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A third motif involves the toggle
2024-02-28
A third motif involves the toggle switch and consists of the conserved FxxCWxP sequence in TM6 of class A GPCRs (Hofmann et al., 2009, Rosenbaum et al., 2009). Rotamerization of Trp in combination with a kink caused by Pro facilitates the outward movement of TM6 upon activation (Hofmann et al., 2009
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It has been demonstrated that the hallmarks of pulmonary fib
2024-02-28
It has been demonstrated that the hallmarks of pulmonary fibrosis are a loss of endothelial function and subsequent activation of the immune system, which is considered as a direct outcome affected by intracellular pro-inflammatory responses [26]. Thus, inhibition of early inflammation could be an i
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K02288 synthesis Since artemisinin shows low solubility and
2024-02-28
Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-
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The AMP Activated Protein Kinase AMPK has evolved as an
2024-02-28
The 5′AMP-Activated Protein Kinase (AMPK) has evolved as an important cellular sensor of reduced energy status that can subsequently phosphorylate its target proteins, slowing the rates of key biosynthetic processes and promoting energy producing pathways; for these reasons AMPK has been proposed as
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br Results br Discussion Using primarily an
2024-02-28
Results Discussion Using primarily an electrophysiological analysis of dysbindin-deficient hippocampal neurons in cultures and slices, we have uncovered a previously unreported role for dysbindin in enhancing CA3–CA1 AMPAR-mediated transmission. An earlier study, however, has reported a reduct
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br Serine glycine and one
2024-02-28
Serine/glycine and one-carbon metabolism Altered serine metabolism in tumors was noted nearly half a century ago, and elevated flux through the de novo serine synthesis pathway (SSP) is a common phenomenon in cancer SRT2104 [43]. The SSP branches from glycolysis at the point of 3-phosphoglycerat
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In addition to it we also showed that
2024-02-27
In addition to it, we also showed that glycine increases miR-301a expression which directly binds to PTEN 3′UTR target sites [13]. Glycine confers neuroprotection through microRNA-301a/PTEN signaling in rats cortical neurons in oxygen deprivation model [13]. Substantial studies indicate that inhibit
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OCT also is known as
2024-02-27
OCT4 (also is known as POU5F1) plays an important role in embryonic stem cell self-renewal, development and reprogram somatic cell into pluripotent stem cell [[5], [6], [7]]. Recently, many studies also find OCT4 promotes the progression of many tumors. For example, Wnt/β-catenin promotes the expans
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To further clarify the vascular cell types expressing
2024-02-27
To further clarify the vascular cell types expressing AR subtypes, double immunofluorescence staining for ARs and vascular endothelial rxr receptor or vascular smooth muscles was performed. As shown in Fig. 3, Fig. 4, overlay images show the expression of all ARs subtypes that we examined in vascul
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br Antioxidative stress and anti inflammation Oxidative
2024-02-27
Antioxidative stress and anti-inflammation Oxidative stress is a major cause of reduced endothelial NO bioavailability in hypertension, and inflammatory response is thought to play an important role in these processes (Blake and Ridker, 2001, Landmesser et al., 2006). Reactive oxygen species (ROS
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GSK1324726A In this paper we describe the formation of a
2024-02-27
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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br Results and discussion br Conclusion A series of aminoben
2024-02-27
Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen Oxonic acid pota
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This study evaluated the anti tumor influences of
2024-02-27
This study evaluated the anti-tumor influences of LA against HepG2 NVP-BKM120 Hydrochloride in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the mit
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tamoxifen citrate Apelin induced G i activation has been dem
2024-02-27
Apelin induced Gαi activation has been demonstrated as a benefiting effect on cardiac contractility [12], [38], [39], and a vasodilator activity that protects against angiotensin-II-induced cardiovascular fibrosis and atheroma [40], [41]. In contrast, stretch causes hypertrophy through diminishing G
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The functional similarity between GPR and APLNR ie
2024-02-27
The functional similarity between GPR25 and APLNR, ie both can be activated by Apelin and Apela and are coupled to Gi-cAMP signaling pathway (Fig. 2, Fig. 3, Fig. 4), strongly suggests that GPR25 signaling may play important physiological and pathological roles in vertebrates more or less similar to
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