bluuebunny/crossref_metadata_2025_split huggingface dataset:
Diphenyl Ether Non‐Nucleoside Reverse Transcriptase Inhibitors with Excellent Potency Against Resistant Mutant Viruses and Promising Pharmacokinetic Properties
Authors: Sweeney Zachary K. , Kennedy‐Smith Joshua J. , Wu Jeffrey , Arora Nidhi , Billedeau J. Roland , Davidson James P. , Fretland Jennifer , Hang Julie Q. , Heilek Gabrielle M. , Harris Seth F. , Hirschfeld Donald , Inbar Petra , Javanbakht Hassan , Jernelius Jesper A. , Jin Qingwu , Li Yu , Liang Weiling , Roetz Ralf , Sarma Keshab , Smith Mark , Stefanidis Dimitrio , Su Guoping , Suh Judy M. , Villaseñor Armando G. , Welch Michael , Zhang Fang‐Jie , Klumpp Klaus 
Published: November 2008

AbstractNon‐nucleoside reverse transcriptase inhibitors (NNRTIs) are part of the preferred treatment regimens for individuals infected with HIV. These NNRTI‐based regimens are efficacious, but the most popular NNRTIs have a low genetic barrier to resistance and have been associated with adverse events. There is therefore still a need for efficacious antiviral medicines that facilitate patient adherence and allow durable suppression of viral replication. As part of an extensive program targeted toward the discovery of NNRTIs that have favorable pharmacokinetic properties, good potency against NNRTI‐resistant viruses, and a high genetic barrier to drug resistance, we focused on the optimization of a series of diaryl ether NNRTIs. In the course of this effort, we employed molecular modeling to design a new set of NNRTIs that that are active against wild‐type HIV and key NNRTI‐resistant mutant viruses. The structure–activity relationships observed in this series of compounds provide insight into the structural features required for NNRTIs that inhibit the replication of a wide range of mutant viruses. Selected compounds have promising pharmacokinetic profiles.
Improved survival for fallopian tube cancer
Authors: Wethington Stephanie L. , Herzog Thomas J. , Seshan Venkatraman E. , Bansal Nisha , Schiff Peter B. , Burke William M. , Cohen Carmel J. , Wright Jason D. 
Published: November 2008

AbstractBACKGROUND.Fallopian tube cancers are rare neoplasms. These malignancies are thought to behave biologically and clinically like ovarian cancer. The purpose of this study was to compare the clinical behavior and outcome of fallopian tube and ovarian cancer.METHODS.The Surveillance, Epidemiology, and End Results database was reviewed to identify women with tumors of the fallopian tube (FT) and ovary (OV) diagnosed between 1988 and 2004. Demographic and clinical data were compared, and the impact of tumor site on survival was analyzed using Cox models and the Kaplan‐Meier method.RESULTS.A total of 55,825 patients were identified, 1576 (3%) with FT and 54,249 (97%) with OV cancer. FT patients were more likely to present with early stage tumors (P < .001). Among FT patients, 47% had stage I/II tumors compared with 29% of OV cancers. In an adjusted Cox model of all patients, cancer‐specific mortality was 48% lower in FT patients (hazard ratio, 0.52; 95% confidence interval [CI], 0.48‐0.56) compared with OV cancer. Among patients with FT tumors, advanced age and stage were independent predictors of decreased survival. When stratified by stage, survival was similar for stage I and II tumors, but stage III and IV FT patients had an improved survival. The 5‐year survival for stage III FT cancer was 54% (95% CI, 48%‐60%), compared with 30% (95% CI, 29%‐31%) for OV.CONCLUSIONS.Fallopian tube cancers present earlier and at advanced stage have a better overall survival than primary ovarian malignancies. Future clinical trials should recognize the possible distinct clinical behavior of fallopian tube cancers. Cancer 2008. © 2008 American Cancer Society.
Galanin is a selective marker of the retrotrapezoid nucleus in rats
Authors: Stornetta Ruth L. , Spirovski Darko , Moreira Thiago S. , Takakura Ana C. , West Gavin H. , Gwilt Justin M. , Pilowsky Paul M. , Guyenet Patrice G. 
Published: November 2008

