gebhart/patrepeval huggingface dataset:
Protecting groups for the pyrrole and indole nitrogen atom. The [2-(trimethylsilyl)ethoxy]methyl moiety. Lithiation of 1-[[2-(trimethylsilyl)ethoxy]methyl]pyrrole (1984)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTProtecting groups for the pyrrole and indole nitrogen atom. The [2-(trimethylsilyl)ethoxy]methyl moiety. Lithiation of 1-[[2-(trimethylsilyl)ethoxy]methyl]pyrroleJoseph M. Muchowski and Dennis R. SolasCite this: J. Org. Chem. 1984, 49, 1, 203–205Publication Date (Print):January 1, 1984Publication History Published online1 May 2002Published inissue 1 January 1984https://pubs.acs.org/doi/10.1021/jo00175a053https://doi.org/10.1021/jo00175a053research-articleACS PublicationsRequest reuse permissionsArticle Views4787Altmetric-Citations81LEARN 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
Endocannabinoids enhance lipid synthesis and apoptosis of human sebocytes via cannabinoid receptor‐2‐mediated signaling (2008)

We had previously shown that both locally produced endocannabinoids and exocannabinoids, via cannabinoid receptor-1 (CB1), are powerful inhibitors of human hair growth. To further investigate the role of the cannabinoid system in pilosebaceous unit biology, we have explored in the current study whether and how endocannabinoids have an impact on human sebaceous gland biology, using human SZ95 sebocytes as cell culture model. Here, we provide the first evidence that SZ95 sebocytes express CB2 but not CB1. Also, prototypic endocannabinoids (arachidonoyl ethanolamide/anandamide, 2-arachidonoyl glycerol) are present in SZ95 sebocytes and dose-dependently induce lipid production and (chiefly apoptosis-driven) cell death. Endocannabinoids also up-regulate the expression of key genes involved in lipid synthesis (e.g., PPAR transcription factors and some of their target genes). These actions are selectively mediated by CB2-coupled signaling involving the MAPK pathway, as revealed by specific agonists/antagonists and by RNA interference. Because cells with "silenced" CB2 exhibited significantly suppressed basal lipid production, our results collectively suggest that human sebocytes utilize a paracrine-autocrine, endogenously active, CB2-mediated endocannabinoid signaling system for positively regulating lipid production and cell death. CB2 antagonists or agonists therefore deserve to be explored in the management of skin disorders characterized by sebaceous gland dysfunctions (e.g., acne vulgaris, seborrhea, dry skin).
Stability of anthracycline antitumor agents in four infusion fluids (1981)

The stabilities of doxorubicin hydrochloride, daunorubicin hydrochloride, zorubicin, and aclacinomycin A hydrochloride were studied in various infusion fluids at ambient temperature. Reversed-phase high-pressure liquid chromatographic procedures developed and used in these studies employed internal standards and readily separated each drug from its degradation products. Dilute solutions of the anthracyclines were prepared by appropriate dilutions of the reconstituted solutions of the formulated products with 5% Dextrose Injection, USP (D5W); 0.9% Sodium Chloride Injection, USP (NS); Lactated Ringer's Injection, USP (LR); and Normosol-R pH 7.4. The stability of the anthracyclines was dependent on the pH of the admixture solution which, in turn, was dependent on infusion fluid composition. Daunorubicin and aclacinomycin A exhibited acceptable stability (≥ to 90% of the original concentration) in D5W, NS, and LR for more than 48 hours. Doxorubicin manifested similar stability in the first two fluids. Zorubicin showed similar stability only in Normosol-R pH 7.4 fluid for 22 hours.
The inophyllums, novel inhibitors of HIV-1 reverse transcriptase isolated from the Malaysian tree, Calophyllum inophyllum Linn (1993)

