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Natural progestogens play an important role in the stimulati
2020-04-10
Natural progestogens play an important role in the stimulation of oocyte growth and maturation as well as in spermatogenesis and sperm maturation, and they act as sex pheromones in teleost fish (Kime, 1990, Kobayashi et al., 2002, Nagahama and Yamashita, 2008, Scott et al., 2010). A complex series o
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br Genomic actions in the breast
2020-04-10
Genomic actions in the breast Conclusion Clinical studies suggest that progesterone and/or progestins may play a decisive role in the development of breast cancer in women using hormone therapy or oral contraceptives [3], [4]. However, this data are controversial to most experimental investiga
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Grapiprant is a selective antagonist for prostaglandin E PGE
2020-04-10
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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p Kip is a critical
2020-04-09
p27Kip1 is a critical component of the cell cycle machinery [15]. As an inhibitor of cyclin E-Cdk2, p27Kip1 plays a pivotal role in controlling cell proliferation, S-phase entry, and G1-phase exit during development and tumorigenesis [16]. p27Kip1 is predominantly regulated via posttranslational mod
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tranylcypromine Increasing age among middle aged subjects ye
2020-04-09
Increasing age among middle-aged subjects (30–59years old) was associated with higher levels of cholesterol synthesis markers (although without statistical significance) and also of cholesterol tranylcypromine markers (with statistical significance for campesterol and sitosterol); this finding is c
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Reports on the participation of NDH
2020-04-09
Reports on the participation of NDH2 along with other respiratory complexes in the formation of a large supercomplex (Grandier-Vazeille et al. 2001) or even a respirosome-like structure in S. cerevisiae mitochondria (Matus-Ortega et al. 2015) are very intriguing. Similarly, in Y. lypolytica mitochon
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In this study we reported that over expressed endogenous cen
2020-04-09
In this study, we reported that over-expressed endogenous central ET-1 exerted anti-allodynic and anti-hyperalgesic effects on SNL-induced NP for the first time. Furthermore, we showed that ETA-R mRNA acetylcholinesterase inhibitor together with the level of ET-1 was increased in the CNS up to 21da
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While previously reported optimizations on compound focused
2020-04-09
While previously reported optimizations on T7 High Yield Cy3 RNA focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to e
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By stratifying EOC cell lines
2020-04-09
By stratifying EOC cell lines according to their EMT stages, we observed a significant higher expression of DDR1 in the epithelial-like cell lines compared to low or undetectable DDR1 in mesenchymal-like cell lines. Similar trend was observed in the tumour samples, with the lowest expression of DDR1
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br Introduction Analyses of genomic alterations in cancer
2020-04-09
Introduction Analyses of genomic alterations in cancer have identified epidermal growth factor receptor (EGFR) as one of the most potent “oncogenic driver” kinases that is present in many epithelial tumors including endometrial, breast, prostate, skin, esophagus, lung, stomach, colorectal, and re
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The effect of transformation of the linker Y
2020-04-09
The effect of transformation of the linker Y between the carboxylic AZD8931 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 activity
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In conclusion we designed novel E inhibitors based
2020-04-09
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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br Conclusion In this study we investigated functional
2020-04-09
Conclusion In this study, we investigated functional alterations of ECs following exposure to mechanical and/or physicochemical stimuli. Specifically, hypoxia induced phosphorylation with significant increases after 30 min and the maximum increase was after 180 min. Our data show that a combinati
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br Experimental Procedures br Acknowledgments
2020-04-09
Experimental Procedures Acknowledgments We thank S. Tangye and A. Swarbrick for helpful discussions and critical reading of the manuscript; K. Wood, T. Camidge, and V. Turner for technical assistance; C. Brownlee for cell sorting; the staff of the Garvan Institute Biological Testing Facility f
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A possible explanation for these observations has been provi
2020-04-08
A possible explanation for these observations has been provided by a recent study showing that EWS-FLI-1 increases the Skp2-mediated 26S proteasome degradation, decreasing p27 protein stability and preventing cell senescence [42]. Mechanism of action of EWS-FLI-1 Molecular analysis has revealed
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