bluuebunny/crossref_metadata_2025_split huggingface dataset:
Efficient methods for the synthesis of 5‐(4‐[18F]fluorophenyl)‐10,15,20‐tris(3‐methoxyphenyl)porphyrin as a potential imaging agent for tumor
Authors: Kavali Rajesh R. , Chul Lee Byung , Seok Moon Byung , Dae Yang Seung , Soo Chun Kwon , Woon Choi Chang , Lee Chang‐Hee , Yoon Chi Dae 
Published: July 2005

AbstractF‐18‐labeled porphyrins, the potential tracing and detecting agents for tumor have been synthesized and characterized by two convenient routes: one is a mixed aldehyde condensation, which involves acid‐catalyzed condensation of pyrrole, m‐anisaldehyde and 4‐[18F]fluorobenzaldehyde. The other is the acid‐catalyzed condensation of tetrapyrrane with 4‐[18F]fluorobenzaldehyde. The synthetic methodologies including solvents, reaction concentrations and catalysts are optimized for radiolabeled porphyrins. The methods also provide the desired product in reasonable radiochemical yield (20–26%) compared with those of cold chemical synthesis (1–3%) and with high radiochemical purity (>95%). The methods described here would be effective and convenient ways to produce radiolabeled porphyrin. Copyright © 2005 John Wiley & Sons, Ltd.
Microscale synthesis of isotopically labeled 6R‐N5, N10 methylene‐5, 6, 7, 8‐tetrahydrofolate
Authors: Hong Baoyu , Kohen Amnon 
Published: July 2005

AbstractA one‐pot chemo‐enzymatic microscale synthesis of isotopically labeled R‐[6‐YH; 11‐XH] N5, N10 methylene‐5, 6, 7, 8‐tetrahydrofolate (CH2H4folate) is presented, where Y=1 or 2 represents protium or deuterium, and X=1, 2 or 3 represents protium, deuterium or tritium, respectively. In this procedure, Thermoanaerobium brockii alcohol dehydrogenase (tbADH) and Escherichia coli dihydrofolate reductase (ecDHFR) were used simultaneously in the reaction mixture. First, tbADH stereospecifically catalyzes a hydride transfer from [2‐YH] iPrOH to the re face of C‐4 NADP+. The ecDHFR then reduced 7, 8‐dihydrofolate (H2folate) to form (6S)‐H4folate. Finally, the enzymatic reactions were followed by chemical trapping with isotopically labeled formaldehyde ([XH]‐HCHO) to form the final product. The preparation of deuterium‐ and tritium‐labeled formaldehyde is also presented. Two reverse phase HPLC methods were developed for analysis and purification of product R‐[6‐YH; 11‐XH] CH2H4folate. This isotopically labeled cofactor can be used to study 1° and 2° kinetic isotope effects (KIEs) with any CH2H4folate dependent enzyme as demonstrated by studies with E. coli thymidylate synthase (TS). Copyright © 2005 John Wiley & Sons, Ltd.
Synthesis of [18F]fluoroalkyl esters of carfentanil
Authors: Henriksen Gjermund , Herz Michael , Schwaiger Markus , Wester Hans‐Jürgen 
Published: July 2005

