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Notably AR and AR signaling can also
2023-04-21
Notably, β2AR and β3AR signaling can also occur via mechanisms independent from G protein [13]. Additionally, the response to GPCR stimulus can be modified by various parameters, including chronic stimulation, cell hypoxia, acidosis, and aging [14], [15], [16]. GRKs have a significant role in the r
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Previous studies have demonstrated the presence of soluble N
2023-04-20
Previous studies have demonstrated the presence of soluble NTPDases, 5′-nucleotidase and adenosine deaminase in rat blood serum as well as in human blood (Doleski et al., 2016; Oses et al., 2004; Yegutkin, 1997; Yegutkin et al., 2007). In addition, our earlier reports have shown that these membrane-
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Taken together BRP represents a
2023-04-20
Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP
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TGX-221 As mentioned above variation of the A
2023-04-20
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to TGX-221 (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comparable inhibi
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br Research perspective In vitro and in vivo studies
2023-04-20
Research perspective In vitro and in vivo studies have demonstrated that increased LPA/ATX signaling contributes to cancer initiation and progression. Recent findings on the role of non-tumoral ATX in cancer progression and metastasis highlighted a new functional contribution for the microenviron
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The finding of the apelin APJ axis
2023-04-20
The finding of the apelin/APJ axis represents an impressive event in cardiovascular studies. As a result of various experimental and clinical studies conducted in vivo and in vitro, it has been indicated that apelin/APJ is a crucial mediator of cardiovascular homeostasis, which takes part in the pat
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The current antifungal pipeline contains several categories
2023-04-20
The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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Kidney contributes importantly to the
2023-04-20
Kidney contributes importantly to the long-term blood pressure control via regulating sodium homeostasis. Renal proximal tubule (RPT) is one of the most critical segments for sodium reabsorption within kidney and therefore involved in blood pressure adjustment. This process is regulated by numerous
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Under some pathological conditions AT R internalization
2023-04-20
Under some pathological conditions, AT1R internalization is decreased when agonist exposure is prolonged. This weakens or removes the AT1R desensitization effect and leads to AT1R and downstream signal overactivation. AT1R overactivation can result in continued biological effects such as sustained v
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A Belgian review on perioperative
2023-04-20
A Belgian review [9] (2011) on perioperative management of drugs recommends not using ACEI/ARBs due to the same reason. Another 2014 French [10] publication on the management of antihypertensive drugs in the perioperative period suggests withholding this medication before surgery even though they a
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Amyloid fibrils are insoluble high molecular weight non
2023-04-20
Amyloid fibrils are insoluble, high-molecular-weight, non-crystalline aggregates and traditional experimental techniques for structure determination such as X-ray and solution NMR cannot resolve their high resolution structures [64], [68]. However, amyloid fibrils exhibit various advantageous featur
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Here we found that AMPK directly phosphorylates
2023-04-20
Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status sup
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Circular dichroism CD provides useful information about prot
2023-04-20
Circular dichroism (CD) provides useful information about protein structure, the extent and rate of structural changes and ligand binding. CD is a form of light AH 7614 spectroscopy that measures differences in the absorbance of right- and left-circularly polarized light (rather than the commonly u
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br Conclusions br Introduction During numerous physiological
2023-04-20
Conclusions Introduction During numerous physiological processes, aldehydes are generated from a variety of endogenous and exogenous precursors including amino acids, carbohydrates, and lipids [1]. Most aldehydes are highly reactive and cytotoxic due to the strong electrophilic nature of the t
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br Distribution of OCT in rat brain
2023-04-20
Distribution of OCT3 in rat brain To understand the potential roles of this corticosterone-sensitive monoamine clearance mechanism in the regulation of monoaminergic neurotransmission and behavior, and its potential contribution to corticosteroid actions on behavior, we examined the rostrocaudal
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