bluuebunny/crossref_metadata_2025_split huggingface dataset:
Can JWH‐210 and JWH‐122 be detected in adipose tissue four weeks after single oral drug administration to rats?
Authors: Schaefer Nadine , Peters Benjamin , Bregel Dietmar , Maurer Hans H. , Schmidt Peter H. , Ewald Andreas H. 
Published: January 2014

ABSTRACTSynthetic cannabinoids such as alkylindole derivatives entered the illicit drug market worldwide a few years ago. Only a few data are available concerning their pharmacokinetics, in particular their distribution and persistence in adipose tissue. For the present study, rats were administered a single 20 mg/kg oral dose of JWH‐210 or JWH‐122. After one month, they were dissected and adipose tissue was taken in order to study whether JWH‐210 and JWH‐122 persisted in this body sample. After extraction, the samples were analyzed by liquid chromatographic–mass spectrometry (LC‐QTrap‐MS). Validation of the analytical method for adipose tissue is also presented. The results of the matrix effects determination ranged between 30.6 and 43.8%. The limits of detection for JWH‐210 and JWH‐122 were 0.8 and 1.0 ng/g and lower limits of quantification were 3.7 and 2.1 ng/g, respectively. Calibration curves ranged from 10 to 75 ng/g for JWH‐210 and from 5 to 50 ng/g for JWH‐122. Intra‐ and interday precision values were lower than 15% and bias values within ±15%. Applying this method, in adipose tissue specimens obtained 4 weeks after single drug administration, JWH‐210 and JWH‐122 were detected in concentrations of 116 and 9 ng/g, respectively. Copyright © 2014 John Wiley & Sons, Ltd.
Simultaneous Inhibition Assay for Human and Microbial Kinases via MALDI‐MS/MS
Authors: Smith Anne Marie E. , Brennan John D. 
Published: January 2014

AbstractSelective inhibition of one kinase over another is a critical issue in drug development. For antimicrobial development, it is particularly important to selectively inhibit bacterial kinases, which can phosphorylate antimicrobial compounds such as aminoglycosides, without affecting human kinases. Previous work from our group showed the development of a MALDI‐MS/MS assay for the detection of small molecule modulators of the bacterial aminoglycoside kinase APH3′IIIa. Herein, we demonstrate the development of an enhanced kinase MALDI‐MS/MS assay involving simultaneous assaying of two kinase reactions, one for APH3′IIIa, and the other for human protein kinase A (PKA), which leads to an output that provides direct information on selectivity and mechanism of action. Specificity of the respective enzyme substrates were verified, and the assay was validated through generation of Z′‐factors of 0.55 for APH3′IIIa with kanamycin and 0.60 for PKA with kemptide. The assay was used to simultaneously screen a kinase‐directed library of mixtures of ten compounds each against both enzymes, leading to the identification of selective inhibitors for each enzyme as well as one non‐selective inhibitor following mixture deconvolution.
Heat shock‐induced dissociation of TRF2 from telomeres does not initiate a telomere‐dependent DNA damage response
Authors: Petrova Nadezhda V. , Velichko Artem K. , Kantidze Omar L. , Razin Sergey V. 
Published: January 2014

AbstractTelomeric repeat binding factor 2 (TRF2) is a well‐studied shelterin complex subunit that plays a major role in the protection of chomosome ends and the prevention of the telomere‐associated DNA damage response. We show that heat shock induces the dissociation of TRF2 from telomeres in human primary and cancer cell cultures. TRF2 is not simply degraded in response to heat shock, but redistributed thoughout the nucleoplasm. This TRF2 depletion/redistribution does not initiate the DNA damage response at chomosome termini.
Metal‐Ion‐Regulated Miniature DNA‐Binding Proteins Based on GCN4 and Non‐native Regulation Sites
Authors: Oheix Emmanuel , Peacock Anna F. A. 
Published: January 2014

