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As an alternative to chronic receptor blockade we have been
2024-06-28
As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify Pancuronium dibromide receptor adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulat
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br Experimental section br Conflicts of
2024-06-28
Experimental section Conflicts of interest Acknowledgments This work was partly supported by INSA-Rouen, Rouen University, CNRS, Labex SynOrg (ANR-11-LABX-0029), Région Haute-Normandie. Introduction A key component of the integrated management of key pests such as codling moth (Cydia po
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When skeletal muscle ages there is
2024-06-27
When skeletal muscle ages, there is an increase in frailty, which is coincident with a decrease in muscle mass and function—this condition is called sarcopenia (Cruz-Jentoft et al., 2010). It has been shown that one of the major pathways downregulated at the onset of sarcopenia is the mitochondrial
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Previous studies have demonstrated ATR inhibition is
2024-06-27
Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia CW069 to enhance chemotherapy sensitivity [[16], [17], [18],[20], [21], [22]]. VE-822
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The allosteric site of class C receptors is generally locate
2024-06-27
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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Receptors containing an x y
2024-06-27
Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For
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PD research involves the use of many animal
2024-06-27
PD research involves the use of many animal models, which can be categorized into two main types: toxic models—among which the two most widely used are the classical 6-hydroxydopamine (6-OHDA) model in rats and the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) model in mice and monkeys—and gen
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The accumulation of oxidized low density lipoprotein
2024-06-27
The accumulation of oxidized low-density lipoprotein (oxLDL) is one of the many causes of the initiation and progression of atherosclerosis (Virmani et al., 2002; Pirillo et al., 2013; Sun et al., 2016; Huang et al., 2016; Tabas, 2010). oxLDL-induced apoptosis of macrophages contributes to the forma
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br AR signaling and urothelial cancer progression As
2024-06-27
AR signaling and urothelial cancer progression As shown in other types of malignancies, such as prostate cancer cells, it has been documented that androgens induce AR expression and its nuclear translocation as well as ARE promoter activity in urothelial cancer cells (Chen et al., 2003, Izumi et
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LOXs and CYPs are a series
2024-06-27
LOXs and CYPs are a series of iron-containing enzymes that metabolize arachidonic Boceprevir sale to form biologically active products, such as epoxyeicosatrienoic acids (EETs) hydroperoxyeicosatetraenoic acids (HETEs), prostaglandins, leukotrienes and thromboxanes [6]. Among these mediators, 12/15
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In contrast to the beneficial treatment of
2024-06-27
In contrast to the beneficial treatment of skin-inflammation with PAH containing coal tar, epidemiology showed that environmental pollution, containing AHR-activating PAH, lead to more eczema [80]. Of note, other epidemiological data suggested that Th17 cell polarization may be enhanced air pollutio
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To investigate the potential link between G and MT assembly
2024-06-27
To investigate the potential link between Gβγ and MT assembly in vivo, cultured NIH3T3 and PC12 cells were used. The role of Gβγ in MT assembly was demonstrated using nocodazole, a MT depolymerizing drug [14]. We found that Gβγ was preferentially bound to MTs in NIH3T3 and PC12 cells and treatment w
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Numerous studies have reported high glutamate levels in
2024-06-27
Numerous studies have reported high glutamate levels in the brains of patients with depression, indicating that the glutamate system plays a crucial role in depression (Sanacora et al., 2004; Kendell et al., 2005; Hashimoto et al., 2007). Furthermore, several clinically effective antidepressant drug
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br Conclusions The present data suggest that
2024-06-26
Conclusions The present data suggest that homeostatic balance of the cortical/hippocampal adenosinergic tone is necessary for normal working memory function and any deviation appears to impair performance – either as a consequence of A2AR under-activation when adenosine levels are reduced or due
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As a continuation of our search for
2024-06-26
As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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