As part of a search for novel inhibitors of HIV-1 reverse transcriptase, the acetone extract of the giant African snail, Achatina fulica, was shown to be active. Fractionation of the extract yielded inophyllums A, B, C, and E and calophyllolide (1a, 2a, 3a, 3b, and 6), previously isolated from Calophyllum inophyllum Linn., a known source of nutrition for A. fulica. From a methanol/methylene chloride extract of C. inophyllum, the same natural products in considerably greater yield were isolated in addition to a novel enantiomer of soulattrolide (4), inophyllum P (2b), and two other novel compounds, inophyllums G-1 (7) and G-2 (8). The absolute stereochemistry of inophyllum A (1a) was determined to be 10(R), 11(S), 12(S) from a single-crystal X-ray analysis of its 4-bromobenzoate derivative, and the relative stereochemistries of the other inophyllums isolated from C. inophyllum were established by a comparison of their 1H NMR NOE values and coupling constants to those of inophyllum A (1a). Inophyllums B and P (2a and 2b) inhibited HIV reverse transcriptase with IC50 values of 38 and 130 nM, respectively, and both were active against HIV-1 in cell culture (IC50 of 1.4 and 1.6 microM). Closely related inophyllums A, C, D, and E, including calophyllic acids, were significantly less active or totally inactive, indicating certain structural requirements in the chromanol ring. Altogether, 11 compounds of the inophyllum class were isolated from C. inophyllum and are described together with the SAR of these novel anti-HIV compounds.
Peptide Biosynthesis with Stable Isotope Labeling from a Cell-free Expression System for Targeted Proteomics with Absolute Quantification (2016)

Because of its specificity and sensitivity, targeted proteomics using mass spectrometry for multiple reaction monitoring is a powerful tool to detect and quantify pre-selected peptides from a complex background and facilitates the absolute quantification of peptides using isotope-labeled forms as internal standards. How to generate isotope-labeled peptides remains an urgent challenge for accurately quantitative targeted proteomics on a large scale. Herein, we propose that isotope-labeled peptides fused with a quantitative tag could be synthesized through an expression system in vitro, and the homemade peptides could be enriched by magnetic beads with tag-affinity and globally quantified based on the corresponding multiple reaction monitoring signals provided by the fused tag. An Escherichia coli cell-free protein expression system, protein synthesis using recombinant elements, was adopted for the synthesis of isotope-labeled peptides fused with Strep-tag. Through a series of optimizations, we enabled efficient expression of the labeled peptides such that, after Strep-Tactin affinity enrichment, the peptide yield was acceptable in scale for quantification, and the peptides could be completely digested by trypsin to release the Strep-tag for quantification. Moreover, these recombinant peptides could be employed in the same way as synthetic peptides for multiple reaction monitoring applications and are likely more economical and useful in a laboratory for the scale of targeted proteomics. As an application, we synthesized four isotope-labeled glutathione S-transferase (GST) peptides and added them to mouse sera pre-treated with GST affinity resin as internal standards. A quantitative assay of the synthesized GST peptides confirmed the absolute GST quantification in mouse sera to be measurable and reproducible.
Thermodynamic Analysis of Organic Rankine Cycles (2014)