AbstractThe design of artificial peptide dimers containing polypyridine switching domains, for which metal‐ion coordination is shown to regulate DNA binding, is reported. Short peptides, based on the basic domain of the GCN4 transcription factor (GCN4bd), dimerised with either 2,2′‐bipyridine (bipy(GCN4bd)2) or 2,2′:6′,2′′‐terpyridine (terpy(GCN4bd)2) linker units, undergo a conformational rearrangement on CuII and ZnII coordination. Depending on the linker substitution pattern, this is proposed to alter the relative alignment of the two peptide moieties, and in turn regulate DNA binding. Circular dichroism and UV–visible spectroscopy reveal that CuII and ZnII coordination promotes binding to DNA containing the CRE target site, but to a differing and opposite degree for the two linkers, and that the metal‐ion affinity for terpy(GCN4bd)2 is enhanced in the presence of CRE DNA. Binding to DNA containing the shorter AP1 target site, which lacks a single nucleobase pair compared to CRE, as well as half‐CRE, which contains only half of the CRE target site, was also investigated. CuII and ZnII coordination to terpy(GCN4bd)2 promotes binding to AP1 DNA, and to a lesser extent half‐CRE DNA. Whereas, bipy(GCN4bd)2, for which interpeptide distances are largely independent of metal‐ion coordination and less suitable for binding to these shorter sites, displays allosteric ineffective behaviour in these cases. These findings for the first time demonstrate that biomolecular recognition, and specifically sequence‐selective DNA binding, can be controlled by metal‐ion coordination to designed switching units, non‐native regulation sites, in artificial biomolecules. We believe that in the future these could find a wide range of applications in biotechnology.
Tandem Pd/Au‐Catalyzed Route to α‐Sulfenylated Carbonyl Compounds from Terminal Propargylic Alcohols and Thiols
Authors: Biswas Srijit , Watile Rahul A. , Samec Joseph S. M. 
Published: January 2014

AbstractAn efficient and highly atom‐economical tandem Pd/Au‐catalyzed route to α‐sulfenylated carbonyl compounds from terminal propargylic alcohols and thiols has been developed. This one‐step procedure has a wide substrate scope with respect to substituents at the α‐position of the alcohol. Both aromatic and aliphatic thiols generated the α‐sulfenylated carbonyl products in good to excellent yields. A mechanism is proposed in which the reaction proceeds through a Pd‐catalyzed regioselective hydrothiolation at the terminal triple bond of the propargyl alcohol followed by an Au‐catalyzed 1,2‐hydride migration.
Silver‐Catalyzed Cross‐Coupling of Propargylic Alcohols with Isocyanides: An Atom‐Economical Synthesis of 2,3‐Allenamides
Authors: Liu Jianquan , Liu Zhenhua , Wu Nannan , Liao Peiqiu , Bi Xihe 
Published: January 2014

AbstractCross‐coupling reactions between propargylic alcohols and isocyanides, by means of silver catalysis, have been described. This new reaction is both atom and step efficient and is applicable to a broad scope of substrates, allowing the synthesis of a range of synthetically valuable 2,3‐allenamides in moderate to excellent yields.
Favoring Trienamine Activation through Unconjugated Dienals: Organocatalytic Enantioselective Remote Functionalization of Alkenes
Authors: Prieto Liher , Talavera Garazi , Uria Uxue , Reyes Efraim , Vicario Jose L. , Carrillo Luisa 
Published: January 2014

AbstractUnconjugated 2,5‐dienals are more reactive substrates than the corresponding fully conjugated α,β,γ,δ‐unsaturated aldehydes towards organocatalytic activation through trienamine intermediates. This difference in reactivity has been demonstrated in the Diels–Alder reaction with nitroalkenes, a reaction that proceeds with clean β,ε‐selectivity to afford the final products in high yields and stereoselectivities, the related polyconjugated 2,4‐dienals being completely unreactive.
Stable Nanosuspensions via the Deposition of Gas‐Borne Nanoparticles of Active Pharmaceutical Ingredients in Bubble Columns
Authors: Koch Dagmar , Weber Alfred P. 
Published: January 2014

AbstractDer Transport von Partikeln aus der Gasphase in eine Flüssigkeit in Blasensäulen kann zur Herstellung stabiler Nanosuspensionen aus pharmazeutischen Wirkstoffen eingesetzt werden. In der vorliegenden Arbeit wird das Verhalten gasgetragener Nanopartikel (Kohlenstoff und Phytosterol) beim Übergang aus aufsteigenden Gasblasen in die Suspensionsflüssigkeit für Wasser und zwei Stabilisatorlösungen (Polyvinylpyrrolidon K25 und Tween®80) untersucht. Neben einem Modell zur Beschreibung der Abscheideeffizienz wird auch die Langzeitstabilität der Phytosterol‐Suspensionen diskutiert.
Experimental Investigation and Kinetic Modeling of p‐Nitrophenol and Phenol by Kissiris‐Immobilized Ralstonia eutropha in a Batch Reactor
Authors: Motamedi Mahdi , Habibi Alireza , Maleki Mohammad , Vahabzadeh Farzaneh 
Published: January 2014

