bluuebunny/crossref_metadata_2025_split huggingface dataset:
Bicyclic Substituted Hydroxyphenylmethanone Type Inhibitors of 17 β‐Hydroxysteroid Dehydrogenase Type 1 (17 β‐HSD1): The Role of the Bicyclic Moiety
Authors: Oster Alexander , Klein Tobias , Henn Claudia , Werth Ruth , Marchais‐Oberwinkler Sandrine , Frotscher Martin , Hartmann Rolf W. 
Published: February 2011

AbstractAn attractive target that has still to be explored for the treatment of estrogen‐dependent diseases, such as breast cancer and endometriosis, is the enzyme responsible for the last step in the biosynthesis of estradiol (E2): 17β‐hydroxysteroid dehydrogenase type 1 (17β‐HSD1). It catalyzes the reduction of the weakly active estrone (E1) into E2, which is the most potent estrogen in humans. Inhibition of 17β‐HSD1 lowers intracellular E2 concentrations and thus presents a therapeutic target for estrogen‐dependent pathologies. Recently, we reported a new class of highly active and selective 17β‐HSD1 inhibitors: bicyclic substituted hydroxyphenylmethanones. Here, further structural variations on the bicyclic moiety are described, especially focusing on the exchange of its hydroxy function. Twenty‐nine novel inhibitors were synthesized and evaluated for 17β‐HSD1 inhibition in a cell‐free and cellular assay, for selectivity toward 17βHSD2 and estrogen receptors (ER) alpha and beta, as well as for metabolic stability. The best compound exhibited IC50 values of 12 nM (cell‐free assay) and 78 nM (cellular assay), high selectivity for 17β‐HSD1, and reasonable metabolic stability. A molecular docking study provided insight into the protein–ligand interactions of this compound with 17β‐HSD1.
Cellular Selectivity and Biological Impact of Cytotoxic Rhodium(III) and Iridium(III) Complexes Containing Methyl‐Substituted Phenanthroline Ligands
Authors: Geldmacher Yvonne , Kitanovic Igor , Alborzinia Hamed , Bergerhoff Katharina , Rubbiani Riccardo , Wefelmeier Pascal , Prokop Aram , Gust Ronald , Ott Ingo , Wölfl Stefan , Sheldrick William S. 
Published: February 2011

AbstractThe antiproliferative properties and biological impact of octahedral iridium(III) complexes of the type fac‐[IrCl3(DMSO)(pp)] containing pp=phenanthroline (1) and its 4‐ and 5‐methyl (2, 3) and 4,7‐ and 5,6‐dimethyl derivatives (4, 5) were investigated for both adherent and non‐adherent cells. A series of similar rhodium(III) complexes were studied for comparison purposes. The antiproliferative activity toward MCF‐7 cancer cells increases eightfold from IC50=4.6 for 1 to IC50=0.60 μM for 5, and an even more pronounced 18‐fold improvement was established for the analogous rhodium complexes 6 and 8, the respective IC50 values for which are 1.1 and 0.06 μM. Annexin V/propidium iodide assays demonstrated that the 5,6‐dimethylphenanthroline complexes 5 and 8 both cause significant inhibition of Jurkat leukemia cell proliferation and invoke extensive apoptosis but negligible necrosis. The percentages of Jurkat cells exhibiting high levels of reactive oxygen species correlate with the percentages of cells undergoing apoptosis. The antiproliferative activity of 5 and 8 is strongly selective toward MCF‐7 and HT‐29 cancer cells over normal HFF‐1 and immortalized HEK‐293 cells. Complex 5 also exhibits high selectivity toward BJAB lymphoma cells relative to healthy leukocytes. Both 5 and 8 invoke permanent decreases in the adhesion and respiration of MCF‐7 cells.
FLIM FRET Technology for Drug Discovery: Automated Multiwell‐Plate High‐Content Analysis, Multiplexed Readouts and Application in Situ
Authors: Kumar Sunil , Alibhai Dominic , Margineanu Anca , Laine Romain , Kennedy Gordon , McGinty James , Warren Sean , Kelly Douglas , Alexandrov Yuriy , Munro Ian , Talbot Clifford , Stuckey Daniel W. , Kimberly Christopher , Viellerobe Bertrand , Lacombe Francois , Lam Eric W.‐F. , Taylor Harriet , Dallman Margaret J. , Stamp Gordon , Murray Edward J. , Stuhmeier Frank , Sardini Alessandro , Katan Matilda , Elson Daniel S. , Neil Mark A. A. , Dunsby Chris , French Paul M. W. 
Published: February 2011

