gebhart/patrepeval huggingface dataset:
Realization of dual-frequency and wide-band VSWR performances using normal-model helical and inverted-F antennas (1998)

The effects of parasitic elements on the voltage standing wave ratios (VSWR's) of two antennas are investigated. First, a parasitic monopole is used for a normal-mode helical antenna. The VSWR investigation shows that dual-frequency operation is obtained by the parasitic element effects. The dual-frequency operation is revealed as a function of monopole position above a ground plane (monopole height). As the monopole height decreases, the separation of a higher resonance frequency f/sub H/ from a lower resonance frequency f/sub L/ increases. For a monopole length of L/sub MP//spl ap/0.4/spl lambda//sub HX/, where /spl lambda//sub HX/ is the resonance wavelength of the helix, the frequency bandwidth for a VSWR=2 criterion is 12.5% in the lower frequency f/sub L/ region and 5.2% in the higher frequency f/sub H/ region, with a frequency separation ratio of f/sub H//f/sub L/=2.14. Secondly, L-figured parasitic elements are used for an inverted-F antenna (IFA). The parasitic elements improve the VSWR performance. The frequency bandwidth for a VSWR=2 criterion is approximately two times as wide as that of the single IFA. It is also found that bending the horizontal sections of the IFA and parasitic elements contributes to reducing the antenna size while not significantly deteriorating the VSWR bandwidth. The radiation patterns are also presented and discussed.
Electrospray Ionization High-Field Asymmetric Waveform Ion Mobility Spectrometry−Mass Spectrometry (1999)

High-field asymmetric waveform ion mobility spectrometry (FAIMS) is a new technique that separates gas-phase ions at atmospheric pressure (760 Torr) and room temperature. A FAIMS instrument acts as an ion filter and can be set to continuously transmit one type of ion. Despite the stringent requirement for a flow of clean, dry gas in the FAIMS analyzer region, a method of coupling electrospray to FAIMS has been developed. The identity of the electrospray ions separated by FAIMS was determined using mass spectrometry (FAIMS-MS). The theory of FAIMS is discussed, and electrospray FAIMS-MS spectra of several compounds in modes P1, P2, N1, and N2 are presented. Ions appearing in P1 and N1 modes tend to have mobilities that increase as a function of increasing electric field strength, whereas ions appearing in P2 and N2 modes tend to have mobilities that decrease. In general, low-mass ions are focused in P1 and N1 modes, whereas larger ions (e.g., proteins) are focused in P2 and N2 modes. Short-chain peptides, (Gly)(n) where n = 1-6, are shown to cross over from P1 mode into P2 mode as the chain length increases. The removal of the low-mass solvent cluster ions, combined with a reduction of the background noise in electrospray FAIMS-MS, results in an improved signal-to-noise ratio for mass spectra of larger ions (e.g., cyctochrome c) when compared with conventional electrospray-MS. Preliminary results also suggest that various charge states of cytochrome c can be distinguished by FAIMS, implying that the ion mobility of these species at high electric field strength is sensitive to the structure of the protein ion. The linearity of response of electrospray FAIMS-MS was investigated using leucine enkephalin and shows the calibration curve to be linear for ∼3 orders of magnitude.
K-252a, a novel microbial product, inhibits smooth muscle myosin light chain kinase. (1988)

