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The ETA receptor has a higher affinity for
2022-09-03

The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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The molecular mechanisms underlying VSMC ETB receptor upregu
2022-09-03

The molecular mechanisms underlying VSMC ETB receptor upregulation have been studied after 24–48h organ culture in both coronary and cerebral arteries. The increased expression of contractile ETB receptor at these time points has been shown to depend on transcriptional mechanisms and PKC and the ext
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Accumulating evidence suggests that the NGF
2022-09-03

Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, BCA Protein Quantitation Kit derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [3
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Prolonged sGC oxidative inhibition occurs in many
2022-09-02

Prolonged sGC oxidative inhibition occurs in many diseases [46,[86], [87], [88]]. Keeping sGC membrane-bound and functional under conditions of high oxidative stress requires a mechanism for restoring oxidized sGC (Fe3+) heme iron to its reduced (Fe2+) state. Without this redox regulation, the sGC
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br S NO signalling during
2022-09-02

(S)NO signalling during the plant immune response Redox signalling molecules must exhibit specificity for their target substrate. Moreover, a given redox-based modification must be reversible to ensure transient signalling. Oxidative cysteine (Cys) modifications are integral to a variety of redox
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br FFA GPR was deorphanised
2022-09-01

FFA4 GPR120 was deorphanised as the second receptor for long-chain fatty acids in 2005 [5]. Initial focus highlighted expression in the lower gut, the capacity of unsaturated fatty acids to promote release of the incretin glucagon-like peptide-1 (GLP-1) from the enteroendocrine cell line STC-1, a
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Thyroid Hormone Receptor Antagonist (1-850) br GPR is a clas
2022-09-01

GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine Thyroid Hormone Receptor Antagonist (1-850) which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated invol
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In previous work we showed that benzophenanthridines do not
2022-09-01

In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in t
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In the present study participants reported a significant
2022-09-01

In the present study, participants reported a significant decrease in symptoms of anxiety and depression along with other symptoms of psychological distress and PTSD. These results are in agreement with a study in which hospitalized patients diagnosed with psychotic and mood disorders demonstrated s
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Although the overall structures of mGlu and mGlu
2022-09-01

Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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nmda br Dysregulation of glutamate transporter expression
2022-09-01

Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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In order to discover novel small
2022-09-01

In order to discover novel small-molecule compounds with the activity of GLUT4 translocation, we conducted a cell-based phenotype screening in L6-GLUT4-myc myoblasts by measuring appearance of GLUT4 on the plasma membrane (GLUT4 translocation activity). Evaluation of total 183,400 compounds gave sev
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Two types of processes intrinsic and extrinsic contribute
2022-09-01

Two types of processes, intrinsic and extrinsic, contribute synergistically to the age-related change on structural integrity and physiological function of the skin (Farage, Miller, Elsner, & Maibach, 2008). Intrinsic aging arise from genetically programmed cell aging, normal metabolic activities, a
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Growing evidence supporting the anti inflammatory and
2022-09-01

Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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The C terminal regions in both FGF and FGF define
2022-09-01

The C-terminal regions in both FGF19 and FGF21 define their KLB interaction [15], [16], [23], [25]. However, less than 40% identity in comparative alignment of C-terminal sequences for these two proteins (Table 1) suggests that their interaction with KLB may require higher-order association with oth
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