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G protein coupled receptor kinases GRKs are another group of
2022-01-11
G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor
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Importance of glucokinase in glucose homeostasis and a
2022-01-10
Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of gl
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Ketamine has recently been found to exert rapid
2022-01-10
Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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Somatostatin analogues are among the first peptide based dru
2022-01-10
Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B
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Galanin was shown to play an important role in pain
2022-01-10
Galanin was shown to play an important role in pain and pain processing [14] and the involvement of neuropeptides in the development of migraine is well established [[24], [25], [26]], however, so far it has not been examined whether systemic galanin levels correlate with migraine. Therefore, we use
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br Conflicts of interest br Acknowledgment br Introduction
2022-01-10
Conflicts of interest Acknowledgment Introduction The Dyngo-4a mg growth factor receptors (FGFRs) are a family members of receptor tyrosine kinase (RTK) that represent attractive therapeutic targets for anti-cancer therapy gaining more and more attention in recent years [1], [2]. This famil
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Therefore the histomorphology and the comprehensive analysis
2022-01-10
Therefore, the histomorphology and the comprehensive analysis of TMJ-RA pathogenesis need to be completed although clinical findings in TMJ-RA are similar to RA in other joints [41]. Especially for the dentist, the difficulties associated with diagnosing TMJ-RA patients [49] posing challenges to dia
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There has been conflicting evidence on
2022-01-10
There has been conflicting evidence on the possible receptor mechanisms that mediate the neuro-immuno-modulatory effects of FAAH substrates. Evidence from in vitro studies indicates that AEA-mediated modulation of TLR4-induced neuroinflammation may be mediated by CB1/CB2 receptor dependent (Correa e
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As illustrated in among all synthesized compounds biphenyl
2022-01-10
As illustrated in , among all synthesized compounds, biphenyl derivatives , , , , and with substitutions at the 3-position possessed the best FAAH inhibitory capacity. These 5 compounds demonstrated a good activity against FAAH with IC values in a submicromolar range. Nevertheless, when replacing th
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Recent studies are beginning to explore this complex interpl
2022-01-10
Recent studies are beginning to explore this complex interplay of pathways. For example, intracellular trafficking of poly(lactic-co-glycolic acid)(PLGA) based nanoparticles was studied in detail using 30 different Rab proteins as markers for intracellular transport vesicles (involved in exocytosis,
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Taken together the four HRs couple with several different
2022-01-10
Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc
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Several mechanisms have been suggested
2022-01-10
Several mechanisms have been suggested to underline the release of signalling molecules from astrocytes: reverse operation of glutamate transporters, volume-regulated anion channels, gap-junctional hemi channels, diffusional release through purinergic receptors and Ca2+-dependent exocytosis [2], [15
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Histamine functions as a key neurotransmitter in multiple ci
2022-01-10
Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, histamine is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling pathway
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Nazar and colleagues reported a normal HER gene number in
2022-01-10
Nazar and colleagues reported a normal HER2 gene number in 13 primary and 2 recurrent ethmoid sinus adenocarcinomas, without any histological and immunohistochemical characterization, so a comparison with the present findings is impossible [14]. More recently, 552 head and neck carcinomas have been
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The inhibition of HDAC increases the level
2022-01-10
The inhibition of HDAC increases the level of histone acetylation and consequently turns the chromatin to be loose and active, allowing multiple transcription factors to access to promoters of diverse genes including tumor suppressor genes []. As compound possessed potent HDAC inhibitory activity a
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