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Whereas more research is needed to identify the
2023-11-21

Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the Harringtonine that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reversed the b
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br Regulation and pharmacology of
2023-11-21

Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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TKI-258 In order to increase the oral bioavailability abirat
2023-11-21

In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral TKI-258 of abiraterone acetate (156), it is recommended that this drug should be taken on an em
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Over the past decade extensive research has
2023-11-21

Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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The LO has so far only been
2023-11-21

The 15-LO-1 has so far only been found in humans and rabbit reticulocytes [3], [20] and the rabbit 15-LO-1 protein demonstrate 81% identity to the human 15-LO-1. However, rabbit monocytes express an enzyme with mainly 12-LO activity [20], [21]. The high degree of sequence conservation between these
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Despite these conflicting data about COX ER correlations a l
2023-11-21

Despite these conflicting data about COX-2/ER correlations, a large body of evidence supports that elevated COX-2 expression in breast cancer is a constant feature of high stage disease and a predictor of worse outcome. Upregulation of COX-2 protein has been identified in approximately 40% of cases
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br Technical Note Fungal spoilage of dairy products remains
2023-11-21

Technical Note Fungal spoilage of dairy products remains a major concern for dairy manufacturers despite the use of preventive and control approaches, including the use of chemical preservatives. Among methods that are increasingly used by industries for microbial contaminant control, biopreserva
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The RE compartment has been shown to be
2023-11-21

The RE compartment has been shown to be critical for supplying AMPAR during LTP (Hanley, 2010; Park et al., 2004), but whether they also supply AMPAR for synaptic scaling has been less clear (Gainey et al., 2015; Tan et al., 2015). Interestingly, although an increase in μ3A is necessary for scaling,
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Similar to Cys Met can undergo
2023-11-20

Similar to Cys, Met can undergo ROS-mediated oxidation to Met sulfoxide, which can result in changes in protein conformation and activity [43]. In our results, the Met content in wild ginseng is higher compared to cultivated ginseng (1.3 times, Table 1). Met is a substrate for the synthesis of vario
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Further evidence for action mechanism was
2023-11-20

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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Mitochondria from frozen thawed bull sperm are capable of pr
2023-11-20

Mitochondria from frozen-thawed bull sperm are capable of producing energy using pyruvate and lactate as substrates through oxidative pathways (Beorlegui et al., 1997). Based on the present study, heparin capacitated sperm had a lesser lactate concentration in the incubation medium, supporting the h
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On another hand pyrazoles are widely found as the core
2023-11-20

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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Several approved and or experimental drugs together with nat
2023-11-20

Several approved and/or experimental drugs, together with natural compounds, have been reported to induce autophagy in different cancer types [70], [71], [72] (Table 1). In the next paragraphs, we will review more in detail a group of these agents selected in relation to their promising future outco
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BMS 193885 receptor Phagosomes acquire some hydrolases early
2023-11-20

Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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Thymoquinone TQ is the major active compound
2023-11-20

Thymoquinone (TQ) is the major active Poziotinib derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005, Badr et al., 2
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