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In this paper we describe the formation
2024-09-10
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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Five alternatively spliced isoforms of ATX have been describ
2024-09-10
Five alternatively-spliced isoforms of ATX have been described and all are catalytically active [16], [17]. The original ATX described in 1992 is termed ATXα, whereas the most abundant isoform is ATXβ and is the same isoform responsible for plasma lysoPLD activity [18]. Full length ATX is synthesize
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Screening a selection of analogues from this
2024-09-10
Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to Carmoxirole hydrochloride 3 (Fig. 3, Fig. 6). The benzamide analogue 16
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In our approach using BRET and FRET there
2024-09-10
In our approach using BRET and FRET, there is a substantial increase in BRET and FRET signals between Giα2 or Giα3-YFP and CFP- Gγ2/Rluc-Gγ2 upon apelin-13 activation, indicating that Gαi2, Gαi3 and N-terminus of Gβ1γ2 subunits become closer without subunit dissociation. In contrast, both the FRET a
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Expression subcellular localization transcriptional activity
2024-09-10
Expression, subcellular localization, transcriptional activity and protein stability of Foxo are regulated by proteins such as STAT3, PKB, JNK and AMPK (Sun et al., 2017; Zhang et al., 2011). STAT3 is a member of the signal transducer and activator of transcription (STAT) protein family that plays c
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br Materials and method br Results br Discussion Although se
2024-09-10
Materials and method Results Discussion Although several studies have showed the crude extracts of K. senegalensis possessed the anti-inflammatory and hypertensive activities (Olayinka et al., 1992). However, the anti-inflammatory effect and underlying molecular mechanisms of its bioactive
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In order to further explore
2024-09-10
In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 mrna synthesis is a consequence of the breakdown of the endogenous antioxidant defence mechanism, we measured the LDH release, MDA levels, GSH levels and SOD activity. A large
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Recently dairy proteins obtained from whey have received con
2024-09-10
Recently, dairy proteins obtained from whey have received considerable attention for their antioxidant bioactivity (Bayram et al., 2008; Haraguchi et al., 2011; Zhang et al., 2012). Bovine whey proteins (WP) are widely used in various foods for their nutritional, health-promoting, and functional val
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Weak and transient interactions of
2024-09-10
Weak and transient interactions of HMGB proteins in such hit-and-run mechanisms are understandable given that “fluorescence loss in photobleaching” (FLIP) experiments employing GFP-labeled HMGBs have shown that in living cells they are the most mobile of all nuclear proteins [144]. The entire pool o
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Inhibition of autophagy has been shown
2024-09-10
Inhibition of autophagy has been shown to alleviate neuronal damage after cerebral ischemia, both in cell culture and rodent models (Koike et al., 2008, Li et al., 2015, Wang et al., 2016, Zhang et al., 2014, Zheng et al., 2014). Therefore, blockage of autophagy is a potential target for prevention
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The rescue of the behavioral
2024-09-10
The rescue of the behavioral deficit was associated with a significant reduction in the levels of both soluble and insoluble Aβ peptides and their deposition in the 54011 of the same animals. In search for the mechanism behind the reduced amyloidosis, we assessed APP metabolism. Confirming previous
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br Effects of BCAAs on glucose metabolism Insulin plays
2024-09-10
Effects of BCAAs on glucose metabolism Insulin plays an exclusive role in regulation of glucose metabolism, and obesity and type 2 diabetes induce hyperinsulinemia due to insulin resistance. Plasma BCAA concentrations are increased by 14–20% in patients with hyperinsulinemia under overnight fasti
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Estudos de biomarcadores mostram que as concentra
2024-09-10
Estudos de biomarcadores mostram que as concentrações de proteína amiloide no LCR estão inversamente relacionadas com o grau de doença de Alzheimer. No entanto, quer as placas amiloides quer a diminuição da proteína amiloide podem ser encontradas em idosos sem clínica de disfunção cognitiva, pelo qu
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br Materials and methods br Results and discussion First
2024-09-10
Materials and methods Results and discussion First, we examined whether hypothalamic Akt-mediated signaling pathways are regulated postprandially in chickens. Refeeding significantly (P mCAP receptor concentrations significantly increased in chicks after 1 h of refeeding (958 ± 245% of 24 h-fa
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Last decade has provided a number of
2024-09-10
Last decade has provided a number of studies indicating that AhR signaling could play a role both in the development and in progression of multiple cancer types, with potential implications for cancer therapy (for review see (Kolluri et al., 2017; Murray et al., 2014)). Activation of AhR is consider