In this thesis, investigations are carried out in order to find the best suitable working fluid for a given temperature limits of Organic Rankine Cycles (ORCs) with the focus on thermodynamic analysis, safety and environmental aspect. Making a suitable choice of working fluid for the ORC is of vital importance for the cycle efficiency and net work output. In this study only the dry and isentropic working fluids are investigated from different perspectives. Engineering Equation Solver (EES) software package was used as the main source to find thermo-physical properties of the working fluids. The data from EES were transferred to the VisSim software package and different block models were developed for the simulation of ORCs. Five organic working fluids used for this study are Butane, Isobutane, R245fa, R236fa and R124. The cycle operating parameters are varied and the effect of these parameters on the cycle performance and net work produced are investigated. Based on the simulations utilizing VisSim software, the cycle using butane as working fluid achieved the highest thermal efficiency (21.42%). The thermal efficiencies obtained for the ORCs using R245fa, Isobutane, R236fa and R124 as working fluids are 21.09, 20.87, 20.37 and 19.6% respectively. Although the thermal performance of the ORC utilizing R245fa is higher than the cycle utilizing Isobutane, specific net work produced by the cycle using isobutane is higher than the cycle using R245fa. Butane has better thermodynamic properties but it is not environmentally friendly because it is highly flammable and highly toxic with no ozone depletion potential (ODP) but with a global warming potential (GWP) of 20. The R245fa which also has good thermodynamic properties is not flammable and nearly non-toxic with no ODP and a GWP of 950. The five working fluids are investigated and the choice of the working fluid is based on the safety and its environmental characteristics. The R245fa is found to be the most suitable organic working fluid compared with the other four working fluids. Keywords: Organic Rankine Cycle, Low grade heat, Simulation
Modification of the density profile in a toroidal plasma source using a bias electric field (1997)

As in other plasma devices with a curved magnetic field geometry, an asymmetric density profile is observed in the PLADEPUS, a toroidal plasma source, at the University of Sydney. In this letter, we demonstrate that the asymmetric density profile can be improved by means of a positive bias electric field at the edge of the plasma. With the bias field, the density profile becomes symmetric and broadened, and the plasma density is enhanced.
The Inhibition of Mevalonic Kinase by Geranyl and Farnesyl Pyrophosphates (1968)

Abstract The inhibition in vitro of a highly purified preparation of mevalonate kinase by terpenyl pyrophosphates has been studied. Geranyl-PP and farnesyl-PP are potent inhibitors, while isopentenyl-PP, dimethylallyl-PP, and inorganic pyrophosphate do not inhibit significantly. The kinetics of geranyl-PP inhibition were investigated further and found to be uncompetitive with respect to mevalonic acid and competitive with respect to MgATP2-. Computer analysis of the data gave values of 2.65 ± 0.14 µm for Kii and 1.19 ± 0.12 µm for Kis. These results are consistent with the suggestion that geranyl-PP and farnesyl-PP act as physiological controls over farnesyl-PP biosynthesis and ATP utilization.
Homo‐ and Heterovalent Polynuclear Cerium and Cerium/Manganese Aggregates (2009)

