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However not all inhibitory profiles by
2020-05-07
However, not all inhibitory profiles by metals can be a priori considered artifacts of the methodology used to quantify the activity of such enzymes. Metals can indeed interfere with cholinesterases, and the mechanisms are varied. The inhibitory effect of specific metals may derive from their abilit
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G007-LK synthesis In recent years there has
2020-05-07
In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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The enantiomeric ratio ER of chiral compounds accumulated in
2020-05-06
The enantiomeric ratio (ER) of chiral compounds accumulated in organisms has been found to be different among species (Borga and Bidleman, 2005, Harner et al., 1999, Warner et al., 2005, Wiberg et al., 2000), indicating enantioselective accumulation of chiral compounds are species-specific. The ER o
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gsk3 inhibitor At baseline mutant allele frequency
2020-05-06
At baseline, mutant allele frequency of EGFR in tissue and plasma samples did not correlated with anti-tumor response (Supplementary Fig. 1). Among 35 patients who were positive for cell-free DNA (cfDNA) at baseline, changes of cfDNA during treatment were analyzed. Negative conversion (NC) of cfDNA
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D-NMAPPD mg It is also critical that APC CCDC
2020-05-06
It is also critical that APC/CCDC20 is inhibited by MCC during the spindle assembly checkpoint, prior to correct chromosome alignment on the mitotic spindle (Box 1, reviewed in 13, 34). As proposed in [13] and demonstrated in [82], human MCC is a heterotetrameric complex consisting of its own molecu
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Several DA receptors heteromers with a
2020-05-06
Several DA receptors heteromers with a therapeutic potential have been described, including D1R/D3R (Fiorentini et al., 2010), but their roles remain to be established. Moreover, most studies on receptor heteromers in addiction focused on the striatum because of its key role in the pathology and its
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br Results and discussion In
2020-05-06
Results and discussion In the present study, we used a set of compounds (Fig. 2) consisting of ATP (a), dATP (b), an ATP analog containing β,γ-nonhydrolyzable hypophosphate P-P bond (c), and three pairs of P-diastereoisomers of α-thio-ATP analogs (d,e,f) containing a sulfur n-acetyl-l-cysteine i
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BMS265246 In contrast DAG phosphorylation to PA
2020-05-06
In contrast, DAG phosphorylation to PA by diacylglycerol kinases (DGKs) represents a quantitatively minor metabolic pathway, but is generally regarded as a main disposal pathway for “signaling” DAG. PA produced by DGKs is an intermediate of the synthesis of CDP-DAG, cardiolipin and PI. However, PA i
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Primary human GBM neurospheres expressed high levels of
2020-05-06
Primary human GBM neurospheres expressed high levels of the metabolic enzyme fatty acyl-CoA synthetase VL3 (ACSVL3) that were associated with CSCs self-renewal and tumorigenic capacity. ACSVL3 knockdown significantly decreased ALDH levels, indicating its contribution to cell metabolism and maintenan
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We aim to apply the same technology to
2020-05-06
We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that
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Similar to Bdnf acute administration of RG did
2020-05-06
Similar to Bdnf4, acute administration of RG108 did not alter gene expression of Gria1 and Hdac2, despite their relevance for the task. Gria1 belongs to the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic NPPB sale receptor (AMPAR) family that is known to be crucial for LTP and the strengthening of
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SW033291 sale br Introduction br Multiple levels of
2020-05-06
Introduction Multiple levels of CK2/AKT cross-talk Isoform-specific signaling in CK2/AKT cross-talk Particularly relevant to the scope of this review, it has been shown that depletion of the CK2 catalytic α′ subunit is more effective than that of the α subunit at reducing AKT Ser129 phospho
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br Experimental br Declaration of
2020-05-06
Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR Fmoc-D-Phe(4-Cl)-OH library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound was
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p Kip is a critical component
2020-05-06
p27Kip1 is a critical component of the cell cycle machinery [15]. As an inhibitor of cyclin E-Cdk2, p27Kip1 plays a pivotal role in controlling cell proliferation, S-phase entry, and G1-phase exit during development and tumorigenesis [16]. p27Kip1 is predominantly regulated via posttranslational mod
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Methylated CpGs can recruit transcriptional co repressors
2020-05-06
Methylated CpGs can recruit transcriptional co-repressors to prevent transcription factors (TFs) from promoting gene expression by tightly packing CDK4 inhibitor structures [38]. Two CpG islands in the IPT5b promoter region showed higher methylation level in M9 rootstock compared to Mr (Fig. 3b). H
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