gebhart/patrepeval huggingface dataset:
Synthesis and preliminary characterization of a high-affinity novel radioligand for the dopamine transporter (2000)

In our effort to develop a novel radioligand selective for the dopamine transporter, compound 1b (O-972) was designed and characterized. The compound 1b was characterized for its binding both in monkey and rat striatum tissue, which demonstrated its high selectivity for the dopamine transporter (DAT) when its binding was compared with that at the serotonin transporter (SERT). The compound 5, which is a precursor for the tritiated radiolabel ligand [3H]O-972, was synthesized and biologically characterized. The preliminary characterization of this novel radioligand revealed its strong binding affinity for the DAT. Thus, the pharmacological profile of [3H]O-972 indicated that DAT inhibitors, which include GBR 12909, mazindol, CFT, and cocaine, could potently displace this novel radioligand from monkey brain striatum tissue. On the other hand, compounds known to be not selective for and potent at the DAT were very weak to do so. Initial binding results also indicate that [3H]O-972 may interact with the DAT in a manner that is not identical to that for GBR 12909 and tropane analogs.
New oxidizing agents from the dehydration of hydrogen peroxide (1979)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNew oxidizing agents from the dehydration of hydrogen peroxideJ. Rebek, R. McCready, S. Wolf, and A. MossmanCite this: J. Org. Chem. 1979, 44, 9, 1485–1493Publication Date (Print):April 1, 1979Publication History Published online1 May 2002Published inissue 1 April 1979https://pubs.acs.org/doi/10.1021/jo01323a026https://doi.org/10.1021/jo01323a026research-articleACS PublicationsRequest reuse permissionsArticle Views536Altmetric-Citations43LEARN 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
Nonsymmetrical Bis-Azine Biaryls from Chloroazines: A Strategy Using Phosphorus Ligand-Coupling (2019)

Distinct approaches to synthesize bis-azine biaryls are in demand as these compounds have multiple applications in the chemical sciences and are challenging targets for metal-catalyzed cross-coupling reactions. Most approaches focus on developing new reagents as the formal nucleophilic coupling partner that can function in metal-catalyzed processes. We present an alternative approach using pyridine and diazine phosphines as nucleophilic partners and chloroazines where the heterobiaryl bond is formed via a tandem S<sub><i>N</i></sub>Ar-phosphorus ligand-coupling sequence. The heteroaryl phosphines are prepared from chloroazines and are bench-stable solids. A range of bis-azine biaryls can be formed from abundant chloroazines using this strategy that would be challenging using traditional approaches. A one-pot cross-electrophile coupling of two chloroazines is feasible, and we also compared the phosphorus-mediated strategy with metal-catalyzed coupling reactions to show advantages and compatibility.
Enzymatic measurement of phosphatidylserine in cultured cells (2011)

Phosphatidylserine (PS) is a quantitatively minor membrane phospholipid involved in diverse cellular functions. In this study, we developed a new fluorometric method for measuring PS using combinations of specific enzymes and Amplex Red. The calibration curve for PS measurement was linear and hyperbolic at low (0-50 µM) and high (50-1000 µM) concentrations, respectively, and the detection limit was 5 µM (50 pmol in the reaction mixture). This assay quantified PS regardless of the chain length and the number of double bonds. We applied this new method to the determination of PS content in HEK293 cells, which was validated by a recovery study and comparison with TLC-phosphorus assay. We showed that the PS content was high in sparse cells. The overexpression of PS synthase 1 elevated not only the cellular PS content but also the phosphatidylcholine (PC) and phosphatidylethanolamine (PE) contents, suggesting the conversion of PS into PE and the enhancement of PC production. This new assay for PS measurement is simple, specific, sensitive, and high throughput, and it will be useful to clarify the metabolism and biological functions of PS.
Model-based Camera Calibration Using Analysis by Synthesis Techniques (2002)

S.307-314
Craving research: future directions (2000)

