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The subcellular redistribution of some metabolic enzymes is
2021-10-29
The subcellular redistribution of some metabolic enzymes is dynamic and responsive to metabolic conditions. In the absence of glucose, Glucokinase (GK) is bound to its regulatory protein in the nucleus of the hepatocyte and translocates to the cytoplasm when sugar levels increase [12]. Muscle glycog
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Two classes of histones demethylases have thus far been iden
2021-10-29
Two classes of histones demethylases have thus far been identified: the Jumonji C (JmjC) domain-containing proteins and the amine oxidase domain (AOD)-containing proteins. They have distinct enzymatic mechanisms and substrate specificity. The JmjC domain is conserved through evolution and belongs to
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Toxoplasma gondii is an exceptionally tractable apicomplexan
2021-10-28
Toxoplasma gondii is an exceptionally tractable apicomplexan parasite that expresses a limited yet representative subset of apicomplexan cyclase orthologs, making it an ideal model for investigating cyclic nucleotide signaling in Apicomplexa. Of the five putative nucleotide cyclases, only TgACα1 and
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br FXR Agonists Azepinol b indole hEC nM efficacy
2021-10-28
FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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Many studies support that the increase of P improves embryon
2021-10-28
Many studies support that the increase of P4 improves embryonic survival and reduces embryonic losses in ruminants [6,[18], [19], [20]]. However, experimental results are variable, contradictory and often inconclusive results. Certain studies showed that administration of GnRH or hCG after artificia
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First class II fusion proteins are
2021-10-28
First, class II fusion proteins are known to transition from a (homo- or hetero-) pre-fusion dimer to a post-fusion trimer [57], [58], [59], [60], [61], [62] through a monomeric intermediate [63], [64], and a crystalline structure of a monomer of Rift Valley fever virus (a phlebovirus, member of the
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br Introduction Most organisms require glucose as a
2021-10-28
Introduction Most organisms require glucose as a key metabolite, and it is critical that mammalian cells regulate glucose levels properly to maintain bioenergetic homeostasis. The major transporters responsible for the uptake of glucose from systemic circulation into cells are the GLUTs, members
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br Conflict of interest br Acknowledgements
2021-10-28
Conflict of interest Acknowledgements Introduction Second generation antipsychotic drugs (SGAs) such as olanzapine are widely used in treating individuals with schizophrenia and bi-polar disorder and are increasingly prescribed for other conditions such as anxiety (Pringsheim and Gardner, 2
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Among sensitizers tested in the previous study six test chem
2021-10-28
Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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corticotropin releasing factor In the intestine ethanol expo
2021-10-28
In the intestine, ethanol exposure can change the composition of gut microbiota and promotes the growth of intestinal gram-negative bacteria, which results in the accumulation of endotoxins such as, LPS. Ethanol also impacts the integrity of the gastrointestinal mucosal barrier, increasing intestina
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Compound and several additional FPR antagonists identified h
2021-10-28
Compound 10 and several additional FPR1 antagonists identified here specifically blocked fMLF-induced responses mediated via FPR1 in FPR1-HL60 calcium ionophore and human neutrophils, but not responses mediated via FPR2 or FPR3 (in human neutrophils and transfected HL60 cells) or Fpr1 (murine neutro
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DAMPs are endogenous danger signals that can
2021-10-28
DAMPs are endogenous danger signals that can initiate and perpetuate a noninfectious Canagliflozin sale during cell death [23]. HMGB1 is a well-studied nuclear DAMP in various types of regulated necrosis and has been implicated in the pathogenesis of infection and sterile inflammation. Our current d
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The physicochemical properties of the prodrugs provided impo
2021-10-28
The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala
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Phosphorylation of the p Rel A dimer
2021-10-28
Phosphorylation of the p50-Rel A dimer, the most common form of NF-κB, leads to ubiquitination of IκB proteins (Fig. 2). Poly-ubiquitination of IκB proteins identifies them for rapid degradation by 26S proteasomes, thereby allowing NF-κB dimers to undergo nuclear translocation and activate the trans
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br Conclusions and perspectives br Acknowledgements This wor
2021-10-28
Conclusions and perspectives Acknowledgements This work was supported by the National Natural Science Foundation of China (Grant Nos. 21802173, 21405182 and 21773315), the Natural Science Foundation of Guangdong Province (Grant Nos. 2018A030310301, 201710010019 and 2014A030313232, 201804020025
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