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Here we have used transcriptome
2024-03-04
Here, we have used transcriptome analysis of primary neonatal rat cardiomyocytes treated with either the ETR agonist endothelin-1 or the α1-AR agonist phenylephrine to assess differences in their respective signalling networks, and further probed these differences using a panel of fluorescent resona
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Furthermore we found up regulated protein and mRNA levels
2024-03-04
Furthermore, we found up-regulated protein and mRNA levels of adenosine kinase in mouse retina with TON. The up-regulation of ADK was previously demonstrated in diabetic retinopathy (Pang et al., 2010). Greater levels of ADK in activated macrophages and microglial cells abrogate the immune response.
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A high throughput small molecule ACK biochemical
2024-03-04
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found lactacystin to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was
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Our studies also reveal the normal functional roles
2024-03-04
Our studies also reveal the normal functional roles of the MIR. Interaction between the MIR loop and the N-terminal α helix nucleates conformational maturation of AChR subunits, thereby promoting assembly of mature AChRs [52], [55]. This interaction in homologous parts of all AChR subunits appears t
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Additional evidence for a putative role of COXs and LOX
2024-03-04
Additional evidence for a putative role of COXs and 5-LOX in AD derives from pharmacological studies using inhibitors of these enzymes (for review, see Firuzi and Praticò, 2006). In addition to helping delineate the pathobiological mechanisms of AD, these results raise hope for discovering novel the
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The synthetic route to M developed by Rice was utilized
2024-03-04
The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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A rational approach for the design of
2024-03-04
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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V ATPase is a complex enzyme that is composed
2024-03-04
V-ATPase is a complex enzyme that is composed of several subunits, which are assembled into two domains: trans-membrane (V0) and cytosolic (V1) domains [3,5]. Epididymal epithelial Phosphatase Inhibitor Cocktail (2 Tubes, 100X) of rats has been reported to contain V-ATPase which is distributed at t
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br Ataxia telangiectasia and Rad
2024-03-04
Ataxia–telangiectasia and Rad3 related as a therapeutic target Several concerns revolving around functional inhibition of ATR have hindered the exploitation of ATR as therapeutic target in cancer therapy and delayed the development of specific ATR kinase inhibitors. It was anticipated that pharma
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Placental cells also express P aromatase CYP A
2024-03-04
Placental cells also express P450 aromatase (CYP19A1, encoded by CYP19A1). In the placenta, this enzyme requires an external source of androgens, provided by the adrenal gland of the fetus, to form estrogen. The fetal adrenal gland produces dehydroepiandrosterone (DHEA) [9] and, in the placenta, it
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The relationship between the apelinergic and
2024-03-04
The relationship between the apelinergic and opioid systems has been previously reported (Lv et al., 2011, Yang et al., 2010). Lv and colleagues showed that naloxone has a suppressive effect on apelin-induced depression-like behavior in mice (Lv et al., 2012a). Furthermore, heterodimerization of GPC
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The transcription factor activator protein AP is
2024-03-04
The transcription factor activator protein-1 (AP-1) is a redox-sensitive transcription factor whose activity is controlled by agents that perturb intracellular thiol concentrations [10,11]. AP-1 is mainly composed of Jun, Fos, and ATF protein dimers [12,13]. AP-1 mediates the regulation of numerous
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Because antioxidants have a strong radical scavenging
2024-03-04
Because antioxidants have a strong radical scavenging efficiency, a mixture of H2O2 and antioxidants should exhibit a much weaker depolymerization process than H2O2 alone. Therefore, we expected the redox behavior of silver could be affected by the presence of the antioxidant. The schematic diagram
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br Experimental and computation Standard samples
2024-03-04
Experimental and computation Standard samples of artemisinin (1) and artemether (2) were purchased from China National Institutes for Food and Drug Control. Their ECD spectra, at a concentration of 1.0–5.0mg/mL in ethanol, were recorded in a quartz cuvette of 1mm optical path length using a Jasco
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Evidence from basic science studies suggests that Cd may pla
2024-03-02
Evidence from basic science studies suggests that Cd may play a role in prostate cancer through disruption of the androgen receptor (AR). AR, a hormone-activated transcription factor, is the key driver of prostate cancer progression [6]. Ironically, the AR is also required for normal prostate growth
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