Many prospective clinical studies have concluded that craving does not reliably predict relapse and that the concept is of little or no clinical utility. Contrary to earlier more simplistic clinical models of addiction, more recent models do not require that craving be present for relapse to occur. New approaches to study human craving may enhance its predictive validity and yield more knowledge of its nature, course, behavioural sequelae and regulatory function in alcohol/drug consumption. These approaches include empirical research that focuses on: (1) the elucidation of the domains of craving (i.e. subjective experience, physiological responses, behavioural sequelae and their inter-relationships); (2) the temporal dynamics of craving (i.e. its course over minutes or days, as well as its natural history over the course of a drinking career); (3) the factors that may mediate/moderate/determine the development and resolution of craving; (4) studies of the predictive validity of craving measures; and (5) the development of valid methods of measuring the different domains of craving. The conclusions are that future craving research should: (1) incorporate more sophisticated general theories of behaviour (conditioning, cognitive social learning, neurobiological, and genetic); (2) apply more sophisticated and standardized measurement methods and experimental paradigms, including studies in which alcohol is made available to human subjects; and (3) effective development of new pharmacological and behavioural therapies for relapse prevention depend on greater understanding of the nature and measurement of craving.
A convenient procedure for bromomethylation of aromatic compounds. Selective mono-, bis-, or trisbromomethylation (1993)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA convenient procedure for bromomethylation of aromatic compounds. Selective mono-, bis-, or trisbromomethylationA. W. Van der Made and R. H. Van der MadeCite this: J. Org. Chem. 1993, 58, 5, 1262–1263Publication Date (Print):February 1, 1993Publication History Published online1 May 2002Published inissue 1 February 1993https://doi.org/10.1021/jo00057a046RIGHTS & PERMISSIONSArticle Views5055Altmetric-Citations233LEARN 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 (305 KB) Get e-Alerts Get e-Alerts
Identification of circulating microRNAs as diagnostic biomarkers for use in multiple myeloma (2012)

We have developed a biomarker signature using microRNAs extracted from serum, which has potential as a diagnostic and prognostic tool for multiple myeloma.
Tip-based chemical vapor deposition with a scanning nano-heater (2013)

In this preliminary effort, a moving nano-heater directs a chemical vapor deposition reaction (nano-CVD) demonstrating a tip-based nanofabrication (TBN) method. Localized nano-CVD of copper (Cu) and copper oxide (CuO) on a silicon (Si) and silicon oxide (SiO2) substrate from gasses, namely sublimated copper acetylacetonate (Cu(acac)2), argon (Ar), and oxygen (O2), is demonstrated. This technique is applicable to other materials.
The accuracy of ultrasound evaluation of amniotic fluid volume in singleton pregnancies: The effect of operator experience and ultrasound interpretative technique (1997)

The objective of this study was to evaluate the effect of operator experience and ultrasound interpretation technique on the accuracy of ultrasound estimates of amniotic fluid volume. Ultrasound evaluation was carried out by an obstetric resident, a nurse sonographer, a maternal-fetal medicine fellow, and a maternal-fetal medicine staff member to subjectively estimate (visual interpretation without sonographic measurements) amniotic fluid volume in 63 pregnancies. Amniotic fluid volume was also evaluated using ultrasound measurements based on the largest vertical pocket technique, the amniotic fluid index, and the two-diameter pocket method. The accuracy of these ultrasound estimates was assessed by comparing the ultrasound results to actual amniotic fluid volume as determined by a dye-dilution technique. For analysis, amniotic fluid volumes were classified as oligohydramnios, normal, or hydramnios using established volumetric criteria for singleton pregnancies. Subjective estimates ranged from 65% to 70% correct and did not differ by operator experience except for the more accurate diagnosis of hydramnios by the maternal-fetal medicine staff. The three sonographic measurements were similar in overall accuracy (59–67%). The two-diameter pocket method was, however, significantly more accurate in identifying oligohydramnios. It appears that neither operator experience nor sonographic technique greatly affects the accuracy of ultrasound estimates of amniotic fluid volume. © 1997 John Wiley & Sons, Inc. J Clin Ultrasound 25:249–253, 1997
The Complete Idiot's Guide to Microsoft Windows Vista (2007)

From the Publisher:
If you one day sit down at your desk to discover Windows installed on your computer, you're going to want some guidance on how to use it. The Complete Idiot's Guide to Windows Millennium is aimed at people who, through no fault of their own, have ended up with Microsoft's latest consumer operating system. Computers are now an integral part of many people's lives, but that doesn't mean every user is an expert. This book uses a light, irreverent tone that engages your interest and has a little fun at Windows Millennium's expense. All the new Windows Millennium features are covered, including personalized menus, the latest version of Internet Explorer and Outlook Express, MSN Messenger Server, networking, digital camera and scanners and more.
Cellulose Derivatives : Synthesis, Properties and Applications (2009)

