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br Results br Discussion Tapinarof GSK is
2023-09-20

Results Discussion Tapinarof (GSK2894512) is a naturally derived investigational topical medicine with demonstrated clinical efficacy for patients with AD and psoriasis (Bissonnette et al., 2010, Bissonnette et al., 2012a). The drug substance is a polyphenol produced by bacteria that is struct
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The numbers and types of molecules needing
2023-09-20

The numbers and types of molecules needing to be transported across membranes are very large, and there is a corresponding very large and diverse number of transporters expressed throughout the body. Hundreds of proteins that have been assigned as having transporter function are broadly divided into
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Young et al described the
2023-09-20

Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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Further evidence for action mechanism was provided by assays
2023-09-20

Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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AdK as an important upstream regulator of adenosine
2023-09-20

AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi
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Despite these efforts to prevent
2023-09-20

Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of a
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br Conclusion br Conflicts of interest br Introduction
2023-09-20

Conclusion Conflicts of interest Introduction RNA interference is a specific post-transcriptional gene silencing mechanism within a cell via the transfection of microRNAs (miRNA), exogenous small interfering RNAs (siRNA) or small hairpin RNAs (shRNA) [1–3]. Transfection of shRNA can be done
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br Phosphorylation of P c Initial
2023-09-20

Phosphorylation of P450c17 – Initial studies In addition to the molar ratio of POR to P450c17 and the allosteric action of cytochrome b5, a third factor that governs 17,20 lyase activity is the serine/threonine (Ser/Thr) phosphorylation of P450c17 itself. In a search for post-translational factor
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In our H K ATPase
2023-09-20

In our H+, K+-ATPase assay (Fig. 1 and Supplementary Fig. 1), myricetin (IC50 = 0.58μM) was more potent than acid-activated omeprazole (IC50 = 1.50μM). In contrast, in oral administration in mice (Fig. 3), omeprazole (20mg/kg) more effectively inhibited gastric rvx secretion compared to myricetin (
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In liver the essential organ of lipoprotein synthesis ACL pl
2023-09-20

In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic muscarinic receptor antagonists to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an imp
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Whole body loss of ACLY
2023-09-20

Whole-body loss of ACLY is early embryonic lethal, indicating that it serves non-redundant roles during development (Beigneux et al., 2004). Silencing or inhibition of ACLY suppresses the proliferation of many cancer cell lines and impairs tumor growth (Bauer et al., 2005, Hanai et al., 2012, Hatziv
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It has also been reported that
2023-09-20

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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The PDZ domains of DLG
2023-09-20

The PDZ domains of DLG interact with tumor suppressor proteins, APC and PTEN, as well as with several viral oncoproteins such as the E6 protein present in oncogenic human papillomavirus (reviewed in [177]). It has been reported that overexpression of DLG in fibroblasts impairs the events in the G0/G
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Another important finding of our study is
2023-09-19

Another important finding of our study is the observation that high glucose per se does not affect TER in mature HREC monolayers; but at the same time it does upregulate ICAM-1 directly and activates HRECs to leukocyte adhesion. This would imply that high glucose affects TER in mature HREC monolayer
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Tissue distribution showed that ctrp was
2023-09-19

Tissue distribution showed that ctrp9 was abundantly expressed in the kidney of male and female tilapia. In mice, the Ctrp9 was identified in adipose tissue, and the expression levels were higher in females than that of males (Wong et al., 2009). Recent studies indicated that Ctrp9 was also expresse
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