AbstractA fluorescence lifetime imaging (FLIM) technology platform intended to read out changes in Förster resonance energy transfer (FRET) efficiency is presented for the study of protein interactions across the drug‐discovery pipeline. FLIM provides a robust, inherently ratiometric imaging modality for drug discovery that could allow the same sensor constructs to be translated from automated cell‐based assays through small transparent organisms such as zebrafish to mammals. To this end, an automated FLIM multiwell‐plate reader is described for high content analysis of fixed and live cells, tomographic FLIM in zebrafish and FLIM FRET of live cells via confocal endomicroscopy. For cell‐based assays, an exemplar application reading out protein aggregation using FLIM FRET is presented, and the potential for multiple simultaneous FLIM (FRET) readouts in microscopy is illustrated.
A stereoscopic video transmission algorithm for an IPTV network based on empirical data
Authors: Lloret Jaime , Garcia Miguel , Canovas Alejandro , Turro Carlos 
Published: February 2011

AbstractIPTV service is one of the topics where industry and academia are providing more efforts with the purpose of enhancing the systems in existence. One of the potentially biggest advantages of IPTV is the existence of a return channel from the customer to the IPTV service provider, which makes this technology the upcoming TV distribution system. The next big step is to serve stereoscopic video over IP networks. In this paper, we evaluate the stereoscopic video transmission over IP by taking measurements of the bandwidth, delay and jitter. These measurements are useful to test the QoS and QoE of the ITPV service and to demonstrate the need for high‐performance stereoscopic compression codecs. Then, we study the performance of four free codecs in order to propose an algorithm to perform the appropriate decisions to transmit stereoscopic video in the IPTV network properly. The algorithm is based on the empirical data obtained from our test and on some analytical considerations. Finally, we show the impact on the network given by the algorithm, and we compare the QoS parameters when each codec is chosen. Copyright © 2011 John Wiley & Sons, Ltd.
Pancreas organogenesis: From bud to plexus to gland
Authors: Pan Fong Cheng , Wright Chris 
Published: February 2011

AbstractPancreas oganogenesis comprises a coordinated and highly complex interplay of signaling events and transcriptional networks that guide a step‐wise process of organ development from early bud specification all the way to the final mature organ state. Extensive research on pancreas development over the last few years, largely driven by a translational potential for pancreatic diseases (diabetes, pancreatic cancer, and so on), is markedly advancing our knowledge of these processes. It is a tenable goal that we will one day have a clear, complete picture of the transcriptional and signaling codes that control the entire organogenetic process, allowing us to apply this knowledge in a therapeutic context, by generating replacement cells in vitro, or perhaps one day to the whole organ in vivo. This review summarizes findings in the past 5 years that we feel are amongst the most significant in contributing to the deeper understanding of pancreas development. Rather than try to cover all aspects comprehensively, we have chosen to highlight interesting new concepts, and to discuss provocatively some of the more controversial findings or proposals. At the end of the review, we include a perspective section on how the whole pancreas differentiation process might be able to be unwound in a regulated fashion, or redirected, and suggest linkages to the possible reprogramming of other pancreatic cell‐types in vivo, and to the optimization of the forward‐directed‐differentiation of human embryonic stem cells (hESC), or induced pluripotential cells (iPSC), towards mature β‐cells. Developmental Dynamics 240:530–565, 2011. © 2011 Wiley‐Liss, Inc.
MESD is essential for apical localization of megalin/LRP2 in the visceral endoderm
Authors: Lighthouse Janet K. , Zhang Liqun , Hsieh Jen‐Chih , Rosenquist Thomas , Holdener Bernadette C. 
Published: February 2011