Effects of K-252a, (8R*, 9S*, 11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8, 11-epoxy-1H,8H,11H-2,7b,11a-triazadibenzo[a,g]cycloocta [cde]trinden-1-one, purified from the culture broth of Nocardiopsis sp., on the activity of myosin light chain kinase were investigated. 1) K-252a (1 x 10(-5) M) affected three characteristic properties of chicken gizzard myosin-B, natural actomyosin, to a similar degree: the Ca2+-dependent activity of ATPase, superprecipitation, and the phosphorylation of the myosin light chain. 2) K-252a inhibited the activities of the purified myosin light chain kinase and a Ca2+-independent form of the enzyme which was constructed by cross-linking of myosin light chain kinase and calmodulin using glutaraldehyde. The degrees of inhibition by 3 x 10(-6) M K-252a were 69 and 48% of the control activities with the purified enzyme and the cross-linked complex, respectively. Chlorpromazine (3 x 10(-4) M), a calmodulin antagonist, inhibited the native enzyme, but not the cross-linked one. These results suggested that K-252a inhibited myosin light chain kinase by direct interaction with the enzyme, whereas chlorpromazine suppressed the enzyme activation by interacting with calmodulin. 3) The inhibition by K-252a of the cross-linked kinase was affected by the concentration of ATP, a phosphate donor. The concentration causing 50% inhibition was two orders magnitude lower in the presence of 100 microM ATP than in the presence of 2 mM ATP. 4) Kinetic analyses using [gama-32P]ATP indicated that the inhibitory mode of K-252a was competitive with respect to ATP (Ki = 20 nM). These results suggest that K-252a interacts at the ATP-binding domain of myosin light chain kinase. The direct action of the compound on the enzyme would explain the multivarious inhibition of myosin ATPase, of superprecipitation, and of the contractile response of smooth muscle.
Transposition of R factor genes to bacteriophage lambda. (1975)

Transpositions of segments of R factor (antibiotic resistance plasmids) to bacteriophage lambda have been selected and characterized. Cells of Escherichia coli harboring R factors that determine kanamycin resistance were infected with phage lambda, and lambdakan transducing lines were obtained. Each of the three examined is unusual when compared to lambda transducing phages containing E. coli chromosomal genes: the kan insertions (a) occur at several sites, each well removed from the integration region POP', (b) are not associated with deletion of lambda phage DNA, and (c) are separable from the lambda genome during transduction or during lytic growth. Two insertions from the same R factor contain 1.5 kilobase sequences repeated in inverted order. The properties of the lambdakan phage suggest that R factors contain systems capable of mediating genetic exchange in the absence of extensive DNA homology. It is suggested that such systems of exchange may have played important roles in R factor evolution.
Analogues of tamoxifen: the role of the basic side-chain. Applications of a whole-cell oestrogen-receptor binding assay to N-oxides and quaternary salts. (1986)

Derivatives of tamoxifen (1) and 4-hydroxy-2-methyltamoxifen (2) in which the basic side chain has been modified by N-oxidation or by quaternization have been investigated with respect to the effects on affinity for the oestrogen receptor and on cytostatic activity towards the MCF-7 cell line in vitro. In addition to the conventional cytosol assay for receptor binding affinity (RBA) a recently developed whole-cell assay was employed. N-oxidation (e.g. 2----3) produced no significant alteration in RBA value either in cytosol or in whole cells, nor in activity towards the MCF-7 line. Quaternization with methyl iodide (1----4, 2----6) or ethyl bromide (1----5, 2----7b: the cis isomer 7a also formed) did not alter receptor binding in the cytosol assay but almost abolished binding in the whole cell and cytostatic activity. The whole-cell RBA values for 2 (0.45) and 3 (0.5) were lower than those for 4-hydroxytamoxifen (2.9), suggested to be due to the lower oestrogenicity of the 2-methyl derivatives since activity against MCF-7 cells was unimpaired. The even lower values of whole-cell RBA (0.01-0.02) for the quaternary ethyl bromide derivatives 7a and 7b were ascribed to poor penetration into the cell since these compounds had minimal cytostatic activity.
Successful Cardiopulmonary Resuscitation After Cardiac Arrest as a “Sepsis-Like” Syndrome (2002)

Altogether, the high levels of circulating cytokines, the presence of endotoxin in plasma, and the dysregulated production of cytokines found in these patients recall the immunological profile found in patients with sepsis.
Structural energetics of peptide recognition: Angiotensin II/antibody binding (1993)

