bluuebunny/crossref_metadata_2025_split huggingface dataset:
Design, Synthesis, and Biological Evaluation of Novel Fluorinated Ethanolamines
Authors: Fustero Santos , Cuñat Ana C. , Flores Sonia , Báez Claribel , Oliver Judit , Cynamon Michael , Gütschow Michael , Mertens Matthias D. , Delgado Oscar , Tresadern Gary , Trabanco Andrés A. 
Published: November 2011

AbstractThe preparation of novel fluorinated allylamines and their use as key fragments for the stereoselective synthesis of hydroxyethyl secondary amine (HEA)‐type peptidomimetics is described. Our strategy employs chiral sulfinyl imines as synthesis intermediates, by treatment of hemiaminal precursors with two equivalents of vinylmagnesium bromide. The subsequent oxidation of the allylic amines to the corresponding epoxides was achieved by treatment with methyl(trifluoromethyl)dioxirane. Finally, epoxide ring opening with a range of nitrogen nucleophiles provided a library of HEA‐derived peptidomimetics with a phenyldifluoromethylene moiety. The biological evaluation of these derivatives revealed compounds with remarkable BACE1 inhibitory activity. Docking studies revealed the influence of the fluorine atoms in the binding mode of the synthesized ligands. Furthermore, the biological evaluation of our final products and synthesis intermediates led to the discovery of compounds with antimicrobial activity against Mycobacterium and Nocardia species.
Fiber‐reinforced calcium phosphate cement formulations for cranioplasty applications: A 52‐week duration preclinical rabbit calvaria study
Authors: Kim Jinku , McBride Sean , Fulmer Mark , Harten Robert , Garza Zach , Dean David D. , Sylvia Victor L. , Doll Bruce , Wolfgang Tahlia L , Gruskin Elliott , Hollinger Jeffrey O. 
Published: November 2011

AbstractThe in vivo tissue response to a newly developed fiber‐reinforced calcium phosphate cement (CPC) formulation was assessed using a well‐established rabbit calvarial defect model. Bilateral subcritical sized (8‐mm diameter) defects were surgically created in the parietal bones of each rabbit (a total of 48 rabbits), and randomized to be filled with either the new fiber‐reinforced formulation, a conventional CPC (positive control), or left unfilled (negative control). The implant sites were subsequently retrieved after 12, 24, and 52 weeks postsurgery. Each specimen, including the parietal bone craniotomy and underlying brain, were recovered at necropsy and the tissue responses were assessed by histology. The resulting histological slides indicated that there was no evidence of severe inflammatory responses or osteolysis. The data showed new dural and pericranial bone formation along the implants, as well as excellent bone‐to‐implant interfaces in all of the CPC‐filled defects. These results suggest that the biologic response to the new fiber‐reinforced CPC formulations and conventional nonreinforced CPC are very similar, and both demonstrate excellent biocompatibility as well as an overall osteophylic response. © 2011 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2012.
Contact fatigue response of porcelain‐veneered alumina model systems
Authors: Stappert Christian F. J. , Baldassarri Marta , Zhang Yu , Stappert Dina , Thompson Van P. 
Published: November 2011

AbstractFatigue damage modes and reliability of hand‐veneered (HV) and over‐pressed (OP) aluminum‐oxide layer structures were compared. Influence of luting cement thickness on mechanical performance was investigated. Sixty‐four aluminum‐oxide plates (10 × 10 × 0.5 mm) were veneered with hand built‐up or pressed porcelain (0.7 mm) and adhesively luted (50‐ or 150‐μm cement thickness) to water‐aged composite resin blocks (12 × 12 × 4 mm). Single‐load‐to‐failure and fatigue tests were performed with a spherical tungsten carbide indenter (d = 6.25 mm) applied in the center of the veneer layer. Specimens were inspected with polarized‐reflected‐light and scanning electron microscopy. Use‐level probability Weibull curves were plotted with two‐sided 90% confidence bounds, and reliability at 75,000 cycles and 250 N load was calculated. For all specimens but two OP with 50‐μm cement thickness, failure was characterized by flexural radial cracks initiating at the bottom surface of the alumina core and propagating into the veneering porcelain before cone cracks could extend to the porcelain/alumina interface. HV specimens showed higher reliability compared to OP. Those with 50‐μm cement thickness were more reliable relative to their 150‐μm counterparts (HV_50 μm: 95% (0.99/0.67); HV_150 μm: 55% (0.92/0.01); OP_50 μm: 69% (0.84/0.48); OP_150 μm: 15% (0.53/0.004)). Similar failure modes were observed in HV and OP specimens. Radial cracks developing in the core and spreading into the veneer are suggested to cause bulk fracture, which is the characteristic failure mode for alumina core crowns. However, the highest resistance to fatigue loading was found for the HV specimens with thin cement thickness, while the lowest occurred for the OP with thick cement layer. © 2011 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater 100B: 508–515, 2012.
Epitaxial growth of GaN films on Si(110) substrates by rf‐MBE
Authors: Shen X. Q. , Ide T. , Shimizu M. 
Published: November 2011