AbstractLow‐density lipoprotein receptor family mediated endocytosis in the mouse visceral endoderm. Photo shows a whole mount view of a E7.5 wild‐type embryo that was incubated with 50nM receptor associated protein (RAP) tagged with AlexaFluor 488 to visualize endocytosis in the visceral endoderm. Embryos were then fixed and counterstained with Alexa 594‐Phalloidin to mark cell boundaries (color‐corrected to magenta in Photoshop) and DAPI to mark nuclei (blue). From Lighthouse et al., Developmental Dynamics 240:577–588, 2011.
Treatment of low‐concentration hydrogen by use of proton exchange membrane
Authors: Araki Takuto , Ichihara Keiji , Nagahama Mituyuki , Minamoto Yasuo , Onda Kazuo 
Published: February 2011

AbstractThe proton exchange membrane fuel cell (PEMFC) cannot react 100% of fuel, because the cell potential becomes zero if all of the fuel is consumed in the PEMFC. Therefore, a small amount of fuel is always released from the PEMFC. The exhausted H2 should be treated for safety. The VCell–iave characteristics were measured while varying the hydrogen concentration from 99.99% to 1%. In addition the VCell of the constant voltage control was selected with reference to the measured VCell–Iave characteristics. It was found that low‐concentration hydrogen could be treated at VCell = 0.15 to 0.3 V by the hydrogen pump and at VCell = 0.4 to 0.6 V by PEMFC. The exhaust hydrogen concentration was reduced to several tens of ppm. © 2011 Wiley Periodicals, Inc. Electron Comm Jpn, 94(3): 51–59, 2011; Published online in Wiley Online Library (wileyonlinelibrary.com). DOI 10.1002/ecj.10292
Formulae for second‐ and third‐order electric field induced by uniform ELF magnetic field in eccentric two‐sphere conductor configuration
Authors: Masutani Keigo , Hamada Shoji , Kobayashi Tetsuo 
Published: February 2011

AbstractThis paper describes analyses of the electric fields induced in two eccentrically arranged spherical conductors by a uniform ELF magnetic field, utilizing the equivalent multipolar‐moment method with re‐expansion (RE‐EMMM). Although an approximation formula has already been derived by Tarao for this situation, it is limited to a first‐order approximation. Here we mathematically derive a general form of the governing linear equations for unknown multipole and local coefficients. We also derive the first‐, second‐, and third‐order electric field formulae by manually solving the linear equations. We confirm that the accuracy of the first‐order formula is almost the same as that of Tarao's. The accuracies of the second‐ and third‐order formulae are confirmed to be more precise. © 2011 Wiley Periodicals, Inc. Electron Comm Jpn, 94(3): 20–32, 2011; Published online in Wiley Online Library (wileyonlinelibrary.com). DOI 10.1002/ecj.10304
Synthesis of a Focused Chemical Library Based on Derivatives of Embelin, a Natural Product with Proapoptotic and Anticancer Properties (Eur. J. Org. Chem. 7/2011)
Authors: Viault Guillaume , Grée Danielle , Das Saibal , Yadav Jhillu Singh , Grée René 
Published: February 2011

AbstractThe cover picture shows the design and synthesis of two successive generations of analogues of embelin, a natural product with proapoptotic and anticancer properties. This research was performed in the Indo‐French “Joint Laboratory for Sustainable Chemistry at Interfaces&2dquo; between the University of Rennes I/CNRS and the Indian Institute of Chemical Technology/CSIR, Hyderabad. This cooperation is highlighted by the best‐known monuments from both cities (Charminar in Hyderabad and Parliament of Brittany in Rennes). Details of this research are discussed in the article by R. Grée, et al. on p. 1233 ff.
Azure A Mediated Polypyrrole‐Based Amperometric Nitrate Biosensor
Authors: Adeloju Samuel B. , Sohail Manzar 
Published: February 2011

