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Recently we have observed that pharmacological PPAR and
2019-09-19
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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E protein was studied using specific anti E antibodies
2019-09-19
E1 protein was studied using specific anti-E1 cpmt clinical in wild type cells and in transfected cells overexpressing the enzyme. The results revealed several unusual characteristics, which are unique to this ubiquitin-activating enzyme. The E1 was translated as a full-length protein and then quick
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A range of inhibitors were therefore synthesized containing
2019-09-19
A range of inhibitors were therefore synthesized containing either carboxylic DCPIB or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively (). Analysis of t
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br Protein acetylation Several reports show that MTX
2019-09-19
Protein acetylation Several reports show that MTX is able to induce acetylation of histones and other proteins. Extensive studies have established that histone acetylation is primarily associated with gene activation. Acetylation occurs at lysine residues on the amino-terminal tail of the protein
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2750 We found that both DDR and
2019-09-19
We found that both DDR1 and DDR2 ECD increased matrix mineralization as compared to native cells, with the effect of DDR2 ECD being more prominent. Both soluble (DDR2/ECD) and membrane-bound DDR2 ECD (DDR2/-KD), when compared to wild-type cells, induced larger mineral deposits. In this regard, a rec
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The synthesis of tricyclic analogs is described in
2019-09-19
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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It is particularly notable that CYP D appears to
2019-09-18
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 DMP 777 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 consistent over time and between indiv
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Here we explored the relative contribution of D like
2019-09-18
Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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Several highly potent CysLT receptor
2019-09-18
Several highly potent CysLT1 receptor antagonists with large structural NU 9056 have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiazoles.
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Several highly selective COX inhibitors coxibs have
2019-09-18
Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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Unlike previous studies examining COMT genotyping in healthy
2019-09-18
Unlike previous studies examining COMT genotyping in healthy controls seeking to explain impulsive behaviors, this study sought to examine COMT genotypes in a large sample of individuals with varying levels of gambling behavior to determine whether COMT D-erythro-Sphingosine (synthetic) was associa
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The enzymatic activity of recombinant sponge P H was assayed
2019-09-18
The enzymatic activity of recombinant sponge P4H was assayed in vitro both at 37°C, the standard enzymatic kinetics temperature, and at 15°C, the typical sea temperature of C. reniformis marine environment (Fig. 2C). Surprisingly the data obtained indicate that the sponge enzyme has a lower activity
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Introduction Obesity constitutes a global
2019-09-18
Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV
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br Materials and Methods br Results
2019-09-18
Materials and Methods Results Discussion ROS generated by SFN target many signaling pathways involved in initiating cancer cell death (Sestili and Fimognari, 2015). For example, ROS have been shown to activate both intrinsic and extrinsic caspase cascades in prostate cancer cells (Singh et
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br Materials and methods br
2019-09-18
Materials and methods Results To investigate the effect of 17βE on cell proliferation in the human renal tubular epithelia, BrdU uptake was measured in HRTEC primary and 3D-HRTEC cultures, allowing determination of the DNA replication rate. Representative microphotographs show BrdU uptake in H
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