gebhart/patrepeval huggingface dataset:
Practical Alkoxythiocarbonyl Auxiliaries for Iridium(I)‐Catalyzed C−H Alkylation of Azacycles (2017)

The development of new and practical 3-pentoxythiocarbonyl auxiliaries for Ir<sup>I</sup> -catalyzed C-H alkylation of azacycles is described. This method allows for the α-C-H alkylation of a variety of substituted pyrrolidines, piperidines, and tetrahydroisoquinolines through alkylation with alkenes. While the practicality of these simple carbamate-type auxiliaries is underscored by the ease of installation and removal, the method's utility is demonstrated in its ability to functionalize biologically relevant l-proline and l-trans-hydroxyproline, delivering unique 2,5-dialkylated amino acid analogues that are not accessible by other C-H functionalization methods.
Wnt-3, a gene activated by proviral insertion in mouse mammary tumors, is homologous to int-1/Wnt-1 and is normally expressed in mouse embryos and adult brain. (1990)

We have isolated a common insertion site, Wnt-3, for proviruses of the mouse mammary tumor virus (MMTV). Of mammary tumors induced by the GR variant of MMTV, 5% contains a provirus at Wnt-3, which is located on mouse chromosome 11. The gene is transcribed into a 3.8-kilobase (kb) mRNA in tumors with nearby proviral insertions but not in tumors with proviruses at other loci or in most adult tissues. Normal expression of Wnt-3 is detected in mouse embryos (with a peak around day 12 of gestation) and at low levels in adult brain. The transcriptional unit of the Wnt-3 gene spans approximately 55 kb, with a first intron of 36 kb. The deduced amino acid sequence of the Wnt-3 protein is 47% identical to the int-1/Wnt-1 gene product.
N‐Heterocyclic Carbene Catalyzed Oxidative Macrolactonization: Total Synthesis of (+)‐Dactylolide (2012)

Three key steps constitute the total synthesis of (+)-dactylolide: the 1,6-oxa conjugate addition reaction of a 2,4-dienal for the facile synthesis of the 2,6-cis-2-(4-oxo-2-butenyl)tetrahydropyran subunit, the umpolung alkylation reaction of a cyanohydrin, and the NHC-catalyzed oxidative macrolactonization reaction for the synthesis of the 20-membered macrocyle. NHC=N-heterocyclic carbene. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
On the Mode of Activation of the Catalytically Essential Sulfhydryl Group of Papain (1973)

The reaction of the thiol group of papain with chloroacetamide, iodoacetamide, d ‐ and l ‐2‐bromopropionamides was studied. In the acidic pH‐range the reaction rate is higher than expected for an ordinary SH‐group and shows a double‐sigmoid pH‐rate profile. In addition to the already described p K a of 8.5, we found a p K a of 4.0. This indicates that in the pH‐range where the enzyme is catalytically active the thiol group of Cys‐25 interacts with some amino acid side chain, presumably with the imidazole group of the neighboring His‐159. In the light of the X‐ray diffraction studies (Drenth et al. , 1971), it is probable that the anomalous P K a of His‐159 is due to its interaction with Trp‐177. The comparison of the pH‐rate profiles of d ‐ and l ‐2‐bromopropionamide reactions indicates that there is no sifgnificant alteration in the geometry of the active site around pH 4, whereas at slightly alkaline pH structural changes can be observed. 2 H 2 O has no effect on the rate constants of the alkylation reaction. This rules out the possibility of general base catalysis by the imidazole group of His‐159. The experimental data indicate that the dissociated thiol group forms an ion pair with the protonated imidazole group. On the basis of the formation of thiolate‐imidazolium ion pair, the mechanism of action of papain is reconsidered. It is concluded that the acylation and deacylation steps are not symmetrical processes, and they are one‐encounter type reactions. The interaction between His‐159 and Trp‐177 may be important in the catalysis.
Phase diagram of QCD (1998)