Abstract The ability to predict the strength of the association of peptide hormones or other ligands with their protein receptors is of fundamental importance in the fields of protein engineering and rational drug design. To form a tight complex between a flexible peptide hormone and its receptor, the large loss of configurational entropy must be overcome. Recently, the crystallographic structure of the complex between angiotensin II and the Fab fragment of a high affinity monoclonal antibody has been determined (Garcia, K. C., Ronco, P. M., Verroust, P. J., Brünger, A. T., Amzel, L. M. Three‐dimensional structure of an angiotensin II–Fab complex at 3 Å: Hormone recognition by an anti‐idiotypic antibody. Science 257:502–507, 1992). In this paper we present a study of the thermodynamics of the association by high sensitivity isothermal titration calorimetry. The results of the experiments indicate that at 30°C the binding is characterized by (1) a Δ H of −8.9 ± 0.7 kcal mol −1 , (2) a Δ C p of −240 ± 20 cal K −1 mol −1 , and (3) the release of 1.1 ± 0.1 protons per binding site in the pH range 6.0–7.3. Using these values and the previously determined binding constant in phosphate buffer, Δ G at 30°C is estimated as −11 kcal mol −1 and Δ S as 6.9 cal K −1 mol −1 . The calorimetric data indicate that binding is favored both enthalpically and entropically. These results have been complemented by structural thermodynamic calculations. The calculated and experimentally determined thermodynamic quantities are in good agreement. Entropically, the loss of configurational entropy is more than compensated by the entropy gain from solvent release associated with the hydrophobic effect. Enthalpically, binding is favored by polar interactions (hydrogen bonding). Consequently, the problem of binding flexible hormones is solved in much the same way as the folding of an unstructured polypeptide chain into a globular protein. © 1993 Wiley‐Liss, Inc.
New synthesis of the antibiotic phosphonomycin (1970)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNew synthesis of the antibiotic phosphonomycinEdward J. Glamkowski, George Gal, Robert Purick, Alan J. Davidson, and Meyer SletzingerCite this: J. Org. Chem. 1970, 35, 10, 3510–3512Publication Date (Print):October 1, 1970Publication History Published online1 May 2002Published inissue 1 October 1970https://doi.org/10.1021/jo00835a070Request reuse permissionsArticle Views607Altmetric-Citations69LEARN 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 (461 KB) Get e-Alertsclose Get e-Alerts
Regulation of Aromatase mRNA and Estradiol Biosynthesis in Rat Ovarian Granulosa and Luteal Cells by Prolactin (1990)

Regulation by PRL of aromatase (P450arom) mRNA and protein and estradiol (E) biosynthesis was examined in granulosa cells during early stages of luteinization in vitro and in vivo. PRL caused a dose-dependent (10-1000 ng/ml) decrease in P450arom mRNA and E biosynthesis (greater than 99%) in luteinized rat granulosa cells in vitro, even when the cells were cultured in the presence of insulin and hydrocortisone (hormones known to synergize with PRL to induce proteins in mammary tissue) or in the presence of forskolin (a nonhormonal stimulator of cAMP). PRL also prevented the marked increases in aromatase mRNA and E biosynthesis stimulated by FSH and forskolin in nonluteinized preovulatory granulosa cells in culture. These effects of PRL on granulosa cells in culture were specific for aromatase and were not observed for other proteins, such as cholesterol side-chain cleavage cytochrome P450 (P450scc) and alpha 2-macroglobulin. PRL also decreased P450arom mRNA and protein during the early stages of luteinization in vivo. PRL administered to rats beginning day 1 postovulation to mimic hormone release during pseudopregnancy reduced the progressive increase in P450arom mRNA occurring in corpora lutea on days 3-4 in ovulated rats not treated with PRL. CB 154, a dopamine agonist that inhibits pituitary release of PRL, caused P450arom mRNA and protein to decrease 50% if given to pregnant rats on days 8-10 of gestation, but increased P450arom mRNA and protein if given to pregnant rats on days 10-12 of gestation. These diverse effects of PRL in pregnancy suggest that placental factors may modify the response of luteal cells to PRL during gestation.(ABSTRACT TRUNCATED AT 250 WORDS)
Identification of a cholesterol-regulated 53,000-dalton cytosolic protein in UT-1 cells and cloning of its cDNA. (1982)

