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br Conclusion br Author contributions br Acknowledgements We
2021-11-05
Conclusion Author contributions Acknowledgements We thank WM-1119 synthesis USC Center for Craniofacial Molecular Biology (CCMB) for their extensive guidance and teaching in biochemical techniques. We acknowledge Laurel Fisher, PhD for her contribution to statistical analysis of the data. W
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Efficiency of methylated process was assessed
2021-11-04
Efficiency of methylated process was assessed by calculating PMI and SMI. On average, PMI was 0.9 and ranged from 0.1 to 3.8 while SMI was 4.9 and ranged from 0.3 to 21.3. The observed differences in the arsenic methylation can be associated with the inter-individual variations caused by a genetic p
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BQ-788 sodium salt br Discovery of GPR A The murine niacin
2021-11-04
Discovery of GPR109A The murine niacin receptor, protein upregulated in macrophages by interferon-γ (PUMA-G), was identified as a G-protein-coupled receptor (GPCR) expressed in adipocytes and spleen [22], [23]. This finding suggested a role of this receptor in macrophage function [24]. In 2003, t
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Conjugated BAs via S PR
2021-11-04
Conjugated BAs via S1PR2 also activate ERK1/2- and AKT-signaling pathways leading to the growth and invasion of cholangiocarcinoma cells. The role of conjugated BAs via S1PR2 to regulate apoptosis or cancer progression remains to be dissected. Nevertheless, there is no doubt that the composition of
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br Glucocorticosteroid receptor structure and function The g
2021-11-04
Glucocorticosteroid receptor structure and function The gene encoding for the human GR is composed of 9 exons (Oakley and Cidlowski, 2011) and the translated protein is described as having 4 functional regions. The protein contains a highly conserved central DNA-binding domain (DBD) or C-domain,
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It is possible that regulation
2021-11-04
It is possible that regulation of adiposity and glucose homeostasis by GIP are in part mediated by altering leptin levels and/or leptin signaling. However, we are unaware of reports that support this mechanism of action of GIP. In addition, leptin levels in GIP receptor knockout mice [12], [52] and
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br Materials and methods br
2021-11-04
Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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Taken together our results show
2021-11-04
Taken together, our results show that, at least in the in vitro cell line model, methylation within the proximal promoter region of GHSR is an important determinant of its expression; however, to determine whether this represents a physiologically and or pathophysiologically relevant event, further
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br Prospects The prospects for GABAergic pesticides can be p
2021-11-04
Prospects The prospects for GABAergic mmae can be projected from the rate at which new compounds have been introduced (Fig. 1) and the amounts used. More than three billion pounds of NCA-IA insecticides were used in the past seven decades. There was no target site cross-resistance of the NCA-IA
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br BA induced activation of
2021-11-04
BA-induced activation of TGR5 TGR5 is a membrane-bound G protein-coupled receptor for BAs and its activation is dependent on cAMP formation and further stimulation of protein kinase A [53], [31]. The receptor is expressed in the enterochromaffin cells, smooth muscles, immune cells and more import
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In the light of the above
2021-11-04
In the light of the above-mentioned considerations, it is interesting to note that the FPR-related research with regards to bias agonism did not prosper during considerably during the last decade (possible exceptions are [[8], [9], [10], [11]]. However, with new insights in receptor chemistry and fu
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This hypothesis is in line with our
2021-11-04
This hypothesis is in line with our phylogenetic analysis of FBPase sequences which revealed that vertebrate FBP2 evolved significantly faster than FBP1 (Fig. 2). An average distance between FBP2 and ancestral vertebrate FBPase was higher than that for FBP1. Moreover, preliminary study on amphibia
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MMV s distinct mode of inhibition
2021-11-04
MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al
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The FAAH inhibitor activity of the
2021-11-04
The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compoun
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Despite all efforts for development of reliable laboratory m
2021-11-04
Despite all efforts for development of reliable laboratory methods, according to WHO/UNAIDS technical update on HIV incidence assays, none of the assays evaluated by Consortium for the Evaluation and Performance of HIV Incidence Assays (CEPHIA) have completely met the criteria for an incidence assay
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