Abstract Reactions of Ce III (NO 3 ) 3 ⋅6 H 2 O or (NH 4 ) 2 [Ce IV (NO 3 ) 6 ] with Mn‐containing starting materials result in seven novel polynuclear Ce or Ce/Mn complexes with pivalato ( t BuCO $\rm{{_{2}^{-}}}$ ) and, in most cases, auxiliary N,O‐ or N,O,O‐donor ligands. With nuclearities ranging from 6–14, the compounds present aesthetically pleasing structures. Complexes [Ce IV 6 ( μ 3 ‐O) 4 ( μ 3 ‐OH) 4 ( μ ‐O 2 C t Bu) 12 ] ( 1 ), [Ce IV 6 Mn III 4 ( μ 4 ‐O) 4 ( μ 3 ‐O) 4 (O 2 C t Bu) 12 (ea) 4 (OAc) 4 ]⋅4 H 2 O⋅4 MeCN (ea − =2‐aminoethanolato; 2 ), [Ce IV 6 Mn III 8 ( μ 4 ‐O) 4 ( μ 3 ‐O) 8 (pye) 4 (O 2 C t Bu) 18 ] 2 [Ce IV 6 ( μ 3 ‐O) 4 ( μ 3 ‐OH) 4 (O 2 C t Bu) 10 (NO 3 ) 4 ] [Ce III (NO 3 ) 5 (H 2 O)]⋅21 MeCN (pye − =pyridine‐2‐ethanolato; 3 ), and [Ce IV 6 Ce III 2 Mn III 2 ( μ 4 ‐O) 4 ( μ 3 ‐O) 4 ( t bdea) 2 (O 2 C t Bu) 12 (NO 3 ) 2 (OAc) 2 ]⋅4 CH 2 Cl 2 ( t bdea 2− =2,2′‐( tert ‐butylimino]bis[ethanolato]; 4 ) all contain structures based on an octahedral {Ce IV 6 ( μ 3 ‐O) 8 } core, in which many of the O‐atoms are either protonated to give ( μ 3 ‐OH) − hydroxo ligands or coordinate to further metal centers (Mn III or Ce III ) to give interstitial ( μ 4 ‐O) 2− oxo bridges. The decanuclear complex [Ce IV 8 Ce III Mn III ( μ 4 ‐O) 3 ( μ 3 ‐O) 3 ( μ 3 ‐OH) 2 ( μ ‐OH)(bdea) 4 (O 2 C t Bu) 9.5 (NO 3 ) 3.5 (OAc) 2 ]⋅1.5 MeCN (bdea 2− =2,2′‐(butylimino]bis[ethanolato]; 5 ) contains a rather compact Ce IV 7 core with the Ce III and Mn III centers well‐separated from each other on the periphery. The aggregate in [Ce IV 4 Mn IV 2 ( μ 3 ‐O) 4 (bdea) 2 (O 2 C t Bu) 10 (NO 3 ) 2 ]⋅4 MeCN ( 6 ) is based on a quasi‐planar {Mn IV 2 Ce IV 4 ( μ 3 ‐O) 4 } core made up of four edge‐sharing {Mn IV Ce IV 2 ( μ 3 ‐O)} or {Ce IV 3 ( μ 3 ‐O)} triangles. The structure of [Ce IV 3 Mn IV 4 Mn III ( μ 4 ‐O) 2 ( μ 3 ‐O) 7 (O 2 C t Bu) 12 (NO 3 )(furan)]⋅6 H 2 O ( 7 ⋅6 H 2 O) can be considered as {Mn IV 2 Ce IV 2 O 4 } and distorted {Mn IV 2 Mn III Ce IV O 4 } cubane units linked through a central ( μ 4 ‐O) bridge. The Ce 6 Mn 8 equals the highest nuclearity yet reported for a heterometallic Ce/Mn aggregate. In contrast to most of the previously reported heterometallic Ce/Mn systems, which contain only Ce IV and either Mn IV or Mn III , some of the aggregates presented here show mixed valency, either Mn IV /Mn III (see 7 ) or Ce IV /Ce III (see 4 and 5 ). Interestingly, some of the compounds, including the heterovalent Ce IV /Ce III 4 , could be obtained from either Ce III (NO 3 ) 3 ⋅6 H 2 O or (NH 4 ) 2 [Ce IV (NO 3 ) 6 ] as starting material.
Rx PC: the anti-virus handbook (1993)

Part 1 The anatomy of a virus: what is a virus? basic prescription for anti-virus protection. Part 2 The anti-virus programs: Virus-PC from MicroCom the Norton anti-virus PC-cillin 3.0 and PC Rx from Trend Micro Devices the shareware solution-McAfee Associates Virus Scan, VShield, and Clean-up anti-virus programs worth a second look case studies viruses can happen to anyone.
Gallium nitride based transistors (2001)

An overview is presented of progress in GaN electronic devices along with recent results from work at UCSB. From 1995 to 2001, the power performance of AlGaN/GaN high electron mobility transistors (HEMT) improved from 1.1 to 11 W mm(-1), respectively. The disadvantage of the low thermal conductivity of the sapphire substrate was mitigated by flip-chip bonding onto AIN substrates, yielding large periphery devices with an output power of 7.6 W. A variety of HEMT amplifier circuits have been demonstrated. The first AlGaN/GaN heterojunction bipolar transistor (HBT) was demonstrated in 1998, with a current gain of about 3. By developing the technique of emitter regrowth, a current gain of 10 was achieved in both GaN BJTs and AlGaN/GaN HBTs. A common emitter current gain cutoff frequency of 2 GHz was measured. Critical issues involved in the growth of high quality AlGaN/(AlN)/GaN heterostructures and GaN:Mg by metal-organic chemical vapour deposition (MOCVD) and molecular beam epitaxy (MBE) and the device fabrication are discussed.
Solution Synthesis of Ultrastable Luminescent Siloxane-Coated Silicon Nanoparticles (2004)

