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Collectively our results indicate that GSK A
2019-11-14

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 (Fig
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Despite the important agronomic traits regulated by SUMO mos
2019-11-14

Despite the important agronomic traits regulated by SUMO, most research studies on SUMOylation have been mainly limited to model plants, such as Arabidopsis and rice (Wang et al., 2011), due to the lack of molecular tools specific to other economically relevant plants. On the other hand, plants harb
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Next we evaluated whether DPP inhibitor
2019-11-14

Next, we evaluated whether DPP-4 inhibitor suppressed osteoclast formation by downregulating LPS-induced RANKL expression in stromal cells; DPP-4 inhibitor did not inhibit LPS-induced RANKL expression. Furthermore, we evaluated the effect of DPP-4 on LPS-induced RANKL expression in stromal cells, bu
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Indeed the alkyl group is not seen
2019-11-14

Indeed, the -alkyl group is not seen in the original crystallographic electron density omit map prior to positioning either inhibitor in DHODH, nor can it be found in the final maps. Rather, the electron density maps are consistent with hydrolysis of the amide to the acid. Once the scaffold was cle
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In order to derive a better understanding of the
2019-11-14

In order to derive a better understanding of the results from our SAR study, we utilized Glide to model the binding of the SAR compounds with the non-active site pocket of TS-DHFR shown in C. The majority of models position the phenolic moiety of these compounds within the non-active site pocket, wh
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mu opioid receptor antagonist br Materials and methods br Re
2019-11-14

Materials and methods Results Discussion In this study we characterized in more detail the interrelationship between the expression levels of the B. malayi Bm-cpl-3 and Bm-cpl-6 cysteine proteases and the fitness of Wolbachia, and consequently that of the parasite. Our present in vitro data
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br Materials and methods br Results The BUN
2019-11-14

Materials and methods Results The BUN and creatinine levels in the saline-treated CRF group were found to be significantly higher than those in the sham-operated control rats treated with either montelukast or saline (p damage (pand atipamezole tissues, were found to be significantly higher in
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Raloxifene is a second generation SERM that has tissue speci
2019-11-14

Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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br Materials and methods br Results br Discussion Our
2019-11-14

Materials and methods Results Discussion Our previous study showed that ERRγ negatively regulates osteoblast differentiation via inhibiting Runx2 transactivity (Jeong et al., 2009). In the present study, we found that ERRγ also induced miR-433 in osteogenic mesenchymal cell lineage C3H10T1/
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In the present study promoting bile acid synthesis by
2019-11-14

In the present study, promoting bile membrane transport synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for liver t
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Furan analogs and N methylpyrrole analogs had completely
2019-11-14

Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 Cucurbitacin I affinity and an increased antagonist activity, while the corresponding chemical mo
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Digoxin br Acknowledgements This research was supported by S
2019-11-14

Acknowledgements This research was supported by Slovenian Research Agency (ARRS). We thank prof. R. Marinšek Logar for helpful advice, Dr. T. Kranjc for help with data management, N. Vrhovnik and G. Lavrič for technical help with preliminary growth experiments and dr. J. Burkeljca for help with g
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Ample evidence has shown that ET
2019-11-14

Ample evidence has shown that ET-1 system plays a pivotal role in the development of cardiovascular anomalies and pharmacological inhibition of ETA prevents the development of cardiac hypertrophy [[37], [38], [39]]. Yanagisawa and coworkers, who first reported the cardiomyocyte-specific endothelin A
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For this study we have used
2019-11-14

For this study we have used the intermediate affinity mutant antigen HEL2× for immunization. However, we have observed a similar defect in the plasmablast differentiation of EBI2-deficient SWHEL IY-5511 over a 10,000-fold affinity range by using WT HEL or the low-affinity mutant HEL3× (data not sho
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Since both the Ub and
2019-11-14

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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