gebhart/patrepeval huggingface dataset:
THE RELATIONSHIP OF STRUCTURE TO ACTIVITY OF SULFANILAMIDE TYPE COMPOUNDS (1944)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTHE RELATIONSHIP OF STRUCTURE TO ACTIVITY OF SULFANILAMIDE TYPE COMPOUNDSPaul H. Bell, J. Foster Bone, and Richard O. Roblin Jr.Cite this: J. Am. Chem. Soc. 1944, 66, 5, 847Publication Date (Print):May 1, 1944Publication History Published online1 May 2002Published inissue 1 May 1944https://pubs.acs.org/doi/10.1021/ja01233a513https://doi.org/10.1021/ja01233a513research-articleACS PublicationsRequest reuse permissionsArticle Views120Altmetric-Citations6LEARN 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
Thyroid Hormone Promotes Postnatal Rat Pancreatic β-Cell Development and Glucose-Responsive Insulin Secretion Through MAFA (2013)

Neonatal β cells do not secrete glucose-responsive insulin and are considered immature. We previously showed the transcription factor MAFA is key for the functional maturation of β cells, but the physiological regulators of this process are unknown. Here we show that postnatal rat β cells express thyroid hormone (TH) receptor isoforms and deiodinases in an age-dependent pattern as glucose responsiveness develops. In vivo neonatal triiodothyronine supplementation and TH inhibition, respectively, accelerated and delayed metabolic development. In vitro exposure of immature islets to triiodothyronine enhanced the expression of Mafa, the secretion of glucose-responsive insulin, and the proportion of responsive cells, all of which are effects that were abolished in the presence of dominant-negative Mafa. Using chromatin immunoprecipitation and electrophoretic mobility shift assay, we show that TH has a direct receptor-ligand interaction with the Mafa promoter and, using a luciferase reporter, that this interaction was functional. Thus, TH can be considered a physiological regulator of functional maturation of β cells via its induction of Mafa.
Rapid and Enantioselective Synthetic Approaches to Germanicol and Other Pentacyclic Triterpenes (2008)

Two exceedingly short synthetic routes to the key intermediate 2 for the synthesis of the pentacyclic triterpene germanicol 1 have been developed. In the first, the ( S)-epoxide of farnesyl bromide is transformed in just three steps to the tetracyclic intermediate 7, which is converted to chiral 2 by treatment with polyphosphoric acid. The second synthetic route to 2 involves the coupling of the ( S)-epoxide 8 with vinyl iodide 9 to give 10 and two-stage acid-catalyzed cyclization of 10 to form 2. During the course of this work we have also discovered a very unusual intramolecular 1,5-proton shift from a carbocation to a C-C double bond. The details of the process have been confirmed by (2)H-labeling experiments.
Crystal Structure of the Ectodomain of Human Transferrin Receptor (1999)

The transferrin receptor (TfR) undergoes multiple rounds of clathrin-mediated endocytosis and reemergence at the cell surface, importing iron-loaded transferrin (Tf) and recycling apotransferrin after discharge of iron in the endosome. The crystal structure of the dimeric ectodomain of the human TfR, determined here to 3.2 angstroms resolution, reveals a three-domain subunit. One domain closely resembles carboxy- and aminopeptidases, and features of membrane glutamate carboxypeptidase can be deduced from the TfR structure. A model is proposed for Tf binding to the receptor.
Dominant‐negative inhibition of breast cancer resistance protein as drug efflux pump through the inhibition of S‐S dependent homodimerization (2001)

