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br Conclusions Enzyme can be delivered
2019-12-11
Conclusions Enzyme can be delivered to the tumour by using humanised or fully human Celastrol or even loaded into synthetic nanospheres produced from silica [64] or liposomally entrapped [65]. For any future ADEPT developments, a number of basic points need to be considered. As immunogenicity ha
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In the present study we
2019-12-11
In the present study, we investigated the deeper role of eNOS in the pathogenesis of nasal polyps and analyzed the influence of 1,8-cineol on nasal polyp gene and protein expression of eNOS in vitro. Different studies dealt with the localization and expression of eNOS in nasal polyps and nasal mucos
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Another clinical study indicated the daily consumption of gr
2019-12-10
Another clinical study indicated the daily consumption of green tea with low concentrations of theanine and catechin would improve cognitive function (Ide et al., 2014). Further, in a double blind randomized clinical study involving 102 patients, the Hypericum extract was examined in terms of effica
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While agnathans appear to have reduced their Ednr repertoire
2019-12-10
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 total reduced glutathione content was determined in both
2019-12-10
The total reduced glutathione content was determined in both triptolide to examine whether retinol was decreasing glutathione concentrations and thus decreasing the conjugation of NAPQI. Total hepatic (3.9±0.3 vs 4.9±1.0 μmol/g, retinol vs untreated, respectively) and renal (0.4±0.1 vs 0.2±0.1 μmol
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Till date several predictive models have been
2019-12-10
Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow
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Ultrasound is an acoustic wave with
2019-12-10
Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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br Materials and methods br Result and discussion qRT PCR
2019-12-10
Materials and methods Result and discussion qRT-PCR was utilized to explore the effect of acetamizuril on the mRNA level of enolase. The results were analyzed according to the Livak 2−ΔΔCT method (Schmittgen and Livak, 2008): the mean CT of the enolase in treated and untreated samples was 29.8
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When six chemical inhibitors were
2019-12-10
When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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Solasodine receptor Interestingly our analyses of human PBMC
2019-12-10
Interestingly, our analyses of human PBMCs using a monoclonal antibody against EBI2 showed that the expression pattern of human EBI2 is largely overlapping with that in mice. Especially Th17 Solasodine receptor showed homogeneous high expression of EBI2 compared with Th1 cells, which contained a fr
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Given that dimethylamine substitution was tolerated as in SR
2019-12-09
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated protease activated receptor amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version
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In our former work our interest was in
2019-12-09
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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For the current studies we used the selective Epac agonist
2019-12-09
For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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br Halogenases Enzymatic C H activation leading
2019-12-09
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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Enhanced responses to varying concentrations of bronchoconst
2019-12-09
Enhanced responses to varying concentrations of bronchoconstrictors, such as MCh, and airway obstruction are characteristic of cdk9 inhibitor and common to other clinical states, including chronic obstructive pulmonary disease, lung transplantation, and infection- or chemical agent-induced airway i
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