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In the liver ghrelin has opposite effects to insulin on
2022-09-21
In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty (-)-epicatechin oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a GH-indepe
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estrone Because FPR is expressed in VSMCs
2022-09-21
Because FPR-1 is expressed in VSMCs and its role in non-hematopoietic cells is still unclear, we questioned whether FPR-1 would have physiological relevance for vascular behavior, in the same way as it does in neutrophils (Ca2+ homeostasis and estrone polymerization). First, we tested if FPR-1 is i
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We reviewed the results of comprehensive genomic profiling C
2022-09-21
We reviewed the results of comprehensive genomic profiling (CGP) in 26,054 cases of NSCLC and examined the frequency and clinical characteristics of patients whose tumors harbor FGFR fusions. To our knowledge, this is the most in-depth evaluation of FGFR fusions exclusively in NSCLC. Here we will de
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T16Ainh - A01 It has been reported that the
2022-09-21
It has been reported that the pathway upstream of YAP phosphorylation is operative in a tissue or context-specific manner. LPA or S1P bound to their corresponding membrane GPCRs and act through Rho GTPases to activate YAP/TAZ [11]. Consistently, another report showed that activation of PAR1 (a GPCR)
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br Materials and methods br
2022-09-20
Materials and methods Results Discussion The innate immune system plays an important role in protecting against IAV infections. However, the virus has the ability of escaping the innate immune system. Activating or enhancing an innate immune response before or during a viral infection will
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Several bacterial functional pathways were observed
2022-09-20
Several bacterial functional pathways were observed after DON administration, of which signal transduction, metabolism and genetic information processing displayed the highest levels of enrichment. Importantly, these three pathways were reported to be closely associated with DON's toxicity. Many evi
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These inhibitors possess a cap group build from
2022-09-20
These inhibitors possess a cap group build from cyclization of several amino-acid or non-amino-acid residues, four or more, with one residue bearing an alkyl arm terminated by ZBGs of various types: thiols, ketones or epoxides. In the case of romidepsin 30 (Fig. 7), the thiol group is initially in a
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Substrate affinity and specificity can
2022-09-20
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of CBiPES hydrochloride bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognit
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In our previous studies examining erectile responses
2022-09-20
In our previous studies examining erectile responses in sGCα1−/− mice, we found that the sGCα1 subunit was required to obtain proper erectile responses to substances generally known to exert their actions by sGC.17, 18 Based on our previous observation of residual relaxing responsiveness to exogenou
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Pharmacologic approaches of inhibiting GSNOR activity have
2022-09-20
Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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br Materials and methods br Results Our data indicated that
2022-09-20
Materials and methods Results Our data indicated that 1,8-cineol leads to a noticeable but not significant (p = 0.07) 45% decreased phosphorylation of GSK-3α/β at Ser-9/21. Phosphorylation of GSK-3α/β at Tyr-279/216 was not affected (Fig. 1A/B). To ensure, that the decreased phosphorylation of
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br Introduction Activation of the lipid sensing
2022-09-20
Introduction Activation of the lipid sensing receptor, GPR55, by lysophosphatidyl inositol (LPI) has been well documented, and implicated in endocannabinoid signaling [1]. Intracellular events resulting from GPR55 activation include; enhanced β-arrestin activity, calcium mobilization and ERK1/2 p
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Antibiotic treatment suggests that cancer
2022-09-20
Antibiotic treatment suggests that cancer-promoting bacteria arise from the osmi of Grp109a mice. How does the lack of Gpr109a signaling lead to expansion of potentially cancer-promoting bacteria? Is this phenomenon related to improper development of intestinal Treg cells? Biome with cancer-promoti
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br TGR Agonists br FXR TGR Dual Agonists In a
2022-09-20
TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency
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br TGR Agonists br FXR TGR Dual Agonists In a
2022-09-20
TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency
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