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br Future perspectives Understanding how peptides
2021-03-15
Future perspectives Understanding how peptides are degraded, particularly those which may be therapeutically useful, such as GLP-1, has proved to be invaluable in providing a rationale for the development of a novel class of therapeutic agents. However, while DPP-4 plays an important role in the
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br Conclusion The role of DNA PK target in DNA
2021-03-15
Conclusion The role of DNA-PK target in DNA DSB repair renders this Liproxstatin-1 kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for desi
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br DGKs inhibition and signaling Local DAG levels are strict
2021-03-15
DGKs inhibition and signaling Local DAG levels are strictly controlled by a balance between synthesis and degradation rates. Both receptor controlled PLC-mediated production and DGK-mediated degradation are classically implicated in the control of “signaling” DAG. However, this dogma is starting
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Analysis of Table shows that compound b
2021-03-15
Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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The present study provides the
2021-03-15
The present study provides the first evidence that the human uroepithelial eht library mg in vitro respond directly, within 48h, to this carcinogen by promoting extensive vacuolation and DAPK expression. By using the TEM, ICC and Western blotting, we found that the arsenite-induced vacuoles were de
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Presumably LBPs have health promoting activities such as
2021-03-15
Presumably, LBPs have health-promoting activities, such as antioxidant, immune regulation, anti-stress, anticancer, neuroprotective and antidiabetic activities [[7], [8], [9], [10], [11]]; LBPs can improve the whole-body health status of mice and stimulate the expressions of IL-2, IL-12 and TNF-α,
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br Acknowledgements These studies were supported
2021-03-15
Acknowledgements These studies were supported by a research grant from the NIH (R01 AR065594) to C. Putterman. Introduction Macrophages integrate and adapt to their locally encountered cytokine and chemokine milieu. In tumors characterized by an unresolving inflammation, the tumor cell-killin
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Acknowledgments br PGD is an aracha http
2021-03-15
Acknowledgments PGD is an arachadonic acid-derived prostaglandin produced in large quantities when asthmatic lung tissues are challenged by allergens. PGD contracts the airway tissue as well as stimulating an inflammatory response. PGD was also found to be the ligand for a second receptor, DP2 (
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br Materials and methods br
2021-03-13
Materials and methods Results Discussion Recently it has been found that prostaglandins play an important role in modulating the host immune system [1,3,22,23], and some parasites produce these eicosanoid mediators to survive into their hosts [6,[10], [11], [12],24,25]. The discovery that p
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To further verify the effect of BBR on ACAT protein
2021-03-13
To further verify the effect of BBR on ACAT2 protein expression, we have conducted an in vitro permeability assay using Caco-2 monolayer. This assay has long been used to predict the in vivo 3MB-PP1 synthesis and bioavailability of a compound. It was observed that the amount of cholesterol esters i
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The phenolic hydroxyl group of ezetimibe
2021-03-13
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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In some pancreatic and non
2021-03-13
In some pancreatic and non-pancreatic tissues, the chloride and calcium channels are heavily regulated by phosphorylation by protein kinases, such as PKC, cyclic AMP-dependent protein kinase (PKA), PKCaMKII, PI3K and protein tyrosine kinases [7,36,37]. Since the interaction of triterpenes with recep
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Determination of relative potency EC
2021-03-13
Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an
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More importantly Santagata et al have suggested a new
2021-03-13
More importantly, Santagata et al. have suggested a new breast cancer subtyping method according to ER, androgen receptor (AR), and VDR with a higher prognostic value than the ordinarily used method based on ER, progesterone receptor (PR) and Her2 (Santagata et al., 2014). This implies that such com
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At one time the biological effects of cAMP were
2021-03-13
At one time, the biological effects of cAMP were thought to be mediated exclusively by Protein Kinase A (PKA). Consistent with this, PKA inhibitors have been shown to reverse the effects of cAMP-elevating agents on VSMC proliferation [5]. However, we recently reported that cAMP-mediated inhibition o
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