Silicon nanoparticles (NPs) of ∼4.5(1.10) nm from a room-temperature solution route are terminated by a silanization method for the first time. Energy-selected emission is observed, consistent with the distribution of sizes obtained by this route. The NPs are photochemically stable in nonpolar organic solvents and when exposed to air/water under ambient conditions for up to 1 year. The nanoparticles were characterized by TEM, HRTEM, EDX, SAED, FTIR, 1H/13C NMR, UV−vis, and photoluminescence (PL) spectroscopy.
An Expedient Phosphine-Catalyzed [4 + 2] Annulation:  Synthesis of Highly Functionalized Tetrahydropyridines (2003)

Ethyl 2-methyl-2,3-butadienoate acts as a 1,4-dipole synthon and undergoes [4 + 2] annulation with N-tosylimines in the presence of an organic phosphine catalyst. The resulting adducts, ethyl 6-substituted-1-(4-tosyl)-1,2,5,6-tetrahydro-pyridine-3-carboxylates, are formed in excellent yields with complete regioselectivity. Mechanistic reasoning for this new annulation has led to an expansion of the reaction scope by employing ethyl 2-(substituted-methyl)-2,3-butadienoates to give ethyl 2,6-cis-disubstituted-1-(4-tosyl)-1,2,5,6-tetrahydro-pyridine-3-carboxylates with high diastereoselectivities.
Toxic tau oligomer formation blocked by capping of cysteine residues with 1,2-dihydroxybenzene groups (2015)

Neurofibrillary tangles, composed of hyperphosphorylated tau fibrils, are a pathological hallmark of Alzheimer's disease; the neurofibrillary tangle load correlates strongly with clinical progression of the disease. A growing body of evidence indicates that tau oligomer formation precedes the appearance of neurofibrillary tangles and contributes to neuronal loss. Here we show that tau oligomer formation can be inhibited by compounds whose chemical backbone includes 1,2-dihydroxybenzene. Specifically, we demonstrate that 1,2-dihydroxybenzene-containing compounds bind to and cap cysteine residues of tau and prevent its aggregation by hindering interactions between tau molecules. Further, we show that orally administered DL-isoproterenol, an adrenergic receptor agonist whose skeleton includes 1,2-dihydroxybenzene and which penetrates the brain, reduces the levels of detergent-insoluble tau, neuronal loss and reverses neurofibrillary tangle-associated brain dysfunction. Thus, compounds that target the cysteine residues of tau may prove useful in halting the progression of Alzheimer's disease and other tauopathies.
Information filtering for mobile augmented reality (2002)

The use of augmented reality (AR) techniques can revolutionize the way people interact with unfamiliar environments. By tracking the user's position and orientation, complicated spatial information can be registered against the real world. My colleagues and I are researching the problem of developing mobile AR systems to be worn by individual users operating in large, complicated environments such as cities. However, an urban environment is extremely complicated. It is populated by large numbers of buildings, each of which can have numerous facts stored about it. Therefore, it is easy for a user to experience information overload. This problem is illustrated. To minimize problems of information overload, we have begun to develop algorithms for information filtering. These tools automatically restrict the amount of information displayed.
Patterns of medical practice in cystic fibrosis: Part II. Use of therapies (1999)

