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171.
Hua ZhangZeinab Khalil Melissa M. ConteFabien Plisson Robert J. Capon 《Tetrahedron letters》2012,53(29):3784-3787
Biological screening of a deep-water Great Australian Bight marine sponge, Axinella sp., detected inhibition against the neurodegenerative disease kinase targets CDK5/p25, CK1δ, and GSK3β, as well as significant levels of antibacterial activity. Chemical fractionation returned 18 secondary metabolites identified by detailed spectroscopic analysis as three new bromopyrrolo-2-aminoimidazoles, 14-O-sulfate massadine (1), 14-O-methyl massadine (2), and 3-O-methyl massadine chloride (3), together with the known metabolites massadine chloride (4), massadine (5), stylissadine B (6), axinellamines A-C (7-9), hymenin (10), stevensine (also known as odiline) (11), tauroacidin A (12), hymenidin (13), taurodispacamide A (14), oroidin (15), debromohymenialdisine (16), hymenialdisine (17), and aldisin (18). Armed with this focused natural product chemical diversity library, we re-established that 16 and 17 were nM kinase inhibitors, and determined that 3, 6, and 12-15 were sub μM antibacterials. 相似文献
172.
Marie Kissane Orla A. McNamara David Mitchell David M. Coppert Humphrey A. Moynihan Kurt T. Lorenz Anita R. Maguire 《Tetrahedron letters》2012,53(4):403-405
The palladium-catalysed decarboxylative cross-coupling of heterocyclic aromatic carboxylates and aryl halides is described. The cross-coupling proceeds under relatively mild conditions using catalytic Pd(0) and tetrabutylammonium bromide (TBAB). Utilizing a mixed solvent system consisting of N,N-dimethylformamide (DMF) and N-methyl-2-pyrrolidone (NMP), the cross-coupling system operated at temperatures ranging from 80 to 140 °C. 相似文献
173.
RR Rustandi JW Loughney M Hamm C Hamm C Lancaster A Mach S Ha 《Electrophoresis》2012,33(17):2790-2797
Many CE-based technologies such as imaged capillary IEF, CE-SDS, CZE, and MEKC are well established for analyzing proteins, viruses, or other biomolecules such as polysaccharides. For example, imaged capillary isoelectric focusing (charge-based protein separation) and CE-SDS (size-based protein separation) are standard replacement methods in biopharmaceutical industries for tedious and labor intensive IEF and SDS-PAGE methods, respectively. Another important analytical tool for protein characterization is a Western blot, where after size-based separation in SDS-PAGE the proteins are transferred to a membrane and blotted with specific monoclonal or polyclonal antibodies. Western blotting analysis is applied in many areas such as biomarker research, therapeutic target identification, and vaccine development. Currently, the procedure is very manual, laborious, and time consuming. Here, we evaluate a new technology called Simple Western? (or Simon?) for performing automated Western analysis. This new technology is based on CE-SDS where the separated proteins are attached to the wall of capillary by a proprietary photo activated chemical crosslink. Subsequent blotting is done automatically by incubating and washing the capillary with primary and secondary antibodies conjugated with horseradish peroxidase and detected with chemiluminescence. Typically, Western blots are not quantitative, hence we also evaluated the quantitative aspect of this new technology. We demonstrate that Simon? can quantitate specific components in one of our vaccine candidates and it provides good reproducibility and intermediate precision with CV <10%. 相似文献
174.
Hart-Smith G Low JK Erce MA Wilkins MR 《Journal of the American Society for Mass Spectrometry》2012,23(8):1376-1389
When localizing protein post-translational modifications (PTMs) using liquid-chromatography (LC)-tandem mass spectrometry (MS/MS), existing implementations are limited by inefficient selection of PTM-carrying peptides for MS/MS, particularly when PTM site occupancy is sub-stoichiometric. The present contribution describes a method by which peptides carrying specific PTMs of interest-in this study, methylarginines-may be selectively targeted for MS/MS: peptide features are extracted from high mass accuracy single-stage MS data, searched against theoretical PTM-carrying peptide masses, and matching features are subjected to targeted data acquisition LC-MS/MS. Using trypsin digested Saccharomyces cerevisiae Npl3, in which evidence is presented for 18 methylarginine sites-17 of which fall within a glycine-arginine-rich (GAR) domain spanning <120 amino acids-it is shown that this approach outperforms conventional data dependent acquisition (DDA): when applied to a complex protein mixture featuring in vivo methylated Npl3, 95% more (P=0.030) methylarginine-carrying peptides are selected for MS/MS than DDA, leading to an 86% increase (P=0.044) in the number of methylated peptides producing Mascot ion scores ≥20 following electron-transfer dissociation (ETD). Notably, significantly more low abundance arginine methylated peptides (maximum ion intensities <6×10(4) cps) are selected for MS/MS using this approach relative to DDA (50% more in a digest of purified in vitro methylated Npl3). It is also demonstrated that relative to collision-induced dissociation (CID), ETD facilitates a 586% increase (P=0.016) in average Mascot ion scores of methylarginine-carrying peptides. The present PTM-specific targeted data acquisition approach, though described using methylarginine, is applicable to any ionizable PTM of known mass. 相似文献
175.
