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AKT activity is also self
2025-02-13
AKT activity is also self-limiting through its substrate GSK3β; the kinase activity of which is negatively regulated by AKT phosphorylation (Fig. 3; Li, Liu, & Gao, 2009). GSK3β activation results in phosphorylation and subsequent ubiquitin mediated degradation of PHLPP (Li et al., 2009). AKT activa
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Corticosterone induced inhibition of OCT mediated
2025-02-13
Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge
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Unlike in humans hepatic expression of FGF increases
2025-02-13
Unlike in humans, hepatic expression of FGF21 increases in mice consuming KD and is a necessary mediator of the physiologic adaptations to the diet. FGF21 knockout (KO) mice gain, rather than lose weight on the diet [6]. FGF21 also activates BAT in part by increasing SNS drive [3,7]. In addition, th
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412 2 NLX a k a F or befiradol
2025-02-13
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in 412 2 to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has sho
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br Introduction Epilepsy is characterized by spontaneous
2025-02-13
Introduction Epilepsy is characterized by spontaneous recurrent seizures and represents one of the most frequent neurological diseases affecting about 60 million people worldwide (McNamara, 1999). It is estimated that up to 50% of all cases are triggered by “initial precipitating injuries”, such
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ACK can be localized to clathrin coated vesicles
2025-02-13
ACK1 can be localized to clathrin-coated vesicles [1]. The association of SNX9 with synaptojanin-1 would suggest the two cooperate during endocytosis at the synapse by coupling the sorting nexin to changes in phospholipid composition. ACK1 in turn negatively regulates the association of SNX9 with ta
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br Material and methods br Results br
2025-02-13
Material and methods Results Discussion Clinical gene therapy trials with viral vectors have been in use for treatment of various genetic disorders and diseases, however efficacious, targetable and highly reliable non-viral delivery systems are needed for safe and long-term applications. De
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CYP A is one of the key metabolizing enzymes of
2025-02-13
CYP3A4 is one of the key metabolizing Applications of EGFP in fluorescence microscopy of the cytochrome P450 (CYP) superfamily of heme-containing monooxygenases. As the CYP family of enzymes plays important roles not only in the xenobiotic metabolism and detoxification of a large number of drugs, b
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Pompe disease is accompanied by the
2025-02-13
Pompe disease is accompanied by the deficiency of the lysosomal α-1,4-glucosidase that makes the Fenofibrate synthesis unable to hydrolyze glycogen to glucose, thereby resulting in the accumulation of glycogen in lysosomes, especially in skeletal muscles and cardiac tissues. This accumulation resul
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What can we learn about the
2025-02-13
What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito
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To help ensure the fidelity of mitosis and cytokinesis cells
2025-02-13
To help ensure the fidelity of mitosis and cytokinesis cells monitor these processes and delay cell cycle progression in response to certain defects. The spindle assembly checkpoint (SAC) is a surveillance system which delays Levonorgestrel mg onset until a bipolar spindle has been correctly assemb
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br Aurora A Aurora B
2025-02-13
Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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br Colorectal carcinoma The growth rate of
2025-02-13
Colorectal carcinoma The growth rate of murine colon adenocarcinoma tumors decreased upon inhibition of 5-LOX, an enzyme that harbors counteracting properties to 15-LOX [28]. It is not clear whether 15-LOX was associated with this phenomenon, but its expression is induced in the colon carcinoma c
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Recent studies have demonstrated that in
2025-02-13
Recent studies have demonstrated that in response to IR, hundreds of substrates are phosphorylated in an ATM-dependent manner, clearly demonstrating the complexity of the ATM-mediated DDR pathways (Matsuoka et al., 2007, Bennetzen et al., 2010, Bensimon et al., 2010). However, evidence suggesting th
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The relationship between the apelinergic and opioid systems
2025-02-12
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 GP
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