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Beside the previously reported Topo I inhibition
2020-02-20
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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br APC C Uses a
2020-02-20
APC/C Uses a Dynamic Cullin–RING Mechanism to Elongate Polyubiquitin Chains Human APC/C generates Lys11-linked poly-Ub chains through an entirely different mechanism, via the distinctive E2 enzyme, UBE2S 30, 31, 32. Although APC2 and APC11 are necessary and sufficient to activate UBE2S, the mecha
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DNA replication checkpoint kinases in both yeast and human
2020-02-20
DNA replication checkpoint kinases in both yeast and human cpi 1 upregulate dNTP levels under replication stress to mediate their essential function at replication forks (Yeeles et al., 2013). It is possible that upregulation of dNTP levels under replication stress helps fork restart once replicati
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In summary in the present study we found
2020-02-20
In summary, in the present study we found that CysLT1 receptor attenuates while CysLT2 receptor facilitates OGD-induced PC12 cell death as confirmed by receptor over-expression and antagonism. However, we cannot explain why their roles are distinct and why the cell size is increased in the CysLT2 re
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Among the high value compounds derived from agricultural res
2020-02-20
Among the high value compounds derived from agricultural residues there are enzymes with industrial application. The extraction processes have been focused on the development of new strategies that guarantee high recovery rates with maximum activity (Nadar et al., 2017). The residues of these two fr
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The present study was the
2020-02-19
The present study was the first to examine how COMT genotype and estradiol are associated with proteasome inhibitor functioning in healthy postmenopausal women. We hypothesized that with decreased circulating estradiol after menopause, the COMT genotype relationship to cognition would remain and pe
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Previously published data showed an interaction of tubulin
2020-02-19
Previously published data showed an interaction of α-tubulin and CK1δ [15] that was validated in the present study using SPR (Fig. 1A). The dominant motifs involved in the CK1δ/α-tubulin interface were defined using a peptide library of peptides covering the CK1δ amino guanylyl cyclase sequence (Su
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br Materials and methods br Results br Discussion We
2020-02-19
Materials and methods Results Discussion We have evaluated the breast cancer prevention potential of PR blockade under conditions that included exposure to progestogens that are relevant to women (progesterone and MPA) and are known to differ in their receptor-binding and down-stream effect
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AZ20 br The estrogen receptors History
2020-02-19
The estrogen receptors: History and discovery In 1958, Elwood Jensen discovered the estrogen receptor, the first receptor ever encountered for any hormone, by showing that reproductive female tissues were able to uptake estrogen from the circulation by binding to proteins. He later demonstrated t
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br Substrate Specificity Discrimination and Binding Energy
2020-02-19
Substrate Specificity, Discrimination, and Binding Energy In 8380 to catalytic efficiency, which can be gauged in reference to an absolute scale of ‘catalytic perfection’ 10, 11, specificity is a relative concept because it requires comparison between given alternative substrates. In fact, speci
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In the preclinical evaluation of CRF receptor
2020-02-18
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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bupropion hydrochloride While lowering the TID exposure of e
2020-02-18
While lowering the TID exposure of electronics is fairly straightforward, there are other bupropion hydrochloride induced effects that are not as easily mitigated, especially with COTS components. Single Event Effects (SEE) occur when a high-energy particle strikes the active area of an integrated
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Although several genomic technologies including the generati
2020-02-18
Although several genomic technologies, including the generation of ERRγ-specific knockout mice, have revealed that ERRγ plays a pivotal role in cellular bioenergetics [1], its involvement in other metabolic pathways has been appreciated only recently. Therefore, we highlight recent findings on the r
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The glycolytic pathway is a catabolic
2020-02-18
The glycolytic pathway is a catabolic route that ends with the synthesis of pyruvate (Pyr). In Arabidopsis embryos, the conversion of phosphoenolpyruvate (PEP) to Pyr, catalyzed by pyruvate kinase (PK), is mainly located in the plastids [10], [11]. The preceding reaction is catalyzed by enolase (ENO
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Oxytocin The only in vivo evidence for a role of
2020-02-17
The only in vivo evidence for a role of DDR2 in fibrotic disease showed that DDR2 knockout mice exhibited exaggerated severity of chronic hepatic fibrosis. Although a previous in vitro study has demonstrated that DDR2 promotes lung fibroblast proliferation and migration, till now it remains unclear
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