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Cys loop GABA receptors are well
2022-02-23
Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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More recently Serna Marquez and colleagues investigated LA
2022-02-23
More recently, Serna-Marquez and colleagues investigated LA-induced migration and invasion of MDA-MB-231 breast cancer cells. In this study, LA was shown to induce AKT-2 phosphorylation and cell invasion and migration in MDA cells. LA-induced cell migration was inhibited by siRNA that selectively ta
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br FGF FGFR pathway as
2022-02-23
FGF/FGFR pathway as predictive factor Several studies have identified FGFR1 amplification as the major predictive factor of response to FGFR inhibitors [26], [27]. However, in a recent study on lung cancer cell lines with ponatinib, FGFR1 mRNA and protein expression, together with FGF2 and FGF9 m
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However Gingrich and Hen reported that absence of the gene
2022-02-23
However, Gingrich and Hen reported that absence of the gene at all stages of ontogenesis of mice may interfere with the normal developmental program and/or the organism may undergo changes in other systems to compensate for gene absence (46). In addition, potentially altered maternal behavior of GPR
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Through the analysis of various synthetic GPR agonists as
2022-02-23
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic GW441756 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK-
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In the Medicines for Malaria
2022-02-23
In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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In Arabidopsis GCN containing protein
2022-02-23
In Arabidopsis, GCN5-containing protein complexes are found to be involved in cell differentiation, leaf and floral organogenesis [[8], [9], [10]]. AtHAC1 has involvement with root elongation, flowering, fertility and de novo shoot regeneration [11,12]. AtHAM1 and AtHAM2 control flowering time by ep
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A compound structurally similar to PF has been
2022-02-23
A Temsirolimus structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-
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It was noted elsewhere that several of
2022-02-22
It was noted elsewhere that several of the variants (i.e., Indel19 and SNP63) that make up the risk haplotypes had unusually large differences in allele frequencies between Africans and non-Africans, as compared with a set of likely neutral loci (Fullerton et al. 2002). This finding was interpreted
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Methods br Results br Discussion In this report the therapeu
2022-02-22
Methods Results Discussion In this report, the therapeutic effect of a GCGR antagonistic antibody REMD2.59 was tested in 2 mechanistically divergent disease models of heart failure without confounding defects in global metabolism. Based on histological and functional analyses in both MI-injur
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The SNPs of candidate genes may exert
2022-02-22
The SNPs of candidate genes may exert their effect on associated traits through changing of gene expression (Bonafe et al., 2003, Wyszynska-Koko et al., 2006). In agreement, GHSR SNPs were significantly associated with upregulation of this gene in the pituitary gland of GG/GG chickens. The GHRL/GHSR
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FPR ligands comprise structurally very diverse classes
2022-02-21
FPR ligands comprise structurally very diverse (+)- Corydaline sale of compounds, ranging from naturally occurring peptides/proteins or “danger signals” such as PAMPs and DAMPs (see 1.1), respectively, to endogenous lipids and even various synthetic non-peptides, such as benzimidazoles, pyrazolones
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Reducing the molecular weight According to a thorough analys
2022-02-21
Reducing the molecular weight: According to a thorough analysis of a large, structurally diverse Caco-2 permeability dataset using a variety of statistical techniques by AstraZeneca researchers, logD and molecular weight are suggested the most important factors in determining the permeability of dru
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Polyphyllin VII Thus aldolase catalyzing the reversible reac
2022-02-21
Thus, aldolase catalyzing the reversible reaction of F1,6-P2 synthesis is involved in the formation of the glyconeogenic or glycolytic complex, dependently on the physiological state of the cell. In the process of glycogen synthesis, the enzyme not only supplies the substrate for FBPase and desensit
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The present study also demonstrated that edoxaban inhibited
2022-02-21
The present study also demonstrated that edoxaban inhibited both free and clot-bound FXa activity. The IC50 values for free and clot-bound FXa in this study are well consistent with Ki values for free FXa and FXa incorporated in prothrombinase complex (0.561 and 2.98nM, respectively) in our previous
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