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Furthermore we also found that
2022-06-10

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 show that lactate activates the
2022-06-10

Here we show that lactate activates the Gi-coupled receptor GPR81, which is exclusively expressed on adipocytes, and that lactate released from adipocytes in response to glucose and insulin mediates insulin-induced antilipolysis by activation of GPR81. Results Discussion Nutrients and their m
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By contrast pentameric glycine receptors
2022-06-09

By contrast, pentameric glycine receptors (GlyR) in humans have four functional subunits, α1− α3 and β (Lynch, 2004) whereas the retina of other mammals have an additional α4 subunit (Harvey et al., 2000), and in humans the α4 subunit is considered a pseudogene as it lacks the 4th transmembrane dom
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Growing evidence suggests that the glycine
2022-06-09

Growing evidence suggests that the glycine site seems to play a pivotal role in NMDAR-related function. For example, it or has been demonstrated in a hippocampal slice study that the glycine site sub-serves the spatiotemporal detection of synaptic activity (Li et al., 2009). Moreover, mice with poin
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Conformational changes are observed in
2022-06-09

Conformational changes are observed in the LBDs after ligand binding, including partial cleft closure for GluN2A and complete cleft closure for GluN1. For GluN2A, additional conformational rearrangements in the protein and ligand may be required before the ligand can be accommodated within lobe 2. F
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In teleosts GR is expressed in almost every cell and
2022-06-09

In teleosts, GR is expressed in almost every cell and regulates genes controlling development, metabolism, and immune response [17,18]. Several teleosts contain two GR genes, GR1 and GR2 [8]. Other groups have found only one GR in some species thus far, such as the Japanese flounder, brown trout, an
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In the course of our synthetic
2022-06-09

In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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Analysis of genomic neighborhoods has helped
2022-06-09

Analysis of genomic neighborhoods has helped resolve questions concerning the orthology of receptors for peptides similar to glucagon (Ng et al., 2010, Irwin and Prentice, 2011, Wang et al., 2012, Hwang et al., 2013). Using a diverse array of species with available genome sequence (see Fig. 4) the g
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Cx mimetic peptides short synthetic peptides corresponding
2022-06-09

Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino GSK2606414 sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a concent
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In the course of our ongoing attempts
2022-06-09

In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric niclosamide type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the proc
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Through the analysis of various synthetic GPR agonists
2022-06-09

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic CCT007093 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TA
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While earlier reports on ferroptosis did not clarify mitocho
2022-06-09

While earlier reports on ferroptosis did not clarify mitochondrial damage and consequent death signaling in this paradigm of oxidative death, evidence from recent studies in neuronal systems strongly suggested a mechanistic link between enhanced lipid peroxide formation and loss of mitochondrial int
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Several transgenic and knockout congenic
2022-06-09

Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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br Materials and methods All
2022-06-09

Materials and methods All studies were performed in 230–250g timed-pregnant Sprague Dawley rats (Harlan, Indianapolis, Indiana). Animals were housed in a temperature controlled room with a 12:12 light:dark cycle. All experimental procedures in this study were in accordance with the National Insti
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The FAAH inhibitor activity of the ethoxycarbonyl phenyl
2022-06-09

The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compound
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