Breast cancer resistance protein (BCRP) is a half-molecule ABC transporter highly expressed in mitoxantrone-resistant cells. In our study we established PA317 transfectants expressing Myc-tagged BCRP (MycBCRP) or HA-tagged BCRP (HABCRP). The exogenous BCRP protein migrated as a 70-kDa protein in SDS-PAGE under reducing condition, but migrated as a 140-kDa complex in the absence of reducing agents. The 140-kDa BCRP complex was heat-stable but dissociated into 70-kDa BCRP with the addition of 2-mercaptoethanol. The 140-kDa BCRP complex was immunoprecipitated with anti-Myc antibody from the lysates of PA317 cells double-transfected with MycBCRP and HABCRP. The 140-kDa complex reacted with anti-HA and anti-BCRP antibodies and after the addition of reducing agents, a 70-kDa protein reacting with anti-Myc, anti-HA and anti-BCRP antibodies was detected. These results clearly indicate that BCRP forms a homodimer bridged by disulfide bonds. To assess the possible dominant-negative inhibition of BCRP drug efflux pump, various mutant BCRP cDNAs were isolated by PCR mutagenesis. First, mutant BCRP cDNAs were introduced to parental PA317 cells and tested for their function as drug-resistance genes. Next, inactive BCRP cDNA clones were introduced to MycBCRP-transfected cells and tested for the ability to lower drug resistance. Among the 8 inactive mutant cDNA clones tested, HABCRP cDNA clone 15 with an amino acid change from Leu to Pro at residue 554 in the fifth transmembrane domain of BCRP partially reversed the drug resistance of MycBCRP-transfected cells. These results suggest that homodimer formation is essential for BCRP drug resistance, implicating this dominant-negative inhibition as a new strategy to circumvent drug resistance.
A low-power, high-speed 0.25µm GaAs D-FF (1997)

A design for low-power, high-speed static GaAs HJFET flip-flops (D-FFs) is discussed in detail. Four different types of delay latches based on NOR gates were designed. These latches were used to design 16 different types of D-FFs. A D-FF named 1POP was chosen for fabrication using 0.25 µm GaAs HJFET technology. Experimental results showed that both the maximum operating clock frequencies (f mc ) and power dissipations at f mc were proportional to supply voltage (V D ). The 1P0P D-FF operated at f mc of 5.17 GHz on V D =0.6 V consuming only 2.03 mW that is the world's lowest power dissipation. Clear, wide eye openings were obtained in a f mc range up to 7.15 GHz. Operating speeds were confirmed at an error rate of less than 10-9with a (29-1) pseudo-random signal.
Wharton's Jelly Mesenchymal Stem Cells as Off-The-Shelf Cellular Therapeutics: A Closer Look into their Regenerative and Immunomodulatory Properties (2011)

Mesenchymal stem/stromal cells (MSCs) are isolated from most post-natal tissues and are broadly reported to have similar immuno-phenotype, mesenchymal lineage-differentiation potential and bio-distribution in peri-vascular niches. Thus, several stromal substitutes of bone marrow mesenchymal stem cells (BMMSCs) are being considered for regenerative therapy. Wharton's jelly mesenchymal stem cells (WJMSCs) seem to be the most promising alternative because of easy donor accessibility, high proliferative capacity and greater sample to sample identity.
Synthesis of 2-C-Methyl-D-erythritol and 2-C-Methyl-L-threitol; Determination of the Absolute Configuration of 2-C-Methyl-1,2,3,4-butanetetrol Isolated fromPhlox sublata L (2000)

2-C-Methyl-D-erythritol (A) and 2-C-methyl-L-threitol (B) were respectively synthesized from D-glucose and D-galactose. The 2-C-methyl-1,2,3,4-butanetetrol compound (C) recently isolated from Phlox sublata L was confirmed to be A by comparing the CD and 1H-NMR spectra of its tri-O-benzoate with those of A and B.
Recurrent Bilateral Pleural Effusions Secondary to Superior Vena Cava Obstruction as a Complication of Central Venous Catheterization (1983)

Five babies (birth weight 730 to 1,120 g) who developed bilateral pleural effusions as a complication of the use of central venous catheters are described. The effusions occurred seven to 19 days after initial placement or change of a central venous catheter. All required repeated thoracenteses to remove fluid accumulation of up to 200 mL/kg/d. The fluid was a clear transudate, but it became chylous when feedings were given. Venograms and autopsies demonstrated obstruction of the superior vena cava with drainage occurring through collaterals to the azygous vein and inferior vena cava. Silastic gas-sterilized catheters implanted in animals for four and 24 hours showed fibrin deposition when scanned by electron microscopy. No deposition occurred on autoclaved catheters after four hours and there was minimal deposition after 24 hours. It may be concluded that the pleural effusions resulted from obstruction of thoracic lymph flow into the venous system. Vena caval thrombosis may have been enhanced by 2-chloroethanol or ethylene oxide residues from gas sterilization of Silastic catheters.
Synthesis of 1‐amino‐4‐chloroisoquinoline. A new approach to 1‐aminoisoquinoline (1978)