We analyze the phase diagram of QCD with two massless quark flavors in the space of temperature $T$ and chemical potential of the baryon charge \ensuremath{\mu} using available experimental knowledge of QCD, insights gained from various models, as well as general and model independent arguments including continuity, universality, and thermodynamic relations. A random matrix model is used to describe the chiral symmetry restoration phase transition at finite $T$ and \ensuremath{\mu}. In agreement with general arguments, this model predicts a tricritical point in the $T\ensuremath{\mu}$ plane. Certain critical properties at such a point are universal and can be relevant to heavy ion collision experiments.
A pseudo-CCM/DCM SIMO switching converter with freewheel switching (2003)

This paper presents a single-inductor multiple-output (SIMO) converter operating in pseudo-continuous conduction mode (PCCM) and/or discontinuous conduction mode (DCM). With the proposed freewheel switching control, this converter can handle large load currents with a much smaller current ripple, while retaining low cross regulation. It can also work in DCM for high efficiency at light loads. A prototype of a single-inductor dual-output (SIDO) boost converter was fabricated with a standard 0.5-μm CMOS n-well process. The two outputs are regulated at 2.5 and 3.0 V, respectively. At an oscillator frequency of 1 MHz, the efficiency reaches 89.4% at a total output power of 320 mW. Compared with prior designs, both current and voltage ripples are reduced. This design can be extended to have multiple outputs and for different types of dc-dc conversions, or be applied to single-output converters for fast transient response.
Expression of Heat Shock Factor 2 in Mouse Testis: Potential Role as a Regulator of Heat-Shock Protein Gene Expression during Spermatogenesis1 (1994)

We have examined the expression and function of heat shock transcription factor 2 (HSF2) in spermatogenic cells of mouse testis. The results of in situ RNA hybridization analysis, RNA filter hybridization, and reverse transcription-polymerase chain reaction (RT-PCR) analysis indicate that HSF2 mRNA expression in testis is subject to developmental and cell type-dependent, as well as stage-dependent, regulation. Localized expression of HSF2 mRNA in testis first appears between Day 14 and Day 21 of postnatal development. In adult testis, HSF2 mRNA is found at highest levels in spermatocytes and round spermatids. Immunocytochemical staining and gel mobility shift analysis demonstrate that HSF2 protein is localized to the nuclei of spermatocytes and round spermatids and that this transcription factor exists in testis in a constitutively active DNA-binding state. We further demonstrate that the constitutive HSF2 DNA-binding activity present in testis is able to interact with promoter sequences of the hsp70.2 gene, a testis-specific member of the hsp70 gene family. Taken together, our results show that the expression and functional properties of HSF2 are regulated in spermatogenic cell types of the mouse testis, supporting a role for this transcription factor as a regulator of hsp gene expression during spermatogenesis.
Improved Synthesis of (E)-3-Alkoxy- and (E)-3-Phenoxyacryloyl Chlorides (1993)

A one-step preparation of (E)-3-alkoxy- and (E)-3-phenoxyacryloyl chlorides by reaction of vinyl ethers and oxalyl chloride with subsequent decarbonylation is presented.
A Current-Sensitive Front-End Amplifier for Nano-Biosensors with a 2MHz BW (2007)

Active resistors up to 300GOmega operating down to the fA range are implemented in the feedback path of an integrator-differentiator transimpedance amplifier for high-sensitivity current measurements. The system has 4fA/radicHz noise up to 100kHz, a 2MHz bandwidth, and ensures unlimited measuring time even with nA DC input currents
THE FAS/FAS-LIGAND PATHWAY DOES NOT MEDIATE THE APOPTOSIS IN ELASTASE-INDUCED EMPHYSEMA IN MICE (2007)

Porcine pancreatic elastase (PPE), which induces emphysema via apoptosis, was administered to wild-type and Fas-deficient (lpr) mice. On days 3 and 28 after administration, the mean linear intercepts within lung tissues were significantly higher in PPE-treated wild-type and lpr mice than in control mice, though there were no significant differences between the PPE-treated groups. Likewise, the numbers of TUNEL-positive cells were increased in the lungs of PPE-treated wild-type and lpr mice, and again the effect was similar in the two PPE-treated groups. These findings suggest that apoptosis associated with PPE-induced emphysema is not mediated via the Fas/Fas-ligand pathway.
A Stem Cell Molecular Signature (2002)

