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Species specificity of small molecular GPR agonists
2022-03-22
Species specificity of small molecular GPR40 agonists have been reported by Takeda scientist. In the binding pocket of TM5, a Leu186 in human GPR40/FFA1 is replaced with Phe in rat, resulting in dramatic inter-species GPR40 activity discrepancy in certain scaffolds of small molecular GPR40 agonists.
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To validate that our natural
2022-03-22
To validate that our natural experiment operates primarily through a large negative shock to the risk-taking incentives provided by option compensation measured by vega, we do two sets of tests. First, we confirm a significant drop in vega after the adoption of FAS 123R for treated firms relative to
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br Acknowledgment br Introduction Non steroidal anti inflamm
2022-03-22
Acknowledgment Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are widely utilized to treat pain and inflammation [1], but their chronic use is hindered by a variety of potentially serious adverse events that include gastrointestinal (GI) mucosal lesions, bleeding and perforations
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br Materials and methods br Results
2022-03-22
Materials and methods Results Discussion The major findings of the present study are that: 1) the response to inverse agonists may be crossregulated by the activation of either (±)-Bay K 8644 sale H1 or H2 receptors, 2) histamine H1 and H2 receptor inverse agonists crossdesensitize the rece
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Mycophenolate Mofetil synthesis Hypoxia HIF and Inflammation
2022-03-22
Hypoxia, HIF, and Inflammation Cellular responses to hypoxia are essential for life and are now recognized to be dysregulated in a wide range of disease processes. The key players in these pathways are a family of transcription factors, the hypoxia-inducible factors (HIFs; see Glossary), as well as
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HER genotype was determined in breast cancer tissue of
2022-03-22
HER2 genotype was determined in breast cancer tissue of 73 breast cancer patients. As previously reported, Ile655Val and Ala1170Pro genotypes measured in breast cancer tissues were available for 71 and 69 breast cancer patients, respectively. Briefly, 77.5% (55/71) of patients were homozygous for th
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Considering that TGF plays a pivotal role in
2022-03-21
Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG
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It was revealed that various injured or
2022-03-21
It was revealed that various injured or infected organs of Hippeastrum produce a mixture of an orange-colored chalcone and flavans which can be oxidized to red-colored dimer (Wilmowicz et al., 2014, Wink and Lehmann, 1996), preventing the penetration of injured tissues by Phoma narcissi, Botrytis ci
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Little is known about the
2022-03-21
Little is known about the endocrinological control of reproduction in polychaetes. In vertebrates, gonadal maturation is regulated by the hypothalamo-pituitary-gonadal axis. GnRH, GTHs, and steroid hormones are involved in this axis (see Okubo and Nagahama, 2008). In two polychaete species, Perinere
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To investigate if such an effect is
2022-03-21
To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m
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Glutamate is a ubiquitous principal excitatory neurotransmit
2022-03-21
Glutamate is a ubiquitous principal excitatory neurotransmitter in the pde-5 inhibitors that plays a central role in a variety of brain functions (Delgado, 2013, Hawkins, 2009). Several studies reported that CSF glutamate was associated with mental illness, including major depressive disorder, anxio
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In respect of clinical development Takeda has pioneered the
2022-03-21
In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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br Declaration of interest br Acknowledgments This work was
2022-03-21
Declaration of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 31471615), the Introduction of Talent Research Start-up Fund of Anhui Polytechnic University (No. 2017YQQ017) and the Pre-research Project of National Natural Sc
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Yeast two hybrid screening studies have provided the foundat
2022-03-21
Yeast two-hybrid screening studies have provided the foundation for countless investigations of protein-protein interactions [[141], [142], [143]]. To identify additional hepatic proteins similar to GKRP that are implicated in GCK regulation, a group of researchers conducted a two-hybrid study using
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ampar Although in in vitro analyses GANT sensitized Daoy cel
2022-03-21
Although in in vitro analyses GANT61 sensitized Daoy ampar to RITA treatment, this was not fully reflected in the in vivo xenograft studies in nude mice, as the combinatorial treatment elicited a comparable reduction of tumor growth. However, the dual drug administration reduced within-group variati
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