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Recently we have observed that
2019-09-02
Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti
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Valproic acid VPA is a first line treatment for
2019-08-30
Valproic hydroxylase (VPA) is a first-line treatment for epilepsy and bipolar disorder, although its therapeutic mechanism of action is not fully understood. Considerable evidence suggests that VPA can act through the GABAergic system, NMDA receptors, and/or sodium channels (for review, see Löscher,
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br Material and methods br Results and
2019-08-30
Material and methods Results and discussion Conclusions Prostanoid-E receptor selective antagonists that inhibit EP2 or EP4 receptor activities may be used as a pharmacological strategy to limit cyst formation and ADPKD progression. Our study follows on from our previous observations of the
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Accordingly we prepared three compounds
2019-08-30
Accordingly, we prepared three compounds (, , and ) as shown in . Condensation of commercially available Angiotensin 1/2 (1-5) with glycine methyl ester gave amide . A Friedel–Crafts reaction between compound and 4-methyl valeryl chloride in the presence of aluminum chloride mainly produced unde
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Biochemically the primary function of PPIP K is kinase
2019-08-30
Biochemically, the primary function of PPIP5K2 is 1-kinase-mediated phosphorylation of 5-IP7 to form 1,5-IP8 (Shears, 2018). To a lesser extent, PPIP5K2 also phosphorylates IP6 to produce 1-IP7. Furthermore, PPIP5K2 has been shown to catalyze a reverse reaction, that is, dephosphorylation of 1,5-IP8
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In the present study we investigated
2019-08-30
In the present study, we investigated the deeper role of eNOS in the pathogenesis of nasal polyps and analyzed the influence of 1,8-cineol on nasal polyp gene and protein expression of eNOS in vitro. Different studies dealt with the localization and expression of eNOS in nasal polyps and nasal mucos
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CYP A and CYP D are among the
2019-08-30
CYP3A4/5 and CYP2D6 are among the main drug-metabolizing enzymes in humans that are responsible for the metabolism of more than 50% of marketed drugs [19], [21]. Drugs metabolized by CYPs are prone to drug–drug interactions, thereby modifying their response [18], [32]. Metabolic inhibition is also i
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From these and other studies it is clear that
2019-08-30
From these and other studies, it is clear that acriflavine is an interesting Sildenafil Citrate with pleiotropic anticancer effects [21], [22], [43]. Its past systemic use in the clinical setting as an antibiotic without any major toxicity reported encourages further development of the drug for canc
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A different example of substrate dependent activation is see
2019-08-30
A different example of substrate-dependent activation is seen in CSN5, a JAMM-type DUB found in the eight subunit COP9 signalosome (CSN) [34]. The CSN deconjugates NEDD8 (neural precursor cell expressed developmentally downregulated 8) from Cullin Ring ubiquitin E3 ligases (CRLs). Through this activ
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DPP is show two relevant benefits in the clinical
2019-08-30
DPP-4is show two relevant benefits in the clinical management of type 2 diabetic patients: negligible risk of severe hypoglycemia, particularly when compared with sulphonylureas [[33], [34]], and weight neutrality, in contrast with the weight gain generally observed with insulin therapy, sulfonylure
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In most cases patients will not present immediately after SM
2019-08-30
In most cases, patients will not present immediately after SM exposure because SM-induced clinical symptoms typically occur after a latency period of several hours [8], [9], [10]. When they do present, the detection of free, unbound alkylating agent is highly unlikely. For this reason, available rap
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br Acknowledgements br This work was supported
2019-08-30
Acknowledgements This work was supported by grants from the National Natural Science Foundation of China (Grant No.: 30260088) and the prophase research for National “973” Project of China (Grant No.: 2007CB116203). The DNA sequences of Hbvp1 and the Hbvp1 promoter were deposited in GenBank, an
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Pyrazolopyrimidines are bioisostere of purine exhibit
2019-08-30
Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase Senegenin [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour and leuk
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This review focuses on the
2019-08-30
This review focuses on the atomic basis of CRM1-mediated nuclear export. There are now 27 crystal structures of CRM1 in the Protein Data Bank (PDB) (www.rcsb.org) [64]. Collectively, this large body of work explains various aspects of CRM1 function. Here we summarize the structure–function studies t
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The best characterized APC C substrates are recruited
2019-08-29
The best-characterized APC/C substrates are recruited via various linear motifs (e.g., D boxes, KEN boxes, and ABBA motifs) that serve as degrons, binding to distinct regions of the β-propeller domain of a coactivator (Figure 1, Figure 3B) (reviewed in [44]). In addition, D boxes also simultaneously
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