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MCC950 sodium Some studies using RNAi have recently been inv
2021-10-12
Some studies using RNAi have recently been invalidated by CRISPR/Cas9 [25] due to significant off-target effects of RNAi [26]. In this study, we have used both RNAi and CRISPR/Cas9 techniques and have observed consistent and similar phenotypes thus; knockdown or knockout of PATZ1 resulted in reducti
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The mechanism study demonstrated that BDNF
2021-10-12
The mechanism study demonstrated that BDNF is one of the fundamental mechanisms underlying JMJD2A effects during neuropathic pain. BDNF is a neurotrophin with essential functions in neuronal development and neuroplasticity. Accumulating evidence suggests that alterations in BDNF expression levels un
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In various models histamine has been shown to induce
2021-10-12
In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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There were hub genes identified
2021-10-12
There were 11 hub genes identified by WGCNA among which KIBRA was the hub gene of the black module. The bioinformatics method is an effective and powerful tool to analyze mRNA Melittin profiles and the related pathways. For instance, the lung cancer risk modules that were closely related to lung can
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In addition to lifestyle factors genetic factors may
2021-10-12
In addition to lifestyle factors, genetic factors may also influence the efficacy of antineoplastic drugs in breast cancer patients.16, 17 The HER2 gene contains several single nucleotide polymorphisms (SNPs). Two of the most investigated HER2 SNPs are Ile655Val (rs1136201) and Ala1170Pro (rs1058808
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To date several studies have suggested
2021-10-12
To date, several studies have suggested that serum HER2 could be used as a biomarker for monitoring the disease course and the patient's response to therapy [110], [111]. However, the clinical usefulness of serum HER2 has not been fully validated because of conflicting data [31]. The enzyme-linked i
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Fatty acids have been repeatedly shown
2021-10-12
Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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Limitations of our study are the following
2021-10-12
Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we
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The in vivo biological activity of the four novel
2021-10-11
The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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Extending time action is another strategy to increase in
2021-10-11
Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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Arena Pharmaceutical introduced a biaryl sulfone derivative
2021-10-11
Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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Histamine functions as a key neurotransmitter
2021-10-11
Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, histamine is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling pathway
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We recently reported that the human derived PancCa
2021-10-11
We recently reported that the human-derived PancCa cell line PANC-1 and the human-derived hepatocellular HepG2 cell line express GPR55 mRNA and protein [21]. In PANC-1 and HepG2 cells, knockdown of GPR55 with specific siRNAs abrogates cellular uptake of Tocrifluor 1117, a selective GPR55 ligand [21]
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For some agonists these stable GPR responses
2021-10-11
For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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The neuronal glycine receptor HSOR allopregnanolone pathway
2021-10-11
The neuronal glycine receptor/3α-HSOR/allopregnanolone pathway may also be extended to the central nervous effects of gelsemine and koumine in brain. 3α-HSOR is expressed in certain brain regions in rats and humans, such as the limbic system including hypothalamus, hippocampus and amygdala, in addit
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