Mechanisms regulating self-renewal and cell fate decisions in mammalian stem cells are poorly understood. We determined global gene expression profiles for mouse and human hematopoietic stem cells and other stages of the hematopoietic hierarchy. Murine and human hematopoietic stem cells share a number of expressed gene products, which define key conserved regulatory pathways in this developmental system. Moreover, in the mouse, a portion of the genetic program of hematopoietic stem cells is shared with embryonic and neural stem cells. This overlapping set of gene products represents a molecular signature of stem cells.
Wilms' Tumor Gene Expression in Human CD34+ Hematopoietic Progenitors During Fetal Development and Early Clonogenic Growth (1997)

To the Editor:

The Wilms' tumor gene ( WT1 ) located on chromosome 11p131 encodes a transcription factor, which is involved in control of growth and differentiation of various cell types including hematopoietic cells.[2][1] It activates or suppresses the transcription of target genes depending on
Enhanced arsenic excess in low-temperature grown GaAs due to indium doping (1997)

We have found that isovalent indium doping enhances arsenic excess in GaAs films grown by molecular beam epitaxy at low temperature. An increase in lattice expansion and near infrared optical absorption, as well as higher density of As clusters, have been observed in the indium-doped films when compared to the conventional indium-free ones.
Maternal endothelial function and serum concentrations of placental growth factor and soluble endoglin in women with abnormal placentation (2008)

Maternal serum concentrations of PlGF and sEng are altered in women who develop PE. However, these alterations do not correlate directly with maternal endothelial dysfunction.
Influence of strain on chemical reactivity. Relative reactivity of torsionally strained double bonds in 1,3-dipolar cycloadditions (1992)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTInfluence of strain on chemical reactivity. Relative reactivity of torsionally strained double bonds in 1,3-dipolar cycloadditionsKenneth J. Shea and Jang Seob KimCite this: J. Am. Chem. Soc. 1992, 114, 12, 4846–4855Publication Date (Print):June 1, 1992Publication History Published online1 May 2002Published inissue 1 June 1992https://doi.org/10.1021/ja00038a059RIGHTS & PERMISSIONSArticle Views1407Altmetric-Citations64LEARN 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 InReddit PDF (1 MB) Get e-Alerts Get e-Alerts
Inhibition of Cellular Protein Synthesis by Double-Stranded RNA: Inactivation of an Initiation Factor (1973)

Inhibition of protein synthesis in rabbit reticulocyte lysates by double-stranded RNA is caused by the inactivation of IF-3, an initiation factor required for the recycling of ribosomes and for their binding to messenger RNA. The evidence for this is that (i) the inhibition can be overcome by addition of exogenous If-3; (ii) double-stranded RNA inactivates stoichiometric amounts of IF-3; (iii) double-stranded RNA forms a complex with IF-3; and (iv) double-stranded DNA, which lacks inhibitory activity, also binds to IF-3, but with a much lower affinity than double-stranded RNA. It is concluded that double-stranded RNA inhibits cellular protein synthesis by tightly complexing with IF-3. It is suggested that IF-3 normally recognizes a double-stranded region in messenger RNA.
Highly Sensitive Fluorescent Probes for Zinc Ion Based on Triazolyl-Containing Tetradentate Coordination Motifs (2007)

Two new 1,2,3-triazolyl-containing N4-tetradentate ligands show nanomolar affinity for Zn2+ under physiological conditions. Furthermore, they are easily derivatizable to afford fluorescent probes suitable for sensitive Zn2+ detection. Structural characterizations in both solid and solution states suggest that N3 and N2 in the 1,2,3-triazolyl moiety coordinate with Zn2+ in A and B to afford five-membered and six-membered coordination rings, respectively. The probes show sensitive fluorescence enhancement and ratiometric responses to Zn2+.
Multiple pathways of rapid beta 2-adrenergic receptor desensitization. Delineation with specific inhibitors. (1990)

