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Prenylation may turn a flavonoid from an agonist to
2020-10-30
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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br O GlcNAcase Human OGA is a multidomain
2020-10-30
O-GlcNAcase Human OGA is a multidomain protein with an N-terminal domain similar to glycoside hydrolase family 84 (GH84) enzymes, a stalk domain, a C-terminal pseudo histone acetyltransferase (HAT) domain, and several low-complexity regions (Figure 1f) [43]. A splice variant that lacks the HAT do
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Dual inhibition of ACE and NEP as a
2020-10-30
Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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In addition PK studies on indicate
2020-10-29
In addition, PK studies on indicate that it displays excellent bioavailability, pharmacological and toxicological parameters., A concern was initially raised about compound that it may cause EPAC denaturing properties and false positives. To address this issue, Cheng and co-workers have conducted
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Introduction Cognitive impairment is a core
2020-10-29
Introduction Cognitive impairment is a core, stable feature of schizophrenia that limits patient functioning and well-being (Keefe and Harvey, 2012) and associates with poor functional outcome (Fervaha et al., 2014, Kontaxaki et al., 2014). Studies also indicate that cognitive deficits occur prior
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Although the implication of DA and glutamate signaling
2020-10-29
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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Once sufficient single stranded DNA
2020-10-29
Once sufficient single-stranded DNA (ssDNA) has been exposed at origins, synthesis of leading and lagging strands is initiated by the DNA polymerase α-primase complex (Pol α). Lagging-strand synthesis requires repeated cycles of Pol α-dependent priming and subsequent primer extension by Pol δ. Pol α
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Recently naphthoquinone derivatives have shown promising res
2020-10-29
Recently, naphthoquinone derivatives have shown promising results as antiparasitic lead compounds [28]. Conjugated hybrid compounds could be an effective path to discovery of new drugs by associating two different pharmacophore groups with different mechanisms of action in a single molecule [29,30],
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br Materials and methods br Results br Discussion In
2020-10-29
Materials and methods Results Discussion In general, CI symptoms are often visible only after the chilled products have been removed from coolstore to a warmer temperature (Schirra and Cohen, 1999). However, in the present work, \'satsuma’ mandarin fruit stored at 2°C showed chilling sympto
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br Endothelial mechanotransduction br Apoptosis br Death
2020-10-29
Endothelial mechanotransduction Apoptosis Death associated protein kinase Conclusion DAPK is localized to the indy 6 sale network, and promotes actomyosin contractility. DAPK stabilizes stress fibers by phosphorylation of MLC (Bialik et al., 2004, Kuo et al., 2003). In endothelial cells
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CGS 21680 HCl Apart from neutrophil mediated inflammation th
2020-10-29
Apart from neutrophil-mediated inflammation, the production of pro-inflammatory cytokines and chemokines from PGD2/CRTH2 activated macrophages could further aggravate LPS-induced lung injury (Eguchi et al., 2011; Jandl et al., 2016). Interestingly, genetic ablation of CRTH2 diminishes the TNF-α prod
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Although in vitro and in vivo immunosuppressive effects of f
2020-10-29
Although, in vitro and in vivo immunosuppressive effects of female steroids have been described in fish (Yamaguchi et al., 2001, Law et al., 2001), their mode of action was not evaluated in detail. Consequently, it is of considerable interest to investigate the intracellular pathways that regulate t
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These findings further extend our knowledge of how P and
2020-10-29
These findings further extend our knowledge of how P4 and/or E2 can mediate anxiety and fear responses. Female rats in behavioral estrous and ovx rats administered systemic P4 and/or E2 demonstrated significantly less anxiety in the open field and/or elevated plus maze, compared to diestrous rats, a
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br Expression data suggest involvement of additional TRIMs
2020-10-29
Expression data suggest involvement of additional TRIMs in heart function Given the complexity of the cardiac function, involved molecular pathways and processes, and the fact that only a few of the TRIMs have thus far been shown to have a cardiac role, we hypothesized that there would be more TR
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aminoisobutyric acid BAIBA is a natural
2020-10-29
β-aminoisobutyric T7 High Yield Fluorescein RNA (BAIBA) is a natural catabolite of the branched-chain amino acid thymine. BAIBA was recently found to reduce inflammation in skeletal muscle via the AMP-activated protein kinase (AMPK)-peroxisome proliferator-activated receptor (PPAR)δ signaling pathw
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