AbstractThe rat retrotrapezoid nucleus (RTN) contains CO2‐activated neurons that contribute to the central chemoreflex and to breathing automaticity. These neurons have two known markers, the transcription factor Phox2b and vesicular glutamate transporter 2 (VGLUT2). Noncatecholaminergic galanin‐immunoreactive (ir) neurons within a region of the lower brainstem that seems identical to what is currently defined as the RTN have been previously described. Here we ask whether these galanin‐expressing neurons are the same cells as the recently characterized CO2‐sensitive neurons of the RTN. By using in situ hybridization, we found that pre‐pro‐galanin (PPGal) mRNA is expressed by an isolated cluster of neurons that is co‐extensive with the RTN as defined by a population of strongly Phox2b‐ir neurons devoid of tyrosine hydroxylase (Phox2b+/TH− neurons). This bilateral structure contains about 1,000 PPGal mRNA‐positive neurons in the rat. The PPGal mRNA‐positive neurons were Phox2b+/TH− and as susceptible to destruction by the toxin [Sar9, Met (O2)11]‐substance P as the rest of the RTN Phox2b+/TH− cells of the RTN. CO2‐activated neurons were recorded in the RTN of anesthetized rats and were labeled with biotinamide. Many of those cells (7/17, 41%, five rats) contained PPGal‐mRNA. In conclusion, galanin mRNA is a very specific marker of the glutamatergic Phox2b+/TH− neurons of the RTN, but galanin mRNA identifies only half of these putative central respiratory chemoreceptors. J. Comp. Neurol. 512:373–383, 2009. © 2008 Wiley‐Liss, Inc.
Dopamine's role in social modulation of infant isolation‐induced vocalization: I. Reunion responses to the dam, but not littermates, are dopamine dependent
Authors: Shair Harry N. , Muller Jeff M. , Moore Holly 
Published: November 2008

AbstractRat pups' vocalization during social separation and the cessation of vocalization upon social reunion (contact quieting) model early life affiliative relationships. The present study examined the roles of dopamine (DA) receptors in regulating contact quieting. Contact quieting to the dam, but not to littermates, was disrupted by either blockade or exogenous stimulation of DA D1‐like receptors. The D2 antagonist raclopride also prevented the quieting effect of reunion with the dam and had a lesser effect on the quieting properties of littermates. In contrast, the D2 agonist quinpirole permitted or enhanced contact quieting. Combined systemic and local striatal administration of D2 ligands showed that stimulation of striatal D2 receptors can enhance, but is not necessary for, contact quieting to the dam. These results are consistent with the literature linking the neural mechanisms of affiliation and reinforcement. This is also the first demonstration that the neurochemical substrates of an infant comfort response to dams differ from a behaviorally similar response to siblings. © 2008 Wiley Periodicals, Inc. Dev Psychobiol 51: 131–146, 2009
Palladium‐Catalyzed Oligocyclizations of 2‐Bromoalk‐1‐ene‐(n+1),(m+n+1)‐diynes – Influence of Tether Lengths and Substituents on the Outcome of the Reaction (Part I)
Authors: Tokan Wajdi M. , Meyer Frank E. , Schweizer Stefan , Parsons Philip J. , de Meijere Armin 
Published: November 2008

