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To further verify the effect of BBR on
2020-08-10

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 egfr pathway and bioavailability of a compound. It was observed that the amount of cholesterol esters in the
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We observed the IVM potentiation of currents induced by
2020-08-10

We observed the IVM potentiation of currents induced by the EC5 of Glu or GABA and the IVM inhibition of currents induced by the EC90 of Glu or GABA in wild-type GluCls and GABACls. The EC50 of IVM for the potentiation in GluCls was 3.5-fold smaller than that in GABACls (Fig. 4, Fig. 8B, Table 2), a
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Building s constructional elements should
2020-08-10

Building\'s constructional elements should be able to protect residents from the negative effect of noise caused by surroundings [19]. The World Health Organization estimates that each year more than one million Healthy Life Years are lost in the European Union member states and other Western Europe
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N Cyclopentylmethyl analog exhibited fold less potent recept
2020-08-10

N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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PR619 In this study we have explored a
2020-08-10

In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta
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Mulan is one of three E ubiquitin ligases that are
2020-08-09

Mulan is one of three E3 ubiquitin ligases that are present in the mitochondria along with MARCH5/MITOL (membrane associated RING-CH5) and RNF185 [14], [15], [16], [17]. Mulan is a 352-residue polypeptide that crosses the mitochondrial outer membrane (OMM) twice, its amino-terminus, which includes t
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br Estrogen receptors activate mGluR
2020-08-08

Estrogen receptors activate mGluR signaling pathways In order to distinguish the opposing effects of estradiol on CREB phosphorylation, we turned to a “bottom-up” approach, working backwards from CREB phosphorylation to pharmacologically isolate the two signaling pathways (Boulware et al., 2005).
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Since clinical studies mostly involved cases that used MPA
2020-08-08

Since clinical studies mostly involved cases that used MPA, data from studies that examined other types of progestogens are very limited. While the WHI study examined the combination of conjugated equine estrogens plus MPA [1], the Million Women Study [2] that also demonstrated an increased risk of
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Finally by injecting zymosan A into
2020-08-08

Finally, by injecting zymosan A into the hindpaw the contribution of EP1 to pain sensitization was studied in a model that resembles a more complex natural inflammation (). This was particularly important as the expression of EP receptors might change during inflammation. In wild-type mice, zymosan
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We next focused our design building into the
2020-08-07

We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po
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Epac proteins consist of a carboxyl terminal
2020-08-06

Epac proteins consist of a carboxyl-terminal catalytic region and an amino-terminal regulatory region, which harbors one cAMP-binding domain in Epac1 and two in Epac2 [22], [32], [51]. In the absence of cAMP, the regulatory region covers the CDC25-homology domain and autoinhibits Epac\'s enzymatic a
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Inasmuch as hepatocytes are initially refractory to the enzy
2020-08-06

Inasmuch as hepatocytes are initially refractory to the enzyme inducing effects of CYP450 inducers, cultures must be maintained for at least 36–48 h before treatment with test articles and/or known CYP450 inducers, at which time the hepatocytes are expressing liver-specific genes and a near-normal m
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br Conclusions First it should be noted that even
2020-08-06

Conclusions First, it should be noted that even though non-linagliptin DPP-4 inhibitor SPCs specified thresholds for dose adjustment in CrCl via the use of the Cockcroft-Gault formula at the time of the patients’ treatment, in January 2018, the sitagliptin SPC was changed to include glomerular Za
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According to the docking study results
2020-08-06

According to the docking study results, the difference in biological activity of the tested compounds despite of their similar chemical structure could be explained. For the active molecules like 26, the presence of aromatic substituent with its conformational freedom seems to be crucial for the int
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br Results and discussion To check the hypothesis
2020-08-06

Results and discussion To check the Index Kit 2 that the charge of α-synuclein can be altered due to the glycation, we measured zeta potential of native α-synuclein and α-synuclein glycated by two different glycating agents, methylglyoxal (MG) and glyceraldehyde-3-phosphate (GA-3-P). The value f
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