AbstractWith the aim to develop and evaluate new ligands for depicting the µ‐opioid receptor with positron emission tomography, the 18F‐fluoroalkyl esters of carfentanil, 3‐carboxy‐(2‐[18F]fluoroethyl)fentanyl, (2‐[18F]fluoroethyl‐carfentanil) and 3‐carboxy‐(3‐[18F]fluoropropyl)fentanyl (3‐[18F]fluoropropyl‐carfentanil) were prepared by a two‐step radiosynthesis. Reacting carfentanil carboxylate sodium salt, added 0.96 eqv. of tetrabutyl ammonium hydroxide (TBAH), with no‐carrier‐added (n.c.a.) 2‐[18F]fluoroethyltosylate for 20 min at 150°C in dimethyl formamide (DMF) provided 2‐[18F]fluoroethyl carfentanil in an isolated radiochemical yield (RCY) of 36 ± 8%, a specific activity (SA) of 35 ± 5 TBq/mmol (n=4) within a synthesis time of ∼100 min. Similarly, 3‐[18F]fluoropropyl carfentanil could be obtained by reacting the carfentanil TBA/Na salt with 3‐[18F]fluoropropyl iodide at 160°C in DMF (isolated RCY=6 ± 2%; ∼100 min, SA=27 ± 5 TBq/mmol, n=4). The developed methods allow the production of the two 18F‐labeled carfentanil derivatives in amounts and specific activities necessary and relevant for a detailed preclinical evaluation of these new potential µ‐opioid receptor ligands in vitro and in animal models. Copyright © 2005 John Wiley & Sons, Ltd.
The neuroprotective KDI domain of γ1‐laminin is a universal and potent inhibitor of ionotropic glutamate receptors
Authors: Möykkynen Tommi , Liebkind Ron , Sjöberg Jari , Korpi Esa R. , Liesi Päivi 
Published: July 2005

AbstractPrevious work from this laboratory indicates that the KDI (Lys‐Asp‐Ile) domain of γ1‐laminin promotes functional regeneration of adult rat spinal cord injuries and protects adult rat hippocampal neurons against massive neuronal death induced by intracerebral injection of the glutamate analogue kainic acid. In the present study, we used patch clamp recordings on cultured human embryonic neocortical neurons and HEK 293 cells expressing recombinant glutamate receptor subunits to study a putative interaction of the KDI with the glutamate system. We show that the KDI domain of γ1‐laminin is a universal and potent inhibitor of AMPA, kainate, and NMDA subclasses of glutamate receptors, with a noncompetitive action on the AMPA receptor channel activity. Glutamate neurotoxicity plays a key role in both CNS trauma and neurodegenerative disorders, so this unexpected, novel function of the γ1‐laminin‐derived tripeptide may prove clinically valuable in treatment of CNS trauma and/or disease. © 2005 Wiley‐Liss, Inc.
Two‐stage dilute acid‐catalyzed hydrolytic conversion of softwood sawdust into sugars fermentable by ethanologenic microorganisms
Authors: Kim Kyoung Heon 
Published: July 2005

AbstractSoftwood hemlock residues generated in a sawmill were tested as a feasible agricultural feedstock for the production of high‐value bio‐based products using the concept of two‐stage dilute acid hydrolysis. To convert the carbohydrate contained in the hemlock sawdust, two‐stage dilute‐acid catalyzed hydrolysis was conducted. In the first stage, sawdust was hydrolyzed at 190 °C for 150 s with 1.1wt% sulfuric acid and 46.0 wt% total solids. As a result, 69.3% mannose, 74.2% galactose, 67.7% xylose, and 17.4% glucose of their theoretical maximum yields were achieved, which reveals that hemicellulose was the major target in the first‐stage hydrolysis. After recovering soluble sugars by washing from the first‐stage hydrolysate with water, the washed first‐stage hydrolysate solids were hydrolyzed again in the second stage at more severe conditions, such as 2.6 or 3.5 wt% H2SO4, 205 or 210 °C, and 80–135 s. After the two stages, the highest overall yields from 100 g of dry hemlock sawdust were a total of 39.3 g of fermentable sugars (36.0 and 3.3 g of hexose and pentose sugars, respectively). These results indicate that hemlock sawdust could be used to produce fermentable sugars which can be converted into other value‐added bio‐based products. Copyright © 2005 Society of Chemical Industry
Southern French thyme oils: chromatographic study of chemotypes
Authors: Kaloustian Jacques , Abou Lydia , Mikail Céline , Amiot Marie J , Portugal Henri 
Published: July 2005

