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Myelin Basic Protein (87-99) ERR induces the expression of P
2020-02-21
ERRγ induces the expression of P450c17 in MA-10 cells and in mouse primary Leydig cells (Fig. 2). Deletion mutant analysis of putative ERRγ-binding sites in the P450c17 promoter suggested that only the proximal third site located between −269 bp and −136 bp within the P450c17 promoter is functional
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Generally glycines and other small residues such as alanine
2020-02-20
Generally, glycines (and other small residues such as alanine) present in a helical GxxxG-motif that are facing the same side of the helix form a uniform surface that enables direct contact with a second helix. Crystal structures of multipass membrane proteins have demonstrated that GxxxG-motifs are
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More unusual modifications also regulate DUBs Recent reports
2020-02-20
More unusual modifications also regulate DUBs. Recent reports have illustrated how reactive oxygen species (ROS) can regulate DUB activity 87, 88, 89, 90. ROS can serve as potent signaling molecules by reacting with active site cysteines of tyrosine phosphatases and some cysteine peptidases to form
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Multiple sequence alignment of the proteins in the DGAT sub
2020-02-20
Multiple sequence alignment of the proteins in the DGAT1 sub-family shows that there are about 41 conserved amino glucocorticoid receptor residues distributed over seven sequence motifs [74]. Unlike DGAT2, a large number of DGAT1 residues, including a majority of the conserved residues, are found i
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Preparation of the pyridyl ether analogs was
2020-02-20
Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate,
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LUF6000 Among the down regulated genes were several of inter
2020-02-20
Among the down-regulated genes were several of interest. Coronin2a (Coro2a), a component of the nuclear receptor co-repressor complexes, contributes to de-repression of inflammatory response genes (Huang et al., 2011). Mill1, an MHC family member expressed in hair follicles, represses wound healing
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In vitro studies in NSCLC
2020-02-20
In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC Apatinib with Growth inhibition (GI50) values ranging from 7 to 32 nmol/L. I
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A range of inhibitors were therefore synthesized containing
2020-02-20
A range of inhibitors were therefore synthesized containing either carboxylic C527 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 th
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To analyze EBI expression and its function in T
2020-02-19
To analyze EBI2 expression and its function in T cells in vivo, we created an EGFP reporter/knockout mouse strain, termed EBI2EGFP. This mouse strain in heterozygous configuration allows for a systematic analysis of the expression of EBI2 in distinct cell types in steady-state and under inflammatory
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CK enzymes belong to a conserved family of serine
2020-02-19
CK1 enzymes belong to a conserved family of serine/threonine protein kinases that plays an important and diverse role in vesicular trafficking, DNA repair, gsk-3 progression and cytokinesis in organisms from yeast to humans [15]. In multicellular organisms CK1 enzymes also regulate developmental pat
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Several studies have already shown that mPR activation can
2020-02-19
Several studies have already shown that mPR activation can significantly reduce intracellular cAMP levels in different kind of cells, such as GT1-7 neuronal cells [32], MDA-MB-468 breast cancer cells [55] and primary vascular endothelial cells [56]. The experiments performed with PTXa and 8-Br-cAMP
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Synthetic progestogens also known as synthetic
2020-02-19
Synthetic progestogens (also known as ‘synthetic gestagens’, ‘synthetic progestins’ or simply ‘progestins’) are designed to mimic the effects of progesterone (P4) and are the active pharmaceutical ingredient in many contraceptives and hormone replacement therapies. Since most progestins are derived
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In vasculature NADPH oxidases NOXs
2020-02-19
In vasculature, NADPH oxidases (NOXs) are the main sources of O2− generation that involve in the transfer of electrons to molecular oxygen. Endothelin-1 [25] and thromboxane A2 [26] were reported to induce eNOS uncoupling via upregulation of NOXs. Additionally, inhibition of p47 phox, a subunit of N
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Besides EGFR other tyrosine kinase receptors are currently g
2020-02-19
Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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PBMC derived macrophages not only
2020-02-19
PBMC-derived macrophages not only express EBI2 but also have the ability to respond to their natural agonist 7α,25-OHC by activating downstream signal transduction pathways. In line with previous findings, our data confirm that receptor stimulation induces calcium mobilization which can be blocked b
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