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In our studies the EC values
2022-01-11
In our studies, the EC50 values for long-chain unsaturated fatty acids added to the short form of human GPR120 receptor (BC101175), were higher than the EC50 values previously reported (Hirasawa et al., 2005) for the long form of GPR120 (NM_181745), which was co-expressed with Gα16 protein.(Table 2)
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br Clinical development of anti NASH drug therapies The curr
2022-01-11
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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To investigate the potential molecular mechanism
2022-01-10
To investigate the potential molecular mechanism of FXR-mediated regulation of liver cancer cell proliferation, gene expression profiles were determined using Agilent arrays in SK-Hep-1-FXR and NC after treatment with the FXR agonist GW4064. The results indicate that mTOR and S6k are involved in div
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Enhancer of Zeste Homolog EZH
2022-01-10
Enhancer of Zeste Homolog 2 (EZH2) is a core component of the Polycomb Repressive Complex2 (PRC2) which also includes SUZ12 and EED. PRC2 represses gene transcription through trimethylation of Lys27 of histone H3 (H3K27), and contribute to the maintenance of cell identity, epothilone regulation and
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The biochemical cell culture activities and
2022-01-10
The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chlori
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br Discussion Our study found that
2022-01-10
Discussion Our study found that 62.6% of MSM from Natal had been tested for HIV before. This rate was higher than the national average of 37% estimated for the general p-gp inhibitors in 2011 and the 51.6% found by Brito et al. in MSM from 10 Brazilian cities in 2009. These rates are rather disa
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Furthermore we observed a striking difference between
2022-01-10
Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic Calyculin A type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced a significant melting temperature increase of sGC. In comb
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MMP-2/MMP-9 Inhibitor I synthesis br Introduction The discov
2022-01-10
Introduction The discovery that the nitric oxide (NO), soluble guanylate cyclase (sGC), and cyclic guanosine monophosphate (cGMP) pathway mediates erection has led to the use of phosphodiesterase type 5 (PDE-5) inhibitors as the gold standard for treating erectile dysfunction (ED) through the inh
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To date very little is known about the
2022-01-10
To date, very little is known about the GEFs that regulate RhoA during amoeboid migration. GEF-H1, a RhoA GEF, is activated response to microtubule destabilization and promotes amoeboid migration (Eitaki, Yamamori, Meike, Yasui, & Inanami, 2012). Interestingly, the majority of 5 alpha reductase inhi
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Protease Inhibitor Cocktail (EDTA-Free, 100X in DMSO) Previo
2022-01-10
Previous studies have shown that Cu(I) neurotoxicity includes induction of ROS with involvement of the NF-kB pathway and apoptosis (Butterworth, 2010) and that, in its Cu(I) state, Cu(I) alters microglia phenotype and inhibits nitric oxide release (Rossi-George et al., 2012). Cu(I) has a great affin
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Armed with this knowledge we looked
2022-01-10
Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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N1-Methyl-ATP br Spatial working memory is GluR
2022-01-07
Spatial working memory is GluR-A-dependent The radial maze task also allowed us to study hippocampus-dependent spatial working memory. On spatial working memory tasks, the correct spatial response that the animal must make varies from trial to trial and is dependent on some conditional, trial-spe
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br Competing interests br Acknowledgements br Introduction F
2022-01-07
Competing interests Acknowledgements Introduction - Factors Regulating Glucose Tolerance Strictly speaking, the incretin effect refers to the amplification of insulin secretion, which occurs when benzbromarone is taken in orally as compared to infused intravenously [1]. Normally, the insul
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Another consistent observation in our studies was the
2022-01-07
Another consistent observation in our studies was the lower plasma catecholamine concentrations in the exercised GHSR-null mice, suggesting a diminished sympathoadrenal response. A proper sympathoadrenal response is essential for increasing substrate utilization during exercise [81]. Thus, the reduc
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br Materials and methods br Conflicts of interest Some
2022-01-07
Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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