AbstractCo‐metabolic degradation of p‐nitrophenol (PNP) and phenol by kissiris‐immobilized Ralstonia eutropha cells was studied in a batch bioreactor operated in recycling mode (30°C, initial pH of 7.7, aeration rate of 0.5 vvm, and recycling flow rate of 25 mL min−1). Decreasing trends of specific degradation rates of phenol (qSg) and PNP (qSng) with an increase of initial PNP concentration, were mathematically modeled considering the competitive inhibition between growth and non‐growth substrates and self‐inhibition of non‐growth substrate. A non‐linear regression on the equations used in defining of qSg, and qSng, was used to estimate the relevant kinetic parameters. On the best fitted curve, the kinetic parameters were qmax Sg = 0.032 g Phenol g Cell−1 h−1, Km Sg = 442.9 mg L−1, qmax Sng = 0.0056 g Phenol g Cell−1 h−1, Km Sng = 181.2 mg L−1, and KSng = 0.489 mg L−1. These parameters were used for dynamic prediction of the substrates concentration feature during co‐metabolic degradation experiments.
Sharpening the focus on causes and timing of readmission after radical cystectomy for bladder cancer
Authors: Hu Michael , Jacobs Bruce L. , Montgomery Jeffrey S. , He Chang , Ye Jun , Zhang Yun , Brathwaite Julien , Morgan Todd M. , Hafez Khaled S. , Weizer Alon Z. , Gilbert Scott M. , Lee Cheryl T. , Lavieri Mariel S. , Helm Jonathan E. , Hollenbeck Brent K. , Skolarus Ted A. 
Published: January 2014

BACKGROUNDReadmissions after radical cystectomy are common, burdensome, and poorly understood. For these reasons, the authors conducted a population‐based study that focused on the causes of and time to readmission after radical cystectomy.METHODSUsing Surveillance, Epidemiology, and End Results‐Medicare data, at total of 1782 patients who underwent radical cystectomy from 2003 through 2009 were identified. A piecewise exponential model was used to examine reasons for readmission as well as patient and clinical factors associated with the timing of readmission.RESULTSOne in 4 patients (25.5%) were readmitted within 30 days of discharge after radical cystectomy. Compared with patients without readmission, those readmitted were similar with regard to age, sex, and race. Readmitted patients had more complications (33.8% vs 13.9%; P < .001) and were more likely to have been discharged to skilled nursing facilities from their index admission (P < .001). The average time to readmission and subsequent length of stay were 11.5 days and 6.7 days, respectively. The majority of readmissions (67.4%) occurred within 2 weeks of discharge, 66.8% had emergency department charges, and 25.9% involved intensive care unit use. Although the spectrum of reasons for readmission varied over the 4 weeks after discharge, the most common included infection (51.4%), failure to thrive (36.3%), and urinary (33.2%) and gastrointestinal (23.1%) etiologies; 95.8% of patients had ≥ 1 of these diagnosis groups present at the time of readmission.CONCLUSIONSReadmissions after radical cystectomy are common and time‐dependent. Interventions to prevent and reduce the readmission burden after cystectomy likely need to focus on the first 2 weeks after discharge, take into consideration the spectrum of reasons for readmission, and target high‐risk individuals. Cancer 2014;120:1409–1416. © 2014 American Cancer Society.
Immigration factors and prostate cancer survival among Hispanic men in California: Does neighborhood matter?
Authors: Schupp Clayton W. , Press David J. , Gomez Scarlett Lin 
Published: January 2014

BACKGROUNDHispanics are more likely than other racial/ethnic groups in the United States to be diagnosed with later stage of prostate cancer, yet they have lower prostate cancer mortality rates. The authors evaluated the impact of nativity and neighborhood‐level Hispanic ethnic enclave on prostate cancer survival among Hispanics.METHODSA total of 35,427 Hispanic men diagnosed with invasive prostate cancer from 1995 through 2008 in the California Cancer Registry were studied; vital status data were available through 2010. Block group‐level neighborhood measures were developed from US Census data. Stage‐stratified Cox proportional hazards models were used to assess the effect of nativity and ethnic enclave on prostate cancer survival.RESULTSIn models adjusted for neighborhood socioeconomic status and other individual factors, foreign‐born Hispanics were found to have a significantly lower risk of prostate cancer survival (hazards ratio [HR], 0.81; 95% confidence interval [95% CI], 0.75‐0.87). Living in an ethnic enclave appeared to modify this effect, with the survival advantage slightly more pronounced in the high ethnic enclave neighborhoods (HR, 0.78; 95% CI, 0.71‐0.86) compared with low ethnic enclave neighborhoods (HR, 0.86; 95% CI, 0.76‐0.98).CONCLUSIONSDespite lower socioeconomic status, Hispanic immigrants have better survival after prostate cancer than US‐born Hispanics and this pattern was more striking among those living in ethnic enclaves. Identifying the modifiable individual and neighborhood‐level factors that facilitate this survival advantage in Hispanic immigrants may help to inform specific interventions to improve survival among all patients. Cancer 2014;120:1401–1408. © 2014 American Cancer Society.
The role of voltage‐gated calcium channels in neurotransmitter phenotype specification: Coexpression and functional analysis in Xenopus laevis
Authors: Lewis Brittany B. , Miller Lauren E. , Herbst Wendy A. , Saha Margaret S. 
Published: January 2014

