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As expected the nortestosterone derived progestins
2019-08-29
As expected, the 19-nortestosterone-derived progestins tested were moderate agonists of hAR (C), with EC50s ranging from 2 to 10nM, however all were less potent than the endogenous ligand DHT by at least a factor of 6, with relative potencies ranging from 0.0301 to 0.164. This is in agreement with p
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br Oxidoreductase like MEM for
2019-08-29
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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L-Stepholidine br Conflict of interest statement br Referenc
2019-08-29
Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We acknowledge financial support by the Swiss State Secretariat for Education, Research and Innovation (Federal
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To our knowledge this is the first report of
2019-08-29
To our knowledge, this is the first report of an oncocytoma expressing alpha-enolase or causing autoimmune retinopathy and optic neuropathy. Although generally considered benign, oncocytomas have rarely been associated with paraneoplastic syndromes, including tumor-induced hypertension, erythrocytos
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Many studies have documented that enolase acts as
2019-08-29
Many studies have documented that enolase acts as a plasminogen-binding protein and this interaction is involved in the tissue invasion and pathogenicity of the causative agents (Almeida et al., 2004; Avilan et al., 2000; Marcilla et al., 2007; Mundodi et al., 2008; Vanegas et al., 2007). Furthermor
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It is particularly notable that
2019-08-29
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 DPP4 Activity Fluorometric Assay Kit in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consisten
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PI3K Akt mTOR Compound Library Contrary to the downregulatio
2019-08-29
Contrary to the downregulation of S1PR family GPCRs, CLL cells have increased mRNA expression of the lysophosphatidic PI3K Akt mTOR Compound Library (LPA) family receptors LPAR1, LPAR3 and LPAR4 compared to normal B cells [47]. Increased LPAR1 mRNA has been shown to be associated with more aggressiv
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As an endogenous negative modulator CRBN inhibits AMPK
2019-08-29
As an endogenous negative modulator, CRBN inhibits AMPK’s activation (phosphorylation of Thr172) by directly binding to the α-subunit of AMPK, disrupting γ-subunit recruitment to the AMPK complex (Lee et al., 2011, Lee et al., 2013). In our study, we did not focus on AMPK activation, since only a si
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It is of interest to
2019-08-29
It is of interest to consider an explanation for the apparent phosphorylation of hSSB1 in undamaged cells. One such may be that in order to execute a rapid response to replication inhibition, basal S134 phosphorylation could function to keep hSSB1 in a ‘primed’ state prior to stress. Such an arrange
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In the belief that DNA based nanosensors
2019-08-29
In the belief that DNA-based nanosensors and DNA microarrays should be easier to operate, faster, more accurate and more economically viable than PCR-based techniques, an electrochemical DNA biosensor was designed for detection of G. boninense[9], [10]. This was developed based on a gold electrode m
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Nociceptive and hyperalgesic actions of ET are produced thro
2019-08-28
Nociceptive and hyperalgesic actions of ET-1 are produced through ETA and ETB receptors. Previous reports indicate that ETA receptor antagonists in peripheral tissues are effective in inhibiting ET-1 induced hyperalgesia, and attenuation of neuropathic pain in rats [16]. Studies have also shown that
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To develop antagonists selective for the mouse EP
2019-08-28
To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic hundreds of people () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable a
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Ageing is associated with increased
2019-08-28
Ageing is associated with increased reactive oxygen species (ROS) production, oxidative stress and oxidative damage [43,44]. Overproduction of ROS can impair endothelial function by suppressing NO synthesis and scavenging NO thereby decreasing its overall bioavailability. Moreover, sustained oxidati
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In summary the metabolism of
2019-08-28
In summary, the metabolism of GEF in HLM and MLM was extensively studied using a LC–MS-based metabolomic approach. This study identified a total of 34 metabolites and adducts related to GEF (Fig. 10) and identified three new potential reactive metabolites, including two aldehydes and one iminium. Pr
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The imbalance that renders greater lipid uptake
2019-08-28
The imbalance that renders greater lipid uptake toxic is unclear, but the comparison of our in vitro studies with those in mice illustrates the importance of TAG storage versus accumulation of less non-polar molecules. Protective effects of ACSL1 and PPARγ have been reported in other cell types. Par
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