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Considering all these facts in the present study we
2021-04-15
Considering all these facts, in the present study, we investigated the effects of two highly selective CRF receptor 2 antagonists (antisavaugine-30, ASV-30; and astressin-2B, AST-2B) on anxiety behavior in rats. The rationale for such an experimental approach was based on the premise that fear and s
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br Results br Discussion Drug resistance poses the greatest
2021-04-15
Results Discussion Drug resistance poses the greatest hurdle of achieving high efficacy with AADs in cancer patients. AAD-treated cancer patients often encounter intrinsic and evasive drug resistance that diminishes the therapeutic efficacy to only minor survival benefits in most cancer types.
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Haggar et al reported the synthesis of
2021-04-15
Haggar et al. reported the synthesis of two new series of 8-(2-imino/oxo/thioxo pyrimidin-4-yl)-4-methyl-6-nitro-2-oxo-2H-chromen-7-yl benzoates 56 (X=O, S, NH) and 8-(pyrazol-3-yl)-4-methyl-6-nitro-2-oxo-2H-chromen-7-yl benzoates 57 [Y=C(O)CH3, 2,4-(NO2)2C6H3]. The 8-acetyl-4-methyl-6-nitro-2-oxo-2
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Due to the results of
2021-04-15
Due to the results of the experiment we decided to deploy our cloud service infrastructure with two platform-independent servers instead of one or three. This decision was based on two factors: (a) the use of more than one server is useful to avoid a bottleneck in the system, and (b) using more than
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Since protein kinase CK has over known substrates
2021-04-15
Since protein kinase CK2 has over 300 known substrates we examined if the inhibitory effects described above could also be detected using another substrate. Therefore, we employed the synthetic peptide RRRADDSDDDDD which is often used in CK2 inhibitory studies. Quite contrary to the phosphorylation
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br Materials and methods br
2021-04-15
Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen
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The four other mutations S
2021-04-15
The four other mutations (S281T, V317I, T328A and A329S) were not detected in the absence of the A286S. This could suggest that when all of them are present, there would be a tri-dimensional structural modification that would interfere with the binding of the insecticide and produce different levels
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br Results and Discussion br Conclusion
2021-04-15
Results and Discussion Conclusion What we have shown here is that highly specific antagonist can be a very useful tool, can mimic gene KO experiments or even further dissect receptor function. We just took ETA antagonist as an example and found that ETA mediates physiological closure of DA whi
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br Materials and methods br Results br Discussion
2021-04-15
Materials and methods Results Discussion We have evaluated the breast cancer prevention potential of PR blockade under conditions that included exposure to progestogens that are relevant to women (progesterone and MPA) and are known to differ in their receptor-binding and down-stream effect
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Another milestone in the field is the de
2021-04-15
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of aldehyde dehydrogenase , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pat
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br Introduction Prostaglandin E PGE
2021-04-15
Introduction Prostaglandin E2 (PGE2) signals through 4 separate G-protein coupled receptor sub-types (EP1, EP2, EP3 and EP4) to elicit a variety of physiological and pathophysiologic effects. EP2 and EP4 increase cAMP levels in the cell via adenylate cyclase activation, whereas EP3 inhibits cAMP
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Three kinase inhibitors dasatinib type
2021-04-15
Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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In conclusion we provide convincing evidence
2021-04-15
In conclusion, we provide convincing evidence that the PRRSV-induced SGs are indeed bona fide SGs. While we determined that mRNA is present in the PRRSV-induced SGs, we did not distinguish its origin. Future studies will need to determine whether the mRNA stored in PRRSV-induced SGs is of cellular
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br Competing interests br Acknowledgments
2021-04-15
Competing interests Acknowledgments This work was supported by grants from Fujian Fujian Provincial Natural Science Foundation (2016J01612). Introduction Cancer is still one of the most serious diseases in the world. According to the World Health Organization (WHO), cancer is the second mo
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Likewise the conserved cysteine in
2021-04-15
Likewise, the conserved cysteine in the E2 protein is the only residue shown to be essential for the transfer of Ub/Ubl from E2 to the HECT ligases (Dye and Schulman, 2007, Wu et al., 2003). However, all other terminal Ub/Ubl transfer reactions involving E2 enzymes suggest a critical role for the ta
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