ABSTRACTCalcium activity has been implicated in many neurodevelopmental events, including the specification of neurotransmitter phenotypes. Higher levels of calcium activity lead to an increased number of inhibitory neural phenotypes, whereas lower levels of calcium activity lead to excitatory neural phenotypes. Voltage‐gated calcium channels (VGCCs) allow for rapid calcium entry and are expressed during early neural stages, making them likely regulators of activity‐dependent neurotransmitter phenotype specification. To test this hypothesis, multiplex fluorescent in situ hybridization was used to characterize the coexpression of eight VGCC α1 subunits with the excitatory and inhibitory neural markers xVGlut1 and xVIAAT in Xenopus laevis embryos. VGCC coexpression was higher with xVGlut1 than xVIAAT, especially in the hindbrain, spinal cord, and cranial nerves. Calcium activity was also analyzed on a single‐cell level, and spike frequency was correlated with the expression of VGCC α1 subunits in cell culture. Cells expressing Cav2.1 and Cav2.2 displayed increased calcium spiking compared with cells not expressing this marker. The VGCC antagonist diltiazem and agonist (−)BayK 8644 were used to manipulate calcium activity. Diltiazem exposure increased the number of glutamatergic cells and decreased the number of γ‐aminobutyric acid (GABA)ergic cells, whereas (−)BayK 8644 exposure decreased the number of glutamatergic cells without having an effect on the number of GABAergic cells. Given that the expression and functional manipulation of VGCCs are correlated with neurotransmitter phenotype in some, but not all, experiments, VGCCs likely act in combination with a variety of other signaling factors to determine neuronal phenotype specification. J. Comp. Neurol. 522:2518–2531, 2014. © 2014 Wiley Periodicals, Inc.
Distribution of neurotransmitter receptors and zinc in the pigeon (Columba livia) hippocampal formation: A basis for further comparison with the mammalian hippocampus
Authors: Herold Christina , Bingman Verner P. , Ströckens Felix , Letzner Sara , Sauvage Magdalena , Palomero‐Gallagher Nicola , Zilles Karl , Güntürkün Onur 
Published: January 2014

ABSTRACTThe avian hippocampal formation (HF) and mammalian hippocampus share a similar functional role in spatial cognition, but the underlying neuronal mechanisms allowing the functional similarity are incompletely understood. To understand better the organization of the avian HF and its transmitter receptors, we analyzed binding site densities for glutamatergic AMPA, NMDA, and kainate receptors; GABAA receptors; muscarinic M1, M2 and nicotinic (nACh) acetylcholine receptors; noradrenergic α1 and α2 receptors; serotonergic 5‐HT1A receptors; dopaminergic D1/5 receptors by using quantitative in vitro receptor autoradiography. Additionally, we performed a modified Timm staining procedure to label zinc. The regionally different receptor densities mapped well onto seven HF subdivisions previously described. Several differences in receptor expression highlighted distinct HF subdivisions. Notable examples include 1) high GABAA and α1 receptor expression, which rendered distinctive ventral subdivisions; 2) high α2 receptor expression, which rendered distinctive a dorsomedial subdivision; 3) distinct kainate, α2, and muscarinic receptor densities that rendered distinctive the two dorsolateral subdivisions; and 4) a dorsomedial region characterized by high kainate receptor density. We further observed similarities in receptor binding densities between subdivisions of the avian and mammalian HF. Despite the similarities, we propose that 300 hundred million years of independent evolution has led to a mosaic of similarities and differences in the organization of the avian HF and mammalian hippocampus and that thinking about the avian HF in terms of the strict organization of the mammalian hippocampus is likely insufficient to understand the HF of birds. J. Comp. Neurol. 522:2553–2575, 2014. © 2014 Wiley Periodicals, Inc.
A unique ion channel clustering domain on the axon initial segment of mammalian neurons
Authors: King Anna N. , Manning Colleen F. , Trimmer James S. 
Published: January 2014

