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br Introduction AMP activated protein kinase AMPK has been
2023-03-06
Introduction AMP-activated protein kinase (AMPK) has been found to be a key character against cardiovascular diseases and cellular stress. When activated by certain stress, AMPK regulates sugars and fatty acids that are good or detrimental to the heart. For example, targeting AMPK phosphorylation
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Recently Kamoshita et al evaluated a
2023-03-06
Recently, Kamoshita et al. (2016) evaluated a mouse model of retinal neuronal disturbance with the intraperitoneal injection of LPS and found that treatment with AICAR suppressed the reduction of conical function and decreased mRNA levels of TNF-α as well as improved mRNA levels of the mitochondrial
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In conclusion we have shown that mGlu receptors negatively r
2023-03-06
In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, Pam3CSK4 australia tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation of noradrene
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In this article we have outlined the
2023-03-06
In this article, we have outlined the increasing, as yet still circumstantial evidence that the 6TM domains of bacterial ACs might operate as receptors for as yet unknown ligands. Intriguingly, several architectural arguments are also applicable to the 6TM domains of mammalian membrane-bound ACs (mA
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Although the role of mossy fiber
2023-03-06
Although the role of mossy fiber sprouting in epileptogenesis has been challenged (Elmer et al., 1997, Nissinen et al., 2001), in addition to astrogliosis, mossy fiber sprouting is one of the characteristic histopathological findings in TLE (Kharatishvili et al., 2006, Pitkanen et al., 2007, Represa
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AMPK modulates changes in lipid metabolism via
2023-03-06
AMPK modulates changes in lipid metabolism via the regulation of fatty TH588 oxidation and cholesterol synthesis in the liver. The key enzymes involved include ACC and HMGCR [27,28]. Both participate in the rate-limiting steps of fatty acids and cholesterol synthesis and are inactivated on phosphory
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Moreover our results indicate that ADP is
2023-03-06
Moreover, our results indicate that ADP is by far a better phosphate donor than AMP (Table 2). Yet, the bindings of AMP and ATP are mutually exclusive, whereas the bindings of ADP and ATP are additive (Fig. 7). The multiplicity of the phosphate donors in the TgAK reaction (Tables 1 & 2), suggests th
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br Conflict of interest br Ethics
2023-03-06
Conflict of interest Ethics committee Introduction Severe combined immunodeficiency due to adenosine deaminase deficiency (ADA-SCID) is characterized by impaired function and differentiation of T, B, and natural killer (NK) cells. Non-immunological abnormalities may also occur, including fa
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Search sphere This sphere includes the acetylcholine binding
2023-03-03
Search sphere 1: This sphere includes the p450 inhibitors binding site between the α–γ subunits. The center point of the search area was located at x=35.26, y=77.67, z=137.74 and the initial search radius was set to 27Å which assures that the corresponding area outside the channel pore of the two s
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The gene SRD A encodes the
2023-03-03
The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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NLX a k a F or befiradol exhibits nanomolar
2023-03-03
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in CCT007093 to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has
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The cellular mechanism underlying the CGS mediated inhibitio
2023-03-03
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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However although in vitro studies in heterologous systems ha
2023-03-03
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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The syntheses of a and b are shown in Scheme
2023-03-03
The syntheses of 27a and 27b are shown in Scheme 5. Substituted naphthalene 21c was brominated using N-bromosuccinimide (NBS) and 2,2′-azobis(2-methylpropionitrile) (AIBN) to yield 25, which was subjected to lactam cyclization to form 26a and 26b, respectively. Deprotections of each cysteine proteas
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Several mechanisms have been suggested to account for
2023-03-03
Several mechanisms have been suggested to account for the causal association of ICAM-1 induction and leukocyte adhesion with DR, including oxidative stress [16], NF-κB [17], PKC [18], and bioactive lipids [19]. Our previous studies highlighted the role of bioactive lipid metabolites derived from 12/
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