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RNA interference assays have shown that the inhibition of AM
2024-06-27
RNA interference assays have shown that the inhibition of AMPK expression leads to increases in TNF-α, IL-6 and cyclooxygenase-2 (COX-2) levels after LPS stimulus, whereas the transfection of macrophages with a constitutively active form of AMPKα1 results in decreased LPS-induced TNF-α and IL-6 prod
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We recently identified a G A dependent epigenetic mechanism
2024-06-27
We recently identified a G9A-dependent epigenetic mechanism for transcriptional activation of the serine pathway in cancer cells (Ding et al., 2013). G9A, also known as EHMT2 and KMT1C, is a H3K9 methyltransferase that has a primary role in catalyzing H3K9me1 and H3K9me2 in euchromatin (Shinkai and
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4μ8C Ketogenic diets are more effective in promoting
2024-06-27
Ketogenic diets are more effective in promoting weight loss than conventional caloric restriction [26] however, their effect on hepatic glucose and lipid metabolism remains inconclusive. Blood glucose homeostasis is tightly regulated. In both mice and humans consuming KD, baseline blood glucose decr
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To better understand the pathophysiology of ASDs
2024-06-26
To better understand the pathophysiology of ASDs, we would need comprehensive information on a) the functions of ASD-associated proteins in the brain, b) how mutations affect the expression level and function of these proteins, c) how mutations affect their function in neurons, and d) how changed ne
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Although CP has been an important
2024-06-26
Although CP has been an important research subject in the field of antigen processing and presentation, the mechanisms of presentation of intracellular mst1 kinase by MHC II received considerably less attention. Interestingly, pioneering work by the Münz laboratory has pointed to an involvement of
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Losmapimod br Results and discussion br Conclusion
2024-06-26
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic Losmapimod group extending from the C-3 position of the aniline and substituted grou
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The identification of novel kinase inhibitor scaffolds is hi
2024-06-26
The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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br HMG proteins mobile modulators
2024-06-26
HMG proteins: mobile modulators of chromatin structure and cellular phenotype The term “High Mobility Group” was originally coined for the HMG proteins because of their unusual solubility properties, their small size and their rapid mobility, relative to other chromatin proteins, during gel elect
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Most of the latest http www
2024-06-26
Most of the latest works reported that in human hair follicle AR expression is restricted to DPC and is not found in the outer root sheath (ORS), hair bulb or bulge (Itami et al., 1995a, Jave-Suarez et al., 2004, Kariya et al., 2005, Pelletier et al., 2004, Thornton et al., 2003). DPC derived from b
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When arachidonic acid is used as
2024-06-25
When arachidonic UO126 is used as a substrate, the platelet-type 12S-lipoxygenase produces predominantly the 12S-hydroperoxy derivative. In contrast, the leukocyte-type 12S-lipoxygenases generate substantial amounts of the 15-lipoxygenase product in addition to the 12S-hydroperoxy derivative. The r
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The G R mutation is located at the solvent front
2024-06-25
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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These results validate the docked pose
2024-06-25
These results validate the docked pose of the ALR2-3e complex in comparison to the docked complex of the ALR2-4c complex of which the compound docked completely out of the binding pocket of ALR2 (). This concludes to that the removal of the acetic hsp90 inhibitors moiety leads to inactive or weakl
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Various compounds have been designed
2024-06-25
Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic Imiquimod hydrochloride moiety, for example, 3-thiazolidineacetic acid derivative, which has been reporte
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In addition to it we
2024-06-25
In addition to it, we also showed that glycine increases miR-301a expression which directly binds to PTEN 3′UTR target sites [13]. Glycine confers neuroprotection through microRNA-301a/PTEN signaling in rats cortical neurons in oxygen deprivation model [13]. Substantial studies indicate that inhibit
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br Introduction Psychostimulant abuse and addiction remain a
2024-06-25
Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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