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Determination of relative potency EC by dose response
2020-02-24
Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an
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br Membrane receptor Indirect non genomic
2020-02-24
Membrane receptor: Indirect non-genomic signaling As mentioned above, not all 2272 sale responses fit the classical genomic model of steroid action. The observation of excessively fast estrogen-induced biological responses led to the development of the hypothesis that estrogen could be acting by
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br Materials and methods br Results br Discussion In
2020-02-22
Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi
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Thus the exact mechanisms responsible for progestogen induce
2020-02-22
Thus, the exact mechanisms responsible for progestogen-induced changes in immune response are not known but the effects are believed to be exerted through receptor-mediated interactions. Since the mPR α is known to be a G protein-coupled receptor in fish, downstream signaling cascades via secondary
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br Material and methods br Results br Discussion Both proges
2020-02-22
Material and methods Results Discussion Both progesterone and estradiol are major ovarian steroids crucial for the development and homeostasis of the female reproductive tract (Patel et al., 2015). In the cervix, estrogen softens the cervical stroma affecting the extracellular matrix (ECM)
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br Acknowledgments This work was supported
2020-02-22
Acknowledgments This work was supported by a grant from the National Center for GM Crops (PJ008152) of the Next Generation BioGreen 21 Program funded by the Rural Development Administration, Republic of Korea, to W.T.K. Introduction Ubiquitin (Ub) has been considered as one of the most import
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Another notable finding in this study is that Cbl b
2020-02-22
Another notable finding in this study is that Cbl-b-mediated ubiquitination accelerates the degradation of phosphorylated DDR2. Cbl family has been documented to facilitate RTK degradation either in proteasome through K48-linked poly-ubiquitination or in lysosome through mono-, multiple mono- and K6
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The all NTP pyrophosphatase and
2020-02-22
The all-α NTP pyrophosphatase and NUDIX families maintain the deoxynucleotide triphosphate (dNTP) pool balance, limit the incorporation of harmful nucleotides, and represent a promising therapeutic approach to develop anticancer and immunosuppressive agents., , , , Among these housekeeping enzymes i
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Drug drug interactions are frequently attributed to function
2020-02-22
Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is tho
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This study demonstrates that GUL affects
2020-02-22
This study demonstrates that GUL-1 affects multiple pathways/processes. As GUL-1 is likely to function as an RNA-binding protein, it is conceivable that the mRNAs involved are bound to GUL-1 as part of the regulatory function of the protein. In fact, in S. cerevisiae Ssd1 was shown to bind multiple
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Since the aggregation of neurotoxic forms of A plays
2020-02-22
Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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br Materials and methods br Results br Discussion
2020-02-22
Materials and methods Results Discussion DUSP1 is a member of the subfamily of the Dusl specific phosphatases (DUSPs). High levels of DUSP1 observed in lung, liver and placenta, and low levels have been found in the L-Stepholidine and kidney. DUSP1 has been shown to be elevated in various
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Prostanoids typically act in an autocrine
2020-02-22
Prostanoids typically act in an autocrine and paracrine fashion by binding to specific receptors in target NB-598 Maleate and there is evidence that both PGE2 and prostacyclin may be required for the optimal activation of angiogenesis (Hata and Breyer, 2004). PGE2 and prostacyclin bind to their spe
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br Materials and methods Details on materials
2020-02-22
Materials and methods Details on materials and methods can be found in the Supplemental material section. Results Discussion In our experiments we mimicked inflammation by LPS challenge of M0 macrophages. We discovered a strong increase in expression of CH25H and CYP7B1 while CYP27A1 and H
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br Development of the double
2020-02-22
Development of the double strand break repair model for meiotic recombination Meiotic recombination was first described by Frans Alfons Janssens using DGAT-1 inhibitor in the salamander Batracoseps attenuatus in 1909 [21] and then further elaborated at the genetic level in Drosophila by Thomas H
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