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Starting from the hypothesis that the linker portion of
2021-10-18
Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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Preadipocytes are capable of differentiating into lipid lade
2021-10-18
Preadipocytes are capable of differentiating into lipid-laden mature adipocytes. Lipid droplets are a prominent morphological feature of mature adipocytes, which is accumulated and maintained during adipocytes differentiation [26]. In this study, rHhip treatment increased lipid accumulation, as well
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Mathematical models play an important role in understanding
2021-10-18
Mathematical models play an important role in understanding and predicting the dynamic process of HBV infection. In the 1990s, Nowak et al. proposed a basic model to analyze the effect of antiviral treatment on reducing viral loads (Nowak et al., 1996). Since then, many different mathematical models
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All experiments in this study were performed
2021-10-18
All experiments in this study were performed at pD 6.1 for reasons described above. This leaves a question about the implications of stereochemistry in vivo. At physiological pH the GSTP1-1 catalyzed rate of EASG formation is only 1.1-fold higher than the non-enzymatic rate [26]. However, when human
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The inhibition of NSAIDs towards
2021-10-18
The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it benfotiamine and GLOI were probed by NMR titration experiments, no detailed inhibitory m
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Overall ABC transporters are hypothesised to prevent
2021-10-18
Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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The eradication of agonist activity in compound was also
2021-10-18
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary monobenzone sale as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antag
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In summary the SAR of a series
2021-10-18
In summary, the SAR of a series of phenylpropanoic acid-free fatty sennoside receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust efficac
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br Materials and methods br Results br Discussion Induction
2021-10-16
Materials and methods Results Discussion Induction of neuronal cell death is the main neurotoxic mechanism of arsenite (Vahidnia et al., 2007). Previous studies have demonstrated that arsenite may trigger neuronal cell death via apoptosis, autophagy as well as necrosis (Yen et al., 2012; La
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In NAFLD models the first hit is liver
2021-10-16
In NAFLD models, the “first hit” is liver fat accumulation, which causes insulin resistance, whereas the interplay of inflammatory cytokines, which causes inflammation, acts as the representative “second hit” [9]. However, recently, the “multiple hit” hypothesis has taken into consideration that mul
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br Experimental br Acknowledgments br Human immunodeficiency
2021-10-16
Experimental Acknowledgments Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS), and without treatment results in a debilitating disease that cripples the immune system of the patient, increasing susceptibility to opportunistic disease
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Introduction Epigenetic alterations play an
2021-10-16
Introduction Epigenetic alterations play an important role in carcinogenesis. Aberrant promoter CpG island hypermethylation causes transcriptional gene silencing [1], and has been documented for a number of genes in prostate cancer (PCA) [2]. Histone modifications are also important regulators of t
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br Materials and Methods br Results
2021-10-16
Materials and Methods Results All of the studied transporter genes were expressed at detectable levels in all the analyzed samples at mRNA level by means of applied rt-PCR method (CT25 sta receptor was observed for ABCC4, ABCC1, ABCG2, SLC22A3, and SLC22A18 (less than 10% of mean expression f
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Cy5 maleimide (non-sulfonated) The discovery that GLUT in th
2021-10-16
The discovery that GLUT1 in the microvasculature represents an important target of VEGF thereby affecting Cy5 maleimide (non-sulfonated) function is highly relevant. The work of Jais et al. identified VEGF as a determining player in the regulation of cognitive performance and provides an important
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GLI proteins activate or repress
2021-10-16
GLI proteins activate or repress transcription of their target genes by binding to a similar sequence motif within a cis-regulatory module (CRM) (Hallikas and Taipale, 2006, Peterson et al., 2012). Transcriptional responses to the HH pathway can be elicited either by de-repression of GLI-R or in oth
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