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Ligand independent constitutively active variants have also
2019-07-16

Ligand-independent, constitutively active variants have also been found in receptors with associated tyrosine kinases. In approximately 60% of patients harboring inflammatory hepatocellular adenomas (IHCAs), these adenomas have been caused by small in-frame deletions in the cytokine-binding domain o
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P has three subfamilies CYP CYP and
2019-07-16

P450 has three subfamilies (CYP1, CYP2, and CYP3), which contribute largely to the oxidative biotransformation of xenobiotics that include most drugs, dietary chemicals, and environmental pollutants. The CYP1 enzymes have great importance in the bioactivation of mutagens and its isoforms are capable
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In conclusion our work provides the preclinical evidence
2019-07-16

In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer Cyclo where and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly for the tre
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The ability of TKIs in inducing CRTH
2019-07-16

The ability of TKIs in inducing CRTH2 expression could be related to the c-terminal of CRTH2 receptor that is important molecular determinant in the down-stream signaling cascade activation [20]. This requires further studies to prove it or disprove it. Additionally, further studies are needed to ex
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In rats exposed to day of nicotine
2019-07-16

In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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br Materials and methods br Results br Discussion Intra
2019-07-16

Materials and methods Results Discussion Intra-BNST injections of NOC-9 (at all doses) were able to produce freezing and anxiogenic-like effects. Freezing was observed immediately after the NO donor injection and lasted about 2–3min (data not shown). When exposed to the EPM 5min after intra
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Various domains of the HSA molecule have also been
2019-07-16

Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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Two GPCR subtypes of interest in the myocardium are the
2019-07-16

Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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br Results br Discussion The ubiquitin system
2019-07-16

Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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HCV has evolved mechanisms to evade
2019-07-16

HCV has evolved mechanisms to evade humoral immune responses including high functional flexibility and variability of immunogenic portions of its envelope proteins. The highest sequence variability occurs in the first 27 Fmoc-Gln(Trt)-OH of the N-terminus of E2, which is referred to as the hypervar
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The first hint that GLP might
2019-07-16

The first hint that GLP-1 might not be completely stable came from a meeting abstract in 1992, reporting that GLP-1 could be degraded in plasma incubations [16], although the enzyme(s) involved was not identified. A year later, Mentlein and colleagues [17], in a search for peptide substrates of the
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cAMP mediated signaling pathways are important for maintaini
2019-07-15

cAMP-mediated signaling pathways are important for maintaining metabolic homeostasis, and the effects of the glucagon/catecholamine–cAMP–PKA axis on energy balance have been well documented [20]. For example, BEC of the PKA 2β regulatory subunit (RIIβ) in mice leads to increased expression of uncou
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EBI and its ligand s EBI
2019-07-15

EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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The Nile tilapia Oreochromis niloticus is an
2019-07-15

The Nile tilapia (Oreochromis niloticus) is an important farmed fish with an XX/XY sex-determining system. The availability of the whole genome sequence of tilapia and tissue transcriptomes (Brawand et al., 2014), together with its gonadal transcriptomes at different developmental stages (Tao et al.
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Methylation of histone tails is important in regulating chro
2019-07-15

Methylation of histone tails is important in regulating RI-1 where 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 a
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