UT-1 cells, a clone of Chinese hamster ovary (CHO) cells, have a 100- to 1,000-fold elevation in the amount of 3-hydroxy-3-methylglutaryl CoA reductase and therefore grow in the presence of compactin, an inhibitor of reductase. In this paper, we report that UT-1 cells also have a markedly increased amount of another protein with a Mr of 53,000 and an isoelectric point of approximately equal to 6. Whereas the reductase is an enzyme of the endoplasmic reticulum, the 53,000-dalton protein (termed the "53k" protein) is in the cytosol. It is not precipitated by an antireductase antibody. Synthesis of the 53k protein, like that of the reductase, is suppressed when UT-1 cells are incubated with plasma low density lipoprotein (LDL). We prepared a library of recombinant plasmids containing double-stranded cDNAs from UT-1 cells. Using differential colony hybridization, we identified recombinant plasmids containing double-stranded cDNA inserts encoding mRNAs expressed at high levels in UT-1 cells as compared with CHO cells. One of the plasmids, designated p53k-3, contained a 0.97-kilobase double-stranded cDNA that hybridized to a 3.8-kilobase mRNA. When translated in vitro, this 3.8-kilobase mRNA directed the synthesis of a protein identical to the cellular 53k protein as determined by two-dimensional gel electrophoresis. Hybridization studies showed that the mRNA for the 53k protein was present in much larger amounts in UT-1 cells than in parental CHO cells. In both cell types, the content of this mRNA decreased markedly when the cells were incubated with LDL. Although the function of the 53k protein is not known, circumstantial evidence suggests that it may represent cytosolic 3-hydroxy-3-methylglutaryl CoA synthase, the enzyme preceeding the reductase in the cholesterol biosynthetic pathway. The current data indicate that the synthesis of at least two proteins, the reductase and the 53k protein, are induced to high levels in compactin-resistant UT-1 cells and that the synthesis of both is suppressed coordinately by LDL.
SM-20, EGL-9, and the EGLN Family of Hypoxia-inducible Factor Prolyl Hydroxylases (2003)

Key to the transduction of signals from the environment to the cell nucleus are enzymes that post-translationally modify proteins. Modifications such as protein phosphorylation have long been known to regulate protein interactions, stability, and localization, as well as enzyme activity. Recent investigations into how cells respond to varying oxygen levels have identified a new mechanism for regulating signal transduction involving the post-translational hydroxylation of proline. The enzymes that catalyze this reaction comprise a novel family of prolyl hydroxylases, which include a growth-factor-responsive and cell-death-related protein (SM-20) in mammals, and a protein (EGL-9) in C. elegans important for normal egg laying.
Quinoline antifolate thymidylate synthase inhibitors: variation of the C2- and C4-substituents (1992)

Modifications to the bicyclic ring system of the potent thymidylate synthase (TS) inhibitor N-[4-[N-[(2-amino-3,4-dihydro-4-oxo-6- quinazolinyl)methyl]-N-prop-2-ynylamino]benzoyl]-L-glutamic acid (1, CB3717) have led to the synthesis of a series of quinoline antifolates bearing a variety of substituents at the C2 and C4 positions. In general the synthetic route involved the coupling of the appropriate diethyl N-[4-(prop-2-ynylamino)benzoyl]-L-glutamate with a disubstituted 6-(bromomethyl)quinoline followed by deprotection using mild alkali. The compounds were tested as inhibitors of partially purified L1210 TS. As a measure of cytotoxicity, the compounds were tested for their inhibition of the growth of L1210 cells in culture. Good enzyme inhibition and cytotoxicity were found for compounds containing chloro, amino, or methyl substituents at the C2 position with chloro or bromo substituents at C4. The effect on enzyme inhibition of varying the N10 substituent of 2h was similar to that observed in the quinazolinone-containing antifolates, indicating that the quinoline compounds may be interacting with the enzyme in a similar way to the quinazolinones. Also, the introduction of a 2'-fluoro substituent into the benzoyl ring of several of the quinoline antifolates led to an increase in both TS inhibition and the inhibition of L1210 cell growth. These data demonstrate that the N3-H of the pyrimidine ring of the quinazolinone antifolates is not required for binding to TS if appropriate substituents are placed at the C2 and C4 positions of the bicyclic ring system.
Triple-Negative Breast Cancer (2010)

