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Despite potent biological actions the
2022-06-13
Despite potent biological actions, the native hormone undergoes degradation by the enzyme dipeptidylpeptidase-IV (DPP-IV) [17] and is rapidly cleared from the bloodstream by renal filtration [18]. One such approach to prolong the biological half-life of GIP is through conjugation with a polyethylene
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br The Farnesoid X receptor FXR identification and ligands T
2022-06-10
The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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Natural product based drug discovery can be
2022-06-10
Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in Epalrestat binding assays, we used molecular modeling to predict how well these compounds f
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Although drug monitoring is not usually requested there are
2022-06-10
Although drug monitoring is not usually requested, there are some cases where measurement of DOACs in Edrophonium chloride is useful, and of special help for managing patients at risk. These cases include the control of adherence to a therapeutic protocol, surveillance of drug accumulation risk in
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To understand the structural basis for
2022-06-10
To understand the structural basis for the mode of action of indole-based compounds the crystal structures of bound to both the wild type and A128T IN CCDs have been solved. The X-ray crystallography studies have revealed that binds at the IN dimer interface in the principal LEDGF/p75 binding pocket
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The relationship between the attention deficit hyperactivity
2022-06-10
The relationship between the attention deficit hyperactivity disorder (ADHD) and H3Rs is supported by several reports (Berlin et al., 2011; Passani, Bacciottini, Mannaioni, & Blandina, 2000; Vohora & Bhowmik, 2012). ADHD is a neurobehavioral disorder with high prevalence in children, with hyperactiv
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br Acknowledgments We thank Drs Yasuhiro Saito and Mitsuru
2022-06-10
Acknowledgments We thank Drs. Yasuhiro Saito and Mitsuru Futakuchi for helpful discussion. We also thank Drs. Kohei Miyazono and Tadashi Matsuda for cells. This work was supported by Grant-in-Aids for Scientific Research on Innovative Area (16H06373; 16K15273) from MEXT, Japan (to M.H.) and by Pr
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Several studies have indicated that PLD regulated PA signali
2022-06-10
Several studies have indicated that PLD-regulated PA signaling intersects with Rho-mediated cytoskeletal remodeling to drive mesenchymal-like cellular features, and it is known that Rho signaling has the potential to induce YAP/TAZ nuclear activity. Accordingly, Han et al. (2018) provide evidence th
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br Discussion Light plays a central role in plant growth
2022-06-10
Discussion Light plays a central role in plant growth, development and defence responses. It is required for photosynthesis and other metabolic or transcriptional processes (Kangasjärvi et al., 2012, Zhang and Zhou, 2013, Ballaré, 2014). It is well known that darkness promotes leaf senescence, wh
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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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