Exposure of beta-adrenergic receptors (beta ARs) to agonists causes rapid desensitization of the receptor-stimulated adenylyl cyclase response. Three main mechanisms have been implicated in this process: phosphorylation of the receptors by the cAMP-dependent protein kinase (PKA), phosphorylation by the specific agonist-dependent beta AR kinase, and sequestration of the receptors away from the cell surface. By applying inhibitors of these processes to digitonin-permeabilized A431 cells we investigated their contributions to beta AR desensitization. Each process could be selectively inhibited: PKA-dependent phosphorylation by an inhibitor peptide (amino acids 1-24 of the heat-stable inhibitor of PKA (PKI], beta AR kinase-dependent phosphorylation by heparin, and sequestration by concanavalin A. In permeabilized cells, heparin plus PKI completely blocked agonist-induced phosphorylation of the beta ARs. Desensitization was assessed by quantitating the signal transduction efficacy of the system. At high agonist concentrations (approximately 1 microM) up to 70% desensitization occurred. Complete blockade of this desensitization required the concurrent inhibition of all three pathways. When individual pathways were blocked it could be demonstrated that either the PKA or beta AR kinase mechanisms alone resulted in 40-50% desensitization whereas sequestration alone caused 20-30% desensitization. At low agonist concentrations (approximately 10 nM), the PKA pathway was selectively activated. These data indicate that while desensitization mediated via the three different mechanisms can occur independently, the quantitative contributions are not additive. Such findings suggest distinct but overlapping physiological roles for each mechanism in controlling receptor function.
Intratumoral Administration of TLR4 Agonist Absorbed into a Cellular Vector Improves Antitumor Responses (2011)

TLR4 on antigen-presenting cells in the tumor microenvironment may be targeted by using cell-based vectors for improved antitumor response in vivo.
Transcriptional Regulation of the Transforming Growth Factor-β-inducible Mouse Germ Line Ig α Constant Region Gene by Functional Cooperation of Smad, CREB, and AML Family Members (2000)

Smads regulate transcription of defined genes in response to transforming growth factor-beta (TGF-beta) receptor activation. This process involves functional cross-talk of Smads with transcription factors at responsive DNA elements to achieve maximal transcription activation and specificity. TGF-beta has been shown to induce transcription of the germ line (GL) Ig alpha constant region gene and to direct class switching to IgA antibodies. It has been shown that acute myeloid leukemia (AML) transcription factors cooperate with Smad3 to stimulate transcription from the GL Ig alpha constant region gene promoter. We report here that the TGF-beta-induced transcription from this promoter requires DNA binding of cAMP-response element-binding protein (CREB) to the nearby ATF/cAMP-response element site and of Smads to a nearby Smad binding sequence. At these sites, Smad3/4 cooperates with CREB to activate transcription in response to TGF-beta, and disruption of either binding sequence abolished TGF-beta-induced transcription. In addition, AML1 or AML2 also binds to the promoter and cooperates with Smad3/4, and in this way further enhances the TGF-beta-induced transcriptional activation of the GL Ig alpha promoter. Thus, whereas Smad3/4, CREB, and AML family members bind independently to the respective DNA sequences in the GL Ig alpha promoter, functional synergy of Smads with CREB and AML proteins results in maximal TGF-beta-induced transcription.
Transcranial magnetic stimulation for migraine: clinical effects (2006)

The objective was to assess the impact of transcranial magnetic stimulation (TMS) on pain and the autonomic nervous system (ANS) in migraine. Forty-two people [mean age 41.43+/-11.69 (SD) years, 36 females] were randomised into high vs. low TMS stimulation groups and received 2 brief pulses of TMS. Thirty-three (33/42) individuals had heart-rate variability assessed, before and after stimulation. No group effects were found. Pain decreased by 75%; 32% of people after 1 treatment reported no headache after 24 h. Mean heart rate decreased from 79.05+/-10.27 to 72.89+/-11.35 beats/min. The low-frequency (LF) and the high-frequency (HF) areas derived from power spectral analyses increased [mean 6522+/-1277 to 8315+/-1009 beats/min(2) (LF) (p=0.001) and mean 5600+/-1568 to 8755+/-3071 beats/min(2) (HF) (p=0.001)]. The LF:HF ratio decreased from mean 1.31+/-0.51 to 1.13+/-0.48 (NS). TMS produces immediate, sustained reductions in pain and modification of the ANS.
The good, the bad, and the biased (2018)

