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br Discussion Agonist and antagonist
2021-10-23
Discussion Agonist and antagonist action at the GluN1/GluN3 eukaryotic initiation factor is known to be complex [4], [10]. Recombinant GluN1/GluN3 receptors produce only small excitatory currents in response to glycine, likely because of a combination of activation via GluN3 and desensitization
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Active compounds and were further tested and EC and pEC
2021-10-23
Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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Although EAAT may not be
2021-10-23
Although EAAT3 may not be involved in the induction of morphine-induced CPP, our results suggest that other EAATs may play a role in the behavior because riluzole, an EAAT activator (Frizzo et al., 2004, Fumagalli et al., 2008), abolished morphine-induced CPP. Consistent with this suggestion, a few
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VKGILS-NH2 In this study we have investigated
2021-10-23
In this study, we have investigated the expression of FXR and TGR5 in CCA tissues in two independent cohorts of patients and determined their association with tumor clinicopathological parameters. The expression of both BA receptors was also evaluated in CCA human cells and normal human cholangiocyt
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In addition to the regulation
2021-10-22
In addition to the regulation afforded by calcineurin/NFAT axis, it has been shown that deregulation of some microRNAs (e.g. miR-155) can induce activation of Fas/FasL-in various cell types [72]. Furthermore, Fas–FasL interactions appear to be an important mechanism for the maintenance of immune pri
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br Acknowledgments I thank Takeshi
2021-10-22
Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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Integrase inhibitors have been licensed for use in
2021-10-22
Integrase inhibitors have been licensed for use in the UK since 2008. BHIVA now recommend starting all treatment naïve patients on a regimen containing two NRTIs, plus one of the following: a ritonavir boosted PI, an NNRTI, or an integrase inhibitor. They make further recommendations for patients wi
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We demonstrated that bilirubin the product
2021-10-22
We demonstrated that bilirubin, the product of heme metabolism by HO-1, exerted a potent suppression of NADPH oxidase activity (Fig. 2B). Different from the down-regulation of NADPH oxidase subunit by HO-1 induction in macrophages [24], the protein levels of the NADPH oxidase subunits in vascular en
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L-Carnitine inner salt For the SAR study human haspin kinase
2021-10-22
For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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Sepsis was defined as a systemic inflammatory response
2021-10-22
Sepsis was defined as a systemic inflammatory response syndrome (SIRS) associated with severe infection in 1992 [9]. However, in the Third International Consensus Definitions for Sepsis and Septic Shock [10], it was redefined as life-threatening organ dysfunction provoked by a dysregulated host resp
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br Acknowledgements br Introduction Protein translation dema
2021-10-22
Acknowledgements Introduction Protein translation demands high fidelity. There are number of molecular checkpoints to fulfill this demand. Among these, insuring that a particular tRNA gets aminoacylated by its conjugate amino acid, which in turn is catalyzed by a particular aminoacyl-tRNA synt
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br Discussion In the present study
2021-10-22
Discussion In the present study, we have demonstrated the effect of a high-fat diet upon wild-type and glut3 pregestational female phenotype and shown that it leads to obesity due to an increase in white adipose tissue contributing to the overall fat mass. Despite this observed obesity along with
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A number of GCK activators for treating T D
2021-10-22
A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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Given the actions of GIP analogues
2021-10-22
Given the actions of GIP analogues administered as a single dose to ob/ob mice, studies were performed to assess their ability to act in vivo as antagonists of GIP-induced insulinotropic and antihyperglycaemic actions. (Ala3)GIP, (Phe3)GIP, (Tyr3)GIP and (Pro3)GIP all counteracted the glucose-loweri
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Recently several studies addressed cytological and biochemic
2021-10-22
Recently, several studies addressed cytological and biochemical features of oocyte aging. It was reported that cytological changes associated with the mammalian post-ovulatory oocyte aging include chromatin disorganization, abnormal meiotic spindle location or its disruption, partial exocytosis of c
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