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The PAS domains of AHR consist of two regions
2023-12-22
The PAS domains of AHR consist of two regions, PAS-A and PAS-B, which function as interfaces for dimerization with ARNT and for ligand binding, respectively [14]. Although both the bHLH and the PAS-A domains have been shown to be involved in dimerization with ARNT, a recent report suggests that only
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Implicit in this concept is the
2023-12-22
Implicit in this concept is the idea that the β-adrenoceptors in the detrusor would be activated by adrenergic nerves of the sympathetic system: sympathetic activity promoting relaxation and enhancing bladder capacity. However, it has been demonstrated that there is only a sparse adrenergic innervat
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The inflammatory cytokine IL is an
2023-12-22
The inflammatory cytokine IL-6 is an additional factor that has been hypothesized to contribute to epinephrine-mediated repression of drug detoxifying proteins such as CYP3A4 (Aninat et al., 2008). Indeed, this CYP is well-known to be repressed by IL-6 (Dickmann et al., 2011) and epinephrine has pre
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Among all the compounds the
2023-12-22
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The glycerol phosphate synthesis 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC
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The observation that vortioxetine blocks HT
2023-12-22
The observation that vortioxetine blocks 5-HT-induced currents in 5-HT3 receptor-expressing oocytes suggests that vortioxetine acts to functionally antagonize these receptors, and is in line with previously published data (Bang-Andersen et al., 2011). For example, Mørk et al. (2012) demonstrated tha
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br Discussion Mycobacterium tuberculosis infection is a main
2023-12-22
Discussion Mycobacterium tuberculosis infection is a main threat to mankind, with one third of the world population being infected. [9] Over nine million new cases of tuberculosis and two million deaths from this disease occur yearly worldwide. [10] The rising incidence of tuberculosis over the l
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The acetylcholinesterase AChE inhibitor tacrine THA
2023-12-22
The acetylcholinesterase (AChE) inhibitor, tacrine (THA), exerts neuroprotective effects in time- and does-dependent manners against glutamate neurotoxicity (Takada-Takatori et al., 2006a, 2006b) and amyloid-β protein toxicity in PC12, a pheochromocytoma line (Wang et al., 2002; Xiao et al., 2000).
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It has been known that LOX
2023-12-22
It has been known that 5-LOX is the rate-limiting enzyme for the products of LTs, and LTs actively participate in the activation of neutrophils [10]. In our study, we determined whether 5-LOX was upregulated in pancreatic tissues during ANP. Moreover, we investigated whether the inhibition of expres
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On another hand pyrazoles are widely
2023-12-22
On another hand, pyrazoles, are widely found as the core structure in a large variety of compounds of great biological and pharmaceutical value exhibiting anti-HCV [11], antitumor [12], cytotoxic[13], and antioxidant activities [14]. Finally, 1,2,3-triazoles have attracted the interest of medicinal
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br The role of cytochrome
2023-12-22
The role of cytochrome b5 with cytochrome P450 17α-hydroxylase/17,20-lyase Conclusion Acknowledgments LLM and RJR wish to thank the Australian Research Council and the National Health and Medical Research Council of Australia for funding. The problem One area of modern medicine that con
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Because of its role in tumor growth proliferation and metast
2023-12-22
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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br Introduction Stroke is a devastating condition that cause
2023-12-22
Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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Inactivation of autophagy can also impact the surface intern
2023-12-22
Inactivation of autophagy can also impact the surface internalization of MHC I molecules, leading to increased antigen presentation. Inactivation of autophagy factors Atg5 and Atg7 in DCs causes elevation of MHC I surface levels by decreasing endocytosis due to a poor recruitment of adaptor-associat
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In this study we showed that
2023-12-22
In this study, we showed that TRIM48 promotes ASK1 activation through ubiquitination-dependent degradation of a negative regulator of ASK1 activation, protein arginine methyltransferase 1 (PRMT1). Knocking down TRIM48 suppressed oxidative-stress-induced cell death mediated by ASK1, and the additiona
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There is little question that as we become more proficient
2023-12-22
There is little question that as we become more proficient in the diagnosis of arginase 1 deficiency individuals with intermediary elevations in arginine on newborn screening and partial defects in enzymatic activity will be found. There are no reliable data to determine a safe level of arginine and
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