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Determination of relative potency EC by
2021-03-11
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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Estrogen receptor related receptor ERR like
2021-03-11
Estrogen receptor-related receptor γ (ERRγ), like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor, though unlike ERRα and β, it is more selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal musc
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br Epac in cardiovascular pathophysiology Epac orchestrates
2021-03-11
Epac in cardiovascular pathophysiology Epac orchestrates signaling actors that regulate fundamental cellular functions and general biological effects. However, some important gaps still remain in the knowledge of the physiopathological role of Epac in the heart. So far, Epac has been implicated i
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Upon Edn ligand binding endothelin receptors can
2021-03-11
Upon Edn ligand binding, endothelin receptors can induce a variety of intracellular signaling cascades leading to diverse cellular responses such as contraction in the case of smooth muscle cells, or cell growth and mitogenesis. Ednrs are expressed in a variety of cell types and tissues, for example
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While agnathans appear to have reduced their
2021-03-11
While agnathans appear to have reduced their Ednr repertoire to the Ednra gene (that may have been amplified in the Arctic lamprey), gnathostomes in general have been relatively inert to Ednr gene loss. Strikingly, the only Ednr gene that has been lost repeatedly is EdnrB2 (lost in therian mammals,
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The enantiomeric ratio ER of chiral compounds accumulated
2021-03-11
The enantiomeric ratio (ER) of chiral compounds accumulated in organisms has been found to be different among species (Borga and Bidleman, 2005, Harner et al., 1999, Warner et al., 2005, Wiberg et al., 2000), indicating enantioselective accumulation of chiral compounds are species-specific. The ER
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Collectively our results indicate that GSK A
2021-03-11
Collectively, our results indicate that GSK682753A functions as a competitive antagonist and binds to the receptor in the same region as 7α,25-OHC. First, we observe linearity in the Schild plot analysis (Fig. 2B). Second, GSK682753A is highly dependent on F111 at position III:08/3.32 in TM-III (Fi
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In the SUMOylation pathway SCE
2021-03-11
In the SUMOylation pathway, SCE1 as an E2 enzyme has an important role in mediating the conjugation of SUMO to target proteins. The accumulated SUMO conjugates in plants are associated with abiotic stress responses (Castro et al, 2012). We performed a drought stress analysis on WT plants, induced by
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Advances in the total chemical
2021-03-11
Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functio
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The inhibition of DNMT using
2021-03-11
The inhibition of DNMT1 using 5-AZA-dC or DNMT1 siRNA increased TIMP2 protein and mRNA expression, suggesting that TIMP2 expression is down-regulated by DNA methylation in the HDFs. In addition, 5-AZA-dC treatment led to a dose-dependent decrease of DNMT1 protein expression. 5-AZA-dC is a cytosine a
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NMR was employed for the determination of un ligated domain
2021-03-10
NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a
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The absorption rate of polyphenols into the body
2021-03-10
The Cholera Toxin rate of polyphenols into the body is usually low. For example, the absorption rate of epigallocatechin gallate (EGCG), an active component in GP, is approximately 1% (Chen et al., 1997). To increase absorption of GP in the body, people have been increasing their intake of function
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br Introduction Analyses of genomic alterations in cancer ha
2021-03-10
Introduction Analyses of genomic alterations in cancer have identified epidermal growth factor receptor (EGFR) as one of the most potent “oncogenic driver” kinases that is present in many epithelial tumors including endometrial, breast, prostate, skin, esophagus, lung, stomach, colorectal, and re
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br Materials and methods br Results br Discussion In our
2021-03-10
Materials and methods Results Discussion In our tissue array, we demonstrated that 14-3-3 tau mRNA and protein expression levels decreased in the preeclamptic placentas. 14-3-3 proteins are considered to be important in the functional regulation of trophoblasts and maybe associated with adv
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Coumarins also known as benzopyran ones are a family of
2021-03-10
Coumarins also known as benzopyran-2-ones are a family of nature-occurring lactones first isolated from Tonka beans in 1820. They are an important class of oxygen containing heterocycles widely found in nature, so much so that they have been routinely employed as herbal remedies since early days. Ov
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