AbstractOils obtained from seven chemotypes (thymol, linalool, geraniol, borneol, (E)‐sabinene hydrate/terpinene‐4‐ol, p‐cymene and carvacrol) of Thymus vulgaris (thyme) that exist in the South of France were analysed by gas chromatography/mass spectrometry (GC/MS) and characterised. Wild thyme growing in three departments (Bouches du Rhone, Var and Vaucluse) of Provence and in a fourth neighbouring department (Gard) was also studied. This is often the result of a mixture of three chemotypes: thymol, carvacrol and p‐cymene. Linalool and (E)‐sabinene hydrate/terpinene‐4‐ol were observed as minor chemotypes. GC/MS was also used to monitor seasonal variations in the composition of the oil obtained from thyme harvested at the same location (Gemenos, near Marseille, Bouches du Rhone) during the plant vegetative and life cycles (19 samples). Four components were determined: the phenols thymol and carvacrol and the monoterpene hydrocarbon precursors p‐cymene and γ‐terpinene. Results showed maximum oil (34.1 mL kg−1 dry matter) and phenolic terpenoid (95.4 mmol kg−1 dry matter) contents occurring in May, the period of flowering and harvesting. In contrast, in December the oil displayed a higher level of phenolic precursors (p‐cymene and γ‐terpinene, 72.8 mmol kg−1 dry matter) than phenolic terpenoids. Depending on the harvesting date, the oils isolated from southern French thyme (T. vulgaris) could have different potential biological activities. Copyright © 2005 Society of Chemical Industry
Inhibition of epidermal growth factor‐induced cell transformation and Akt activation by caffeine
Authors: Nomura Masaaki , Ichimatsu Daisuke , Moritani Shuzo , Koyama Ichiko , Dong Zigang , Yokogawa Koichi , Miyamoto Ken‐ichi 
Published: July 2005

AbstractWe found that caffeine significantly inhibited epidermal growth factor (EGF)‐ and 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA)‐induced cell transformation in the JB6 mouse epidermal cell line. The tumor promoter‐induced cell transformation was also blocked by treatment with an adenosine A1 receptor antagonist, 8‐phenyltheophylline (8‐PTH). Caffeine slightly attenuated activation of EGF‐induced activator protein 1 (AP‐1) activation, which play important roles in cell transformation, but only at the highest concentration examined (1 mM). Interestingly, pretreatment with caffeine suppressed EGF‐induced phosphorylation and activation of Akt and ribosomal p70 S6 protein kinase (p70 S6K), a target of Akt, without inhibiting phosphatidylinositol 3‐kinase (PI3K) activation. The inhibition of Akt activation of caffeine was not a result of its adenosine receptor antagonism. Because Akt plays a key role in signal transduction pathways leading to cell proliferation and apoptosis, our results provide novel insight into possible mechanisms of the chemotherapeutic effect of caffeine. © 2005 Wiley‐Liss, Inc.
Inhibition of the Akt, cyclooxygenase‐2, and matrix metalloproteinase‐9 pathways in combination with androgen deprivation therapy: Potential therapeutic approaches for prostate cancer
Authors: Miyamoto Hiroshi , Altuwaijri Saleh , Cai Yi , Messing Edward M. , Chang Chawnshang 
Published: July 2005