column Share on The good, the bad, and the biased: five ways visualizations can mislead (and how to fix them) Author: Danielle Albers Szafir University of Colorado Boulder University of Colorado BoulderView Profile Authors Info & Claims InteractionsVolume 25Issue 4July - August 2018 pp 26–33https://doi.org/10.1145/3231772Published:27 June 2018Publication History 33citation16,614DownloadsMetricsTotal Citations33Total Downloads16,614Last 12 Months4,407Last 6 weeks680 Get Citation AlertsNew Citation Alert added!This alert has been successfully added and will be sent to:You will be notified whenever a record that you have chosen has been cited.To manage your alert preferences, click on the button below.Manage my AlertsNew Citation Alert!Please log in to your account Save to BinderSave to BinderCreate a New BinderNameCancelCreateExport CitationPublisher SiteGet Access
p53-independent NOXA induction overcomes apoptotic resistance of malignant melanomas (2004)

Once melanoma metastasizes, no effective treatment modalities prolong survival in most patients. This notorious refractoriness to therapy challenges investigators to identify agents that overcome melanoma resistance to apoptosis. Whereas many survival pathways contribute to the death-defying phenotype in melanoma, a defect in apoptotic machinery previously highlighted inactivation of Apaf-1, an apoptosome component engaged after mitochondrial damage. During studies involving Notch signaling in melanoma, we observed a gamma-secretase tripeptide inhibitor (GSI; z-Leu-Leu-Nle-CHO), selected from a group of compounds originally used in Alzheimer's disease, induced apoptosis in nine of nine melanoma lines. GSI only induced G2-M growth arrest (but not killing) in five of five normal melanocyte cultures tested. Effective killing of melanoma cells by GSI involved new protein synthesis and a mitochondrial-based pathway mediated by up-regulation of BH3-only members (Bim and NOXA). p53 activation was not necessary for up-regulation of NOXA in melanoma cells. Blocking GSI-induced NOXA using an antisense (but not control) oligonucleotide significantly reduced the apoptotic response. GSI also killed melanoma cell lines with low Apaf-1 levels. We conclude that GSI is highly effective in killing melanoma cells while sparing normal melanocytes. Direct enhancement of BH3-only proteins executes an apoptotic program overcoming resistance of this lethal tumor. Identification of a p53-independent apoptotic pathway in melanoma cells, including cells with low Apaf-1, bypasses an impediment to current cytotoxic therapy and provides new targets for future therapeutic trials involving chemoresistant tumors.
Glycosylation of Recombinant Prorenin in Insect Cells: The Insect Cell Line Sf9 Does Not Express the Mannose 6-Phosphate Recognition Signal (1994)

Sf9 cells infected with a recombinant baculovirus containing the gene for human prorenin were cultured in the presence of [3H]mannose. In vivo labeled prorenin was isolated by immunoprecipitation from the culture medium and digested with Pronase. The oligosaccharide structures on the resulting glycopeptides were analyzed by a combination of lectin, ion-exchange, paper, and high-pressure liquid chromatography. Of the N-linked oligosaccharides isolated from the Sf9-produced prorenin, 98% were of a truncated (trimannosyl) high-mannose type, approximately two-thirds of which contained a fucose residue linked to the reducing N-acetylglucosamine. The remaining 2% constituted a mixture of high-mannose-type structures containing six, seven, or eight mannose residues; none of these structures were core-fucosylated. None of the oligosaccharide structures recovered from recombinant prorenin synthesized by Sf9 cells were phosphorylated or contained any other form of charge. Furthermore, assays for UDP-GlcNAc-lysosomal-enzyme N-acetylglucosamine phosphotransferase demonstrated no activity above background in lysates prepared from Sf9 cells. Blotting of Sf9 cell lysates with an 125I-labeled, soluble form of the cation-independent mannose 6-phosphate receptor failed to detect any proteins carrying the mannose 6-phosphate recognition signal. Taken together, the data suggest that Sf9 cells do not synthesize high-mannose-type oligosaccharides containing mannose 6-phosphate, and consequently it appears unlikely that these cells utilize the mannose 6-phosphate receptor mediated pathway for targeting of lysosomal enzymes.