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Binding affinity was measured by a
2019-09-18
Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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These data indicate that in the context of the
2019-09-17
These data indicate that, in the context of the N-terminal 42 amino acids of p53, threonine 18 is a substrate for phosphorylation by CK1 as mediated by prior phosphorylation of serine 15. To determine whether this is a property of full length p53, GST-p53 fusion proteins comprising the full length p
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In conclusion our study has demonstrated that PGE stimulates
2019-09-17
In conclusion, our study has demonstrated that PGE2 stimulates expression of survivin in hepatocellular carcinoma cells. Although there are 4 subtypes of EP receptors, the EP1 receptor appears to be the predominant receptor that regulates PGE2-induced expression of survivin, mainly through trans-act
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TgTCEA from petals TgTCEA and TgTCEB from
2019-09-17
TgTCEA from petals (TgTCEA1) and TgTCEB from pollen grains (TgTCEB1) were used throughout the study. The recombinant enzymes were expressed in , and purified as the His-tag-free forms as described previously., Enzyme reactions were performed at 4 mM substrates under the same conditions as described
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Since the number of peptides hydrolized by
2019-09-17
Since the number of peptides hydrolized by PEP is quite large, it is not easy to relate the increase of enzymatic activity with the altered changes of a concrete peptide. However, it is noticeable that imbalances of several natural substrates of PEP [6], such as angiotensins, bradykinin, vasopressin
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In terms of its protease activity
2019-09-17
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other Cystamine dihydrochloride of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degr
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To further define the importance of
2019-09-17
To further define the importance of CYP3A for OSC metabolism in vivo, a strong CYP3A inhibitor ketoconazole was used to test whether CYP3A would affect its metabolism. As expected, the biotransformation of OSC to SC was significantly decreased by ketoconazole at all three substrate concentrations. H
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Gene expression profiling with corresponding
2019-09-17
Gene muscarinic agonist profiling with corresponding clinical data supported the notion that increased expression of S1PR1 in DLBCL was associated with poor outcome [159], [160], [161]. These studies also identified increased expression of the GPCRs GPR183, CCR7, ADRB2 and CNR2 as risk factors for
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br Conclusions br Acknowledgment br Introduction The role of
2019-09-17
Conclusions Acknowledgment Introduction The role of cholesterol metabolism during multiple sclerosis (MS) is debated and the underlying physiopathology largely unknown. Dyslipidaemia is associated with worsening inflammatory activity and MS disease progression [1], [2], [3]. In the mouse mo
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br Introduction Protein modification by ubiquitin
2019-09-17
Introduction Protein modification by ubiquitin and ubiquitin-like proteins is one of the most common and important regulatory mechanisms in biology (Finley et al., 2004, Pickart, 2004). Ubiquitination is carried out by an enzymatic cascade consisting of three steps. In the first step, ubiquitin i
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br Hypothesis on DDR protective mode of action
2019-09-17
Hypothesis on DDR1 protective mode of action The documented protective role of DDR1 is quite impressive, demonstrated using different preclinical models (immunologic [46,54,58], obstructive [45], and hypertensive [50]) with different intervention paradigms: genetic ablation [45,50,58,72], silenci
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E is a classical initiator protein and as such plays
2019-09-16
E1 is a classical initiator protein and, as such, plays several roles in the initiation and catalysis of viral DNA synthesis. E1 must first recognize a specific segment of the viral caspase pathway known as the “origin of DNA replication”, or “ori” for short. For most PV types examined to date, the
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br Conclusion The results of the current
2019-09-16
Conclusion The results of the current study show that boldness is associated with higher gene expression of drd2a, drd2b and oprd1b in zebrafish males. The results are correlational and additional experiments are needed to clarify the causal role of these receptors in zebrafish behavior. Confl
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In summary these results are consistent with
2019-09-16
In summary, these results are consistent with our hypothesis that chemical nitrosation of BMAA to N-BMAA results in the formation of an alkylating agent. Furthermore, we have shown that N-BMAA is more toxic than BMAA itself. Previously, methylazoxymethanol (MAM), which is also present in the cycad n
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Little information is available regarding the expression of
2019-09-12
Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r
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