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Growing evidence supporting the anti inflammatory and
2022-02-09
Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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The precise mechanism by which erastin inhibits SLC
2022-02-09
The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A
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α-Cyperone Consistently with the above discoveries
2022-02-09
Consistently with the above discoveries, it has been also shown that in cardiomyocytes with shRNA-down-regulated FBP2, mitochondria are more susceptible to depolarisation (Gizak et al., 2012a) and H2O2-induced oxidative stress (Wiśniewski et al., 2017). In α-Cyperone overexpressing FBP2 (cardiomyoc
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PRT-060318 The current study identified the presence and
2022-02-09
The current study identified the presence and location of all four histamine receptors in the GI tract of 6 healthy adult dogs. Although no clinical signs of GI disease were noted, mild inflammation was noted in at least one section of the GI tract in all dogs based on WSAVA guidelines. Interpretati
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Nazar and colleagues reported a normal HER gene number
2022-02-09
Nazar and colleagues reported a normal HER2 gene number in 13 primary and 2 recurrent ethmoid sinus adenocarcinomas, without any histological and immunohistochemical characterization, so a comparison with the present findings is impossible [14]. More recently, 552 head and neck carcinomas have been
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An isoflavone type secondary metabolite Glabrescione B GlaB
2022-02-09
An isoflavone type secondary metabolite, Glabrescione B (GlaB), from Derris glabrescens (Benth.) J.F. Macbr. from the family Fabaceae, was found to possess the capacity to bind the Gli1 zinc finger domain and to further block DNA binding capacity [118]. Pyrvinium, an anthelmintic drug approved by th
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Considering that TGF plays a pivotal role in inflammation re
2022-02-09
Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG
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Recently some published studies showed
2022-02-09
Recently, some published studies showed that HBV can induce autophagy in vitro and vivo [[19], [20], [21]]. The critical role of autophagy in HBV normal life cycle, such as HBV envelopment, has been gradually accepted by researchers from different laboratories [22,23]. HBV can trigger the autophagic
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Initial structural and biochemical work showed
2022-02-09
Initial structural and biochemical work showed that Get3 forms an obligate dimer whose conformation is regulated by the bound nucleotide. Analogous to SRP and SR, Get3 contains a P-loop nucleotide hydrolase domain in which the bound ATPs face one another at the dimer interface (Figure 3A, top right
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GW was also the starting point for a study
2022-02-09
GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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184 3 In summary activated A AR exacerbated the reverse
2022-02-08
In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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Yeast two hybrid screening studies have
2022-02-08
Yeast two-hybrid screening studies have provided the foundation for countless investigations of protein-protein interactions [[141], [142], [143]]. To identify additional hepatic proteins similar to GKRP that are implicated in GCK regulation, a group of researchers conducted a two-hybrid study using
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Of note the intracellular egg compartment exhibiting SA gal
2022-02-08
Of note, the intracellular egg compartment exhibiting SA-β-gal activity also exhibits lipofuscin auto-fluorescence (Fig. 6B), and it is co-stained with the lipid-specific dye SBB (Supplemental Fig. 5). On the one hand, these findings reflect the fact that the pool of yolk protein contains lipoprotei
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To ensure the induction of
2022-02-08
To ensure the induction of CYP enzymes by several inducers, specific monooxygenase activities of variously induced, uninduced and pooled liver microsomes were compared (Fig. 3). Although 3-MC, phenobarbital, acetone, and dexamethasone could induce CYP1A-, CYP2B-, CYP2E1-, and CYP3A-selective enzyme
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Because AM had limited efficacy on rodent
2022-02-08
Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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