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Determination of relative potency EC
2019-11-02
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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Not all of the biological activities exhibited
2019-11-02
Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the CHIR-090 is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the cell to respond to
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EP EP and EP receptor expression on HMVEC L was
2019-11-02
EP1, EP3 and EP4 receptor expression on HMVEC-L was shown recently by flow cytometry [14]. However, only EP4 mRNA expression was previously described in these cells [49]. Our data obtained with RT-PCR showed EP4 mRNA and very low levels of EP1 mRNA, but no EP2 and EP3 mRNA expression was detectable
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br Conclusions Nanoparticles can be used to modulate
2019-11-02
Conclusions Nanoparticles can be used to modulate the catalytic activity of various industrially and clinically useful enzymes, as well as pH, temperature and storage stabilities, which will enable the process to occur more efficiently and less costly. The interaction between an enzyme and nanopa
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This study showed that ER redox disturbance associated ER
2019-11-02
This study showed that ER-redox disturbance-associated ER stress is linked to cytoplasmic chaperone signaling, including HSP90 stability and its client protein, eNOS. The highly increased PERK and IRE-1α lead to dissociation with the chaperone protein, thereby decreasing HSP90 stability (Fig. 5B). S
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DDR was originally cloned by the group of Michele de
2019-11-01
DDR1 was originally cloned by the group of Michele de Luca, at the time named TrkE. The Genoa-based research team identified the skin, and the keratinocytes in particular, as a major site of DDR1-binding activity [20]. DDR1 is also expressed in kidney, liver and lung (Fig. 2). The functional role of
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A range of therapies exists for the treatment of inflammatio
2019-11-01
A range of therapies exists for the treatment of inflammation-driven diseases, which can be summarized as non-steroidal anti-inflammatory drugs (NSAIDs), corticoids and steroidal-related drugs (Ward et al., 2008). Despite of these notable successes, there are still major unmet medical needs in the t
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The structures of the set of pyrazoles of
2019-11-01
The structures of the set of pyrazoles of are contained in the supplied with this manuscript. Acknowledgments Prostaglandin D (PGD) is known to bind with high affinity to two G protein-coupled seven-transmembrane receptors DP1 and DP2. The latter receptor, also known as CRTH2 (chemoattractant
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Allele specific methylation has been observed
2019-11-01
Allele-specific methylation has been observed in CpG islands of imprinted genes.27, 32 In the present study, however, methylation of CpG1 was specific to ALL BAY 61-3606 dihydrochloride australia and occurred in the leukemia cells of 28% of children with ALL, but it was not found in normal leukocyt
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grazoprevir br Halogenases Enzymatic C H activation leading
2019-11-01
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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br Results and discussion br Conclusion
2019-11-01
Results and discussion Conclusion Based on the structure of ThDP, in this study, a series of novel ThDP analogs 6a-6g and 8a-8g were designed by optimizing triazole-benzene linker and modifying the substituent group of triazole ring. Then they were synthesized as potential inhibitors of Cy-PDH
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naloxone hydrochloride br Conclusions Overexpression of DDR
2019-11-01
Conclusions Overexpression of DDR2 might contribute to tumor progression in lung SQCC, and the T681I mutation we found in this work is an inactivating mutation. There is a possibility that not only activating mutation but also overexpression of DDR2 might be a molecular target for treatment of l
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Previous studies revealed the expression of the
2019-11-01
Previous studies revealed the expression of the CCR3 receptor in neurons and its neuroprotective function using mice lacking CCR3 expression (Wainwright et al., 2009). The regulation of CCR3 receptor expression in the microglia and astrocytes was shown in neurological disorders and has been demonstr
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Based on the finding described above
2019-11-01
Based on the finding described above, the present study was designed to investigate the effects of specific CRF receptors, CRF1 and CRF2, in the BLA and CeA on the duration of TI in guinea pigs (Cavia porcellus). To this end, we evaluated whether administration of the CRF1 LJH685 antagonist CP-3763
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The second constraint indicates that if the relationship bet
2019-11-01
The second constraint indicates that if the relationship between two components A and B is two-way, then there are at least two connectors, one with origin A and destination B, and another connector with origin B and destination A (OCL2 of Fig. 4). Therefore, at least one output port of the first co
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