AbstractGaN films grown by rf‐MBE on Si(110) substrates using AlN buffer layers are investigated. Single crystalline AlN films are obtained by Al pre‐deposition during the buffer layer growth. 2‐dimensional epitaxial growth mode of GaN is confirmed by in‐situ RHEED observations. HRXRD results show that the FWHM values of diffraction peaks decrease with the increase of the film thickness. Atomically flat GaN surface morphology with mono‐layer steps is obtained and crack‐free GaN films until 2 μm are successfully achieved. Micro‐Raman measurements show that the tensile strain in the GaN films on Si(110) substrates is reduced compared to those on conventional Si(111) substrates. It is expectable that high‐quality III‐nitrides can be grown by rf‐MBE technique for device applications. (© 2012 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)
Millets, Rice, Social Complexity, and the Spread of Agriculture to the Chengdu Plain and Southwest China
Authors: d’Alpoim Guedes Jade 
Published: November 2011

Abstract
Southwest China played a pivotal role in the spread of agriculture across East and Southeast Asia. Both rice and millet were important in the spread of populations and the expansion of agriculture into this region. Recent finds in the mountainous peripheries of Sichuan Province show that the earliest inhabitants of this region practiced a combination of broomcorn and foxtail millet agriculture (ca 4000–2500 BC). These crops are adapted to high altitude and arid environments, which facilitated their movement across this region and eventually into the Tibetan Plateau. At around 2700 BC, a combined system of rice and foxtail millet agriculture appears suddenly in sites of the Baodun culture on the Chengdu Plain. The use of this double cropping system provided advantages to the inhabitants of this region in both risk reduction and yield. I argue that this had important consequences for spurring population growth, facilitating expansion into new territories and the development of social complexity.
Observing competence in CBT supervision: a systematic review of the available instruments
Authors: Milne Derek L. , Reiser Robert P. 
Published: November 2011

AbstractGovernment policy, like evaluations of clinical practice, indicates the growing importance of supervision in fostering practitioner development and in improving the fidelity of therapies. However, instruments with which to measure competent supervision are often problematic, thereby hampering these key activities (e.g. they are rare, rely on self-ratings by participants, and psychometric data can be limited). To contribute to progress, this paper reviews the current options for measuring competent clinical supervision by means of direct observation, a favoured approach within cognitive behaviour therapy (CBT). We systematically reviewed 10 existing instruments that were designed to observe and quantify competent supervision, focusing on three broad criteria for sound measurement (i.e. an instrument's Design, Implementation, and Yield: DIY). Suggestions for future research on instruments that can fulfil the functions that are provided distinctively through direct observation are outlined.
A novel and versatile computational tool to model translation
Authors: Chu Dominique , Zabet Nicolae , von der Haar Tobias 
Published: November 2011

Abstract
Motivation: Much is now known about the mechanistic details of gene translation. There are also rapid advances in high-throughput technologies to determine quantitative aspects of the system. As a consequence-realistic and system-wide simulation models of translation are now feasible. Such models are also needed as devices to integrate a large volume of highly fragmented data known about translation.
Software: In this application note, we present a novel, highly efficient software tool to model translation. The tool represents the main aspects of translation. Features include a representation of exhaustible tRNA pools, ribosome–ribosome interactions and differential initiation rates for different mRNA species. The tool is written in Java, and is hence portable and can be parameterized for any organism.
Availability: The model can be obtained from the authors or directly downloaded from the authors' home-page (http://goo.gl/JUWvI).
Contact: d.f.chu@kent.ac.uk
Inhibition of the organic anion‐transporting polypeptide 1B1 by quercetin: an in vitro and in vivo assessment
Authors: Wu Lan‐Xiang , Guo Cheng‐Xian , Chen Wang‐Qing , Yu Jing , Qu Qiang , Chen Yao , Tan Zhi‐Rong , Wang Guo , Fan Lan , Li Qing , Zhang Wei , Zhou Hong‐Hao 
Published: November 2011

WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• OATP1B1 is a liver‐specific expression drug transporter and mediates the uptake of a broad range of compounds into hepatocytes. Modulation the activity of OATP1B1 may alter the pharmacokinetics of its substrate drugs, causing potential drug–drug interactions. As a popular dietary supplement in the United States, quercetin has been shown to interact with some drug transporters and efficiently influences their activity, but the effect of quercetin on OATP1B1 activity is not well known.WHAT THIS STUDY ADDS• Quercetin inhibits the OATP1B1‐mediated transport of E3S and pravastatin in vitro, and also has a modest inhibitory influence on the pharmacokinetics of pravastatin in healthy Chinese‐Han male volunteers.AIMTo investigate the effect of quercetin on organic anion transporting polypeptide 1B1 (OATP1B1) activities in vitro and on the pharmacokinetics of pravastatin, a typical substrate for OATP1B1 in healthy Chinese‐Han male subjects.METHODSUsing human embryonic kidney 293 (HEK293) cells stably expressing OATP1B1, we observed the effect of quercetin on OATP1B1‐mediated uptake of estrone‐3‐sulphate (E3S) and pravastatin. The influence of quercetin on the pharmacokinetics of pravastatin was measured in 16 healthy Chinese‐Han male volunteers receiving a single dose of pravastatin (40 mg orally) after co‐administration of placebo or 500 mg quercetin capsules (once daily orally for 14 days).RESULTSQuercetin competitively inhibited OATP1B1‐mediated E3S uptake with a Ki value of 17.9 ± 4.6 µm and also inhibited OATP1B1‐mediated pravastatin uptake in a concentration dependent manner (IC50, 15.9 ± 1.4 µm). In healthy Chinese‐Han male subjects, quercetin increased the pravastatin area under the plasma concentration – time curve (AUC(0,10 h) and the peak plasma drug concentration (Cmax) to 24% (95% CI 15, 32%, P < 0.001) and 31% (95% CI 20, 42%, P < 0.001), respectively. After administration of quercetin, the elimination half‐life (t1/2) of pravastatin was prolonged by 14% (95% CI 4, 24%, P = 0.027), with no change in the time to reach Cmax (tmax). Moreover, quercetin decreased the apparent clearance (CL/F) of pravastatin by 18% (95% CI 75, 89%, P < 0.001).CONCLUSIONSThese findings suggest that quercetin inhibits the OATP1B1‐mediated transport of E3S and pravastatin in vitro and also has a modest inhibitory influence on the pharmacokinetics of pravastatin in healthy Chinese‐Han male volunteers. The effects of quercetin on other OATP1B1 substrate drugs deserve further investigation.
Outcomes of Pneumocystis jiroveci pneumonia infections in pediatric heart transplant recipients
Authors: Ng Benton , Dipchand Anne , Naftel David , Rusconi Paolo , Boyle Gerard , Zaoutis Theo , Edens R. Erik 
Published: November 2011

