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br Conflicts of interest br Introduction Diacylglycerols DAG
2019-07-30
Conflicts of interest Introduction Diacylglycerols (DAGs) and phosphatidic GW441756 (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). Cells
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Kluveromyces lactisSimilar to S cerevisiae K lactis
2019-07-30
Kluveromyces lactisSimilar to S. cerevisiae, K. lactis is a facultative anaerobic respiratory yeast, which lacks Complex I in its mitochondrial respiratory chain. However, both yeasts differ regarding their respiratory-fermentative metabolism as K. lactis exhibits a greater use of the pentose phosph
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Cell Cycle Compound Library where The IP R is a ubiquitously
2019-07-30
The IP3R is a ubiquitously expressed Ca2+-release channel from the ER, activated by IP3, produced upon cellular stimulation by hormones, growth factors or neurotransmitters. Three genes are coding for the IP3R and their gene products (IP3R1, IP3R2, IP3R3) assemble in functional homo- or heterotetram
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Given its high frequency it is not surprising that
2019-07-29
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant EGFR Inhibitor to to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have been
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br Abbreviations br Acknowledgements br
2019-07-29
Abbreviations Acknowledgements Introduction Dopamine β-hydroxylase (DbH) is the enzyme catalysing the conversion of dopamine to norepinephrine, two important neurotransmitters involved in the central nervous system [1]. This enzyme has been isolated from bovine chromaffin granules as a tetr
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DNA methylation is associated with transcriptional silencing
2019-07-29
DNA methylation is associated with transcriptional silencing of tumor suppressors or other genes important for normal cellular function and plays an important role in the development of cancer and other diseases (such as breast and colorectal cancers) [19]. DNA methyltransferases (MTases) are a fami
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In the current study although EP agonist was the
2019-07-29
In the current study, although EP4 agonist was the most effective in relaxing corpus cavernosum, it did not affect the neuronally-mediated relaxation. On the other hand, both alprostadil and iloprost, which were less effective as direct relaxants, potentiated EFS-induced relaxation of rat corpus cav
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chemokine receptor antagonist Although the control group and
2019-07-29
Although the control group and tinnitus group do not significantly differ based on age, gender or hearing loss, a limitation of this study is that the control group is only group-matched, and not individually matched. Furthermore, we only tested hearing acuity in tinnitus patients via standard pure
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Due to the high attractiveness of E and E ligases
2019-07-29
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), Glycyrrhizic acid (Davydov et al., 2004, Huang et al., 2005, Kenten et al., 2
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Calcium dependence of CaM target interaction was analyzed us
2019-07-27
Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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Since free testosterone diffuses into a target organ
2019-07-27
Since free testosterone diffuses into a target organ [1], a remarkable increase in free testosterone in plasma is expected to enhance androgen response in target organs including the prostate. In fact, the results of the present study showed testosterone and DHT levels, and mRNA expression levels of
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SPR was used to measure
2019-07-27
SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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In summary we have identified a series of
2019-07-27
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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br Materials and methods br Results
2019-07-27
Materials and methods Results Discussion Cisplatin, as one member of a class of platinum-containing anti-cancer drugs, which displays a great deal of clinical activity on a wide variety of solid tumors. In addition, cisplatin often used in combination with other chemotherapy drugs to treat
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In sum although it is reasonable to
2019-07-27
In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different or
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