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Our research has demonstrated that the absolute
2021-01-26
Our research has demonstrated that the absolute bioavailability of oxymatrine, having a similar structure with OSC, was only 6.79±2.52%. About 50% of OSC was converted to its active metabolite SC in vivo; hence, the absolute bioavailability of OSC was speculated to be poor as well [24]. Understandin
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br Conclusions When the authors joined the
2021-01-26
Conclusions When the authors joined the field of oxysterol analysis around the turn of the century, oxysterols and cholestenoic acids were mostly considered as uninteresting intermediates of cholesterol metabolism. Some oxysterols had been shown to have biological activity, but the most studied o
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br Results br Discussion Analysis
2021-01-26
Results Discussion Analysis of EBI2 expression showed that EBI2 is highly expressed in central memory CD8+ T cells that is in line with previous data from human T cells in which these Isochlorogenic acid C express higher levels of EBI2 than naive or effector memory CD8+ T cells (Hannedouche et
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br Ubiquitin Capture by the Mobile APC RING Domain Contribut
2021-01-26
Ubiquitin Capture by the Mobile APC11 RING Domain Contributes to Processive Substrate Ubiquitylation Although the rules of Ub-mediated proteolysis are only beginning to emerge, the rate and order in which different APC/C substrates are degraded during the 839 correlates with processivity of thei
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Since both the Ub and
2021-01-25
Since both the Ub and ISG15 systems are crucial for the innate immune response, many prokaryotic and viral pathogens have evolved ways to hijack them in order to create a “window-of-opportunity” for efficient replication. Several viral and bacterial proteins have been found to directly target these
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CAA is a carcinogenic metabolite
2021-01-25
CAA is a carcinogenic metabolite of vinyl chloride, forming several different DNA adducts including the cyclic Tenatoprazole adducts 3,N4-ethenocytosine (εC), 1,N6-ethenoadenine (εA), N2,3-ethenoguanine (εG), and 1,N2-ethenoguanine (1,N2-εG), with the A and C cyclic adducts the most predominant, an
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In conclusion our work provides the preclinical
2021-01-25
In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer SB408124 and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly for the treatm
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COMT expression protein level and activity are down regulate
2021-01-25
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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Our module is designed to allow in process measurement of
2021-01-25
Our module is designed to allow in-process measurement of [C]-tracer molar activity (MA, GBq/μmol at EOB) using a tankyrase detector with a UV detector at the outlet of the HPLC-portion of the system. In the HPLC chromatogram, peak analysis of the chromatographic data utilized PeakSimple software (
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br Allosteric inhibitors In general candidate drugs that bin
2021-01-25
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Evodiamine mg ERR is constitutively active in
2021-01-25
ERRγ is constitutively active in the absence of endogenous ligand. However, several synthetic ligands that can repress or induce ERRγ function by disrupting ERRγ-coactivator interactions have been reported to date. The estrogen receptor modulators diethylstilbestrol (DES) and 4-hydroxytamoxifen (4-O
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bax pathway br Materials and methods br Results and discussi
2021-01-25
Materials and methods Results and discussion Conclusions In the present study, we have shown the important role of miR-204-5p in C2C12 myoblast differentiation. Overexpression of miR-204-5p inhibited myogenic differentiation and decreased the formation of slow-twitch myofibers, whereas miR-
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br Materials and methods br Results br Discussion
2021-01-25
Materials and methods Results Discussion Cisplatin, as one member of a class of platinum-containing anti-cancer drugs, which displays a great deal of clinical activity on a wide variety of solid tumors. In addition, cisplatin often used in combination with other chemotherapy drugs to treat
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Here we report for the first time that EphB
2021-01-25
Here, we report for the first time that EphB4 contains two NLS sequences and localises to the nucleus. This is mediated via an importin-α pathway and we show that EphB4 could potentially have a direct role in gene regulation. These data provide new insight into Eph receptor localisation and action a
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Molecular docking study of compound was performed using the
2021-01-25
Molecular docking study of EW-7197 was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cyano-hydr
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