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cAMP is a key secondary messenger which transduces
2021-11-29
cAMP is a key secondary messenger which transduces extracellular signals at glucagon receptors to intracellular effector molecules. cAMP-protein kinase A (PKA) pathway increases the gene expression of enzymes including phosphoenolpyruvate carboxykinase (PEPCK) and glucose 6-phosphatase (G6Pase) whic
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In our reporter assay system C H T Gli Luc
2021-11-29
In our reporter assay system, C3H10T1/2-Gli1-Luc cells were incubated with Shh CM to induce Gli1-mediated luciferase activity (Fig. 1B). Z-Ajoene inhibited Shh CM-induced luciferase activity in a concentration-dependent manner as seen in Fig. 1C. Z-Ajoene also inhibited SAG (a Smo activator)-induced
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In the a first in vitro indication of modulation
2021-11-29
In the 2003, a first in vitro indication of modulation of FXR expression in CRC showed that FXR expression was absent in undifferentiated colon carcinoma cell line SW480, while it was progressively increasing along with the degree of cell differentiation in Caco2 and HT29 cells, and its transcriptio
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Fmoc-Phe-OH To investigate the potential molecular mechanism
2021-11-29
To investigate the potential molecular mechanism of FXR-mediated regulation of liver cancer cell proliferation, gene expression profiles were determined using Agilent arrays in SK-Hep-1-FXR and NC after treatment with the FXR agonist GW4064. The results indicate that mTOR and S6k are involved in div
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The rationale for developing HDACi as anticancer agents was
2021-11-29
The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and integrin signaling pathway arrest of cancer cells 1, 2, 3. HDACi have been used in the treatm
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Initial structural and biochemical work showed that Get
2021-11-29
Initial structural and biochemical work showed that Get3 forms an obligate dimer whose conformation is regulated by the bound nucleotide. Analogous to SRP and SR, Get3 contains a P-loop nucleotide hydrolase domain in which the bound ATPs face one another at the dimer interface (Figure 3A, top right
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The cytoprotective effects of glyRs have been reported to as
2021-11-29
The cytoprotective effects of glyRs have been reported to associate with the MAPK (JNK, ERK1/2 and p38) signaling pathways [47], [48]. The present study reveals that suppressive phosphorylation of cRaf-MEK1/2-ERK1/2 is initiated by glycine – glyR α2 interactions in cardiomyocytes. As a central regul
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Several observations about structure activity relationships
2021-11-26
Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic STA-21 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of
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Accumulating evidence suggests an important role for
2021-11-26
Accumulating evidence suggests an important role for endothelin ETB receptors in renal homeostasis. ETB receptors promote vasodilation, natriuresis, and diuresis (Davenport and Maguire, 2011) and maintain renal perfusion via counterbalancing the effects of vasoconstrictors and regulation of water re
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In T cells whereas SETDB is implicated in OX dependent
2021-11-26
In T cells, whereas SETDB1 is implicated in OX40-dependent repression of the Il17a locus in Th17 cells (Xiao et al., 2016), SUV39H1 controls Th2 cell stability by depositing H3K9me3 at the Ifng promoter (Allan et al., 2012). However, the deregulation of the Ifng locus observed in Suv39h1−/− cells ca
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br Histamine H R The cloning of the
2021-11-26
Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other OSI-930 receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al., 2009, Liu e
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Treatment with histamine had no
2021-11-26
Treatment with histamine had no effect on histamine H1 receptor expression in HepG2 serine protease inhibitor (Fig. 1), while knockdown of histamine H1 receptor expression prevented histamine from repressing apo A-I gene expression (Fig. 2). Overexpression of the histamine H1 receptor regulated apo
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The finding of histamine action on ASICs also
2021-11-26
The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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In order to find better LODs LOQs
2021-11-26
In order to find better LODs, LOQs and peak shape researchers used different derivatization agents along with dansyl chloride. However, these procedures required longtime for sample preparation, low recovery, the chance of contamination; products instability and some reagents were unable to derivati
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Thus while there is ample evidence to rule out a
2021-11-26
Thus, while there is ample evidence to rule out a generalized blockade of TGF-ß signaling by Hippo pathway activation upon establishment of cell–cell contacts, more recent studies have established that, in specific contexts, Hippo and TGF-ß signaling may either interfere or cooperate with each other
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