AbstractThe co‐entrapment of Aspergillus niger‐nitrate reductase (NaR) and azure A (AzA), as a redox mediator has been investigated for fabrication of a polypyrrole (PPy)‐based electron mediated amperometric nitrate biosensor. Optimum formation of PPy‐NaR‐AzA film was achieved in a monomer solution which contained 0.3 M Py, 0.1 M KCl, 1U/mL NaR, 50 µM AzA with an applied current density of 0.5 mA/cm2 for 240 s. The optimum applied potential of −0.25 V for amperometric detection of nitrate with PPy‐NaR‐AzA biosensor was 50, 100 and 150 mV more positive than those achieved with the use of safranin O (Saf), methyl viologen (MV) and bromophenol blue (BrB) or red (BrR), respectively, as mediators. Similar optimum applied of −0.25 V was achieved with thionin acetate (ThAc) which was in the same phenothiazine group of mediators as AzA. The electron mediated amperometric detection of nitrate with the PPy‐NaR‐AzA biosensor also gave the best performance with a sensitivity of 40.8 nA µM−1 cm−2, detection limit of 0.5 µM, a response time of 18–20 s and a linear concentration range of 20–500 µM.
Electrocatalytic Oxidation of NADH on Functionalized Graphene Modified Graphite Electrode
Authors: Kumar Simson Prasanna , Manjunatha Revanasiddappa , Nethravathi C. , Suresh Gurukar Shivappa , Rajamathi Michael , Venkatesha Thimmappa Venkatarangaiah 
Published: February 2011

AbstractGraphite electrode modified with functionalized graphene (FG) is a new family of electrocatalysts for the oxidation of nicotinamide adenine dinucleotide (NADH). A substantial decrease in the over potential of NADH oxidation is observed on functionalized graphene modified graphite electrode (FGGE). The COO− functionalized graphene is characterized by powder X‐ray diffraction and infrared spectroscopy techniques and the modified FGGE is characterized using cyclic voltammetry (CV), electrochemical impedance spectroscopy and scanning electron microscopy. The modified electrode is found to be stable and reproducible. The FGGE shows rapid and highly sensitive amperometric response to NADH.
Direct and Simple Electrochemical Determination of Morphine at PEDOT Modified Pt Electrode
Authors: Atta Nada F. , Galal Ahmed , Ahmed Rasha A. 
Published: February 2011

AbstractA simple and rapid method for morphine detection is described based on PEDOT electrode in the presence of SDS. The electrochemistry of morphine is investigated by CV, LSV and SWV. The effect of common interferences on the current response of morphine namely AA and UA is studied. The electrode is applied to the selective determination of morphine in urine samples in the linear ranges 0.3–8 µmol L−1 and 10–60 µmol L−1, with low detection limits of 50 and 68 nmol L−1, respectively and recovery of 96.4 %. The application of PEDOT is realized in determination of morphine in tablets successfully.
Multiway Processing of Data Generated with a Potentiometric Electronic Tongue in a SIA System
Authors: Cartas Raul , Mimendia Aitor , Legin Andrey , del Valle Manel 
Published: February 2011

AbstractIn this work a potentiometric electronic tongue based on an array of three Ion Selective Electrodes (ISEs) as sensor elements and multiway partial least squares (N‐PLS2) regression method as processing tool has been developed for simultaneous quantification of Cd2+, Cu2+ and Pb2+ in aqueous solution mixtures. The sensor array was formed by two chalcogenide glass sensors selective to Cd2+ and Cu2+ plus one PVC membrane sensor selective to Pb2+. Preparation, measurement and injection of samples in a step profile were performed by an automated SIA system. Concentration range covered was 1.05 µM to 29.8 µM for Cd2+, 0.05 µM to 1.5 µM for Cu2+ and 0.55 µM to 14.7 µM for Pb2+. Potentiometric recordings were arranged into a three‐way array and treated by N‐PLS2 regression method to obtain the calibration model. Prediction ability yielded RMSE values as low as 4.20±0.37 µM, 0.094±0.007 µM and 0.915±0.006 µM, and correlation coefficients from linear regression analysis of 0.82±0.038, 0.97±0.005 and 0.97±0.004 for Cd2+, Cu2+ and Pb2+, respectively.
On the solution of MHD flow over a nonlinear stretching sheet by an efficient semi‐analytical technique
Authors: Motsa S. S. , Sibanda P. 
Published: February 2011