Even though cellulose is the most abundant polymer on Earth, its utilisation has some limitations regarding its efficient use in the production of bio-based materials. It is quite clear from statistics that only a relatively small fraction of cellulose is used for the production of commodity materials and chemicals. This fact was the driving force in our research into understanding, designing, synthesising and finding new alternative applications for this well-known but underused biomaterial. This thesis focuses on the developing advanced materials and products from cellulose by using novel approaches. \n\nThe aim of this study was to investigate and explore the versatility of cellulose as a starting material for the synthesis of cellulose-based materials, to introduce new synthetic methods for cellulose modification, and to widen the already existing synthetic approaches. Due to the insolubility of cellulose in organic solvents and in water, ionic liquids were applied extensively as the reaction media in the modification reactions. Cellulose derivatives were designed and fine-tuned to obtain desired properties. This was done by altering the inherent hydrogen bond network by introducing different substituents. These substituents either prevented spontaneous formation of hydrogen bonding completely or created new interactions between the cellulose chains. This enabled spontaneous self-assembly leading to supramolecular structures. It was also demonstrated that the material properties of cellulose can be modified even those molecules with a low degree of substitution when highly hydrophobic films and aerogels were prepared from fatty acid derivatives of nanocellulose. Development towards advanced cellulose-based materials was demostrated by synthesising chlorophyllcellulose derivatives that showed potential in photocurrent generation systems. In addition, liquid crystalline cellulose derivatives prepared in this study, showed to function as UV-absorbers in paper.
Laser fabrication of Au nanorod aggregates microstructures assisted by two-photon polymerization (2011)

We demonstrate fabrication of Au nanorod aggregates microstructures by means of a femtosecond near-infrared laser. The laser light was tightly focused into colloidal Au nanorods dispersed in photopolymerizable metyl-methacrylate (MMA) compound to induce two-photon polymerization (TPP). TPP of MMA glued the nanorods together to form solid microstrucures of aggregates. The laser light excited a local surface plasmon, resulting in confinement of TPP in the vicinity of nanorods. Concurrenly occurring optical accumulation of nanorods created a unique mechanism for the formation of nanorod aggregates into desired microstructures. This technique would be a clue for a novel micro/nanofabrication method for plasmonic materials and devices.
PKM2 and HIF-1α regulation in prostate cancer cell lines (2018)

Prostate cancer (PCA) is one of the most common cancer types in men, with cancer progression being linked to hypoxia and the induction of hypoxia-inducible factor (HIF).We investigated the expression of pyruvate kinase M2 (PKM2), its regulation by HIF isoforms 1α and 2α, and its role in HIF stabilization. We additionally examined cell survival in the prostate cancer cell lines PC3 and LNCaP under severe hypoxic (0.1% O2) and normoxic (20% O2) conditions. qRT-PCR showed higher up-regulation of PKM2 mRNA expression in LNCaP cells than in PC3 cells, while western blotting showed that PKM2 protein levels were up-regulated only in LNCaP cells. Inhibition of HIF-1α and HIF-2α by small interfering RNA (si-RNA) demonstrated HIF-1α dependent up-regulation of PKM2 at the mRNA and protein levels in LNCaP cells. PKM2 inhibition by si-RNA significantly decreased hypoxia-response element (HRE) activation in a gene reporter assay and down-regulated HIF-1α target vascular endothelial growth factor (VEGF) mRNA expression in PC3 cells, whereas HIF-1α protein levels were not significantly reduced. Additionally, PKM2 inhibition significantly reduced clonogenic survival in both cell lines in a colony formation assay. Prolyl hydroxylase 3 (PHD3) mRNA expression was up-regulated in both cell lines. It has been shown that PKM2 expression is regulated by HIF-1α and that PKM2 favors HIF-1α transactivation under mild (1% O2) but not severe (0.1% O2) hypoxic conditions, and some of our findings are consistent with these previous results. However, this mechanism was not fully observed in our studied cell lines, as PKM2 regulation and HIF-1α stabilization at the transactivation level occurred under severe hypoxic conditions. This discrepancy suggests that tumor tissue origin and cell type influence this model. Our findings expand the current knowledge of the mechanisms of PCA regulation, and would be important in developing novel therapeutic strategies.
Epidemiology of virus-induced asthma exacerbations: with special reference to the role of human rhinovirus (2014)

Viral respiratory infections may be associated with the virus-induced asthma in adults as well as children. Particularly, human rhinovirus is strongly suggested a major candidate for the associations of the virus-induced asthma. Thus, in this review, we reviewed and focused on the epidemiology, pathophysiology, and treatment of virus-induced asthma with special reference on human rhinovirus. Furthermore, we added our preliminary data regarding the clinical and virological findings in the present review.
Fiber-optic surface plasmon resonance for vapor phase analyses (2005)

Fiber-optic sensors based on surface plasmon resonance (SPR) for direct refractive index (RI) measurements of samples with the RI between 1.00 and 1.30 are described. Most applications of SPR sensors are designed to function near the refractive index of water (1.3330 RI). The RI changes of aqueous solution (RI, ca. 1.34) can easily be monitored by silica-fiber (RI, 1.4601 at 550 nm) based SPR sensor. With regard to gas species detection, the fiber-optic SPR sensor must be modified for sensitivity to changes in refractive index near 1.0008 (i.e., RI of air). However, the silica waveguide has a prohibitively high RI for unmodified monitoring of the RI changes of gas. The silica-fiber based SPR probe design presented here is based upon the modification of the probe geometry to the ability to tune the SPR coupling wavelength/angle pair. In this study, the tapered silica-based fiber SPR sensors are shown to directly determine the RI changes of gas species and the density change of dry air.
<scp>TRPV</scp>3: a ‘more than skinny’ channel (2013)

