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It is well established that Shp can function as a
2019-07-09

It is well established that Shp-2 can function as a substrate for several RTK, such as PDGF or EGFR [23], [36]. To test whether DDR1 recognizes Shp-2 as its substrate, we overexpressed a catalytically inactive Shp-2 mutant together with DDR1b in 293 cells [31]. Immunoprecipitation of Shp-2 followed
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br Results and Discussion br Conclusions Based on their
2019-07-09

Results and Discussion Conclusions Based on their common NTP pyrophosphatase activity, similar size of the catalytic domains, and the conservation of glutamate residues, it was assumed previously that the MazG and HisE families were related to MutT and other Nudix family hydrolases (see Zhang
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br Fragment based drug discovery FBDD is a
2019-07-09

Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical TCS 5861528 space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It
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br Introduction Concern has been raised
2019-07-08

Introduction Concern has been raised over free estrogens (estrone [E1], 17ß-estradiol [E2] and 17α-ethynylestradiol [EE2] particularly) in the past decade due to their endocrine disrupting effects on environmental biota [1], [2]. Estrogens are excreted by vertebrates primarily as sulfate or glucu
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DNMT is the dominating enzyme responsible for maintenance of
2019-07-08

DNMT1is the dominating enzyme responsible for maintenance of the DNA methylation pattern and the primary enzyme responsible for copying methylation patterns following DNA replication (Moore et al., 2013). DNMT1 maintains the mitotic inheritance of the original methylation pattern in a cell lineage d
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Chlorambucil structure Diacylglycerol kinases DGK and are li
2019-07-08

Diacylglycerol kinases (DGK) α and ζ are lipid kinases that limit diacylglycerol (DAG)-dependent activation pathways downstream of the TCR (Merida et al., 2015). Their upregulation in tumor infiltrating lymphocytes (TIL) has been linked to generation of hyporesponsive states that contribute to immun
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As part of a program to explore the
2019-07-08

As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu
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Our data indicate that the ability of these promiscuous kina
2019-07-08

Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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br Introduction Noncanonical nucleoside triphosphates NTPs
2019-07-08

Introduction Noncanonical nucleoside triphosphates (NTPs; such as deoxyinosine triphosphate (dITP), deoxyxanthosine triphosphate (dXTP), 8-oxo-deoxyguanosine triphosphate, and 2-oxo-deoxyadenosine triphosphate are produced from oxidation, deamination, or other modifications of canonical nucleotid
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7ACC2 structure Although several examples of selective reduc
2019-07-08

Although several examples of selective 7ACC2 structure of α-diazoesters to α-hydrazonoesters have been described in the literature, reports on practical and general examples of such a process are scarce. In this context, there was a need to devise a mild and general method for the selective reductio
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In the present study we used a new luminescent
2019-07-08

In the present study, we used a new luminescent method to measure CYP activity with Luciferin-ME as a substrate which is used for wide ranges of mammalian CYPs, including CYP1A2, CYP2C8, CYP2C9, CYP2J2, CYP4A11, and CYP4F3B. As a result, no significant modulations of CYP activities in B[a]P exposure
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A previous report showed that
2019-07-08

A previous report showed that the transfer of the CSF1 gene into tumor Garcinol induced TAM infiltration into syngeneic BALB/c mice. High expressions of CSF-1 and CSF-1R in tumor and stromal cells and a high TAM density are known to be correlated with poor prognoses in many cancer types. CSF-1 prom
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In contrast to drospirenone dydrogestrone acts rather
2019-07-08

In 17-Hydroxyprogesterone structure to drospirenone dydrogestrone acts rather neutral at the aldosterone-, glucocorticoid- and androgen-receptor [12]. This indicates that the assessment of a ‘net-overall effect’ on the vascular system is very difficult based on the often discussed ‘partial effects’
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Bioinformatics analysis for genes encoding proteins ESR
2019-07-08

Bioinformatics analysis for genes encoding proteins (ESR1, IL6, TERT, DNMT3B) showed that NF-kB is one of the transcription factors that might be regulating their expression, especially for IL6, TERT and DNMT3B genes. Previous studies have demonstrated that PA induces NF-kB activation, thus increasi
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FGF ERK signaling has been
2019-07-08

FGF/ERK signaling has been implicated in epithelial-mesenchymal interactions in a wide range of tissues (Huh et al., 2015, Klein et al., 2006, Rice et al., 2004, Zhang et al., 2006, El Ramy et al., 2005, Volckaert and Langhe, 2015). During embryonic organogenesis and in adult organs, we often observ
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