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Determination of relative potency EC
2020-03-13
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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This work started from the standard version of the
2020-03-12
This work started from the standard version of the CPA model [17] and investigated its known weaknesses: 1) not meeting the defined critical temperature, 2) missing the temperature dependence of pure component saturated liquid densities, 3) using an α function in the cubic term that can provide unre
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Kim et al reported for bioactive
2020-03-12
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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As the COMT enzyme is primarily
2020-03-12
As the COMT enzyme is primarily related to prefrontal dopamine degradation (e.g., Yavich et al., 2007), the present study supports the notion that prefrontal dopamine modulates retention of fear extinction rather than within-session extinction (Abraham et al., 2014). Consistent with other studies we
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Tyrphostin 9 Renal injury by cisplatin has
2020-03-12
Renal injury by cisplatin has been associated with oxidative stress, inflammation, and apoptosis (Francescato et al., 2007, Iseri et al., 2007, Kiymaz et al., 2008, Ueki et al., 2012). Specifically, apoptosis is an important mode of cell death in cisplatin nephrotoxicity, and many studies including
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Adding MPA or NETA we
2020-03-12
Adding MPA or NETA we found no impact on the estradiol-induced downregulation of serum-stimulated endothelin synthesis in vitro [40]. Progesterone was also able to inhibit the angiotensin II-induced increase in endothelin production [41]. Several clinical studies on the effect of oral or transdermal
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br Author contributions br Funding M E B was
2020-03-12
Author contributions Funding M.E.B. was supported by Research Fund #3096. Competing interests Introduction Lung cancer has become one of the most common death causes in both male and female malignant tumors (Jemal et al., 2011). Air pollution, smoking and estrogen level are known risk f
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First of all two assumptions just as
2020-03-12
First of all, two assumptions just as in Ref. [30] are need to simplify the penetration process: (1) The crater phases is short and the Ki16198 of EFP is consumed little; thus, the influence of crater on penetration can be ignored; (2) the initial stagnation radial pressure is equal to axial pressu
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We further analyzed the transcriptional mechanisms underlyin
2020-03-12
We further analyzed the transcriptional mechanisms underlying the synergistic action of IL-23 and PGE2 and found that this action is mediated by not only STAT3 but also CREB1 and NF-κB. Involvement of CREB1 is analogous to that in the PGE2-EP2/EP4–mediated Il12rb2 induction during TH1 cell different
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Previous studies demonstrated that cPLA
2020-03-12
Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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A factor that complicates the use of human liver cells
2020-03-12
A factor that complicates the use of human liver Glyoxalase I inhibitor australia is one of variability, which arises in part because many of the human liver samples available for research show various stages of a variety of disease states (steatosis (fatty liver), cirrhosis, carcinogenesis in adja
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Historically covalent drugs have had
2020-03-12
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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br Introduction br Structure of the Ku heterodimer associate
2020-03-11
Introduction Structure of the Ku heterodimer associated to DNA The atomic structure of the Ku heterodimer, alone and bound to a small DNA fragment, was recently determined (Walker et al., 2001) and has significantly improved our understanding of DNA recognition by DNA-PK holoenzyme (Fig. 3). B
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An even more striking difference is observed when comparing
2020-03-11
An even more striking difference is observed when comparing active site residues, which are evolutionarily very well conserved in other soluble PPases 18, 19. In 31 known PPase sequences, 13 functionally important active site residues are conserved in all sequences, but only two of them (D70 and D97
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The first transcription factor TF known to interact with one
2020-03-11
The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone SCH 58261 of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed development
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