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br Conclusion We have demonstrated that ETB
2022-07-14

Conclusion We have demonstrated that ETB receptors negatively regulate the expression of AT1 receptors in renal proximal tubule adrenergic antagonist from WKY rats but not in SHRs. Short-term activation of the ETB receptor increases AT1 receptor phosphorylation in WKY cells but decreases it in S
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Histone acetylation is regulated by two groups
2022-07-14

Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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Multi targeting agents are of
2022-07-14

Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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Several studies have indicated that PLD regulated PA signali
2022-07-14

Several studies have indicated that PLD-regulated PA signaling intersects with Rho-mediated cytoskeletal remodeling to drive mesenchymal-like cellular features, and it is known that Rho signaling has the potential to induce YAP/TAZ nuclear activity. Accordingly, Han et al. (2018) provide evidence th
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Carbon monoxide another key product from the breakdown of he
2022-07-13

Carbon monoxide, another key product from the breakdown of heme by HO-1, also plays an important role in the vasculature. Like NO, CO is endogenously derived from the endothelium [68] and can weakly activate sGC by binding to its heme moiety [69]. CO was found to have vasodepressor activity in rats
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It has been proposed that HCA
2022-07-13

It has been proposed that HCA1 may be a better target than HCA2 to treat dyslipidemia and to prevent progression of atherosclerosis, because HCA1 is less widely expressed, and HCA1 activation does not result in flushing. However, since the antilipolytic effects mediated by HCA2 appear to be not the
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Because of its excellent GPR potency good
2022-07-13

Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, h2 receptor antagonist was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an ext
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In the present study we aimed to
2022-07-13

In the present study, we aimed to investigate the effect of a common dairy and beef genetic background on the mRNA JIB-04 synthesis of the AdipoQ system and GPR109A in different adipose depots and liver. Materials and Methods Results Comparing fat masses between families (fat-type vs. lean-t
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In addition to the role of TGR the FXR FGF
2022-07-13

In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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This study does have important limitations to consider The u
2022-07-13

This study does have important limitations to consider. The utilization of a recombinant gp120 monomer (at a single concentration of 100 ng/ml) instead of live virus particles may limit the validity of our results. Moreover, extrapolation of an in vitro cell culture model to animals or humans cannot
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br Method br Results br Discussion There were two
2022-07-13

Method Results Discussion There were two major sources of fluorescent signals of NADH in the mouse retina. One was a product derived from glutamate and the other was the elevation of intrinsic NADH. In the present study, we observed significant contamination from intrinsic NADH in “the oute
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br Introduction As is now well known obesity
2022-07-13

Introduction As is now well known, obesity is major risk factor for various diseases such as nonalcoholic fatty liver disease, cardiovascular disease, some cancers (McWilliams and Petersen, 2009), type-2 diabetes mellitus (Jakobsen et al., 2007), and hypertension (Aneja et al., 2004), among other
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br Materials and methods br
2022-07-13

Materials and methods Results Discussion In the CNS, GLP-1R is associated with G-protein signal transduction pathways, which can activate adenylyl cyclase and protein kinase A by cyclic adenosine monophosphate, and mediates neuronal activities implicated in various pathophysiological change
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The plasma levels of glucose and amino
2022-07-13

The plasma levels of glucose and amino acids at day 0 likely represent the function in utero since the blood was collected within 2h after birth. To elucidate the roles of intestinal transporters as determinants of plasma levels of glucose and amino acids, we analyzed the correlation between the exp
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br Material and methods br Results br Discussion Functional
2022-07-13

Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a
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