SUMMARYThe problem of magneto‐hydrodynamic fluid flow past a nonlinear stretching sheet in the presence of a transverse magnetic field is analyzed. The governing equations are transformed into a nonlinear ordinary differential equation that is solved using a novel spectral homotopy analysis method and the Matlab in‐built numerical solverttbvp4c. The new technique removes some known limitations of the homotopy analysis method and offers a more systematic way of selecting initial approximations and the optimal auxiliary parameter ℏ. A comparison with the numerical solution confirms the robustness, the computational efficiency, and the accuracy of the technique. Copyright © 2011 John Wiley & Sons, Ltd.
Ca looping technology: current status, developments and future directions
Authors: Anthony E. J. (Ben) 
Published: February 2011

AbstractCalcium looping technology is a promising new technique for high‐temperature scrubbing of CO2 from flue gas and syngases. Current economic projections suggest it might be able to capture CO2 at costs of ∼$20/ton of avoided CO2. Nonetheless there are questions about the long‐term behavior of natural sorbents in such systems, and there is substantial R&D being done on this technology worldwide to answer questions about whether the performance of natural sorbents can be improved, or whether it would be better to use synthetic ones. The current period is particularly interesting as the first pilot plants and demonstration units capable of operating continuously are now coming on stream, and if successful these will lead to large‐scale industrial demonstrations of the technology in the next 10 to 15 years. © 2011 Society of Chemical Industry and John Wiley & Sons, Ltd
The potential of aquatic biomass for CO2‐enhanced fixation and energy production
Authors: Dibenedetto Angela 
Published: February 2011

AbstractIn this review, the use of micro‐ and macroalgae to fix CO2 and produce energy is discussed. The fixation of CO2 into aquatic biomass is an option which has recently come under intensive investigation as it can be utilized to stimulate the growth of seaweed or microalgae. Aquatic biomass has long been cultivated and used at industrial level as a source of chemicals (agar, alginate, carragenans, and fucerellans) or as food for humans or animal feed. Recent interest in its use as a source of biofuels is due to the need to shift from first‐generation biofuels (biodiesel and bioethanol produced from edible biomass) to non‐food sources that may grow without the use of arable land. Aquatic biomass can be grown in salty water or fresh wastewater (municipalities or process water) or else in bioreactors to produce different fuels such as bio‐oil, biodiesel, bioalcohol, biohydrogen. Biogas can be produced from residual biomass after liquid fuel extraction. Microalgae are attracting much attention as they are photosynthetic renewable resources, with high lipid content and faster growth rate than terrestrial plants; they can grow in saline waters which are not suited for agriculture. While the lipid content of microalgae on a dry cellular weight basis usually varies between 20 and 40%, a lipid content as high as 85% has been reported for selected microalgal strains. They can be easily manipulated through physical stress or genetic engineering. They can also produce bioethanol. The barrier to their exploitation is the high cost (up to 5000 US$/t) of growth and processing. Seaweeds produce less biofuel per t‐dry weight, but their growing and processing costs are much lower. In perspective, aquatic biomass can become an interesting and ubiquitous source of energy. © 2011 Society of Chemical Industry and John Wiley & Sons, Ltd
Co‐culture of mesenchymal‐like stromal cells derived from human foreskin permits long term propagation and differentiation of human embryonic stem cells
Authors: Mamidi Murali Krishna , Pal Rajarshi , Mori Nor Azah Binti , Arumugam Greetha , Thrichelvam Saratha Thevi , Noor Puteri J , Abdullah Hj. Mohamad Farouk , Gupta Pawan Kumar , Das Anjan Kumar , Zakaria Zubaidah , Bhonde Ramesh 
Published: February 2011

