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Regulation of gene expression in mammalian cells is
2021-11-24
Regulation of gene expression in mammalian cells is governed by the epigenetic machinery, which includes several distinctive yet entangled branches. DNA and histone modifying enzymes, non-coding regulatory RNAs, and ATPase-dependent chromatin remodeling proteins all contribute to the dynamic alterat
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Based on the aforementioned findings
2021-11-24
Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated
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A series of P P
2021-11-23
A series of P3-P4 ureas were explored first and their anti-NS3 protease activity, antiviral properties in a HCV replicon cell-based assay and PK profiles examined. Installation of a methyl group on the P4 side nitrogen Digoxigenin-11-dUTP sale of the urea yielded , a molecule which retained intrinsi
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br Other Functions of HCA Receptors HCA
2021-11-23
Other Functions of HCA Receptors HCA receptors, in particular HCA1, are expressed in various primary tumor Acitretin 77, 78, 79. This is of interest, as most solid tumors show increased glucose uptake and lactate formation even under normoxic conditions, with lactate concentrations in the tumor m
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In summary through medicinal chemistry design
2021-11-23
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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To further investigate if GPR
2021-11-23
To further investigate if GPR40 was the functional target of these phenylpropiolic wehi analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GPR40 cell
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pHi regulation in astrocytes has been
2021-11-23
pHi regulation in astrocytes has been examined primarily in cell culture rather than in situ. Two HCO3−-dependent transporters, NBC and Na+-driven Cl-HCO3 exchange (NDCBE), have been described [10,16], in addition to Cl-HCO3 anion exchange (AE) [96]. Culture studies indicate that NHE is the principa
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br Introduction Regulation of transcription is a
2021-11-22
Introduction Regulation of transcription is a critical event of the embryonic development and epigenetic mechanisms such as histone modifications and DNA methylation appear important in mediating temporal changes, and differences among cells/tissues, of temporary stabilized transcriptomes (Mas et
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Recently the toxicity of TBT
2021-11-22
Recently, the toxicity of TBT was demonstrated at the vascular level in animal models (Nath, 2008), and the results obtained so far suggest that TBT may be a potential risk factor for cardiovascular diseases. TBT is capable to alter the coronary vascular reactivity to estradiol (dos Santos et al., 2
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Fig illustrates the different signaling pathways
2021-11-22
Fig. 1 illustrates the different signaling pathways elicited or modulated by H3R activation. Collectively, the modulation of the release of histamine and other neurotransmitters through H3R activation could be linked to several neurological disorders such as sleep disorders like narcolepsy, Alzheime
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br Acknowledgement The work was supported by the
2021-11-22
6. Acknowledgement The work was supported by the NSFC through Grant Nos. 11535016 and 11475232. It was also supported by CAS. The authors thank their collaborators for beneficial discussions and enthusiastic supports in the simulations and calculations. Introduction Hypoxia-inducible factors
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Furthermore we also found that both activation of
2021-11-22
Furthermore, we also found that both activation of oncogenes and inactivation of tumor suppressor genes occurred in HBV oval cells, which showed opposite pattern in HBV hepatocytes. These genes might take part in neoplastic transformation of oval cells induced by HBV regarding the multipotent role o
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Here we used Drosophila and mouse models to
2021-11-22
Here, we used Drosophila and mouse models to address the biological function of RALs in the adult intestine. Our results demonstrate a conserved in vivo role for RALs in ISC function during tissue homeostasis and regeneration. ISCs lacking RALs were at a disadvantage compared to wild-type neighbors.
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One of pathogenesis of COPD is oxidant antioxidant
2021-11-22
One of pathogenesis of COPD is oxidant/antioxidant imbalance. Indeed, it is well known that chronic tobacco smoking is a major risk factor for the development of COPD, and a defect in the detoxification of reactive species produced by cigarette smoke may predispose smokers to airflow obstruction and
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The experiments reported herein were designed to test
2021-11-22
The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w
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