Ezio Rizzardo Ming Chen Bill Chong Graeme Moad Melissa Skidmore San H. Thang 《Macromolecular Symposia》2007,248(1):104-116
SUMMARY: Factors affecting the choice of RAFT agent [RSC(Z) = S] for a given polymerization are discussed. For polymerization of methyl methacrylate (MMA), tertiary cyanoalkyl trithiocarbonates provide very good control over molecular weight and distribution and polymerizations show little retardation. The secondary trithiocarbonate RAFT agents with R = CHPh(CN) also gives good control but an inhibition period attributed to slow reinitiation is manifest. Radical induced reduction with hypophosphite salts provides a clean and convenient process for removal of thiocarbonylthio end groups of RAFT-synthesized polymers. Two methods providing simultaneous control over stereochemistry and molecular weight distribution of chains formed by radical polymerization are reported. Polymerization of MMA in the presence of scandium triflate provides a more isotactic PMMA. A similar RAFT polymerization with trithiocarbonate RAFT agents also provides control and avoids issues of RAFT agent instability seen with dithiobenzoate RAFT agents in the presence of Lewis acids. RAFT polymerization of tetramethylammonium methacrylate at 45 °C provides a more syndiotactic PMMA of controlled molecular weight and distribution (after methylation; mm:mr:rr 2:21:77 compared to 3:35:62 when formed by bulk polymerization of MMA). 相似文献
176.
Lee J. Silverberg Carlos Pacheco Debashish Sahu Peter Scholl Hany F. Sobhi Joshua T. Bachert Kaitlyn Bandholz Ryan V. Bendinsky Heather G. Bradley Baylee K. Colburn David J. Coyle Jonathon R. Dahl Megan Felty Ryan F. Fox Kyanna M. Gonzalez Jasra M. Islam Stacy E. Koperna Quentin J. Moyer Duncan J. Noble Melissa E. Ramirez Ziwei Yang 《Journal of heterocyclic chemistry》2020,57(4):1797-1805
A series of 11 novel 3-aryl-2-phenyl-2,3-dihydro-4H-1,3-benzothiazin-4-ones was prepared at room temperature by T3P-mediated cyclization of N-aryl-C-phenyl imines with thiosalicylic acid. This provides simple and ready access to N-aryl compounds in this family, which have been generally difficult to prepare. 相似文献
177.
Dr. Oliver R. Maguire Dr. Albert S. Y. Wong Mathieu G. Baltussen Peer van Duppen Aleksandr A. Pogodaev Prof. Dr. Wilhelm T. S. Huck 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(7):1676-1682
Current efforts to design functional molecular systems have overlooked the importance of coupling out-of-equilibrium behaviour with changes in the environment. Here, the authors use an oscillating reaction network and demonstrate that the application of environmental forcing, in the form of periodic changes in temperature and in the inflow of the concentration of one of the network components, removes the dependency of the periodicity of this network on temperature or flow rates and enforces a stable periodicity across a wide range of conditions. Coupling a system to a dynamic environment can thus be used as a simple tool to regulate the output of a network. In addition, the authors show that coupling can also induce an increase in behavioural complexity to include quasi-periodic oscillations. 相似文献
178.
Analytical and Bioanalytical Chemistry - 相似文献
179.
180.
Paul Slovic Melissa L. FinucaneEllen Peters Donald G. MacGregor 《European Journal of Operational Research》2007
This paper introduces a theoretical framework that describes the importance of affect in guiding judgments and decisions. As used here, “affect” means the specific quality of “goodness” or “badness” (i) experienced as a feeling state (with or without consciousness) and (ii) demarcating a positive or negative quality of a stimulus. Affective responses occur rapidly and automatically—note how quickly you sense the feelings associated with the stimulus word “treasure” or the word “hate”. We argue that reliance on such feelings can be characterized as “the affect heuristic”. In this paper we trace the development of the affect heuristic across a variety of research paths followed by ourselves and many others. We also discuss some of the important practical implications resulting from ways that this heuristic impacts our daily lives. 相似文献