The skin is our largest organ serving different tasks from barrier formation through somatosensing to hair development. Recently, members of the large trp (Transient Receptor Potential, TRP) gene family encoding proteins that form cation selective ion channel have been identified to play a crucial role in skin functions. Within the 28 different mammalian TRP channels, TRPV3 might be the most important member in the skin. This review gives an overview on functional properties of TRPV3 in skin physiology and in certain skin diseases.
Identification, Detection, and Spatial Resolution of <i>Clostridium</i> Populations Responsible for Cellulose Degradation in a Methanogenic Landfill Leachate Bioreactor (2004)

An anaerobic landfill leachate bioreactor was operated with crystalline cellulose and sterile landfill leachate until a steady state was reached. Cellulose hydrolysis, acidogenesis, and methanogenesis were measured. Microorganisms attached to the cellulose surfaces were hypothesized to be the cellulose hydrolyzers. 16S rRNA gene clone libraries were prepared from this attached fraction and also from the mixed fraction (biomass associated with cellulose particles and in the planktonic phase). Both clone libraries were dominated by Firmicutes phylum sequences (100% of the attached library and 90% of the mixed library), and the majority fell into one of five lineages of the clostridia. Clone group 1 (most closely related to Clostridium stercorarium), clone group 2 (most closely related to Clostridium thermocellum), and clone group 5 (most closely related to Bacteroides cellulosolvens) comprised sequences in Clostridium group III. Clone group 3 sequences were in Clostridium group XIVa (most closely related to Clostridium sp. strain XB90). Clone group 4 sequences were affiliated with a deeply branching clostridial lineage peripherally associated with Clostridium group VI. This monophyletic group comprises a new Clostridium cluster, designated cluster VIa. Specific fluorescence in situ hybridization (FISH) probes for the five groups were designed and synthesized, and it was demonstrated in FISH experiments that bacteria targeted by the probes for clone groups 1, 2, 4, and 5 were very abundant on the surfaces of the cellulose particles and likely the key cellulolytic microorganisms in the landfill bioreactor. The FISH probe for clone group 3 targeted cells in the planktonic phase, and these organisms were hypothesized to be glucose fermenters.
Histidine-Rich Cationic Amphipathic Peptides for Plasmid DNA and siRNA Delivery (2012)

Amphipathic, pH-responsive, membrane-active peptides such as LAH4 and derivatives thereof have the ability to effectively deliver genes and small interfering RNA (siRNA) into mammalian cells. Their ability to bind and protect nucleic acids and then disrupt membranes when activated at low pH enables them to harness the endocytic machinery to deliver cargo efficiently and with low associated toxicity. This chapter describes protocols for the chemical synthesis of transfection peptides of the LAH4 family, complex formation with nucleic acids, and their use for the in vitro delivery of either plasmid DNA or siRNA into mammalian cell lines.
Evaluation of the Toxicity of 5-Aryl-2-Aminoimidazole-Based Biofilm Inhibitors against Eukaryotic Cell Lines, Bone Cells and the Nematode Caenorhabditis elegans (2014)

Previously, we have synthesized several series of compounds based on the 5-aryl-2-aminoimidazole scaffold, which showed a preventive activity against microbial biofilms. We here studied the cytotoxicity of the most active compounds of each series. First, the cytostatic activity was investigated against a number of tumor cell lines (L1210, CEM and HeLa). A subset of monosubstituted 5-aryl-2-aminoimidazoles showed a moderate safety window, with therapeutic indices (TIs) ranging between 3 and 20. Whereas introduction of a (cyclo-)alkyl chain at the N1-position strongly reduced the TI, introduction of a (cyclo-)alkyl chain or a triazole moiety at the 2N-position increased the TI up to 370. Since a promising application of preventive anti-biofilm agents is their use in anti-biofilm coatings for orthopedic implants, their effects on cell viability and functional behavior of human osteoblasts and bone marrow derived mesenchymal stem cells were tested. The 2N-substituted 5-aryl-2-aminoimidazoles consistently showed the lowest toxicity and allowed survival of the bone cells for up to 4 weeks. Moreover they did not negatively affect the osteogenic differentiation potential of the bone cells. Finally, we examined the effect of the compounds on the survival of Caenorhabditis elegans, which confirmed the higher safety window of 2N-substituted 5-aryl-2-aminoimidazoles.