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Here we report discovery of
2024-06-17
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of erk pathway bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. T
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CK is considered a central controller of
2024-06-17
CK is considered a central controller of cellular energy homeostasis that catalyzes the reversible transfer of a phosphoryl group from ATP to adenosine diphosphate (ADP) and creatine to produce PCr [5]. This enzyme builds up a large pool of rapidly diffusing PCr for temporal and spatial buffering of
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br Materials and methods br Acknowledgement
2024-06-17
Materials and methods Acknowledgement This work was supported by the Beijing Natural Science Foundation (Grant no. 6151001), and the National Natural Science Foundation of China (Grant no. 31572516). Introduction Staphylococcus aureus is an important microorganism responsible for both clin
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The crucial role of AP in establishing and
2024-06-17
The crucial role of AP-1 in establishing and maintaining cell type-specific gene expression programs and cell identity is further apparent during reprogramming of mouse embryo fibroblasts (MEFs) into iPSCs with either Oct4/Sox2/Klf4/cMyc (OSKM ) factors , or chemicals . Using ATAC-seq to profile ch
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Coumarin Applications for protein switches are numerous
2024-06-17
Applications for protein switches are numerous. In diagnostics, protein switches can detect analytes as components of inexpensive homogeneous assays that do not require specialized equipment or time-consuming incubation and washing steps characteristic of immunoassays [8]. Protein switches have also
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We report here the first study on
2024-06-17
We report here the first study on the inhibitory effects of the organic nitrates – on human erythrocyte GR. The previous reports by Becker et al., investigated other nitro derivatives (including arylizoalloxazines) by using Beutler’s method, monitoring GR inhibition. Data of show inhibition of hGR b
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Recently the FDA approved the first blood based test
2024-06-17
Recently, the FDA approved the first blood-based test for the detection of EGFR mutations in non-small cell lung cancer patients (http://www.fda.gov) (Voelker, 2016). This allows detection of specific, recurrent mutations, which can help the selection of the patients that could benefit from Erlotin
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c-di-AMP Interestingly metabolic dysfunction is also
2024-06-17
Interestingly, metabolic dysfunction is also observed in amyotrophic lateral sclerosis (ALS). Patients and mouse models of familial ALS exhibit higher levels of resting c-di-AMP expenditure and lower fat-free mass, indicating a hypermetabolic phenotype. Lim et al. (2012) found that reducing AMPK act
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br LO synaptic integrity and memory Interestingly several gr
2024-06-14
12/15LO, synaptic integrity, and memory Interestingly, several groups have found that 12/15LO directly modulates synaptic function. Normandin and colleagues reported that pharmacological inhibition of 12/15LO modulates rat hippocampal long-term depression (LTD), a process by which neuronal synapt
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br Acknowledgements This work was supported by
2024-06-14
Acknowledgements This work was supported by a grant from the National Science Foundation (IOS- 1353366), the Hatch Program of the National Institute of Food and Agriculture (VA-135908) and the Virginia Agricultural Experiment Station, to G.P. Introduction With steadily rising number of affect
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There are several strengths and weaknesses of the current
2024-06-14
There are several strengths and weaknesses of the current investigation which merit consideration. Obviously, the current findings are important and less prone to bias than findings from traditional observational epidemiological studies, because causal investigations with the use of genetic variants
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To guide our attempts at achieving AKT potency
2024-06-14
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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Our previous study revealed expression of AhR in human
2024-06-14
Our previous study revealed expression of AhR in human parotid gland in cytoplasm of striated duct gamma secretase inhibitors (Drozdzik, Kowalczyk, Urasińska, & Kurzawski, 2013). In a further study we observed regulation of AhR expression and function by its specific inducer, i.e. 2,3,7,8-tetrachlo
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Unlike in humans hepatic expression of FGF increases in mice
2024-06-14
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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In this study high concentrations mM
2024-06-14
In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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