Abstract The as yet unknown 1‐amino‐4‐chloroisoquinoline was synthesised from 1,4‐dichloroisoquinoline through the 1‐phenoxy‐4‐chloro derivative. This procedure was also suitable for obtaining 1‐aminoisoquinoline from 1‐chloroisoquinoline in good yields.
Preparation of Cell Walls and Protoplasm of Neisseria with the Ribi Cell Fractionator (1969)

The varied pressures required for disruption of Neisseria gonorrhoeae and other species of Neisseria when the Sorvall-Ribi refrigerated cell fractionator is used in the preparation of cell walls and cellular protoplasm are reported. Optimal disruption pressure for the gonococcus was considerably less than that required for other members of the genus Neisseria. Pressures varied from 8,000 psi for N. gonorrhoeae F62, colony type 4, to 22,000 psi for the nonpathogenic Neisseria-N. sicca, N. flava, and N. catarrhalis. Representative electron photomicrographs are shown.
Photocatalytic Layer-by-Layer Coatings for Degradation of Acutely Toxic Agents (2008)

Highly reactive layer-by-layer (LbL) films have been developed as protective coatings intended for application on fibers worn by military personnel. In this work, the anionic species are titanium dioxide nanoparticles ranging from 5 to 10 nm in size, which are prepared in a stable colloidal solution specifically designed for this application, while the cationic species can be one of several traditional synthetic polycations, including weak and strong polyelectrolytes. The resulting coatings are mechanically stable and offer selective protection when the wearer is exposed to UV radiation (e.g.,sunlight); whereas the inherent water transmissive nature of the multilayers allows for much greater water vapor transport rates as compared to an inert rubber barrier material. Permeation tests of coated materials were conducted in a specially engineered cell by exposing the materials to a CWA simulant. In the extreme case, when a coated material is subjected to a saturated vapor of the CWA simulant, UV exposure resulted in a 95% decrease in toxic agent permeation. Furthermore, the coating can be deposited via a spray-LbL technique developed specifically for rapid, uniform deposition over large areas of textile materials at ambient temperatures and moderate pressures.
Antifungal Properties of Polymyxin B and Its Potentiation of Tetracycline as an Antifungal Agent (1972)

High concentrations of polymyxin B inhibited the growth of Candida albicans and Saccharomyces cerevisiae. When these yeasts were incubated with concentrations of polymyxin B too low to affect growth, and were then exposed to tetracycline, protein synthesis was inhibited and at least 99% of the organisms were killed. Neither inhibition of protein synthesis nor cell death occurred in cultures treated with high concentrations of tetracycline alone. We conclude that polymyxin B at high concentrations affects the cell membrane of yeasts, which results in inhibition of growth. At low concentrations, it increases the permeability of the yeast cell membrane to tetracycline, which then inhibits protein synthesis and leads to cell death.
Organization of the crypt-villus axis and evolution of its stem cell hierarchy during intestinal development (1995)

The small intestinal crypt of the adult mouse represents a model system for studying cell renewal. One or more functionally equivalent stem cells located within the crypt fuel a continuous regeneration of the gut's four principal epithelial cell lineages. These lineages differentiate during a geographically well-organized migration along the crypt-villus axis. This axis does not complete its morphogenetic program until the third postnatal week. We examined the organization of the crypt-villus axis and its stem cell hierarchy in postnatal day 1 (P1) to P28 transgenic mice. These mice contained transcriptional regulatory elements from the liver fatty acid binding protein gene linked to a human growth hormone (hGH) reporter. Adult male and female animals exhibit a striped pattern of hGH accumulation in their villus-associated epithelial cells: vertical coherent bands of wholly hGH-positive epithelial cells derived from a monoclonal crypt and vertical coherent stripes of wholly hGH-negative epithelial cells derived from an adjacent crypt extend to the apical extrusion zone of their common villus. Villus striping develops in a proximal-to-distal wave that extends from the duodenum to the jejunum by P7 and to the ileum by P14. Striping occurs as a result of a loss in the ability to support transgene expression. The decision appears to affect all cells within a stripe, irrespective of their position along the basilar-to-apical axis of a villus, suggesting that it is programmed by the nascent crypt's multipotent stem cell(s). Suppression of transgene expression traverses the crypt-villus axis more rapidly than the rate of epithelial cell migration. The boundary between stripes is very sharp and does not contain cells with transitional levels of the hGH reporter, indicating that the epithelial components of the crypt-villus axis have a higher degree of organization at this stage of development than appreciated previously.
The Role of Glutathione and Glutathione Transferases in Chemical Cardnogenesi (1990)

