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Enlarging the ligand binding pocket
2019-08-19
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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Considering these reports and with the aim of
2019-08-19
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b
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During the course of enzymatic digestion
2019-08-19
During the course of enzymatic digestion, protein is digested into large peptides and these large peptides are then further digested into small fragments. αs1-Casein f15–39, which contains 25 amino perk inhibitor residues was the longest iTRAQ-labelled peptide identified in the samples digested wit
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As CP is a crucial player in centriole duplication
2019-08-19
As CP110 is a crucial player in centriole duplication, it is intriguing to ask whether centriole duplication would also be affected in the absence of the CP110-stabilizing effects of USP33. Li et al.[4] found that USP33 depletion did not inhibit normal centriole duplication through loss of centriole
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br Materials and methods br Results br Discussion The
2019-08-19
Materials and methods Results Discussion The 5-HT2A and D2 receptors have a functional crosstalk (Albizu et al., 2011) and they formyl are all richly expressed in the mesolimbic and mesocortical systems (Azmitia and Segal, 1978; McMahon et al., 2001), providing the neuroanatomical basis fo
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After activation AKT phosphorylates target proteins involved
2019-08-19
After activation, AKT phosphorylates target proteins involved in cell growth, metabolism and survival (Manning and Cantley, 2007). For example, AKT phosphorylates the pro-apoptotic protein BAD, preventing it from binding to and inactivating Bcl-xL in mitochondria (Datta et al., 1997). In turn, Bcl-x
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ZLN005 formula Given that CE plays an essential role in schi
2019-08-19
Given that CE plays an essential role in schistosome invasion, its immunoreactivity and protective potential is of significant interest. The native form of SmCE was found to be poorly immunogenic in immunized mice. An earlier study found that sera from S. mansoni patients have shown the presence of
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br DAG kinase activity is
2019-08-19
DAG kinase activity is confined to specific cell compartments A number of reports demonstrating agonist-dependent translocation of DGKs to distinct membrane compartments suggest that DGK activity is restricted to localized DAG pools generated after activation of receptors. Perhaps the best eviden
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The preferences for source of FAs for
2019-08-19
The preferences for source of FAs for DGAT1 and DGAT2 are related to their membrane topologies, subcellular locations, interactions with other proteins or organelles (discussed in the former section), and their differential expression, substrate specificities, and enzyme kinetics. According to UniPr
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Currently it is not known
2019-08-19
Currently, it is not known if drought induces changes in the cysteine protease BI-9564 of soybean nodules. The available annotation of the soybean genome, in Phytozome (www.phytozome.net) has identified 706 C1 cysteine protease sequences and 75 C13 cysteine proteases. We have previously reported ex
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br Conclusion The results of the
2019-08-19
Conclusion The results of the present study demonstrate that cysteinyl leukotrienes LTC4, LTD4 and LTE4 cause moderate to marked whereas the dihydroxy leukotriene LTB4 causes small muscle contraction in the stomach in vitro. The LTD4-induced contraction is mediated by CysLT1 in fundus but by CysL
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Compounds were screened for their activity against the hERG
2019-08-19
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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Regarding the mechanism of action of CRF several studies
2019-08-19
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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The AURA trial was a phase I II study evaluating
2019-08-17
The AURA trial was a phase I/II study evaluating the safety, tolerability and activity of Osimertinib in patients with EGFR-mutated NSCLC progressing after a previous EGFR TKI. The phase I component of the study included a dose escalation part (Osimertinib 20mg to 240mg), using a rolling six design,
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Here we were able to
2019-08-17
Here, we were able to show for the first time that stimulation of VSMCs with two different growth factors resulted in a dramatic decrease in gp130mRNA expression occurring four to six hours after stimulation with Ang II and PDGF-BB. The mRNA level remained extremely low within 12 hours after stimula
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