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CGP 53353 In our preliminary evaluation of this series
2020-02-28
In our preliminary evaluation of this series, we were surprised to discover that CGP 53353 was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is compared with
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The importance of G S phase
2020-02-28
The importance of G1–S phase progression to the formation of malignant tumors has been highlighted by the high incidence of aberrations in the genes involved in this progression in a wide variety of tumors. p27Kip1 is a member of the Cip/Kip family of cyclin-dependent kinase inhibitors (CKI). Its ro
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The kinase activity of DNA PKcs is
2020-02-28
The kinase activity of DNA-PKcs is essential for NHEJ, but the exact role of the enzymatic activity of DNA-PKcs plays in NHEJ is not fully understood [57]. In vitro, DNA-PKcs can phosphorylate each of the canonical NHEJ factors including Ku70/80 [58], [59], XRCC4 [60], [61], Valinomycin IV [62], an
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In contrast to drospirenone dydrogestrone acts rather neutra
2020-02-28
In Gap19 receptor to drospirenone dydrogestrone acts rather neutral at the aldosterone-, glucocorticoid- and androgen-receptor [12]. This indicates that the assessment of a ‘net-overall effect’ on the vascular system is very difficult based on the often discussed ‘partial effects’ of the progestoge
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So far several important flovonoids and polyphenoilc compoun
2020-02-28
So far, several important flovonoids and polyphenoilc compounds were subjected to various human studies regarding their potential therapeutic and adverse effects (Ide et al., 2014; Turner et al., 2015; Witte et al., 2014) (Table 1). Resveratrol (trans-3,4, 5-trihydroxystilbene) is widespread stilbe
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Other GPCRs notable for changes in
2020-02-27
Other GPCRs notable for changes in expression on CLL cells include upregulation of the thromboxane A2 receptor TBXA2R mRNA [61] and up and downregulation of mRNA and protein from the neurotensin receptors NTSR2 and NTSR1, respectively [62]. The Eμ-TCL1 mouse model of CLL has been used to study mult
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Ingested folate needs to be chemically
2020-02-27
Ingested folate needs to be chemically modified in order to become a one carbon donor for cell metabolism. Firstly, folate turns to dihydrofolic Raltitrexed (DHF), it is then converted into tetrahydrofolate (THF) by the dihydrofolate reductase enzyme (DHFR) and finally converted into N5, N10-methyl
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br Discussion The N terminal domain of DDRs has long
2020-02-27
Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon
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br Deubiquitination deubiquitinases and cancer Protein deubi
2020-02-27
Deubiquitination, deubiquitinases and cancer Protein deubiquitination is reverse process of ubiquitination and performed by deubiquitinases or deubiquitinating enzymes (DUBs), which help in removal of ubiquitin from target proteins and involve in ubiquitin maturation, recycling and editing (Pfoh
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Nowadays colorimetric assay has been applied
2020-02-27
Nowadays, colorimetric assay has been applied in detecting DNA MTase activity. Li et al. used DNA modified gold nanoparticles (AuNPs) coupled with enzyme-linkage reactions to detect the activity of methylases [20]. In a previous study, our group presented a label-free colorimetric method, using unmo
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COMT expression protein level and activity are down regulate
2020-02-27
COMT expression, protein level and activity are down regulated by E2. Using estrogen receptor (ER) positive MCF-7 cells, Xie et al. demonstrated an E2 dose dependent (1, 10 and 100 nM) decrease in S-COMT 1.3 kb mRNA that was maximum after 48 h (Xie et al., 1999). A similar decrease was not observed
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The eNOS bp VNTR polymorphism has
2020-02-26
The eNOS 27-bp VNTR polymorphism has been found to be associated with altered plasma NO levels. This polymorphism also has been associated with many vascular diseases including hypertension, diabetic retinopathy, and diabetic nephropathy in various populations. Notably, our results were different fr
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What does this mean for
2020-02-26
What does this mean for cancer therapy? We found that components of the de novo pyrimidine synthesis pathway rarely mutate in cancer, clearly showing its importance. In our experimental models, the pathway, including DHODH itself, was primed to respond when the block in CoQ redox-cycling was removed
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br Signaling of DDR receptor and
2020-02-26
Signaling of DDR2 receptor and its regulation Being the tyrosine kinase receptor, downstream signaling of DDR2 receptor is initiated by phosphorylation of cytoplasmic tyrosine residue upon ligand binding (Type II collagen) but the authentic facts or detail information of tyrosine phosphorylation
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SIRT is a representative member of
2020-02-26
SIRT1 is a representative member of Sirtuins, which is a family of highly conserved NAD+-dependent class III histone deacetylases. SIRT1 deacetylates plentiful nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016; Gu et al., 2016; Tu et al., 2018) to p
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