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Next our exploration shifted to modifications at the lateral
2021-02-07
Next, our exploration shifted to modifications at the lateral chain of the benzoquinone nucleus (SAR 2). Considering that the CK2 inhibitory activity is favoured by the presence of the -Ph-4-NO2 (SAR 1), the subsequent analogues were investigated with this moiety retained. The influence of the side
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cytochalasin d br Conclusions br Statement of authorship br
2021-02-07
Conclusions Statement of authorship Nonaneurysmal subarachnoid hemorrhage (NA-SAH) differs from aneurysmal subarachnoid hemorrhage (SAH) in both clinical course and outcome. In spite of many reports and case series since the first description in 1985, the etiology of NA-SAH remains uncertain
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Although we observed increases in AR mediated cAMP productio
2021-02-07
Although we observed increases in α1-AR mediated cAMP production separately in the nucleus and cytoplasm, compartment specificity was observed for PKA activation. GPCRs and their effector proteins are commonly found in multiprotein signalosomes with A-kinase anchoring proteins (AKAPs) serving as sca
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br Epac in cardiovascular pathophysiology
2021-02-07
Epac in cardiovascular pathophysiology Epac orchestrates signaling actors that regulate fundamental cellular functions and general biological effects. However, some important gaps still remain in the knowledge of the physiopathological role of Epac in the heart. So far, Epac has been implicated i
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The cpm corresponding to bound substrate
2021-02-07
The cpm corresponding to bound substrate in the sample well can be expressed as the difference between the total cpm in the sample well (3Hswtotal; 14Cswtotal) and the cpm for the unbound substrate in the sample well, as illustrated by Eq. (2): By combining Eqs. (1), (2), cpm for the bound substrat
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br Materials and methods br Results br
2021-02-07
Materials and methods Results Discussion Enolase (2-phospho-D-glycerate hydrolase) is a glycolytic enzyme that is also involved with various important roles in the intracellular and extracellular space (Copley, 2003; S. Zhang et al., 2015) such as transcriptional regulation, apoptosis, grow
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A growing number of other post translational modifications
2021-02-07
A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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br Conclusion In the last year significant advances in
2021-02-07
Conclusion In the last year, significant advances in our understanding of ubiquitin transfer by IAPs and related E3 ligases have been made. The three crystal structures of the RING-bound E2~Ub show that the conjugate is bound by the RING domain in the closed conformation, where the I44-centered f
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Hedamycin isolated from Streptomyces griseoruber
2021-02-07
Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of TMN 355 (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(c)). Hed
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Ingested folate needs to be chemically modified in
2021-02-07
Ingested folate needs to be chemically modified in order to become a one carbon donor for cell metabolism. Firstly, folate turns to dihydrofolic TC-I 2000 (DHF), it is then converted into tetrahydrofolate (THF) by the dihydrofolate reductase enzyme (DHFR) and finally converted into N5, N10-methylene
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In addition we investigated if the previously
2021-02-07
In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time depend
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Among the CYP enzymes CYP D has been considered a
2021-02-07
Among the CYP450 enzymes, CYP2D has been considered a crucial protein that involves in the metabolism of xenobiotics and drugs (Zanger and Schwab, 2013). Some isoforms of the CYP2D subfamily have been well characterized, such as CYP2D6 due to its clinical importance and CYP2D14 in black cattle (Hama
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The CYP A genes are regulated physiologically by glucocortic
2021-02-07
The CYP3A genes are regulated physiologically by glucocorticosteroids, growth hormone, thyroid hormones and cytokines [13, 20, 30]. It has been shown that glucocorticoid receptor (GR), pregnane X receptor (PXR), constitutive androstane receptor (CAR) and vitamin D receptor (VDR) play an important ro
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CDK S phosphorylation status influences the differential cel
2021-02-07
CDK5-S47 phosphorylation status influences the differential cellular proliferation versus migration response: Previous work from our laboratory has shown CDK5 to be a critical determinant of the cellular proliferation-migration dichotomy whereby CDK5 activation downstream of stimulated epidermal gro
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Pattern separation is a process that takes
2021-02-05
Pattern separation is a process that takes place in the hippocampus and more specifically in the dentate gyrus (DG) and Cornu Ammonis region 3 (CA3) (Morris, Churchwell, Kesner, & Gilbert, 2012). The main source of input in the hippocampus is derived from the enthorinal cortex (EC) that mainly proje
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