(1990). The Role of Glutathione and Glutathione Transferases in Chemical Cardnogenesi. Critical Reviews in Biochemistry and Molecular Biology: Vol. 25, No. 1, pp. 47-70.
Dramatically Different Phenotypes in Mouse Models of Human Tay-Sachs and Sandhoff Diseases (1996)

We have generated mouse models of human Tay-Sachs and Sandhoff diseases by targeted disruption of the Hexa (alpha subunit) or Hexb (beta subunit) genes, respectively, encoding lysosomal beta-hexosaminidase A (structure, alpha) and B (structure, beta beta). Both mutant mice accumulate GM2 ganglioside in brain, much more so in Hexb -/- mice, and the latter also accumulate glycolipid GA2. Hexa -/- mice suffer no obvious behavioral or neurological deficit, while Hexb -/- mice develop a fatal neurodegenerative disease, with spasticity, muscle weakness, rigidity, tremor and ataxia. The Hexb -/- but not the Hexa -/- mice have massive depletion of spinal cord axons as an apparent consequence of neuronal storage of GM2. We propose that Hexa -/- mice escape disease through partial catabolism of accumulated GM2 via GA2 (asialo-GM2) through the combined action of sialidase and beta-hexosaminidase B.
Identification and characterization of Src SH3 ligands from phage-displayed random peptide libraries. (1994)

We have used the Src homology 3 (SH3) domain to screen two phage-displayed random peptide libraries, each containing 2 x 10(8) unique members, and have identified a series of high affinity peptide ligands. The peptides possess similar proline-rich regions, which yield a consensus Src SH3-binding motif of RPLPPLP. We have confirmed this motif by screening a phage-displayed peptide library biased for SH3 ligands and identifying the same consensus sequence. Binding studies using synthetic peptides suggest that the RPLPPLP motif is important for SH3 binding and confers specificity for the Src SH3 domain, and that residues which flank the motif may also contribute to binding. Peptides that contain the RPLPPLP motif compete Src, but not Abl or phospholipase C gamma, SH3 interactions with SH3-binding proteins from cell lysates (IC50 = 1-5 microM). Furthermore, RPLPPLP-related peptides are able to accelerate progesterone-induced maturation of Xenopus laevis oocytes. A similar acceleration has been observed in oocytes treated with activated, but not normal, Xenopus Src, suggesting the possibility that the peptides are able to antagonize the negative regulation of Src activity by Src SH3 in vivo.
A novel tyrosine kinase inhibitor AMN107 (nilotinib) normalizes striatal motor behaviors in a mouse model of Parkinson’s disease (2014)

Abnormal motor behaviors in Parkinson's disease (PD) result from striatal dysfunction due to an imbalance between dopamine and glutamate transmissions that are integrated by dopamine- and cAMP-regulated phosphoprotein of 32 kDa (DARPP-32). c-Abelson tyrosine kinase (c-Abl) phosphorylates cyclin-dependent kinase 5 (Cdk5) at Tyr15 to increase the activity of Cdk5, which reduces the efficacy of dopaminergic signaling by phosphorylating DARPP-32 at Thr75 in the striatum. Here, we report that in the mouse striatum, a novel c-Abl inhibitor, nilotinib (AMN107), inhibits phosphorylation of both Cdk5 at Tyr15 and DARPP-32 at Thr75, which is negatively regulated by dopamine receptor activation through a D2 receptor-mediated mechanism. Like a D2-agonist, nilotinib synergizes with a D1-agonist for inducing striatal c-Fos expression. Moreover, systemic administration of nilotinib normalizes striatal motor behaviors in a mouse model of PD induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine. These findings suggest that nilotinib could possibly serve as a new and alternative agent for treating PD motor symptoms.
Purification and Characterization of meta-Cresol Purple for Spectrophotometric Seawater pH Measurements (2011)

