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At the organismal level skeletal muscle lung and adipose tis
2023-09-13
At the organismal level, skeletal muscle, lung and adipose tissues mediate net de novo synthesis and release of glutamine, whereas net glutamine catabolism occurs in the kidney [7]. The liver exhibits net glutamine consumption coupled to urea production in the post-absorptive state, and net glutamin
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br Current therapies for metabolic diseases
2023-09-13
Current therapies for metabolic diseases Inborn errors of metabolism caused by deficiency of particular enzymes due to loss of function mutations or deletions have been treated by decreasing the intake of the enzymatic substrate, supplementation with an essential cofactor or vitamin, increasing m
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In the search for more specific
2023-09-13
In the search for more specific inhibitors of uptake2, Iversen and Salt (1970) speculated that steroids may potentiate the actions of catecholamines on vascular smooth muscle by inhibiting uptake2-mediated catecholamine clearance of the transmitters. They went on to demonstrate that a variety of ste
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While HTPCs are not immune cells they produce IL
2023-09-13
While HTPCs are not immune cells, they produce IL-6, MCP-1 and other immunologically relevant factors (Mayer et al., 2016). Our results demonstrated that epinephrine and phenylephrine increased the mRNA expression levels of COX-2, IL-6 and MCP-1 in HTPCs without affecting the mRNA expression level o
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The cellular mechanism underlying the CGS mediated inhibitio
2023-09-13
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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ACh induced changes in respiratory frequency could
2023-09-13
ACh-induced changes in respiratory frequency could be of interest. They may reveal an important mechanism of respiratory modulation at the caudal NTS level. ACh-induced increases in respiratory frequency within this region have been also reported by Furuya et al. (2014). Changes in respiratory timin
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The identification of novel kinase inhibitor scaffolds is hi
2023-09-13
The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1
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In this paper we described synthesis biological
2023-09-13
In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo
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From an historical perspective ligands for GPCRs adrenaline
2023-09-13
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, KW 2449 or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were ra
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Several structural classes of ASK
2023-09-13
Several structural N-Nonyldeoxynojirimycin australia of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GS
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br Experimental section br Acknowledgments br
2023-09-13
Experimental section Acknowledgments Introduction Adipose is a major endocrine organ which releases a range of bioactive agents [1]. Selected adipose depots have been established as sites of sex steroid metabolism [1]. Subcutaneous and visceral adipose express high levels of aromatase, cap
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Cytidine 5-triphosphate Under some pathological conditions A
2023-09-13
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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Circular dichroism CD provides useful
2023-09-12
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 vps34 spectroscopy that measures differences in the absorbance of right- and left-circularly polarized light (rather than the commonly use
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br We approached the definition of AD
2023-09-12
We approached the definition of AD with the distinction between a syndrome and a disease in mind. Some will argue that a specific syndrome, that is, a multidomain amnestic dementia (after other potential etiologies have been excluded), should define AD in living people. Our position, however, is t
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br Conflict of interest statement
2023-09-12
Conflict of interest statement Acknowledgements We are very grateful to Maura Agate for her excellent editorial assistance. The work reported in this article was supported largely by the Italian MIUR. Introduction Atenolol is a selective β1-adrenergic receptor blocker that is orally effect
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