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While phosphorylation site motifs are typically
2021-10-28
While Rimonabant site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinase, w
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The GSTP promoter region in PCA cells without or with
2021-10-28
The GSTP1 promoter region in PCA cells without or with reduced GSTP1 mRNA expression had a different histone modification pattern than BPH-1 cells with GSTP1 mRNA expression: the repressive histone modifications H3K9me3/H3K27me2 were distinctly increased and H3K27me3/H3K9me2 were slightly decreased
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Introduction Multiple sclerosis MS a
2021-10-28
Introduction Multiple sclerosis (MS), a neurological autoimmune disease, is driven by CD4+ Azithromycin Dihydrate of the T helper (TH) cells [1]. There is no curative treatment for MS and the present treatments typically focus on immunomodulation for slowing the progression of the disease. These in
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The ion conduction pathway reported herein accounts for
2021-10-28
The ion conduction pathway reported herein accounts for all known functional properties of EAAT/GltPh anion channels. Simulations reveal unitary current amplitudes and ion selectivities (Figures 3C and 3D) that resemble experimental results (Melzer et al., 2003, Wadiche and Kavanaugh, 1998). The cal
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If some of the experimentally determined tRNAGlu
2021-10-28
If some of the experimentally determined tRNAGlu identity elements are unique to E. coli, then there also must be some unique phylum-specific residues in the corresponding GluRS (E. coli in particular, and proteobacteria in general) as well. In this paper we focus on identifying such residues in E.
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A localization of GK to both a
2021-10-28
A localization of GK to both a cytoplasmic and perinuclear area of normal rat pancreatic beta-cells was reported in 1996 (Noma et al., 1996), which changed on acute hyperglycemia to a more diffuse staining throughout the cytoplasm. The localization of GK within the nucleus was first reported by Mura
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Decreases in LS mean h WMG versus placebo
2021-10-28
Decreases in LS mean 24-h WMG versus placebo were observed with both the 10mg q.d. a.m. (−18.8mg/dL) and 6mg q.d. p.m. (−25.0mg/dL) MK-3577 ‘partial blockade’ regimens, but was not assessed for the 25mg b.i.d regimen. Decreases in FPG versus placebo were observed for both the 10mg q.d. a.m. (−7.2mg/
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More polar substituents introduced on the position of the
2021-10-28
More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in m
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br Introduction The fibroblast growth factor
2021-10-28
Introduction The fibroblast growth factor receptor (FGFR) pathway is an important oncogenic driver in malignant cancer. It controls cellular processes such as cell proliferation, differentiation, migration, Reparixin L-lysine salt progression, metabolism, and survival. In non–small-cell lung can
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In terms of cytotoxicity studies under
2021-10-28
In terms of cytotoxicity studies under two-dimensional cell culture conditions, only two of the above-mentioned publications with liposomal formulations of tyrosine kinase inhibitors reported viability data as compared to respective free drugs. On the one hand, liposomal gefitinib exerted strongly r
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In conclusion a novel series of GPR
2021-10-28
In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen DL-α-Hydroxyglutaric acid disodium salt had a remarkable effect on t
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sodium salt Now we turn to the other channel
2021-10-28
Now we turn to the other channel through which the risk-taking incentives provided by option compensation affect corporate debt maturity. Jensen and Meckling (1976) argue that the payoff structure of debt holders in a levered firm is concave, while that of equity holders is convex, thus, shareholder
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br Development of calibrators and controls for
2021-10-28
Development of calibrators and controls for DiXaIs Method validation and comparison with reference technique (LC:MS) At this stage, anti-Factor Xa bioassays can be established for reliably measuring DiXaI concentrations in plasma, with the available appropriate drug specific calibrators and co
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Two recently developed highly specific EZH
2021-10-28
Two recently developed, highly specific EZH2 enzymatic inhibitors, GSK126 and EPZ-6438, are currently in clinical trials for treating lymphomas (Kim and Roberts, 2016). Although these EZH2 inhibitors have shown antitumor effects in lymphoma cells with enzyme-activating mutations of EZH2 (Knutson et
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Acetylation of histones by histone
2021-10-28
Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing 9292 structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Recent studies demo
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