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VS strategies have been building momentum in
2021-12-09
VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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TXNIP interacts with various proteins
2021-12-09
TXNIP interacts with various proteins, including NLRP3 (Yoshihara et al., 2014, Zhou et al., 2010). Emerging evidence suggests that TXNIP plays a role in ER stress-mediated cell death and in the NLRP3 inflammasome activation step (Abderrazak et al., 2015, Lerner et al., 2012, Oslowski et al., 2012,
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GPR which is also known as FFA receptor
2021-12-09
GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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H R antagonism can prevent
2021-12-09
H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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br Methods br Results br
2021-12-08
Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of
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br Clinical development of anti NASH
2021-12-08
Clinical development of anti-NASH drug therapies The current understanding of NASH pathogenesis has led to broad efforts to target several features of the disease, alone or in combination, even in the absence of liver-guided therapies. Therefore, drug development in NASH is a rapidly changing fie
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br Materials and methods br Results br Discussion In this
2021-12-08
Materials and methods Results Discussion In this study, the supF forward mutation assay showed that 5OHU induced mutations in human cells and that a C→T mutation was the predominant mutation among 5OHU-induced mutations. In addition, the DNA cleavage activity assay revealed that 5OHU was ex
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leukotriene receptor agonist To help resolve the question of
2021-12-08
To help resolve the question of simple binding versus transport, we reasoned that if quercetin is transported by GLUT1, we should be able to block its uptake by other GLUT1 inhibitors. We initially investigated the effects of two newly identified GLUT1 inhibitors, BAY-876 and WZB-117. WZB-117 was fi
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There are also data showing potential beneficial effects of
2021-12-08
There are also data showing potential beneficial effects of SGLT2i on non-alcoholic fatty liver disease (NAFLD) [[14], [15], [16], [17]], a hepatic manifestation of the metabolic syndrome that has been linked to type 2 diabetes mellitus (T2DM) development and increased cardiovascular (CV) as well as
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The effect of GCK NES mutations on
2021-12-08
The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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KX2-391 dihydrochloride receptor br Conclusion In conclusion
2021-12-08
Conclusion In conclusion, we discovered a pair of novel epimers CBC and CBD from plant C. bungei. These two natural compounds inhibit Hh pathway by blocking signaling at the level of Gli. They are effective in suppressing Hh pathway-dependent medulloblastoma growth in vitro and in vivo. Furthermo
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Immunohistochemistry using anti FFAR antibodies
2021-12-08
Immunohistochemistry using anti-FFAR1 antibodies revealed immunoreactivity for FFAR1 in association with the cell membrane of the hepatocytes (Figure 2). However, the anti-FFAR2 antibody was not suitable for immunohistochemistry under the tested conditions (data not shown). Fatty liver is an import
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FDP is considered as key intermediate in
2021-12-08
FDP is considered as key intermediate in the isoprenoid biosynthetic pathway, since it is the common precursor of polyisoprene units and farnesylated proteins (Cao et al., 2012). In order to understand the role of FDP gene in rubber-producing plants it is of critical importance to GW9662 and charac
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br Conclusions Symptoms from bilateral
2021-12-08
Conclusions Symptoms from bilateral thalamic edema caused by increased venous hypertension can be reversed with appropriate management of the inciting vascular lesion. This case demonstrates a rare patient with decreased CBF in the thalamus in SPECT and completely recovered after factor Xa inhibi
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TLRs were originally identified as pathogen associated molec
2021-12-07
TLRs were originally identified as pathogen-associated molecular pattern recognition receptors that recognized exogenous ligands in response to infection [31]. In cirrhotic mice or patients, the gastrointestinal tract produces and absorbs considerable bacterial LPS with increased permeability of the
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