• The rationale for developing HDACi as anticancer agents was

  2022-03-14

  

  The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and 77 arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hematological mal

• A more quantitative view of kinase specificity suggests a

  2022-03-14

  

  A more quantitative view of kinase specificity suggests a continuum of phosphorylation rates for the various substrates of a particular kinase (Figure 4A). Such differences in ‘substrate quality’ can arise from variations in phosphorylation site or docking sequences and may explain why the timing or

• Thyroid hormone triiodothyronine T and

  2022-03-12

  

  Thyroid hormone 3,5,3′-triiodothyronine (T3) and its precursor, thyroxine (T4), are iodinated compounds, which are known to regulate the expression of genes involved in various biological processes, such as development, growth and metabolic control. The iodothyronine deiodinase types I, II and III (

• br Conclusion br Experimental procedures br Introduction The

  2022-03-12

  

  Conclusion Experimental procedures Introduction The glycine receptor (GlyR) is a member of the Cys-loop family of ligand-gated ion channels. It is the primary inhibitory receptor in the brainstem and spinal cord but also plays important roles in higher ML133 HCl australia regions, includin

• Na K ATPase adenosine triphosphate ATP and astrocytic glutam

  2022-03-12

  

  Na+/K+-ATPase, Zaragozic Acid A and astrocytic glutamate transporters act together to maintain sodium and potassium gradients and the proper activities of EAAT1 and EAAT2 (Rose et al., 2009; Sheean et al., 2013); nevertheless, in present study, Na+/K+-ATPase activity was shown to be increased as fr

• br Genetic rescue of GluR A dependent spatial working

  2022-03-12

  

  Genetic rescue of GluR-A-dependent spatial working memory Spatial working memory performance in GluR-A−/− mice can be restored by the forebrain-specific Z-WEHD-FMK of GluR-A subunits labeled with green-fluorescent protein (GFP) on an otherwise GluR-A knockout background (Schmitt et al., 2005). T

• idasanutlin br Genetic manipulation variation of the ghrelin

  2022-03-12

  

  Genetic manipulation/variation of the ghrelin system and alcohol-related outcomes Genetic manipulation of the ghrelin system (either the peptide or the receptor gene) via knockout rodent models has provided further insight into the role of this system in alcohol seeking and consummatory behaviors

• The observed CORT induced increase in Cx

  2022-03-12

  

  The observed CORT-induced increase in Cx43 phosphorylation at S368 may also contribute to GJIC disruption. Gap junction channel permeability is modulated through connexin phosphorylation (Moreno and Lau, 2007). Specifically, the phosphorylation of Cx43 on S368 has been previously shown to decrease i

• The significance of A and tau

  2022-03-12

  

  The significance of Aβ and tau as therapeutic targets is not only derived from pathological evidence of postmortem brain but also from biochemical analysis of cultured human neurons. This is largely based on the induced pluripotent stem cell (iPSC) technology that has been established to study Aβ, t

• Encouraged by the observation obtained from region A

  2022-03-12

  

  Encouraged by the observation obtained from region A, we selected the structure of 1 as the next template to successively pursue the SAR on regions B-D of 1 (lower side of Fig. 2). Next, we turned attention to the external aromatic ring of 1 to verify the impact on the antagonistic activity and prep

• Interestingly the subcellular localization of FBPase in hepa

  2022-03-12

  

  Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Apicidin reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the abilit

• Over of all melanomas have activating BRAF mutations

  2022-03-12

  

  Over 50% of all melanomas have activating BRAF mutations [29] and inhibition of the Ras/Raf/MEK/ERK signaling pathways is one of the most promising treatments for malignant melanoma [30]. However, studies using BRAF inhibitors have identified various feedback mechanisms to activate BRAF pathway in m

• Finally the optimized leads and were tested in

  2022-03-12

  

  Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition

• In patients with breast cancer ZRANB

  2022-03-11

  

  In patients with breast cancer, ZRANB1 gene amplification was found in a subset of cases, and ZRANB1 protein levels correlated with EZH2 protein levels and poor survival (both TNBC and non-TNBC). Moreover, unlike normal mammary epithelial cells, all human breast cancer cell lines examined (both TNBC

• JMJD C is another JmjC domain protein

  2022-03-11

  

  JMJD1C is another JmjC domain protein discovered as a putative oncogene in shRNA screens in MLL-AF9-, HOXA9-, and AML1-ETO-driven AML 40, 41, 42. Depletion of JMJD1C decreased the frequency of LICs by inducing their differentiation and impaired the growth and establishment of leukemia in serial tran

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