ABSTRACTThe axon initial segment (AIS) plays a key role in initiation of action potentials and neuronal output. The plasma membrane of the AIS contains high densities of voltage‐gated ion channels required for these electrical events, and much recent work has focused on defining the mechanisms for generating and maintaining this unique neuronal plasma membrane domain. The Kv2.1 voltage‐gated potassium channel is abundantly present in large clusters on the soma and proximal dendrites of mammalian brain neurons. Kv2.1 is also a component of the ion channel repertoire at the AIS. Here we show that Kv2.1 clusters on the AIS of brain neurons across diverse mammalian species including humans define a noncanonical ion channel clustering domain deficient in Ankyrin‐G. The sites of Kv2.1 clustering on the AIS are sites where cisternal organelles, specialized intracellular calcium release membranes, come into close apposition with the plasma membrane, and are also sites of clustering of γ‐aminobutyric acid (GABA)ergic synapses. Using an antibody specific for a single Kv2.1 phosphorylation site, we find that the phosphorylation state differs between Kv2.1 clusters on the proximal and distal portions of the AIS. Together, these studies show that the sites of Kv2.1 clustering on the AIS represent specialized domains containing components of diverse neuronal signaling pathways that may contribute to local regulation of Kv2.1 function and AIS membrane excitability. J. Comp. Neurol. 522:2594–2608, 2014. © 2014 Wiley Periodicals, Inc.
Single‐Molecule Metal‐Induced Energy Transfer (smMIET): Resolving Nanometer Distances at the Single‐Molecule Level
Authors: Karedla Narain , Chizhik Alexey I. , Gregor Ingo , Chizhik Anna M. , Schulz Olaf , Enderlein Jörg 
Published: January 2014

AbstractWe present a new concept for measuring distance values of single molecules from a surface with nanometer accuracy using the energy transfer from the excited molecule to surface plasmons of a metal film. We measure the fluorescence lifetime of individual dye molecules deposited on a dielectric spacer as a function of a spacer thickness. By using our theoretical model, we convert the lifetime values into the axial distance of individual molecules. Similar to Förster resonance energy transfer (FRET), this allows emitters to be localized with nanometer accuracy, but in contrast to FRET the distance range at which efficient energy transfer takes place is an order of magnitude larger. Our technique can be potentially used as a tool for measuring intramolecular distances of biomolecules and complexes.
The Origin of the “Snap‐In” in the Force Curve between AFM Probe and the Water/Gas Interface of Nanobubbles
Authors: Song Yang , Zhao Binyu , Zhang Lijuan , Lü Junhong , Wang Shuo , Dong Yaming , Hu Jun 
Published: January 2014

AbstractThe long‐range attractive force or “snap‐in” is an important phenomenon usually occurring when a solid particle interacts with a water/gas interface. By using PeakForce quantitative nanomechanics the origin of snap‐in in the force curve between the atomic force microscopy (AFM) probe and the water/gas interface of nanobubbles has been investigated. The snap‐in frequently happened when the probe was preserved for a certain time or after being used for imaging solid surfaces under atmospheric conditions. In contrast, imaging in liquids rarely induced a snap‐in. After a series of control experiments, it was found that the snap‐in can be attributed to hydrophobic interactions between the water/gas interface and the AFM probe, which was either modified or contaminated with hydrophobic material. The hydrophobic contamination could be efficiently removed by a conventional plasma‐cleaning treatment, which prevents the occurring of the snap‐in. In addition, the adsorption of sodium dodecyl sulfate onto the nanobubble surface changed the water/gas interface into hydrophilic, which also eliminated the snap‐in phenomenon.
Ferrocene‐Modified Carbon Nitride for Direct Oxidation of Benzene to Phenol with Visible Light
Authors: Ye Xiangju , Cui Yanjuan , Wang Xinchen 
Published: January 2014

AbstractFerrocene moieties were heterogenized onto carbon nitride polymers by a covalent CN linkage bridging the two conjugation systems, enabling the merging of the redox function of ferrocene with carbon nitride photocatalysis to construct a heterogeneous Photo‐Fenton system for green organocatalysis at neutral conditions. The synergistic donor–acceptor interaction between the carbon nitride matrix and ferrocene group, improved exciton splitting, and coupled photocatalytic performance allowed the direct synthesis of phenol from benzene in the presence of H2O2 under visible light irradiation. This innovative modification method will offer an avenue to construct functionalized two‐dimensional polymers useful also for other green synthesis processes using solar irradiation.