AbstractThe outcomes and the mechanistic pathways of the palladium‐catalyzed Heck‐type cascade oligocyclizations of various 2‐bromoalkenediynes were explored with respect to the lengths of the tethers between the multiple bonds and the nature of the substituent at the acetylenic terminus. Just like substrates containing two three‐atom tethers, 2‐bromotridec‐1‐ene‐6,13‐diynes 10a,b with one three‐ and one four‐atom tether undergo two consecutive intramolecular 5‐ and 6‐exo‐dig carbopalladations with subsequent 6π‐electrocyclization and β‐hydride elimination to form tricycles 35a,b with a central benzene ring in 67 and 61 % yield, respectively, independent of the fact that 10a contains an electron donor and 10b an electron acceptor at the acetylene terminus. However, when 2‐bromotetradec‐1‐ene‐7,13‐diynes 22, 29 on one side and 16, 27, 31 on the other are subjected to Heck reaction conditions, tricycles with a central benzene ring are formed only, when the substituent at the acetylene terminus is not a methoxycarbonyl group as in 22, 29. Thus, the bisannelated benzene derivatives 36 and 37 are formed from 22 and 29 in 79 and 18 % yield, respectively, whereas 16, 27 and 31 with their methoxycarbonyl substituents at the acetylenic end yield tetracyclic systems 38, 39 and 40, consisting of a central five‐membered and two annelated six‐membered as well as an additional annelated three‐membered ring, predominantly (54, 19 and 18 % yield, respectively). The cascade reaction leading to the latter products must involve a 5‐exo‐trig carbopalladation rather than 6π‐electrocyclization as the third step. Apparently, the nature and the substitution pattern of the tether in the substrates 16, 22, 31 linking the vinyl bromide moiety with the internal acetylene affect the yield of the tetracyclic product.(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)
Structural Analysis of the Capsular Polysaccharide from Acinetobacter lwoffii F78
Authors: Hanuszkiewicz Anna , Kaczyński Zbigniew , Lindner Buko , Goldmann Torsten , Vollmer Ekkehard , Debarry Jennifer , Heine Holger , Holst Otto 
Published: November 2008

AbstractThe capsular polysaccharide from Acinetobacter lwoffii F78 was isolated and purified, and its structure was elucidated by chemical analyses, NMR spectroscopy, and mass spectrometry. The presence of a capsule on this bacterium was confirmed by transmission electron microscopy experiments, and the utilization of the antilipid A monoclonal antibody proved the nonendotoxin origin of the isolated material. The structure represents a novel nonbranched aminopolysaccharide with high heterogeneity of amino groups substituents: →3)‐α‐L‐FucNAc‐(1→3)‐β‐D‐QuiNR14NR2‐(1→4)‐β‐L‐GlcNR33NR4A‐(1→, where R1 = 3‐hydroxybutyric acid (3‐HBA) or N‐acetylated alanine (AlaNAc), R2 = AlaNAc or 3‐HBA, R3 = acetyl or 3‐HBA, and R4 = 3‐HBA or acetyl.(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)
Truly Catalytic and Chemoselective Cleavage of Benzylidene Acetal with Phosphomolybdic Acid Supported on Silica Gel
Authors: Kumar Ponminor Senthil , Kumar Gaddale Devanna Kishore , Baskaran Sundarababu 
Published: November 2008

AbstractPhosphomolybdic acid supported on silica gel provides a truly catalytic method for the chemoselective cleavage of benzylidene acetals having sensitive functional groups under mild conditions. It is easy to perform on large scale owing to minimal catalyst loading (0.5 mol‐%). Several sensitive functional groups such as TBDPS ether, ‐OMs, ‐OAc, allyl ether, N‐Boc, N‐Fmoc and N‐Cbz are stable under the reaction conditions. In addition, benzylidene acetal is selectively cleaved in the presence of isopropylidene ketal.(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)
Application of Impedimetric and Voltammetric Genosensor for Detection of a Biological Warfare: Anthrax
Authors: Kara Pinar , Meric Buket , Ozsoz Mehmet 
Published: November 2008

AbstractA strategy for the detection of anthrax, which is a potential biological weapon by using an electrochemical genosensing technology, is investigated. An alkanathiol‐linked or unlabeled capture probe related to B. anthracis is immobilized onto gold or graphite electrode surface. A 101‐mer anthrax target is used for hybridization. The extent of hybridization between probe and target sequences is determined by using differential pulse voltammetry (DPV) and electrochemical impedance spectrometry (EIS). EIS analysis are based on electron transfer resistance (Rct) in the presence of [Fe(CN)6]3−/4− and DPV measurements are based on transduction of both guanine oxidation and Meldola's blue (MDB) reduction signal as hybridization indicator. The response of the probe‐modified electrodes which was interacted with a noncomplementary sequence was the same as the responses of probe‐modified surface and proved the specifity of the hybridization with the target. According to these results the developed genosensors based on EIS and DPV techniques can be employed for rapid and selective detection of B. anthracis.
Public insurance and private savings: who is affected and by how much?
Authors: Maynard Alex , Qiu Jiaping 
Published: November 2008