AbstractAmong the different parameters governing the successful derivation and expansion of human embryonic stem cells (hESC), feeder layers play the most important role. Human feeders in form of human mesenchymal stromal cells (hMSCs) and human foreskin fibroblasts (HFFs) lay the foundation for eradication of animal‐derived hESC culture system. In this study we explored the potential of human foreskin derived mesenchymal like stromal cells (HF‐MSCs) to support self renewal and pluripotency of hESC. The MSCs isolated from human foreskin were found to be resistant to standard concentrations and duration of mitomycin‐C treatment. Growth pattern, gene profiling (Oct‐4, Nanog, Sox‐2, Rex‐1), cytoskeletal protein expression (vimentin, nestin) and tri‐lineage differentiation potential into adipocytes, chondrocytes and osteocytes confirmed their mesenchymal stromal cell status. Further, the HF‐MSCs were positive for CD105, CD166, CD73, CD44, CD90, SSEA‐4, and negative for CD34, CD45, HLA‐DR cell‐surface markers and were found to exhibit BM‐MSC‐like characteristics. hESC lines co‐cultured with HF‐MSC feeders showed expression of expected pluripotent transcription factors Oct‐4, Nanog, Sox‐2, GDF‐3, Rex‐1, STELLAR, ABCG2, Dppa5, hTERT; surface markers SSEA‐4, TRA‐1‐81 and maintained their cytogenetic stability during long term passaging. These novel feeders also improved the formation of embryoid bodies (EBs) from hESC which produced cell types representing three germ layers. This culture system has the potential to aid the development of clinical‐grade hESCs for regenerative medicine and drug screening. Further, we envisage foreskin can serve as a valuable source of alternative MSCs for specific therapeutic applications. J. Cell. Biochem. 112: 1353–1363, 2011. © 2011 Wiley‐Liss, Inc.
Indirubin‐3'‐monoxime, a derivative of a chinese antileukemia medicine, inhibits angiogenesis
Authors: Kim Jin‐Kyung , Shin Eun Kyung , Kang Young‐Hee , Park Jung Han Yoon 
Published: February 2011

AbstractAlthough the antiangiogenic activity of indirubin‐3‐monoxime (I3M), a derivative of a Chinese anti‐leukemia medicine, has been demonstrated using transgenic zebrafish, the detail molecular mechanism has not been elicited. To further establish its role in antiangiogenic activity, we tested its potential against human umbilical vein endothelial cells (HUVECs) and the in vivo Matrigel plug model was applied to evaluate new vessel formation. We also investigated the molecular mechanisms of I3M‐induced antiangiogenic effects in HUVECs. We found that I3M significantly inhibited HUVEC proliferation (2.5–20 µM), migration (2.5–20 µM), and tube formation (10–20 µM) in HUVECs. The number of microvessels growing from the aortic rings was suppressed by I3M treatment. Moreover, I3M suppressed neovascularization in Matrigel plugs in mice. The underlying antiangiogenic mechanism of I3M was correlated with down‐regulation of the vascular endothelial growth factor receptor‐2 activation, at least a part. These findings emphasize the potential use of I3M in pathological situations involving stimulated angiogenesis, such as tumor development. J. Cell. Biochem. 112: 1384–1391, 2011. © 2011 Wiley‐Liss, Inc.
Weak interactions: Potency for stabilization of molecule in solid state
Authors: Dubey Rashmi , Tewari Ashish Kumar , Ravikumar K. , Sridhar B. 
Published: February 2011

AbstractWeak interactions usually show a versatile property to stabilize the molecular conformation and crystal packing in solid state. Crystal packing and conformational property of the synthesized compound 1(3‐cyano‐4,6‐dimethyl nicotinonitril‐1‐yl)‐3‐(phalimido‐1‐yl)‐1‐thioxyethane (2) is stabilized by CH···O, CH···N, and CH···π interactions. J. Heterocyclic Chem., 00, 00 (2011).