This report describes the prescribing pattern of therapeutic interventions in the management of patients with cystic fibrosis (CF), as observed in the Epidemiologic Study of Cystic Fibrosis (ESCF). Use of 20 therapies by 12,622 patients was recorded from each health care encounter (53,024 outpatient visits and 8,561 hospitalizations) during a 1-year period (1995), and analyzed by gender, age, severity of lung disease, and presence of any Pseudomonas species in the respiratory tract. The percentage of patients using the following pulmonary therapies was observed (in descending order): airway clearance techniques (88.2%); inhaled bronchodilators (82.2%); oral antibiotics (excluding quinolones) (68. 2%); dornase alfa (52.9%); intravenous antibiotics (34.4%); oral quinolones (34.4%); inhaled antibiotics (34.3%); mast cell stabilizers (29.5%); inhaled corticosteroids (25.9%); oral corticosteroids (17.1%); oral bronchodilators (16.2%); oxygen (8. 1%); inhaled mucolytic agent acetyl cysteine (6.5%); and diuretics (1.4%). The percentage of patients using nutritional therapies was: pancreatic enzymes (96%); oral nutritional supplements (31.1%); enteral nutrition (7.3%); and parenteral nutrition (0.7%). The percentage of patients using other therapies was: nonsteroidal anti-inflammatory drugs (7.9%); and insulin or oral hypoglycemic agents (6.1%). The general trend was for therapies to be used more by older patients, those with lower pulmonary function, and by those with Pseudomonas in their respiratory tract. Exceptions to this trend occurred for airway clearance, oral antibiotics, mast cell stabilizers, and pancreatic enzymes. Four therapies (oral nutritional supplements, parenteral nutrition, diuretics, and pancreatic enzymes) were used more by males than females. However, there was no gender difference for this group of therapies on pulmonary or nutritional status.
Long-Term and Tight Control of Gene Expression in Mouse Skeletal Muscle by a New Hybrid Human Transcription Factor (2002)

Diseases requiring frequent and lifelong injections of recombinant proteins would be more efficaciously treated by intramuscular delivery of genes encoding secretable proteins. However, the success of this approach largely depends on our capability to temporally regulate transcription of delivered genes. Therefore, we sought to generate a humanized transcription factor to regulate transgene expression in muscle. A novel 4-hydroxytamoxifen (4-OHT)-dependent transcriptional regulator (called HEA-3) was constructed by fusing in-frame the DNA binding domain of the human hepatocyte nuclear factor-1alpha (HNF1alpha), which is not expressed in muscle cells, a G(521)R mutant of the ligand binding domain of human estrogen receptor-alpha (ERalpha), and the activation domain derived from human nuclear factor-kappaB p65 subunit (NF-kappaB p65). We demonstrate that an artificial promoter containing multimeric HNF1alpha binding sites is silent in muscles and in cell lines that lack endogenous HNF1alpha. HEA-3 stimulated transcription from this target promoter in a stringent 4-OHT-dependent manner. The dynamic range of transgene regulation was high, because of the low basal activity and high inducibility of the system. Ex vivo, HEA-3 increased expression of the transfected reporter gene by more than 1000-fold in a ligand-dependent manner. In vivo, HEA-3 stimulated by more than 100-fold, the expression of secreted alkaline phosphatase after delivery as plasmid DNA into mouse muscles. Moreover, long-term modulation of the expression of intramuscularly delivered mouse erythropoietin was achieved in immunocompetent mice.
Immunization with Glycoprotein Subunits of Respiratory Syncytial Virus to Protect Cotton Rats Against Viral Infection (1987)

The cotton rat model of respiratory syncytial virus infection was used to study immunization with viral glycoproteins. Animals immunized with the purified attachment protein (G) or the fusion protein (F) developed complete pulmonary resistance, but only partial nasal resistance, to challenge with respiratory syncytial virus. Antibody produced to the G protein neutralized virus, whereas antibody to the F protein neutralized virus and also inhibited fusion of infected cells. There was no evidence of enhanced pulmonary pathology in any immunized group.