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Contrary to genetic aberrations epigenetic methylation marke
2020-09-14
Contrary to genetic aberrations epigenetic methylation markers with broad coverage of OvCa subtypes were detected in primary tumors [21]. Ibanez de Caceres et al. [22] identified hypermethylation of BRCA1, APC, p16, p14, DAPK or RASSF1A in 50 of 50 primary tumors. Moreover the methylation pattern wa
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During the course of our research on mGlu
2020-09-14
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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To date methods for the simultaneous analysis of multiple pr
2020-09-14
To date, methods for the simultaneous analysis of multiple probe drugs in the plasma have been described by using HPLC-DAD or LC–MS/MS. Although previous cocktail methods have used combinations of those four or other probe drugs with LC–MS/MS methods, most of those studies focused on only the analys
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Testosterone is inactivated through hydroxylation and conjug
2020-09-14
Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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N methyl d aspartate NMDA receptor antagonists such as
2020-09-14
N-methyl-d-aspartate (NMDA) receptor antagonists, such as MK-801 and phencyclidine, induce cognitive dysfunction in both mice and humans [18]. In addition, antipsychotic drugs ameliorate MK-801-induced cognitive dysfunction; therefore, the acute application of MK-801 can be used as an animal model o
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Our study demonstrated that the sequential events
2020-09-14
Our study demonstrated that the sequential events of PKA and AMPK activation were involved in kinsenoside-mediated lipolysis. Within 1 h, PKA transiently inhibited AMPK activation by mitigating LKB1-mediated AMPK phosphorylation at Thr172, and PKA reduced AMPK-mediated phosphorylation at HSL-Ser565
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br Allosteric inhibitors In general candidate drugs that bin
2020-09-11
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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A putative SHBG receptor SHBG R has been
2020-09-11
A putative SHBG 516 3 (SHBG-R) has been postulated for about thirty years [66], [69], [70]. The characterization of this receptor has been researched by several groups. There are different ideas on how this receptor works. On the one hand Fortunati et al. provide evidence that SHBG is already bound
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Table summarizes the literature data available on the occurr
2020-09-11
Table 4 summarizes the literature data available on the occurrence of these two CEP 1347 of steroidal compounds in sludge and sediments. In activated and digested sewage sludge, the concentrations of ethynyl estradiol (17 ng/g), estrone (37 ng/g ), and estradiol (49 ng/g) found in one of the very
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To further investigate mechanisms of rXCI
2020-09-11
To further investigate mechanisms of rXCI, we generated female ESCs with a homozygous RlimKO. We found that these Antagonist G receptor undergo XCI in vivo but that XCI in vitro is strongly influenced by culture conditions, including both method of differentiation and O2 levels. Our results demonstr
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The H E staining and Nissl staining results
2020-09-11
The H&E staining and Nissl staining results showed that damage to the pyramidal neurons in the CA1 and CA3 regions of the hippocampus were observed in the 50 mg/kg/day DBP group, accompanied by an absence of Nissl bodies, suggesting that DBP exposure can lead to pathological changes in the neurons o
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br Introduction Breast cancer is the
2020-09-11
Introduction Breast cancer is the most common malignant tumor in women and the second leading cause of female death [1]. In recent years, with the improvement of early detection and the emergence of new treatment methods, the mortality rate of breast cancer has been greatly reduced. However, the
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The present study was set to characterise the
2020-09-11
The present study was set to characterise the DNMT gene orthologs and describe the expression patterns of these genes during seed development in natural diploid apomict B. divaricarpa and diploid sexual B. stricta. Material and methods Results The B. stricta genome v1.2, was sequenced and as
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br Anti inflammatory effects of MTX In addition to cytotoxic
2020-09-10
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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The in vivo IC M in the adipose tissue assay
2020-09-10
The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free PKR Inh
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