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Furan analogs and N methylpyrrole analogs had
2020-04-22
Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 L002 affinity and an increased antagonist activity, while the corresponding chemical modification
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The role of ETB clearing receptors has
2020-04-22
The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous SC 79 receptor of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all o
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Her eldest daughter individual had a normal birth and health
2020-04-22
Her eldest daughter (individual 4) had a normal birth and health history in early childhood. She developed contractures of her fourth fingers at 4–5 years of age; these contractures were associated with painless, non-erythematous swelling of the involved joints. Her PIP contractures were ∼90 degrees
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br Introduction Acylglycerol acyltransferases AGATs are pred
2020-04-22
Introduction Acylglycerol acyltransferases (AGATs) are predominantly responsible for triglyceride synthesis in the body, via two major pathways: the glycerol phosphate (GP) pathway (Kennedy, 1957) and the monoacylglycerol (MG) pathway (see Coleman and Lee, 2004, Yen et al., 2008). The final step
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The only reported synthesis of the aminobicyclic
2020-04-22
The only reported synthesis of the aminobicyclic core of is based on bis-alkylation of a 4-amino-5,6-dihydroxypyrmidine with dibromoethane. The likelihood of poor regiocontrol/reactivity in utilizing such a transformation for the synthesis of compounds with a substituent on the dioxinyl ring led us
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In general terms PLA s participate in the Lands
2020-04-21
In general terms, PLA2s participate in the Lands cycle of phospholipid fatty Chlorpromazine HCl recycling [1,15,25], whereby the fatty acid composition at the sn-2 position of phospholipids is tightly controlled by a balance between hydrolytic reactions mediated by PLA2s versus activation of the fre
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br Results br Discussion The ubiquitin system has in recent
2020-04-21
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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DNA replication checkpoint kinases in both yeast and human c
2020-04-21
DNA replication checkpoint kinases in both yeast and human Benzamil synthesis upregulate dNTP levels under replication stress to mediate their essential function at replication forks (Yeeles et al., 2013). It is possible that upregulation of dNTP levels under replication stress helps fork restart on
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Apart from neutrophil mediated inflammation the production o
2020-04-21
Apart from neutrophil-mediated inflammation, the production of pro-inflammatory cytokines and chemokines from PGD2/CRTH2 activated macrophages could further aggravate LPS-induced lung injury (Eguchi et al., 2011; Jandl et al., 2016). Interestingly, genetic ablation of CRTH2 diminishes the TNF-α pro
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br Materials and methods br Results br Discussion Our
2020-04-21
Materials and methods Results Discussion Our previous study showed that ERRγ negatively regulates osteoblast differentiation via inhibiting Runx2 transactivity (Jeong et al., 2009). In the present study, we found that ERRγ also induced miR-433 in osteogenic mesenchymal cell lineage C3H10T1/
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Molecular docking study of compound was performed using the
2020-04-21
Molecular docking study of Nucleozin was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cyano-hy
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Introduction Fish commonly employ pheromones
2020-04-21
Introduction Fish commonly employ pheromones to regulate a variety of functions including reproductive communication [1]. Reproductive pheromones induce both primer effects, such as changes in the endocrine or physiological state of conspecifics, and releaser effects such as rapid behavioral respon
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Neuropsychological studies of adults with problem gambling i
2020-04-20
Neuropsychological studies of adults with problem gambling indicate impairments in many cognitive areas including inhibition, working memory, decision-making, cognitive flexibility, and executive planning (Ledgerwood et al., 2012, Goudriaan et al., 2006). Dopamine is a neurotransmitter that regulate
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br Materials and Methods br Results br Discussion The
2020-04-20
Materials and Methods Results Discussion The spatial properties of receptor-ligand interactions can influence receptor activation and signal propagation, but studying this phenomenon requires the development of systems capable of recapitulating complex biophysical traits. In this study, we
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In this study we have explored
2020-04-20
In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta
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