AbstractThis paper employs a recently developed instrumental quantile regression method to investigate the effect of Medicaid on household savings across different wealth groups. It finds that the disincentive effect of Medicaid on household savings is heavily concentrated in the middle net‐worth households. In contrast, the effects on the bottom and top net‐worth households are quite small and insignificant. These heterogeneous incentive effects are partly explained by Medicaid asset tests. Our findings hold regardless of whether affluence is measured in terms of wealth or income. They suggest that despite generating substantial crowd‐out for the mean household, Medicaid expansions are unlikely to discourage the savings of the poorest households. Copyright © 2008 John Wiley & Sons, Ltd.
Biochemical characterization of membrane fractions in murine sperm: Identification of three distinct sub‐types of membrane rafts
Authors: Asano Atsushi , Selvaraj Vimal , Buttke Danielle E. , Nelson Jacquelyn L. , Green Karin M. , Evans James E. , Travis Alexander J. 
Published: November 2008

AbstractDespite enormous interest in membrane raft micro‐domains, no studies in any cell type have defined the relative compositions of the raft fractions on the basis of their major components—sterols, phospholipids, and proteins—or additional raft‐associating lipids such as the ganglioside, GM1. Our previous localization data in live sperm showed that the plasma membrane overlying the acrosome represents a stabilized platform enriched in GM1 and sterols. These findings, along with the physiological requirement for sterol efflux for sperm to function, prompted us to characterize sperm membrane fractions biochemically. After confirming limitations of commonly used detergent‐based approaches, we utilized a non‐detergent‐based method, separating membrane fractions that were reproducibly distinct based on sterol, GM1, phospholipid, and protein compositions (both mass amounts and molar ratios). Based on fraction buoyancy and biochemical composition, we identified at least three highly reproducible sub‐types of membrane raft. Electron microscopy revealed that raft fractions were free of visible contaminants and were separated by buoyancy rather than morphology. Quantitative proteomic comparisons and fluorescence localization of lipids suggested that different organelles contributed differentially to individual raft sub‐types, but that multiple membrane micro‐domain sub‐types could exist within individual domains. This has important implications for scaffolding functions broadly associated with rafts. Most importantly, we show that the common practice of characterizing membrane domains as either “raft” or “non‐raft” oversimplifies the actual biochemical complexity of cellular membranes. J. Cell. Physiol. 218: 537–548, 2009. © 2008 Wiley‐Liss, Inc.
Proteasome inhibitor MG132 induces BAG3 expression through activation of heat shock factor 1
Authors: Du Zhen‐Xian , Zhang Hai‐Yan , Meng Xin , Gao Yan‐Yan , Zou Ren‐Long , Liu Bao‐Qin , Guan Yifu , Wang Hua‐Qin 
Published: November 2008

