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It has been shown that GPR receptors coupled
2021-12-21
It has been shown that GPR55 receptors coupled to G12/13 proteins down-regulate reactive oxygen species (ROS) production and degranulation in human neutrophils [9]. MCs degranulation stimulated by IgE/Ag also requires the generation of ROS [64]; therefore, the possibility to explore the inhibitory a
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br Glucocorticoid receptor and metabolic syndrome GCs acting
2021-12-21
Glucocorticoid receptor and metabolic syndrome GCs acting through the GR regulate key enzymes of glucose metabolism in the liver, skeletal muscle, adipose tissue and the pancreas. In the liver, GCs regulate the expression of major gluconeogenic enzymes such as phosphoenolpyruvate carboxykinase, g
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FXR agonists represent an attractive class of drugs
2021-12-21
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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Ro 3306 br Materials and methods br Acknowledgments We are
2021-12-21
Materials and methods Acknowledgments We are grateful for financial support from the National Natural Science Foundation of China (Grants No. 81661148046 and 81773762, China) and the “Personalized Medicines—Molecular Signature-based Drug Discovery and Development”, Strategic Priority Research
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br Discussion The initial reduction
2021-12-21
Discussion The initial reduction and the subsequent increase in permeability proposes a regulatory process to control bleeding. However, following repeated injury, or during long-term presence of the inflammatory stimuli, these mechanisms may become defective and even detrimental. The expression
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DZNep is a PRC inhibitor that inhibits S adenosylhomocystein
2021-12-20
DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a
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Similar to Rac Cdc and
2021-12-20
Similar to Rac1, Cdc42, and RhoA, expression of Rnd3 is also increased under hypoxic conditions, involving Hif1α mediated transcriptional activity. Here, downregulation of Rnd3 abolishes hypoxia-induced cell migration via a mechanism involving the chemokine receptor C-X-C motif chemokine receptor 4
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DNA methylation is a kind of epigenetic
2021-12-20
DNA methylation is a kind of epigenetic modifications that can be described as a heritable alteration in gene expression, without any changes in the DNA sequence. Recent evidences suggest that the regulation of DNA methylation status is a frequent and early event in prostate carcinogenesis. For exam
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br Materials and methods br Results
2021-12-20
Materials and methods Results Discussion Although there is general agreement that GPR109A has anti-lipolytic activity and that the NEFA reduction in response to nicotinic INCB-024360 sale is mediated by GPR109A, whether GPR109A activation has any impact on plasma TG levels is unclear. Since
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The lactam compounds including ceftriaxone CEF have shown to
2021-12-20
The β-lactam compounds, including ceftriaxone (CEF), have shown to attenuate drug-seeking in several drugs of abuse including methamphetamine [31], cocaine [32,33], nicotine [34] and morphine [35]. Moreover, in our laboratory, we have shown that CEF can reduce chronic alcohol drinking via upregulati
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In this study we intended to explore the
2021-12-20
In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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Macrocycle was synthesized as described in Under SAr conditi
2021-12-20
Macrocycle was synthesized as described in , . Under SAr conditions, 2-chloronicotinonitrile was heated with -butyl 5-aminopentanoate in refluxing ethanol (). The resulting aminopyridine was treated with mesyl chloride and the nitrile was subsequently reduced to afford amine . Chloroaminopyrimidin
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Importantly both genetic deletion and pharmacological inhibi
2021-12-20
Importantly, both genetic deletion and pharmacological inhibition of FAAH also reduced NTG-induced neuronal hyperactivity in the trigeminal nucleus, which receives sensory input from craniofacial deep tissues. NTG is known to evoke the robust neuronal activation, as evidenced by the induction of the
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The current study aimed to understand the roles and the
2021-12-20
The current study aimed to understand the roles and the underlying mechanisms of XIST in LSCC, by focusing on the regulation by miR-124-3p, which was previously identified as a target of XIST [12]. We found that the XIST expression is positively correlated with the stages of LSCC in patients. Knockd
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Obesity is one of the worldwide concerns
2021-12-20
Obesity is one of the worldwide concerns, with high prevalence and adverse effects on human health and life expectancy. According to the World Health Organization (WHO), obesity is defined as abnormal or excessive fat accumulation in the body with body mass index (BMI) of 30 or more. Obesity increa
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