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The authors identified inhibitors of SUMOylation using two
2019-12-13
The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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br Anti inflammatory effects of MTX
2019-12-13
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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Some studies have been conducted
2019-12-13
Some studies have been conducted on the activities of CYP450 [[28], [29], [30], [31]]. For example, Chen et al. reported that low-dose aspirin induced the in vivo activity of CYP2C19 in healthy subjects [30], Krasniqi et al. reported that CYP2C8*3 and CYP2C9*2*3 variants correlated with ibuprofen-in
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br Genomic actions in the breast br
2019-12-13
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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br Materials and methods br Results and
2019-12-13
Materials and methods Results and discussion Summary Acknowledgments We thank Muhammad Anwar for animal rearing and surgery. We also thank Michael M. Myers for editing. Finally, we thank David Hirschberg for his technical advice. Funding for this project was provided by the Einhorn Famil
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UMI-77 synthesis According to our results germination of tra
2019-12-13
According to our results, germination of transgene dgks lines didn’t differ under optimal conditions and 50 mM NaCl, while 100 mM NaCl slightly affected germination rates of dgk mutants. Exogenous application of EBL even diminished the effect of 100 mM NaCl on dgk mutants. The critical effect on ger
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We also determined the uracil content of CJ DNA
2019-12-13
We also determined the uracil content of CJ236 DNA by thin-layer chromatography of in vivo32P- or [6-3H]uracil-labeled CJ236 2′-deoxyribose 5′-monophosphates as well as by LC/MS of deoxyuridine and thymidine 2′-deoxynucleosides (Table 1, Table 2, Table 3). Examination of the 32P data showed that, ba
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Midazolam oral clearance is used for characterization of bot
2019-12-13
Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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Although PGD was initially considered
2019-12-13
Although PGD was initially considered to elicit its biological actions through a classical PGD receptor (DP1), later findings suggested that several PGD-mediated actions of eosinophils arise via DP2,, which is also known as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells).
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Beside the previously reported Topo I inhibition time and co
2019-12-13
Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Cell swelling stimulates the release of certain amino
2019-12-13
Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino indy 6 taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-activated taur
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br Transparency document br Main
2019-12-12
Transparency document Main Text The centrosome is a non-membrane-bound organelle found in most animal cells. It has several important functions, including control of cilia formation, microtubule organization and nucleation, spindle assembly and transport of organelles and vesicles. Centrosomes
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We then evaluated in vivo DHODH mRNA expression using data
2019-12-12
We then evaluated in vivo DHODH mRNA VE-822 using data from TCGA (Lee, Palm, Grimes, & Ji, 2015). To perform a pan-disease comparison of DHODH expression, log2 TPM expression values were converted to z-scores calculated per patient. Fig. 6 shows that across all 34 diseases (9726 unique patient sampl
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br Introduction br Sphingolipid metabolism Sphingolipids are
2019-12-12
Introduction Sphingolipid metabolism Sphingolipids, are fundamental constituents of all eukaryotic membranes and their metabolism is carried out by a broad array of anabolic and dibromide with ceramide as their hub (for a review, (Hannun and Obeid, 2018)). Ceramide can be formed by multiple p
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DDR plays a crucial role in
2019-12-12
DDR2 plays a crucial role in regulating a wide variety of fundamental cellular processes, including cell proliferation, differentiation, and adhesion [17], [28], [29], [30]. The authors revealed compromised cell migration in DDR2-silenced fibroblasts exposed to Ang II, most likely due to the loss of
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