AbstractProstate cancer cells are generally dependent on androgen stimulation mediated by the androgen receptor (AR) for growth and survival, and, therefore, hormonal manipulation, such as castration and/or the use of AR antagonists, results in a regression of the cancer. However, this treatment very rarely leads to the “cure” of advanced disease, and cancers eventually become androgen‐independent. A number of genes/pathways have been reported to be activated in prostate cancer, most of which are possibly associated with disease progression. In this article, among them, we focus on Akt (also known as protein kinase B), cyclooxygenase (COX)‐2, and matrix metalloproteinase (MMP)‐9, whose activities or expressions have been found to be regulated by androgens/AR. Previous studies by us and others, with androgen‐sensitive prostate cancer cell lines, have demonstrated that androgen deprivation results in activation/overexpression of Akt, COX‐2, and MMP‐9 in cells. This suggests that androgen deprivation in clinical settings activates the Akt, COX‐2, and MMP‐9 pathways in prostate cancer, which may increase cell growth and in turn promote the transition to the androgen‐independent state. We hypothesize that androgen deprivation, in combination with inhibition of the Akt, COX‐2, and MMP‐9 pathways, delays the androgen‐independent transition and has more beneficial effects than hormonal therapy alone. © 2005 Wiley‐Liss, Inc.
Inhibition of TPA‐induced cyclooxygenase‐2 (COX‐2) expression by apigenin through downregulation of Akt signal transduction in human keratinocytes
Authors: Van Dross Rukiyah T. , Hong Xiaoman , Pelling Jill C. 
Published: July 2005

AbstractApigenin is a nonmutagenic bioflavonoid that has been shown to be an inhibitor of mouse skin carcinogenesis induced by the two‐stage regimen of initiation and promotion with dimethylbenzanthracene (DMBA) and 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA). These DMBA/TPA‐induced squamous cell carcinomas overexpress cyclooxygenase‐2 (COX‐2). Cyclooxygenases are key enzymes required for prostaglandin (PG) synthesis, converting the arachidonic acid (AA) released by phospholipase A2 into prostaglandins. A large body of evidence indicates that the inducible form of cyclooxygenase, COX‐2, is involved in tumor promotion and carcinogenesis in a wide variety of tissue types, including colon, breast, lung, and skin. In the present study, we have determined that apigenin inhibited the TPA‐induced increase in COX‐2 protein and mRNA in the human keratinocyte cell line; HaCaT. The induction of COX‐2 elicited by TPA correlated with increased activation of Akt kinase and cell treatment with the PI3 kinase inhibitor, LY294002, blocked TPA induction of COX‐2. In cells treated with TPA and apigenin, the inhibition of COX‐2 expression correlated with inhibition of Akt kinase activation. Apigenin‐mediated inhibition of TPA‐induced COX‐2 expression was reversed by transient transfection with constitutively active Akt (CA‐Akt). Chemical inhibitors of MEK (PD98059), p38 (SB202190), but not JNK (SP600125) blocked TPA induction of COX‐2 although apigenin did not inhibit TPA‐mediated COX‐2 expression through these pathways. The TPA‐induced release of AA from HaCaT cells was also inhibited by cell treatment with apigenin. These data show that apigenin inhibits TPA‐mediated COX‐2 expression by blocking signal transduction of Akt and that apigenin also blocks AA release, which may contribute to its chemopreventive activity. © 2005 Wiley‐Liss, Inc.
Differential gene expression in epidermis of mice sensitive and resistant to phorbol ester skin tumor promotion
Authors: Riggs Penny K. , Angel Joe M. , Abel Erika L. , DiGiovanni John 
Published: July 2005

