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Theoretically the expression profile of GluCl variants
2020-12-14
Theoretically, the expression profile of GluCl variants was related to their physiological roles. It was reported that all the three variants (GluCl A, GluCl B, GluCl C) were highly expressed in head tissue of L. striatellus and M. domestica, and the expression level of GluCl A was significantly hig
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Notably we demonstrated that EP
2020-12-14
Notably we demonstrated that EP2/EP4 receptor-coupled activation of the cAMP signaling pathway accounted for both up-regulation of COX-2 and down-regulation of LOX, which is consistent with the roles of the cAMP signaling pathway in regulation of COX-2 and LOX by PGE2 in a number of other tissues or
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In the present study promoting bile acid
2020-12-14
In the present study, promoting bile THZ1 Hydrochloride synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for liver t
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Compound was prepared from chloroindole by acylation to give
2020-12-14
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole AY 9944 dihydrochloride derivative (). Derivative
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br Experimental br Results and discussion br Conclusion br
2020-12-14
Experimental Results and discussion Conclusion Acknowledgements This work was funded by the National Natural Science Foundation of China (81572080, 81873972and81873980), the National Science and Technology Major Project of the Ministry of Science and Technology of China (2018ZX10732202),
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Generally glycines and other small residues
2020-12-12
Generally, glycines (and other small residues such as alanine) present in a helical GxxxG-motif that are facing the same side of the helix form a uniform surface that enables direct contact with a second helix. Crystal structures of multipass membrane proteins have demonstrated that GxxxG-motifs are
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br Methods br Results br Discussion
2020-12-12
Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the Ellipticine with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did not significa
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br Structural and biochemical features of pol
2020-12-12
Structural and biochemical features of pol X family polymerases The X-family DNA polymerase (polX) is specialized in DNA repair. This family is composed of four different DNA polymerases: pol β, pol λ, pol μ and TdT. Only three members of the polX family possess an N-terminal BRCT (BRCA1 carboxy-
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In laboratory strains of Escherichia coli three mechanisms o
2020-12-12
In laboratory strains of Escherichia coli, three mechanisms of repair for alkylated bases are known. The first involves constitutively expressed Ogt and inducible Ada methyltransferases, directly removing methyl groups from O6-methylguanine (O6meG) and O4-methylthymine (O4meT) [1], [2], [3], [4]. In
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Third DGK protein stabilization by myristic acid
2020-12-12
Third, DGKδ2 protein stabilization by myristic Digoxin is cell line specific. Myristic acid had no obvious effects on DGKδ protein stability in the liver cell line HepG2, pancreas cell line MIA-PaCa-2 and neuronal cell line Neuro-2a cells (Fig. 5). Although myristic acid moderately increased the DGK
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The only reported synthesis of the aminobicyclic core
2020-12-12
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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We next examined the effects of
2020-12-11
We next examined the effects of substituents around the carboxylic lactone moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to the carboxylic acid
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Sixty eight male Sprague Dawley rats
2020-12-11
Sixty-eight male Sprague–Dawley rats were acquired from the University of South Dakota Laboratory Animal Services (Vermillion, SD, USA) and housed in pairs at 22°C (60% relative humidity) on reverse 12h light/dark 5-Iodotubercidin (dark cycle started at 10:00a.m.) with food and water freely accessi
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Preparation of the pyridyl ether analogs was accomplished
2020-12-11
Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate,
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Compounds and were outliers for this equation being the two
2020-12-11
Compounds and were outliers for this equation being the two most reactive compounds. The presence of outliers implies that other factors or specific mechanisms are involved in their chemical hydrolysis. Generally urea derivatives prove to be highly stable in aqueous solutions in vitro. Additional
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