Ng B, Dipchand A, Naftel D, Rusconi P, Boyle G, Zaoutis T, Erik Edens R. Outcomes of Pneumocystis jiroveci pneumonia infections in pediatric heart transplant recipients.  Pediatr Transplantation 2011: 15: 844–848. © 2011 John Wiley & Sons A/S.Abstract:  PJP is known to cause significant morbidity and rarely death in immunosuppressed patients. The prevalence and outcomes of PJP in pediatric solid‐organ transplant patients are not well established. This study utilizes data from the PHTS to establish the prevalence and outcome of PJP in pediatric heart transplant recipients. We conducted a retrospective cohort study using data from the PHTS, including data from 24 institutions between January 1, 1993, and December 31, 2004. Infections that occur in PHTS subjects are recorded in a standardized data collection form. The prevalence and outcomes of PJP in pediatric heart transplant recipients were determined. There were a total of 18 patients (1%) with PJP out of the 1854 pediatric heart transplant recipients in the PHTS database. A majority of PJP occurred two months to two yr post‐transplant, and patients with PJP had a significantly decreased mortality compared with other fungal infections. PJP is an infrequent complication experienced by pediatric heart transplant recipients. Patients that have experienced PJP have an increased survival compared to patients with other fungal infections, and most PJP occurred within two yr of transplant.
Validation and comparison of the two Kattan nomograms in patients with prostate cancer treated with 125iodine brachytherapy
Authors: Kaplan Alan , German Larissa , Chen Juza , Matzkin Haim , Mabjeesh Nicola J. 
Published: November 2011

Study Type – Prognostic (cohort)Level of Evidence 2bWhat's known on the subject? and What does the study add?Nomograms are based on large patient population. Their applicability should be externally validated.Among 747 brachytherapy patients we evaluated two kattan nonograms and conclude that they have limited value to predict PSA‐free survival.OBJECTIVE
To validate and compare the preoperative and postoperative Kattan prediction nonograms for prostate cancer recurrence after brachytherapy.
PATIENTS AND METHODS
Patients (n= 747) treated with 125I‐brachytherapy were evaluated.
Both nomograms were used to calculate the prediction of 5‐year biochemical‐freedom from failure (BFFF) based on clinical stage, Gleason score, prostate‐specific antigen (PSA) level, receipt of androgen deprivation therapy and the post‐implant dosimetry variable D90 (values of the minimal dose received by 90% of the prostate volume).
The predicted values using the Kattan nomograms and the observed values were compared.
Predictive accuracy was determined using the concordance index.
RESULTS
The 5‐year BFFF probability was 94% (95% confidence interval [CI], 92–96%) for the modified American Society for Radiation Oncology (ASTRO) definition and 97% (95% CI, 95–98%) for the Phoenix definition using Kaplan–Meier analysis.
The predicted values of BFFF using both Kattan nomograms were lower than the observed rates in our cohort.
The concordance index values were 0.51 and 0.52 for preoperative and postoperative nomograms, respectively.
Concordance correlation coefficient between the two nomograms was 0.15.
CONCLUSIONS
In our population, the 5‐year BFFF outcomes rates were superior to nomogram predictions.
Neither nomogram predicted outcomes after 125I‐brachytherapy in this non‐US cohort.
The postoperative nomogram was also a poor predictor, although it included D90 dosimetry values, as a variable of treatment quality.
Strict inclusion criteria, perhaps more favourable than the ones on which the Kattan nomograms were based, could be the explanation for these discrepancies.
Altered bladder function in elastin‐deficient mice at baseline and in response to partial bladder outlet obstruction
Authors: Jiang Xiaogang , Luttrell Ian , Li Dean Y. , Yang Claire C. , Chitaley Kanchan 
Published: November 2011