AbstractBAG3 protein, a member of the BAG co‐chaperones family, sustains cell survival in a variety of normal and neoplastic cell types, via its interaction with a variety of partners, such as the heat shock protein (HSP) 70, Bcl‐2, Raf‐1 and others. Expression of BAG3 is induced by some stressful stimuli, such as heat shock, heavy metal exposure. We have reported that proteasome inhibitors can also induce BAG3 expression at the transcriptional level and the induction of BAG3 compromises proteasome inhibitors‐mediated apoptosis. However, the molecular mechanism of BAG3 upregulation has not been elucidated. In the current study, we provide evidence that heat shock transcription factor 1 (HSF1) is involved in BAG3 induction by proteasome inhibitor MG132. Using a series of varying lengths of 5′‐flanking region of the BAG3 gene into luciferase reporter vectors, we found that MG132 stimulated the promoter activity via the −326/−233 and −825/−689 regions, which contains one putative heat shock‐responsive element (HSE) for HSF1‐binding, respectively. Site‐directed deletion of the sites abrogated the enhanced reporter activity in response to MG132 treatment. Chromatin immunoprecipitation assay demonstrated that HSF1 directly bound to the MG132‐responsive site on the BAG3 promoter. Activation of HSF1 occurred with MG132 along with BAG3 upregulation. Furthermore, knockdown HSF1 by small interfering RNA attenuated the BAG3 upregulation due to MG132.These results indicate that the proteasome inhibitor MG132 induces BAG3 expression through HSF1 activation. J. Cell. Physiol. 218: 631–637, 2009. © 2008 Wiley‐Liss, Inc.
The epidermal growth factor receptor ligands at a glance
Authors: Schneider Marlon R. , Wolf Eckhard 
Published: November 2008

AbstractThe epidermal growth factor receptor (EGFR) regulates key processes of cell biology, including proliferation, survival, and differentiation during development, tissue homeostasis, and tumorigenesis. Canonical EGFR activation involves the binding of seven peptide growth factors. These ligands are synthesized as transmembrane proteins comprising an N‐terminal extension, the EGF module, a short juxtamembrane stalk, a hydrophobic transmembrane domain, and a carboxy‐terminal fragment. The central structural and functional feature is the EGF module, a sequence containing six cysteines in a conserved spacement which is responsible for binding to the EGFR. While the membrane‐anchored peptide can be biologically active by juxtacrine signaling, in most cases the EGF module is proteolytically cleaved (a process termed ectodomain shedding) to release the soluble growth factor, which may act in an endocrine, paracrine, or autocrine fashion. This review summarizes the structural and functional properties of these fascinating molecules and presents selected examples to illustrate their roles in development, physiology, and pathology. J. Cell. Physiol. 218: 460–466, 2009. © 2008 Wiley‐Liss, Inc.
Topical delivery of interleukin‐13 antisense oligonucleotides with cationic elastic liposome for the treatment of atopic dermatitis
Authors: Kim Sung Tae , Lee Kyung‐Mi , Park Hyun‐Joo , Jin Su‐Eon , Ahn Woong Shick , Kim Chong‐Kook 
Published: November 2008

AbstractBackgroundInterleukin (IL)‐13, overproduced in the skin of atopic dermatitis (AD), has been shown to play an essential role in the pathogenesis of the disease. Thus, inhibition of IL‐13 production should provide a key step to alleviate disease conditions of the atopic skin. In the present study, IL‐13 antisense oligonucleotide (ASO) was designed and formulated with cationic elastic liposome (cEL) to improve transdermal delivery.MethodsASOs were generated against murine IL‐13 mRNA (+4 to + 23) and complexed with cEL. Physicochemical properties of IL‐13 ASO/cEL complex were examined by DNA retardation and DNase I protection assay. An in vitro inhibition study was performed in T‐helper 2 (Th2) cells and cytotoxicity was tested by the XTT assay. The in vivo effect of IL‐13 ASO/cEL complex was tested in a murine model of AD.ResultsIn vitro, the IL‐13 ASO/cEL complex showed dose‐ and ratio‐dependent inhibition of IL‐13 secretion in Th2 cells. At the IL‐13 ASO/cEL ratio of 6, maximum inhibition of IL‐13 secretion was observed. When applied to the ovalbumin‐sensitized murine model of AD, topically administered IL‐13 ASO/cEL complex dramatically suppressed IL‐13 production (by up to 70% of the control) in the affected skin region. In addition, the levels of IL‐4 and IL‐5 were also significantly reduced. Moreover, IL‐13 ASO/cEL‐treated AD mice showed reduced infiltration of inflammatory cells into the epidermal and dermal areas, with concomitant reduction of skin thickness.ConclusionsThese data suggests that IL‐13 ASO/cEL complex can provide a potential therapeutic tool for the treatment of AD and also be applied to other immune diseases associated with the production of Il‐13. Copyright © 2008 John Wiley & Sons, Ltd.
Poly[lactic‐co‐(glycolic acid)]‐Grafted Hyaluronic Acid Copolymer Micelle Nanoparticles for Target‐Specific Delivery of Doxorubicin
Authors: Lee Hyukjin , Ahn Cheol‐Hee , Park Tae Gwan 
Published: November 2008

