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Several research groups have disclosed potent
2020-05-11
Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2
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Introduction The term myeloproliferative disorders was first
2020-05-11
Introduction The term “myeloproliferative disorders” was first proposed by William Dameshek in 1951. With the discovery of the Philadelphia chromosome, myeloproliferative disorders were classified into two groups: BCR-ABL positive chronic myeloid leukemia (CML) and BCR-ABL negative chronic myelopro
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Cell lines which possess microglial or neuronal
2020-05-11
Cell lines which possess microglial or neuronal properties are uncomplicated and convenient in vitro models for studying dihydrofolate reductase injury at the cellular and molecular levels. Microglial BV-2 cells are derived from the immortalized mouse microglia and exhibit many of the morphological
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These evidence prompted us to investigate the effectiveness
2020-05-11
These evidence prompted us to investigate the effectiveness of CT-133, a newly discovered, well-tolerated, selective and potent CRTH2 antagonist, as a treatment of ALI. CT-133 has shown a potential response in treating chronic obstructive pulmonary disease (COPD), allergic rhinitis and EZLink Sulfo-
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Bovine collagen type II a
2020-05-11
Bovine collagen type II, a fibrillar collagen mainly found in cartilage, comprises 24 potentially glycosylated lysine residues within its collagen domain. Detailed analysis revealed that 22 out of 23 of these lysine residues are hydroxylated and carry variable numbers of Gal(β1-O) and Glc(α1-2)Gal(β
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In modern science and technology
2020-05-11
In modern science and technology, many optimization problems need to be solved in real time, while these classical methods cannot render real-time solutions to these optimization problems, especially large-scale problems. As a new metaheuristic, particle swarm optimization (PSO) [18], [19] has prove
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Interestingly selective ETA blockade increased cutaneous blo
2020-05-11
Interestingly, selective ETA blockade increased cutaneous blood flow as measured by laser Doppler fluxmetry. This is a measure of total blood flow in the different vessels in the skin including venules, ap-1 transcription factor as well as arterioles. This finding is in accordance with the previous
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Compound was prepared from chloroindole by acylation to give
2020-05-11
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole CH 223191 derivative (). Derivatives and were prepar
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The effect of transformation of the
2020-05-11
The effect of transformation of the linker Y between the carboxylic Procainamide HCl residue and the phenyl moiety of 2b was also investigated, and is illustrated in Table 5. Analogs 2b, 16, and 17, possessing conformationally restricted carboxylic acid residues, tended to show stronger antagonist
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The Ewing sarcoma breakpoint region
2020-05-09
The Ewing sarcoma breakpoint region 1 gene (EWSR1) is a partner in a large, diverse range of mesenchymal (and some nonmesenchymal) tumors (Tables 1 and 2). As the 5′ partner, EWSR1 is able to fuse with an array of genes. These fusions can generate genetically different but phenotypically identical n
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br RING type E s and their substrates There
2020-05-09
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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MicroRNA miRNA is a class
2020-05-09
MicroRNA (miRNA) is a class of highly conserved, non-coding small molecules containing 19–25 nucleotides. miRNAs are involved in the regulation of genes associated with cancer development and progression and therefore can act as oncogenes, by contributing to tumor formation,17, 18 or as tumor suppre
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br Materials and methods br Results br Discussion PYR
2020-05-09
Materials and methods Results Discussion PYR-41 inhibits UBE1 activity that catalyses an initial step in the ubiquitination reaction. In the present study, we examined the role of this enzyme in sperm-egg fusion by inhibiting UBE1 enzymatic activity in eggs. Our results suggest that PYR-41
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Programmed cellular death or apoptosis is a process
2020-05-09
Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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br Materials and Methods br Acknowledgements We thank the st
2020-05-09
Materials and Methods Acknowledgements We thank the staff of beamlines ID29 and ID30A-1 of the European Synchrotron Radiation Facility. This work was supported by, the Marie Curie Career Integration Grant (PCIG13-GA-2013-630755), the Israel Science Foundation (Grant 1383/17) and the Israeli Ca
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