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The take home message here is that although Aurora A
2024-08-03
The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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To test the compounds metabolic stability we measured the
2024-08-03
To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura
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Recent studies have indicated that V ATPase activity negativ
2024-08-03
Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ Dynorphin A have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pah1Δ cells'
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Since obesity appears to impact leptin and adiponectin level
2024-08-03
Since obesity appears to impact leptin and adiponectin levels in opposite manners, several studies have suggested that the serum adiponectin/leptin ratio may be a key parameter in indicating the relative risk of postmenopausal breast cancer (Ollberding et al, 2013, Cleary et al, 2009). Therapeutic s
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The studies have described that Candida non albicans
2024-08-03
The studies have described that Candida non-albicans are considered as remarkable pathogenic agents of OPC, and among them, C. tropicalis and C. glabrata are known as major strains that may replace C. albicans as the greatest causing agent of this infection [20], [21]. It has been shown that Candida
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The incremental reduction albeit not statistically significa
2024-08-03
The incremental reduction, albeit not statistically significant, in collagen I with LCZ696 compared to perindopril treated animals, may therefore be related to a more compliant ventricle in LCZ696-treated animals. This is not so surprising given the incremental anti-fibrotic effect of the active met
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Kim et al found that hydroxydopamine
2024-08-03
Kim et al. (2013) found that 6-hydroxydopamine (6-OHDA) promoted the atrophy of dopaminergic neurons associated with the activation of poly (ADP-ribose) polymerase (PARP), the translocation of apoptosis inductor factor (AIF) and the depletion of ATP. An increase in p-AMPK and pS6K (upstream kinase o
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Role of APPL in endosomal
2024-08-02
Role of APPL in endosomal signaling pathways Endosomes consist of distinct membrane subdomains within individual organelles and assist in the translation of extracellular stimuli via cytoplasmic transduction cascades to the nucleus [3], [74]. Endosomal abnormalities are associated with the pathogen
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The most widely recognized effects of adenosine are operated
2024-08-02
The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adeno
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A high throughput small molecule
2024-08-02
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 Fluorescein RNA receptor to be both ATP-competitive and reversible. Early structure-activity relationship (S
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br Acknowledgments This work was supported
2024-08-02
Acknowledgments This work was supported by the R&D Program of the Institutional Research Program of KRICT (SI1701-02), and by the Next generation carbon upcycling project of Ministry of Science and ICT. JSC is kindly grateful to the National Research Council of Science and Technology (NST) for fi
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Until now five muscarinic receptor M genes have been cloned
2024-08-02
Until now, five muscarinic receptor (M1-5) genes have been cloned, but, M1-3 receptors are functionally recognized in the lungs. Smooth muscle contraction is mainly mediated by M3. M2 may also participate in the contraction via Gi protein which leads to a decrease in cAMP. On the other hand, M2 is l
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br Results and discussion br Conclusions In this
2024-08-02
Results and discussion Conclusions In this report we present the synthesis, structure determination, and the in vitro and in vivo evaluation of a series of new quinone analogues aiming to find novel lead structures for the development of 5-LO inhibitors. Our findings support that also the hydr
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The synthesis and secretion of adrenal androgens is
2024-08-02
The synthesis and secretion of adrenal androgens is apparently unique to humans and nonhuman primates, and requires the expression of key mediators such as CYP17 [26]. Endocrine control of CYP17 expression in rhesus monkeys is comparable to that in humans [27]. An analysis of baboon cDNA for CYP17 s
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In order to improve the
2024-08-02
In order to improve the methodology of the synthesis of steroidal derivatives, our goal was the investigation of aza-Michael addition of different N-nucleophiles to 16-dehydropregnenolone in the presence of [DBU][OAc] as catalyst and reaction medium. Michael addition of electron deficient steroidal
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