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Testosterone is inactivated through hydroxylation and conjug
2019-09-12

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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br Materials and methods br Results br
2019-09-12

Materials and methods Results Discussion Here we show expression of the EP1 receptor in the hippocampus of mice and the functional influence of the EP1 receptor on kainic palovarotene clinical induced seizures. Mice lacking a functional EP1 receptor gene displayed a lower tendency to enter
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From an industrial perspective the low
2019-09-12

From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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br Cytochrome P monooxygenases Cytochrome P
2019-09-12

Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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In our preliminary evaluation of
2019-09-11

In our preliminary evaluation of this series, we were surprised to discover that AMD3100 8HCl clinical was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is comp
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Distribution of DGTS in basidiomycete
2019-09-11

Distribution of DGTS in basidiomycete fungi has been demonstrated to be heterogeneous. In certain fungal taxons, such as Agaricales, Polyporales and Russulales, there are species that synthesize and species that do not synthesize DGTS that belong to the same order or even family (Dembitsky, 1996, Va
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br Introduction Oral contraceptives OCs are the
2019-09-11

Introduction Oral contraceptives (OCs) are the most commonly used medication for contraception all over the world and are also used in the treatment of menstrual disturbances and hyperandrogenism in women with polycystic ovary syndrome [1]. The impact of OC steroids on cardiovascular pathophysiol
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Given the molecular pharmacology and in
2019-09-11

Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma
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Pursuant to our in vitro data that neutrophilic elastase act
2019-09-11

Pursuant to our in vitro data that neutrophilic elastase activated the elastase-dependent oncolytic virus, we initially hypothesized that tumor-infiltrating neutrophils could be the source for elastase in tumor tissue. However, we did not detect neutrophils in the PANC-1 tumor tissue where we observ
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Impaired dopaminergic systems associated with MA have
2019-09-11

Impaired dopaminergic systems associated with MA have been well-documented (Walsh and Wagner, 1992, Kim et al., 1999, Nakajima et al., 2004, Shin et al., 2012, Shin et al., 2017b, Dang et al., 2016, Dang et al., 2017b). Previous reports have suggested that early MA use may be linked to higher risk f
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Azaserine and br Experiments and Methods br Results and Disc
2019-09-11

Experiments and Methods Results and Discussion Conclusions Here, the interactions between two newly-synthesized carbazole derivative—cationic δ,δ′‑diazacarbazoles and DNA were characterized by several spectroscopic means, including UV–Vis and fluorescence, AFM and fluorescence imaging. The
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Methylation of histone tails is
2019-09-11

Methylation of histone tails is important in regulating OU749 structure and transcription. Methylation occurs at arginine and at mono-, di- or tri-methylated lysine residues. The reversibility of histone methylation was recently revealed by the identification of two histone demethylases, LSD1 and J
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The collagen binding membrane proteins
2019-09-11

The collagen-binding membrane proteins, discoidin domain receptors 1 and 2 (DDR1 and DDR2) belong to the family of receptor tyrosine kinase and are expressed in a variety of mammalian cells.7, 8 These transmembrane glycoproteins (∼125 kDa) have been found to be over-expressed or atypically expressed
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In the present study the expression of the CYP C
2019-09-11

In the present study, the p2y receptor of the CYP2C11 gene and the levels of its protein and activity were decreased in rats with liver insufficiency and in rats after induced dysfunction of the serotonergic system during normal liver function. Moreover, serotonergic system dysfunction during liver
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The objective of the present study was
2019-09-11

The objective of the present study was to investigate the role of the CRF system in the neuroadaptations associated with nicotine dependence. To this aim, the regulation of the gene expression of CRF and its receptors was assessed in cox pathway regions belonging to the reward pathway using a model
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