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br Mechanisms for regulation of intracellular cholesterol ho
2024-10-10
Mechanisms for regulation of intracellular cholesterol homeostasis Cells maintain intracellular free cholesterol levels and distribution within stringent tolerances by several mechanisms [55]: (1) uptake of native LDL (the major extracellular carrier of cholesterol) by LDL receptors and modified
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Adiponectin is an adipokine whose circulating level
2024-10-10
Adiponectin is an adipokine whose circulating level is depleted in a number of metabolic diseases including insulin resistance, diabetes and cancer (Khan et al., 2015, Singh et al., 2014a, Singh et al., 2014b, Yamauchi et al., 2014). Despite its importance in health and pathophysiology, adiponectin
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NLX a k a F or befiradol exhibits nanomolar affinity
2024-10-10
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in Glutathione (GSH/GSSG/Total) Fluorometric Assay Kit to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Ta
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A decrease in lactate concentration in
2024-10-10
A decrease in lactate concentration in the incubation medium was observed in samples treated with heparin and 2′,5′-dideoxyadenosine compared with the control (0.05; Fig. 2B). Discussion In the present study we compared the oxidative metabolism and intracellular signals of heparin, the glycosami
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Adenosine is an endogenous nucleoside that
2024-10-10
Adenosine is an endogenous nucleoside that plays pivotal roles in different physiological and pathophysiological processes by triggering specific cell-surface receptors both in the Magnolol and in the periphery. The adenosine receptors (ARs) are four different subtypes of G protein-coupled receptor
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Although effects of low concentrations of agonist were not
2024-10-09
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major PX 866 α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-esterase-inhibiting
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The reaction of LOX with unlabeled AA generated
2024-10-09
The reaction of 5-LOX with unlabeled AA generated products from hydrogen abstraction at C7 (95% 5-HETE) with minor products derived from abstraction at C10 (5% 8-HETE). With 7,7--AA the selectivity remained skewed towards C7 hydrogen abstraction (59%) compared to C10 hydrogen abstraction products (4
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H-Lys(Ac)-OH.HCl australia This study does have several lim
2024-10-09
This study does have several limitations, mainly related to the DMSO vehicle. While DMSO is a known anti-inflammatory mediator,5, 12 it has been shown to upregulate ALOX5, which was not seen in this study (as we are likely underpowered to detect this difference). A manifestation of this anti-inflamm
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Zhang et al screened three thousand compounds
2024-10-09
Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeffe
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It has also been reported that defects in ATM or
2024-10-09
It has also been reported that defects in ATM or ATR signalling are synthetically lethal with PARP inhibition (Turner et al., 2008, Peasland et al., 2011, Yap et al., 2011, Michels et al., 2014), suggesting that combined inhibition of PARP and ATM or ATR may be an effective therapeutic strategy. In
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br Acknowledgements We would like to thank Dr
2024-10-09
Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A
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Following activation of mGluRs GRIP stabilized AMPARs
2024-10-09
Following activation of mGluRs, GRIP-stabilized AMPARs appear to be the primary target for endocytosis. Consistent with this model, we find that using siRNA to reduce GRIP1/2 expression blocks the AMPAR internalization and the synaptic depression mediated by mGluRs. Reductions in GRIP1/2 expression,
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The dependence of blood cell production on a limited
2024-10-08
The dependence of blood cell production on a limited number of HSC and HPC (hereafter collectively referred to as HSPC) means that protection from potential toxins is essential for maintenance of the hematologic system (see Fig. 1). For example, the generation of blood cells within the intramedullar
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Introduction A defining feature of cancer cells is disruptio
2024-10-08
Introduction A defining feature of cancer cells is disruption of the normal controls of the cell cycle; a tumor suppressor or inhibitor may act by restricting progression of the cell cycle. P27 (also known as cyclin-dependent kinase inhibitor 1B, P27, or Kip1) is a putative cell-cycle inhibitor pro
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br Impact of global AHR deficiency on diet induced
2024-10-08
Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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