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Three kinase inhibitors dasatinib type I imatinib type II an
2020-06-29
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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We propose the following model for how B cell
2020-06-29
We propose the following model for how B cell-guiding EBI2 ligand gradients are established in lymphoid tissues. CH25H and CYP7B1 are needed in radiation-resistant stromal cells, are abundantly expressed and active in CXCL13+ and CCL21+ FRCs, but not lymphocytes, and are poorly expressed in the inne
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(±)-CPSI 1306 While a number of studies have helped elu
2020-06-29
While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub (±)-CPSI 1306 specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in governing s
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Due to the high attractiveness of
2020-06-29
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), TC-I 15 sale (Davydov et al., 2004, Huang et al., 2005, Kenten et al., 2005,
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Regarding eicosanoid production iPLA VIA appears in
2020-06-28
Regarding eicosanoid production, iPLA2-VIA appears, in general terms, not to play a major role in mediating this response in innate immunity and inflammation, as evidenced by the large number of studies highlighting the lack of effect of selective inhibition of the enzyme in stimulus-induced AA rele
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Importantly MPO is not only a marker of cardiovascula
2020-06-28
Importantly, MPO is not only a marker of cardiovascular disease but also emerges as a critical mediator of vascular inflammatory disease: Liberated MPO binds to the endothelium in a leukocyte-independent manner, is subsequently taken up by the endothelium and transcytoses and accumulates in the sube
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br Conflicts of interest br Acknowledgements This work was s
2020-06-28
Conflicts of interest Acknowledgements This work was supported by the Swiss National Science Foundation No 31003A-179400 to AO. We thank Dr. Thierry Langer, University of Vienna and Inte:Ligand GmbH, for providing the LigandScout Software, and Dr. Daniela Schuster, Paracelsus Medical Universit
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Based on our studies presented above
2020-06-24
Based on our studies presented above, atipamezole can be used as a new in vitro and in vivo tool 95 9 mg as a pan-CYP inhibitor for CYP mediated metabolism study. It carries many unique characteristics compared to ABT which is currently being widely used for this purpose. These new characteristics
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br Conclusion Our study demonstrates that the
2020-06-24
Conclusion Our study demonstrates that the effects of Epac activation are strongly conditioned by the steady-state Ca levels at which the myocyte is functioning. As intracellular Ca increases, the activity of CaMKII enhances and the phosphorylation of its SR substrates acquires different relevanc
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Although the mechanisms underlying the EP mediated increase
2020-06-24
Although the mechanisms underlying the EP4-mediated increase in the frequency of mEPSCs via PGE2 remain unclear, mechanisms similar to those driven by EP2 may be involved because activation of both these receptor subtypes increases the intracellular concentration of cAMP (Nishigaki et al., 1995, Sug
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br Methods br Results br Discussion The findings
2020-06-24
Methods Results Discussion The findings of this study indicate that an ET system including ET-1 and ET-2 as well as ET receptors are present in the retina and RPE/choroid, and are up-regulated by both hypertension and diabetes. Specifically, individual antagonism of the ETRA or ETRB deliver
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CYP contributes to the metabolism of more than of currently
2020-06-24
CYP450 contributes to the metabolism of more than 90% of currently available drugs (Shapiro and Shear, 2002). Currently, CYP1A is the most studied xenobiotic-metabolizing isoform in fish and is often used as a biomarker for early effects of pollutants in aquatic organisms (Havelkova et al., 2007). T
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The first ones class A receptors found as heterodimers
2020-06-24
The first ones class A receptors found as heterodimers were reported by Gomes et al. (2000), who identified a heteromer constituted by two subtypes of opioid receptors (μ and δ) in heterologous cells. The same year, Ginés et al. (2000) showed the first heteromer composed of two different receptors,
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Inhibition of DHODH is reflected by an antiproliferative
2020-06-24
Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear Etifoxine hydrochloride australia (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data f
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Studies on the external dehydrogenases of N crassa have
2020-06-24
Studies on the external dehydrogenases of N. crassa have shown that the NDE1 protein is a Ca2+-dependent external NADPH dehydrogenase, while NDE2 is characterized as a dehydrogenase oxidizing both cytosolic substrates (external NADH and/or NADPH) (Carneiro et al., 2004, Melo et al., 2001). All three
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