Study Type – Aetiology (case control)Level of Evidence 3bWhat's known on the subject? and What does the study add?As one of the major components of the extracellular matrix, elastic fibres are believed to enhance tissue compliance. However, the role of elastic fibres in normal bladder function and dysfunction remains speculative. Although transgenic mice overexpressing elastin showed increased bladder compliance, the findings in patients with non‐compliant bladders are inconsistent.Using transgenic elastin‐deficient mouse models, this study provides the first direct evidence that sufficient elastin content is critical for healthy bladder function, and elastin is involved in the detrusor response to partial bladder outlet obstruction.OBJECTIVE
To examine functional and molecular changes of the bladders from elastin‐haploinsufficient mice (Eln+/−) at baseline as well as in response to partial bladder outlet obstruction (pBOO).
MATERIALS AND METHODS
Female Eln+/− and wild type (Wt) mice (3–4 months old) were studied.
The bladder elastin content was quantified by measuring desmosine.
Mice were divided into two groups to undergo surgery to create pBOO or to undergo sham surgery. Three days after surgery, bladder function was evaluated by in vivo cystometry, and the contractile response of bladder strips exposed to electrical field stimulation (EFS) and carbachol was examined by ex vivo myography.
RESULTS
The Eln+/−‐sham mice had a 33.6% decrease in bladder elastin compared with Wt‐sham mice.
Cystometry showed significantly decreased bladder compliance and capacity in Eln+/−‐sham vs Wt‐sham mice; pBOO increased bladder compliance and capacity to a greater extent in Eln+/− mice compared with Wt mice.
Bladder strips from Eln+/−‐sham mice showed a significantly heightened contractile response to both EFS and carbachol compared with Wt‐sham mice.
A significantly increased contractile response to carbachol was detected in Wt‐pBOO vs Wt‐sham but not between Eln+/−‐pBOO and Eln+/−‐sham mice.
CONCLUSION
The results that elastin‐deficient mice had decreased bladder compliance and capacity and increased bladder contractility; and that Wt‐pBOO mice showed an enhanced contractile response to carbachol, but Eln+/−‐pBOO mice did not, suggest that elastin is critical for normal bladder function and is involved in bladder response to pBOO.
Human Annexin A6 Interacts with Influenza A Virus Protein M2 and Negatively Modulates Infection
Authors: Ma Huailiang , Kien François , Manière Maxime , Zhang Yang , Lagarde Nadège , Tse Kong San , Poon Leo Lit Man , Nal Béatrice 
Published: November 2011

ABSTRACTThe influenza A virus M2 ion channel protein has the longest cytoplasmic tail (CT) among the three viral envelope proteins and is well conserved between different viral strains. It is accessible to the host cellular machinery after fusion with the endosomal membrane and during the trafficking, assembly, and budding processes. We hypothesized that identification of host cellular interactants of M2 CT could help us to better understand the molecular mechanisms regulating the M2-dependent stages of the virus life cycle. Using yeast two-hybrid screening with M2 CT as bait, a novel interaction with the human annexin A6 (AnxA6) protein was identified, and their physical interaction was confirmed by coimmunoprecipitation assay and a colocalization study of virus-infected human cells. We found that small interfering RNA (siRNA)-mediated knockdown of AnxA6 expression significantly increased virus production, while its overexpression could reduce the titer of virus progeny, suggesting a negative regulatory role for AnxA6 during influenza A virus infection. Further characterization revealed that AnxA6 depletion or overexpression had no effect on the early stages of the virus life cycle or on viral RNA replication but impaired the release of progeny virus, as suggested by delayed or defective budding events observed at the plasma membrane of virus-infected cells by transmission electron microscopy. Collectively, this work identifies AnxA6 as a novel cellular regulator that targets and impairs the virus budding and release stages of the influenza A virus life cycle.
Hyaluronan Synthase HAS2 Promotes Tumor Progression in Bone by Stimulating the Interaction of Breast Cancer Stem–Like Cells with Macrophages and Stromal Cells
Authors: Okuda Hiroshi , Kobayashi Aya , Xia Bo , Watabe Misako , Pai Sudha K. , Hirota Shigeru , Xing Fei , Liu Wen , Pandey Puspa R. , Fukuda Koji , Modur Vishnu , Ghosh Arnab , Wilber Andrew , Watabe Kounosuke 
Published: November 2011

Abstract
The molecular mechanisms that operate within the organ microenvironment to support metastatic progression remain unclear. Here, we report that upregulation of hyaluronan synthase 2 (HAS2) occurs in highly metastatic breast cancer stem–like cells (CSC) defined by CD44+/CD24−/ESA+ phenotype, where it plays a critical role in the generation of a prometastatic microenvironment in breast cancer. HAS2 was critical for the interaction of CSCs with tumor-associated macrophages (TAM), leading to enhanced secretion of platelet-derived growth factor-BB from TAMs, which then activated stromal cells and enhanced CSC self-renewal. Loss of HAS2 in CSCs or treatment with 4-methylumbelliferone, an inhibitor of HAS, which blocks hyaluronan production, drastically reduced the incidence and growth of metastatic lesions in vitro or in vivo, respectively. Taken together, our findings show a critical role of HAS2 in the development of a prometastatic microenvironment and suggest that HAS2 inhibitors can act as antimetastatic agents that disrupt a paracrine growth factor loop within this microenvironment. Cancer Res; 72(2); 537–47. ©2011 AACR.