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The in vitro cytotoxicity of the prodrugs was assessed
2021-03-05
The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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br Criteria for ER targeted fluorescent probes br Survey of
2021-03-05
Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th
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br Experimental Procedures br Acknowledgments br Bisphenol A
2021-03-05
Experimental Procedures Acknowledgments Bisphenol A (BPA) has been recognized as one of the most potent endocrine disruptors, functioning even at very low doses. Although it is anticipated that Azithromycin Dihydrate receptor (ER) would mediate these effects of low-dose BPA, studies reveale
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Our finding that activating DDR
2021-03-05
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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In conclusion we have recombinantly expressed and purified t
2021-03-05
In conclusion, we have recombinantly expressed and purified the product of the YP_002262821.1 gene from A. salmonicida and confirmed that it possesses ATP-dependent DNA ligase activity. Comparison of the full-length and truncated versions of the protein indicate that the N-terminal 25 Phorbol 12,13-
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DGK is distributed exclusively in
2021-03-05
DGKβ [9] is distributed exclusively in the brain, particularly in the striatum, cerebral cortex, olfactory bulb, and hippocampus [9,10]. This isozyme accumulates at the perisynaptic sites of medium spiny neurons in the striatum [11]. The CHC of DGKβ rapidly increases after 14 days of age, after whi
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In summary the reduction of
2021-03-04
In summary, the reduction of one or more pro-inflammatory cytokines, such as TNF-α, IL-1β, IL-6, IL-8 was observed in almost all the monoterpenes studied. Increased levels of the anti-inflammatory cytokine IL-10 was shown to play a prominent function in the anti-inflammatory effect of monoterpenes,
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aldose reductase inhibitors Based on the ability of CRF
2021-03-04
Based on the ability of CRF to modulate nociception, we hypothesized that stress leads to hyperalgesia by the activation of CRF1 and/or CRF2 receptors in the spinal cord. We tested this hypothesis using an acute forced swim as a widely used and easily reproducible stressor and grip force as a measur
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The inhibition of FAS by C produces an accumulation of
2021-03-04
The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi
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Since protein kinase CK has over known substrates we examine
2021-03-04
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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Previously published data showed an interaction of
2021-03-04
Previously published data showed an interaction of α-tubulin and CK1δ [15] that was validated in the present study using SPR (Fig. 1A). The dominant motifs involved in the CK1δ/α-tubulin interface were defined using a peptide library of peptides covering the CK1δ amino Busulfan sequence (Supplement
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Brg is a core unit
2021-03-04
Brg1 is a core unit of BAF complex and is required for the self-renewal and pluripotency of ESCs (Ho and Crabtree, 2010). We confirmed the interaction of DPF2 and BRG1 by immunoprecipitation and showed that these proteins extensively co-localize in the genome. Although both Brg1 and Dpf2 positively
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Although BPA has been proven to cause many
2021-03-04
Although BPA has been proven to cause many health issues such as obesity and neurological toxicity (Rubin, 2011), the effects and mechanisms of BPA on the human tumorigenesis and cancer development are still not well illustrated. In the present study, we found that 10 to 10M BPA significantly promot
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As EBI is highly important for generation of
2021-03-04
As EBI2 is highly important for generation of an efficient T cell-dependent humoral immune response [[5], [6], [7]] it may be that aberrant expression or other dysregulation of this receptor contributes in B cell pathologies. In line with this, EBI2 expression is down-regulated in diffuse large B-ce
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br Conflicts of interest br Introduction Diacylglycerols DAG
2021-03-04
Conflicts of interest Introduction Diacylglycerols (DAGs) and phosphatidic SB 204070 receptor (PA) play fundamental roles in biology as basic components of membranes, intermediates in lipid metabolism, and secondary messengers in cellular signaling (Carrasco and Merida, 2007, Fang et al., 2001
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