AbstractPrevious data from two‐stage carcinogenesis studies in mouse skin demonstrated that genetic control of susceptibility to skin tumor promotion by the phorbol ester, 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA), in crosses between susceptible DBA/2J and resistant C57BL/6J mice is a multigenic trait. Utilizing a cDNA microarray approach, we compared global gene expression profiles in the epidermis of these two mouse strains treated with TPA or vehicle (acetone). Gene expression in the epidermis was analyzed after the treatment to identify global effects of TPA, as well as potential candidate genes that modify susceptibility to skin tumor promotion. DBA/2J and C57BL/6J mice were treated topically four times with 3.4 nmol TPA or acetone over a 2‐wk period, and RNA was extracted from epidermis 6 h after the final treatment. Labeled cDNA generated from each group was hybridized to commercial cDNA microarrays (Agilent) containing more than 8000 targets. More than 450 genes were significantly influenced, directly or indirectly, by TPA treatment in the epidermis of either strain. Notably, 44 genes exhibited differential expression between the tumor promotion sensitive and resistant mouse strains. Several genes that were differentially expressed in DBA/2J versus C57BL/6J epidermis after TPA treatment were located in chromosomal regions linked to TPA promotion susceptibility. Three genes, Gsta4, Nmes1 (MGC58382), and Serpinb2, located within promotion susceptibility loci Psl1 (chr 9), Psl2 (chr 2), and Psl3 (chr 1), respectively, were identified in this analysis as potential candidates for modifiers of susceptibility to skin tumor promotion by TPA. © 2005 Wiley‐Liss, Inc.
Retrospective evaluation of the dose of dysport and BOTOX in the management of cervical dystonia and blepharospasm: The REAL DOSE study
Authors: Marchetti Albert , Magar Raf , Findley Leslie , Larsen Jan P. , Pirtosek Zvezdan , Růžička Evžen , Jech Robert , Sławek Jaroslaw , Ahmed Fayyaz 
Published: July 2005

AbstractThe original article to which this Erratum refers has been published in Movement DisordersMov Disord (2005) 20 (8) 937–934. © 2005 Movement Disorder Society
Non‐greedy heuristics and augmented neural networks for the open‐shop scheduling problem
Authors: Colak Selcuk , Agarwal Anurag 
Published: July 2005

AbstractIn this paper we propose some non‐greedy heuristics and develop an Augmented‐Neural‐Network (AugNN) formulation for solving the classical open‐shop scheduling problem (OSSP). AugNN is a neural network based meta‐heuristic approach that allows integration of domain‐specific knowledge. The OSSP is framed as a neural network with multiple layers of jobs and machines. Input, output and activation functions are designed to enforce the problem constraints and embed known heuristics to generate a good feasible solution fast. Suitable learning strategies are applied to obtain better neighborhood solutions iteratively. The new heuristics and the AugNN formulation are tested on several benchmark problem instances in the literature and on some new problem instances generated in this study. The results are very competitive with other meta‐heuristic approaches, both in terms of solution quality and computational times. © 2005 Wiley Periodicals, Inc. Naval Research Logistics, 2005.
Optimising communications for charity brand management
Authors: Jenkinson Angus , Sain Branko , Bishop Kevin 
Published: July 2005

AbstractThe paper presents recomendations on how to enhance communications planning through new integration and media neutral planning techniques (open planning) linked to Integrated Marketing practice. The paper is based on best practice research in charity and commercial sectors, including NSPCC and National Trust. Copyright © 2005 John Wiley & Sons, Ltd.
The face and voice of volunteering: a suitable case for branding?
Authors: Hankinson Philippa , Rochester Colin 
Published: July 2005

AbstractVolunteers make a substantial contribution to UK society but the level of volunteering has peaked and may, in part, be due to the poor ‘image’ of volunteering. Through qualitative research, this study explores the need to re‐shape perceptions of volunteering and the extent to which this may be achieved through branding. Key findings suggest that although there is much consistency in perceptions about generic volunteering, perceptions of the different strands of volunteering, such as governance and campaigning, are different and may require individual development as sub‐brands. It is argued that Volunteering England is best placed to lead a brand development programme, supported by managers of national and local bodies as well as volunteers to create a new visual identity and, importantly, key messages that will resonate with current and potential volunteers across different areas of activity. Copyright © 2005 John Wiley & Sons, Ltd.
Valuing not‐for‐profit and charity brands—real insight or just smoke and mirrors
Authors: Haigh David , Gilbert Stephen 
Published: July 2005

