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In prostate cancer PCa glucose metabolism plays
2022-04-20
In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the m
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The eradication of agonist activity in compound was also con
2022-04-19
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary (±)-Nutlin-3 as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagoniz
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br Calcium permeability pathway It has
2022-04-19
Calcium permeability pathway It has been demonstrated that physiological shear stress in the circulation causes a reversible increase in Ca2+ permeability [29], [30], [31], [32], [33] and electrophysiological evidence has been recently reported for transient activation of the Ca2+-sensitive K+ ch
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br Conflict of interest br
2022-04-19
Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr. S
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The regulation of gap junction connexin mediated activities
2022-04-19
The regulation of gap junction-connexin-mediated activities may be achieved through action on the channel gating properties (membrane voltage, pH, interaction with junctional and cytoskeletal proteins, Ca2+ and K+ concentrations, etc) or on the trafficking, turnover and localization of connexins. Sh
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In addition several other considerations were
2022-04-19
In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty Ertapenem sodium salt receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization effor
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br Materials and methods br Results br Discussion The distri
2022-04-19
Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta TTNPB [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract, adipocytes an
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Moving forward to series the
2022-04-19
Moving forward to series , the energy minimized conformation of Pyoluteorin synthesis within the binding pocket is quite interesting. The indole-based tail guides the TZD head for a highly-favored interaction with all residues of the H-bonding triad (). In addition, an extra bonding with H449 in t
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The lack of biological activity
2022-04-19
The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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br Materials and methods br Results and
2022-04-19
Materials and methods Results and discussion To analyze the dependence of lysosomal exocytosis on Cu we exposed HeLa nourseothricin to fresh buffer containing normal levels of free Ca (1mM) and measured β-hex levels in the extracellular medium, followed by measuring β-hex content in the total
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Further investigation of the effects
2022-04-19
Further investigation of the effects of this inhibitor on histone acetylation revealed no HAT inhibitory effects at the level of global histone acetylation after 20h of incubation with C646. After 6h of incubation with C646, however, a slight increase in histone H3 acetylation was observed at lysine
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Nuclear factor erythroid like NFE L
2022-04-19
Nuclear factor erythroid 2-like-2 (NFE2L2; hereafter NRF2) plays a crucial role in the basal and inducible expressions of multiple cytoprotective genes in response to electrophilic and oxidative stress [23]. The cytosolic actin-binding protein Kelch-like ECH-associated protein 1 (KEAP1) primarily re
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br Experimental br Results br Discussion In
2022-04-19
Experimental Results Discussion In this study, we performed molecular docking analysis and in vitro studies to determine whether genistein binds to HIF-1α in BC clofibrate and identify the residues involved in this interaction. We found that some functional groups (residues) mimic the bind
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In addition recent research shows that HK contributes to
2022-04-19
In addition, recent research shows that HK2 contributes to the inhibition of apoptosis through the suppression of the formation of mitochondrial permeability transition pores in association with voltage-dependent anion channel (VDAC) protein [11]. We also found that AKT2 mediates HK2 resistance to a
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Deferoxamine Given the involvement of dysregulated S nitrosy
2022-04-18
Given the involvement of dysregulated S-nitrosylation in multiple pathological conditions, a number of approaches to regulate S-nitrosylation therapeutically are being tried in multiple indications [18]. In the lung, GSNO releasing compounds and GSNOR inhibitors are being considered as potential the
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