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gpr120 agonist For the SAR optimization of the right hand si
2019-09-09
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic gpr120 agonist moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by cond
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Pleuromutilin and The cyclin dependent kinase deactivation
2019-09-09
The cyclin-dependent kinase deactivation is carried out by a particular group of proteins cyclin-dependent kinase inhibitors (CDKIs). These group of proteins blocks kinase activity by interfering with the interaction of cyclin-CDK complex [43]. The inhibition of CDK naturally occurs during a G1 phas
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Data from our in vitro
2019-09-09
Data from our in vitro studies using BEAS-2B cells showed a biphasic response of cells to NNK. The initial phase of decrease in CRM1 expression in NNK-exposed cells was observed in our previous study. In this study, we further showed that p-p53 (Thr55) expression was also decreased during this initi
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br Materials and methods br Results br Discussion Consistent
2019-09-09
Materials and methods Results Discussion Consistent with previous reports (Barr et al., 2010, Vuong et al., 2010), the current study demonstrates that rats treated with amphetamine exhibit heightened anxiety states during withdrawal. Furthermore, icv. infusion of a CRF2 receptor antagonist
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The detection of galactomannan GM a polysaccharide that is r
2019-09-09
The detection of galactomannan (GM), a polysaccharide that is released during Aspergillus growth, is a useful and reliable non-invasive diagnostic test for screening and management of aspergillosis and is often more sensitive than culture (Schelenz et al., 2015, Fisher et al., 2013). The level of ga
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The data correlations from Multiflash
2019-09-09
The data correlations from Multiflash™ [43] and DIPPR [44] were used for the liquid volume and heat of vaporization. For vapour pressure the curves were regressed from the experimental data present on both the DIPPR [44] and TRC [45] databases. As for liquid heat capacities both the latter databases
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The inhibition of CYP activity
2019-09-09
The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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Also important in binding of E
2019-09-09
Also important in binding of E2 to the ER is the hydroxyl on the D ring, which has a stabilizing contact with His-524 in ERα (Fig. 7) and with His-475 in ERβ (Fig. S1) [8,9,36,37]. The spatial relationship of the functional groups on the A and D rings on E2 has been used to develop chemicals contai
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Today many strategies have been developed to
2019-09-07
Today, many strategies have been developed to enhance CXCR-4 receptor GSK2292767 kinase on the cell surface, either by modifying the cell culture medium or by modifying the CXCR-4 gene in BMSCs to stimulate stem cell recruitment (Jiang et al., 2012, Liu et al., 2014b). For instance, the pre-conditi
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The data correlations from Multiflash and DIPPR were
2019-09-07
The data correlations from Multiflash™ [43] and DIPPR [44] were used for the liquid volume and heat of vaporization. For vapour pressure the curves were regressed from the experimental data present on both the DIPPR [44] and TRC [45] databases. As for liquid heat capacities both the latter databases
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VHb expression in recombinant E coli expressing P
2019-09-07
VHb expression in recombinant E. coli expressing P4H improved Hyp production, presumably by enhancing oxygen transfer. VHb expression contributed to improving growth and extending the period of exponential growth in both shaker flask culture and bioreactor fermentation. A similar phenomenon was also
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In contrast irinotecan has shown much less myelosuppression
2019-09-07
In contrast, irinotecan has shown much less myelosuppression and may be more active in Ewing sarcoma both alone and in combination with temozolamide. One phase II study of 13 heavily pretreated Ewing sarcoma patients demonstrated a response rate of 38% including 2 complete responses (Bisogno et al.,
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Given the potency enhancing effect of the butyl
2019-09-07
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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br Oxidoreductase like MEM for prodrug activation br Future
2019-09-07
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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br Materials and methods br Results br
2019-09-07
Materials and methods Results Discussion Although some conditioning therapies have provided satisfactory clinical outcomes, mammalian species have little or no ability to replace injured cardiac tissue [34]. Therefore, therapeutic strategies based on the prevention, rather than treatment af
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