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Compounds and possessed relatively low clogP values
2021-03-18

Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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At first cartilage damage in osteoarthritis reflects
2021-03-18

At first, cartilage damage in osteoarthritis reflects the loss of proteoglycan and collagen network that increases the swelling of tissues. The incremented expression of DDR2 receptor has also co-related with the depletion of cartilage in surgically induced OA model [8]. Osteoarthritis, a degenerati
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Recently cross talk between DDR and the insulin
2021-03-18

Recently, cross-talk between DDR2 and the insulin receptor and between Notch1 and DDR1 was proposed. Stimulation of cells with collagen I and insulin promotes Tyr740 as well as total tyrosine phosphorylation of DDR2 receptor to a greater extent than the phosphorylation stimulated by collagen I alone
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Despite the weak and transient nature
2021-03-18

Despite the weak and transient nature of E2–E3 interactions, this binding is required for the transfer of ubiquitin to the substrate. The low affinity characteristics of this interaction may be due to the fact that E2s use the same surface to interact with E1s and E3s, and hence while binding to an
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br Significance Dysregulation of dopamine homeostasis contri
2021-03-18

Significance Dysregulation of dopamine homeostasis contributes to Parkinson's disease (PD). The nuclear receptor Nurr1 plays a central role in dopamine homeostasis, regulating the transcription of Iberiotoxin governing the synthesis, packaging, and reuptake of dopamine. Efforts to capitalize on
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In light of the overall loss
2021-03-18

In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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br The central role of DNA PK in
2021-03-18

The central role of DNA-PK in the NHEJ NHEJ can be divided in several steps (Fig. 1A): 1) recognition and binding of Ku at each ends of the DSB following by the assembly of the DNA-PK at the break points and bridging; 2) phosphorylation of the DNA ends by DNA-PKcs; 3) ligation of the ends by DNA
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The thermal behavior of the UV sensitive nanocomposites was
2021-03-18

The thermal behavior of the UV-sensitive nanocomposites was investigated by DSC before and after irradiation in an extended temperature range (from −40 to 250 °C). Fig. 4a shows the thermograms of the non-irradiated GNP-DNA/PDMS nanocomposites in comparison with a neat PDMS sample. The filler-loaded
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To date many studies have reported
2021-03-18

To date, many studies have reported significant aberrant methylation patterns in TIMPs in various types of cancer TCS 359 [[16], [17], [18]]. However, little has been reported on the events that lead to the methylation of TIMPs in the UV-irradiated human skin. Therefore, the objective of this study
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br Sphingosine kinase One of the enzymes closely related to
2021-03-18

Sphingosine kinase One of the enzymes closely related to DGKs are the sphingosine kinases (SKs). These enzymes catalyze the conversion of sphingosine (Sph) to sphingosine-1-phosphate (S1P). SKs and DGKs are closely related lipid kinase in term of basic enzymology and the mechanism of regulation a
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Finally the identification of predictive biomarkers
2021-03-18

Finally, the identification of predictive biomarkers of response will also allow the more recently discovered CDK inhibitors to be explored in particular genetically-defined contexts, for example by building on recent observations that KRAS mutant tumors are highly sensitive to CDK1 inhibition, and
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corticosterone DDX belongs to the DEAD box family of protein
2021-03-18

DDX3 belongs to the DEAD-box family of proteins, ATP-dependent RNA helicases characterized by the presence of a highly conserved helicase core domain [13]. This catalytic core is composed of two RecA-like domains containing motifs involved in ATP binding/hydrolysis, RNA binding and helicase activity
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There are some limitations to our study
2021-03-18

There are some limitations to our study. First, the small sample size, even if comparable or higher than most studies, did not offer the possibility to consider other variables, such as frequency of use or age of onset. Second, since most subjects did not report current use, we could not analyze sep
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Urolithin A br Materials and methods br Results
2021-03-18

Materials and methods Results Discussion Adiponectin is one of the most studied adipocytokines. Its release from adipocytes is down-regulated in obesity and other adverse metabolic conditions leading to decreased serum concentrations (Turer and Scherer, 2012). Several factors and conditions
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br Introduction Hematopoietic stem cells and leukemic
2021-03-17

Introduction Hematopoietic stem Ketorolac tromethamine salt australia and leukemic stem cells (HSCs and LSCs, respectively) both have a capacity of self-renewal. Whereas HSCs give rise to all blood lineages during lifetime hematopoiesis, LSCs are responsible for the initiation and propagation o
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