AbstractBrands introduce emotional decision‐making criteria, differentiating all brands across the not‐for‐profit sector. Brands shift the demand curve upwards and the cost curve downwards. The result is higher turnover, profit and surplus ‘consumer utility’. Brand equity is a measure of the emotional reservoir that shows how far the demand curve has moved and what the future cash flows will be. Brand valuation is a snapshot of those future cash flows. David Haigh and Stephen Gilbert's article describes how these three concepts fit together and explains how and why they have become best practice in marketing and financial management. Copyright © 2005 John Wiley & Sons, Ltd.
Building and rebuilding charity brands: the role of creative agencies
Authors: Griffiths Mark 
Published: July 2005

AbstractPeople who work in creative agencies tend to see a charitable organisation as a brand like any in the commercial world, and rightly so. While this is the correct starting point, there is often a huge gap between this simple understanding and the ability to deliver the changes in perception and behaviour that charities need. Besides strict governance and the obvious need for transparency and integrity, charity brands face many other issues, whether rebuilding or starting from scratch. They exist mainly to solve problems, not to meet a demand. Understanding this very different raison d'etre is the second greatest hurdle that creative agencies have to overcome when working on charity brands. The greatest is getting the charity to consider itself a brand and all that entails. When charities get beyond their complacency and suspicion and creative agencies their arrogance and superficiality—as with Breakthrough Breast Cancer and the Fairtrade Foundation—these two obstacles can be overcome. Copyright © 2005 John Wiley & Sons, Ltd.
Fabrication of poly(2‐oxy‐6‐naphthoyl) particles by direct polycondensation of 2‐hydroxy‐6‐naphthoic acid
Authors: Kimura Kunio , Horii Toshiyuki , Kohama Shin‐ichiro , Yamashita Yuhiko 
Published: July 2005

AbstractMorphology control of poly(2‐oxy‐6‐naphthoyl) (PON) was examined by using reaction‐induced crystallization of oligomers during direct polycondensation of 2‐hydroxy‐6‐naphthoic acid with p‐toluenesulfonyl chloride and N,N‐dimethylformamide in pyridine. PON particles were obtained of which the diameter was in the range of 8.0–8.3 µm. The particles were comprised of many lamellae and exhibited spherulitic morphology. They possessed high crystallinity evaluated from wide‐angle X‐ray scattering (WAXS). Formation mechanism of the particles was clarified from the results of morphology observation, yield, density and WAXS. When the number average degree of polymerization of the oligomers exceeded a critical value of ca. 4–5, they were precipitated to form lamellae. The lamellae grew to spherulites through screw dislocation with continuous precipitation of the oligomer from the solution. Finally, further polymerization occurred gradually in the precipitates. Copyright © 2005 John Wiley & Sons, Ltd.
Solubilization of fullerene into ionic liquids by the use of fluoroalkyl end‐capped oligomers
Authors: Sawada Hideo , Kasai Remi 
Published: July 2005

AbstractFluoroalkyl end‐capped oligomers were solubilized into a variety of ionic liquids such as N‐methylpyrazolium tetrafluoroborate, 3‐methylpyrazolium tetrafluoroborate and 1‐butyl‐3‐methylimidazolium hexafluorophosphate, and these fluorinated oligomers were able to reduce the surface tension of these ionic liquids. Interestingly, these fluorinated oligomers were able to solubilize fullerene into ionic liquids effectively. Fluoroalkyl end‐capped fullerene co‐oligomers, which were prepared by the oligomerizations of fluoroalkanoyl peroxides with radical polymerizable monomers such as acryloylmorpholine in the presence of fullerene, were more effective in solubilizing fullerene into ionic liquids compared to the corresponding fluoroalkyl end‐capped homo‐oligomers possessing no fullerene units. Fluoroalkyl end‐capped fullerene co‐oligomers/fullerene/ionic liquid complexes thus obtained were applied to the arrangements of fullerenes above the poly(methyl methacrylate) (PMMA) surface, and the higher fluorescent intensity of fullerene was obtained in the modified PMMA surface, although the reverse side of this modified film surface afforded an extremely weak fluorescent intensity. Copyright © 2005 John Wiley & Sons, Ltd.