LN from non-Tg littermates; 2) T cell clones isolated from HEL-Tg mice also proliferated poorly upon stimulation with HEL and Con A, although lymphokine production from the same stimuli was similar to that obtained from non-Tg clones; 3) invariably, upon repeated antigenic stimulation in vitro, the Tg T cell clones acquired full proliferative capacity to Ag and mitogens.
Reconstitution of a New Cysteine Biosynthetic Pathway inMycobacteriumtuberculosis (2005)

A new pathway for cysteine biosynthesis has been elucidated in Mycobacterium tuberculosis. This pathway involves a protein-bound thiocarboxylate (CysO-SH) as the sulfide donor, similar to thiamin biosynthesis. Cysteine synthase M (CysM) catalyzes the addition of cysteine to the carboxy terminus of the protein-bound thiocarboxylate to generate a CysO-cysteine adduct. A protease, Mec+, hydrolyzes the CysO-cysteine adduct to release cysteine and regenerate CysO. Mec+ contains a JAMM motif, and this work provides the first functional characterization of the JAMM motif in prokaryotes. MoeZ, a paralogue of ThiF, has been shown to transfer sulfur onto CysO.
[Fixing of osteochondral fragments with fibrinogen glue. Clinical experiences (author's transl)]. (1981)

Small osteochondral fragments are well fixed with the fibrinogen glue. This method is really a progress in comparison with the traditional fixation by screws or K-wires. The fragments were revascularized early. This is demonstrated by 31 glued osteochondral fragments which healed well. The joints must be immobilized during a period of 3 weeks.
Human thymocyte development in mouse organ cultures (1990)

A novel system to study human thymocyte development is described in which embryonic mouse thymic rudiments are seeded with human precursor cells in vitro. In these cultures human thymocytes proliferate extensively (greater than 20-fold increase in cell number) and mature, as evidenced by the accumulation of double and single positive (CD4+ and/or CD8+) cells. Data presented here suggest that the survival and ordered development of the mature human thymocytes in chimeric thymuses is dependent on human stromal elements. Immature CD4-CD8- human thymocytes failed to colonize or minimally recolonized mouse thymic lobes unless provided with high density (greater than 1.077 g/ml) human thymic cell fractions. These fractions contain multicellular complexes of epithelial/nurse cells, thymocytes, and dendritic cells/macrophages which dramatically enhanced the recolonizing capacity of purified CD4-CD8- thymocytes. The chimeric organ culture system described here provides not only a new approach for studying human T cell ontogeny but also a direct means for the future dissection of stromal interactions necessary for successful transition of precursor cells (CD4-CD8-) to immature double positive (CD4+CD8+) and mature single positive cells (CD4+ or CD8+) in the thymus.
Use of a single VH family and long CDR3s in the variable region of cattle Ig heavy chains (1997)

We have analyzed transcripts encoding the variable regions of Ig heavy chains from adult and fetal bovine splenocytes and bovine x mouse heterohybridomas. The 13 adult, seven fetal and two heterohybridomas transcripts as well as the six genes that were sequenced had > 83% identity to each other in the VH-encoded regions (FRs 1-3 and CDRs 1 and 2). By this criterion, all the bovine sequences were assigned to one family, which corresponds to the bovine homolog of the murine Q52 family. Southern blot analysis of genomic DNA demonstrated that homologs of other murine VH families such as 7183, S107 and 36-60 were present in the genome, but transcripts from these families were not detected in rapid amplification of cDNA ends (RACE)-PCR amplified products or in individual clones. The sequences of the adult transcripts using the mu isotype showed extensive somatic mutation indicating that the process of somatic hypermutation begins earlier in development of the bovine B cell. The length of CDR3 from V(D)J rearrangements averaged 21 amino acids, which is larger than other mammalian CDR3s. Analysis of CDR3s from 23 fetal transcripts revealed a preference for a reading frame in the putative D genes which is rich in glycine and tyrosine, and is also extensively mutated in adults. The bovine immune system appears to utilize Ig VH genes of a single family, but generates antibody diversity by extensive somatic mutation and long CDR3s which are subsequently hypermutated.
Electrochemical oxidation and the quantitative determination of carbon monoxide on metal–solid polymer electrolyte (SPE) system (1991)

Abstract The electrochemical oxidation of carbon monoxide on a platinum–Nafion electrode was examined. It was found that the oxidation of CO on the Pt‐Nafion electrode is more favored in an acidic solution than in an alkaline medium. This is in contrast with what was reported for bulk metal electrodes, for which the oxidation rate of CO in acid is much smaller than in alkaline solutions. This phenomenon is believed to be directly related to the cation‐exchange capability of the Nafion membrane. The rest potential of the Pt–Nafion electrode was found to be dependent on the partial pressure of CO, which is also in contrast with the behavior of bulk metal electrodes. This result was attributed to a mixed potential phenomenon. A quantitative determination of CO concentration in the gas phase was carried out on the basis of the Pt–Nafion electrode system in a controlled‐potential mode. The results obtained showed a number of attractive properties, including a low detection limit, good reproducibility, and a fast response time.
Large vessel sealing with the argon laser (1987)

This study compared the histology, biochemistry, and tensile strength of laser-welded and sutured canine venotomies, arteriotomies, and arteriovenous fistulas. Twelve animals had bilateral femoral vessels studied, with one repair (control) closed with interrupted 6-0 polypropylene sutures, and the contralateral repair (experimental) welded with the argon laser. Specimens were examined at weekly intervals from 1 to 4 weeks (four animals for each type of repair), and were evaluated histologically by hematoxylin and eosin, elastin, and trichrome stains; biochemically by the formation of [3H]hydroxyproline as an index of collagen synthesis; and mechanically by tensile strength determinations. At removal, all experimental closures were patent without hematomas, aneurysms, or luminal dilatation. Histologic and biochemical examination and tensile strength determinations suggest that laser welding may be an alternative to sutures for repair of large-diameter venotomies, arteriotomies, and arteriovenous fistulas, as healing is comparable to that seen with suture repairs up to 4 weeks postoperatively.