AbstractPLGA‐grafted HA copolymers were synthesized and utilized as target specific micelle carriers for DOX. For grafting hydrophobic PLGA chains onto the backbone of hydrophilic HA, HA was solubilized in an anhydrous DMSO by nano‐complexing with dimethoxy‐PEG. The carboxylic groups of HA were chemically grafted with PLGA, producing HA‐g‐PLGA copolymers. Resultant HA‐g‐PLGA self‐assembled in aqueous solution to form multi‐cored micellar aggregates and DOX was encapsulated during the self‐assembly. DOX‐loaded HA‐g‐PLGA micelle nanoparticles exhibited higher cellular uptake and greater cytotoxicity than free DOX for HCT‐116 cells that over‐expressed HA receptor, suggesting that they were taken up by the cells via HA receptor‐mediated endocytosis.magnified image
Charge/Discharge Properties of Organometallic Batteries Fabricated with Ferrocene–Containing Polymers
Authors: Tamura Kosaku , Akutagawa Nao , Satoh Masaharu , Wada Jun , Masuda Toshio 
Published: November 2008

AbstractA group of ferrocene‐containing polymers were synthesized from vinylferrocene, ethynylferrocene and 1,1′‐dibromoferrocene, and properties of the formed polymers were examined to clarify their potential as a new class of cathode‐active, charge‐storage materials for rechargeable batteries. Vinylferrocene polymerized with 2,2′‐azoisobutyronitrile (AIBN) to give a polymer with number‐average molecular weights of 2 200–5 100 g · mol−1 in 12–41% yields, while ethynylferrocene and 1,1′‐dibromoferrocene polymerized with Rh catalysts and by step‐growth mechanism, respectively, to provide insoluble polymers in 71–96% yields. The capacities of organometallic rechargeable cells fabricated with poly(vinylferrocene), poly(ethynylferrocene), and poly(ferrocene) reached 105, 105, and 95 Ah · kg−1, respectively. In particular, poly(vinylferrocene) displayed completely reversible charge/discharge processes featuring a constant voltage of around 3.5 V.magnified image
Effective utility functions induced by organizational target‐based incentives
Authors: Abbas Ali E. , Matheson James E. , Bordley Robert F. 
Published: November 2008

AbstractMany companies set performance targets for their divisions to decentralize the decision‐making process and communicate with outside investors. This paper analyzes the effects of performance targets on the decision‐making behavior of the divisions. We introduce the notion of an ‘effective utility function’—a function that a division should use in its selection of projects if it wishes to maximize the probability of achieving its targets. We show that many target‐based incentives induce S‐shaped utility functions and discuss the organizational problems they may pose. We then show how an organization can set targets that induce expected utility maximization. Copyright © 2008 John Wiley & Sons, Ltd.
Transplanted dopaminergic neurons develop PD pathologic changes: A second case report
Authors: Kordower Jeffrey H. , Chu Yaping , Hauser Robert A. , Olanow C.Warren , Freeman Thomas B. 
Published: November 2008

AbstractThis report describes pathological changes within the grafted neurons of another patient with Parkinson's disease (PD) who died 14 years posttransplantation. Although numerous healthy appearing grafted neurons were present at this long‐term time point, some displayed Lewy bodies as evidenced by alpha‐synuclein, ubiquitin, and thioflavin‐S staining. Additionally, there was a general loss of dopamine transporter‐immunoreactivity in grafted neurons. Some grafted cell displayed a loss of tyrosine hydroxylase. These data support the emerging concept that PD‐like pathology is seen in young grafted neurons when they survive long term. © 2008 Movement Disorder Society