Spectrophotometric procedures allow rapid and precise measurements of the pH of natural waters. However, impurities in the acid-base indicators used in these analyses can significantly affect measurement accuracy. This work describes HPLC procedures for purifying one such indicator, meta-cresol purple (mCP), and reports mCP physical-chemical characteristics (thermodynamic equilibrium constants and visible-light absorbances) over a range of temperature (T) and salinity (S). Using pure mCP, seawater pH on the total hydrogen ion concentration scale (pHT) can be expressed in terms of measured mCP absorbance ratios (R = λ2A/(λ1)A) as follows: [formula in text] where -log(K(2)Te2) = a + (b/T) + c ln T – dT; a = -246.64209 + 0.315971S + 2.8855 × 10(-4)S2; b = 7229.23864 – 7.098137S – 0.057034S2; c = 44.493382 – 0.052711S; d = 0.0781344; and mCP molar absorbance ratios (ei) are expressed as e1 = -0.007762 + 4.5174 × 10(-5)T and e3/e2 = -0.020813 + 2.60262 × 10(-4)T + 1.0436 × 10(-4) (S – 35). The mCP absorbances, λ1A and λ2A, used to calculate R are measured at wavelengths (λ) of 434 and 578 nm. This characterization is appropriate for 278.15 ≤ T ≤ 308.15 and 20 ≤ S ≤ 40.
Ex Vivo Gene Therapy Approaches for the Treatment of Globoid Cell Leukodystrophy (2009)

Globoid cell leukodystrophy (GLD) is a rare lysosomal storage disorder (LSD) due to the deficiency of the lysosomal enzyme Galactocerebrosidase (GALC). The enzymatic deficiency results in intracellular storage of undegraded metabolites in the nervous system, leading to progressive dysmyelination. We are testing the feasibility and efficacy of a gene therapy strategy based on hematopoietic stem/progenitor cells (HSPC) and lentiviral vectors (LV) in the murine model of GLD. Differently from what observed with other lysosomal enzymes, GALC gene transfer and expression in HSPC causes apoptosis and functional impairment of the transduced cells due to an inbalance of the intracellular content in bioactive sphingolipids consequent to de novo enzyme expression. Differentiated cells of the myeloid and lymphoid lineages are not affected by GALC expression, suggesting a unique sensitivity of HSPC to enzyme toxicity. <br><br>To overcome this issue, we explored strategies aimed at de-targeting vector expression from HSPC, while permitting GALC over-expression in differentiated cells. The first approach aims at a transcriptional regulation of GALC expression by the microglia/macrophage specific promoter CD11b. The second strategy exploits endogenous microRNAs for post-transcriptional regulation of GALC expression. The use of LV containing the target sequence of miRNA126, expressed only in HSPC, allows expressing GALC only in the differentiated progeny of transduced HSPC. Although these two approaches proved to be very promising in protecting HSPC from enzyme toxicity both <i>in vitro</i> and <i>in vivo</i> in heterozygous GLD mice, gene-corrected HSPC failed to repopulate lethally irradiated homozygous GLD mice. This poor result might be explained by the existence of a niche defect in homozygous GLD mice, which might hamper the engraftment of HSPC.
Electrochemical detection of histamine and 5-hydroxytryptamine at isolated mast cells (1995)

The electrochemical oxidation of histamine has been investigated as an analytical tool. In a physiological buffer, histamine is oxidized at carbon fiber microelectrodes at potentials close to the background in a chemically irreversible process. Cylindrical carbon fiber electrodes were used as amperometric detectors for histamine separated with a reversed-phase capillary column, and detection limits of 240 amol were achieved. Electrodes with beveled tips were used as real-time sensors by monitoring with repetitive cyclic voltammograms at a scan rate of 800 V/s with a 16.7-ms repetition rate, and detection limits of 1.4 microM were achieved. Both techniques were used to probe histamine and 5-hydroxytryptamine (5-HT) stored in rat peritoneal mast cells. The content in single cells was measured by capillary HPLC, and both substances were found in single cells. Although the analysis revealed a large cell-to-cell variation in the amount of histamine and 5-HT, the average amount was 150 and 4 fmol of histamine and 5-HT, respectively. Release of histamine and 5-HT was measured with the electrode placed 1 microm from the cell surface. Release was observed as a series of sharp concentration spikes, consistent with corelease of the two substances from individual vesicles following exocytosis.
Complementary sequence correlations with applications to reflectrometry studies (1996)

The principles of complementary correlation time domain reflectometry are presented. A demonstration experiment is described which uses a digital signal processing system for generation of complementary sequences, time averaging and performing cross-correlations. Results from simulation of an optical fiber reflectometer of this kind are given.