The androgen receptor (AR), a member of the steroid hormone receptor family, is expressed in more than 70% of breast cancers and has been implicated in breast cancer pathogenesis. The role of the AR is of particular interest in patients with estrogen- and progesterone receptor negative and HER2-negative cancers, which represent approximately 25% of all breast cancers. The "triple-negative" subset of tumors generally has a more aggressive clinical course and does not benefit from conventional endocrine targeted therapies. However, emerging evidence suggests that the AR may serve as a therapeutic target for a subset of triple-negative breast cancers. Herein, we review the role of the AR in breast cancer tumorigenesis and current progress and future directions in the development of AR-targeted therapies.
Esterification (1953)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTEsterificationE. Emmet ReidCite this: Ind. Eng. Chem. 1953, 45, 9, 1936–1943Publication Date (Print):September 1, 1953Publication History Published online1 May 2002Published inissue 1 September 1953https://pubs.acs.org/doi/10.1021/ie50525a030https://doi.org/10.1021/ie50525a030research-articleACS PublicationsRequest reuse permissionsArticle Views721Altmetric-Citations1LEARN 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 options Get e-Alerts
A comparative study of the iron-clearing properties of desferrithiocin analogues with desferrioxamine B in a Cebus monkey model (1993)

A comparative study of the iron-clearing properties of subcutaneously administered desferrioxamine B (DFO) with those of orally administered desferrithiocin sodium salt (1), desmethyl desferrithiocin (2), desazadesmethyl desferrithiocin sodium salt (3), desazadesmethyl desferrithiocin pivaloyloxymethyl ester (4), and desazadesmethyl-5,5-dimethyl desferrithiocin (5) in an iron-loaded Cebus monkey model and a non-iron overloaded bile duct-cannulated rat model is presented. All six drugs, which performed well in rodent studies, demonstrated increased efficiency in the Cebus monkey model. When administered to rodents at a daily dosage of 384 mumol/kg over a period of 10 days, drug 1 demonstrated severe renal toxicity. whereas drugs 3, 4, and 5 exhibited severe gastrointestinal (GI) toxicity. Under the same experimental protocol, drug 2 did not show significant toxic side effects. In addition, to further evaluate the iron-clearing properties of analogue 2, a dose-response study was performed in the primates that showed that iron excretion increased in a dose-dependent fashion.
Hyperopic refractive surgery (2001)

Although the first attempts at hyperopia correction were made more than 100 years ago, it is only in the past several years that the success of hyperopic refractive surgery has begun to approach the efficacy of myopia surgery. Corneal surgery for the correction of hyperopia includes older lamellar techniques such as automated lamellar keratoplasty and epikeratophakia, and more recently photorefractive keratectomy and laser in situ keratomileusis. The latter two procedures have shown the most success. Using large diameter laser ablations and improved keratomes, laser in situ keratomileusis has become a realistic alternative for corrections of up to 4 or 5 diopters with astigmatic corrections. Laser thermal keratoplasty using the Holmium or diode laser and contact techniques also have gained popularity and shown some potential. Collagen shrinkage procedures are easy to perform and have relatively few complications, but over correction and regression are problems. Crystalline lens surgery and phakic intraocular lenses are being investigated actively and are promising; however, safety issues persist. The surgical treatments of hyperopia present a significant challenge and reward for the ophthalmic surgeon.
Surface Plasmon Mediated Emission from Organic Light-Emitting Diodes (2002)

Surface plasmons limit the efficiency of organic light-emitting diodes (OLEDs). Up to 40 % of the radiative power may be lost to surface plasmon (SP) modes associated with the metallic cathodes of OLEDs. Calculations show the importance of material selection and device geometry in this process. Experiments reveal the presence of the SP modes and suggest ways in which this power may be recovered using periodic nanostructure.