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In the a first in vitro indication of modulation of
2022-06-09
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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A mutation in stearoyl coenzyme A desaturase gene
2022-06-09
A mutation in stearoyl coenzyme A desaturase 1 gene was reported to reduce sebum production and monounsaturated fatty acids (MUFA) synthesis in mice, which was accompanied with impaired clearance of gram-positive bacteria-induced skin infection (Georgel et al., 2005). Interestingly, gram-positive ba
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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 GSK J4 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK-87
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In summary PPARG and FFAR are connected
2022-06-09
In summary, PPARG and FFAR1 are connected in several ways, and the presented interaction is mechanistically reasonable. Additional investigations are required to elucidate the exact details of the underlying physiology. However, our findings are of immanent importance for the treatment of type 2 dia
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br Materials and methods br Results br Discussion Cell
2022-06-09
Materials and methods Results Discussion Cell migration not only plays major roles in physiological events, such as embryo implantation, embryogenesis, morphogenesis, neurogenesis, angiogenesis, wound healing and inflammation [[29], [30], [31]], but it is also implicated in the pathophysiol
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br Role of funding source
2022-06-09
Role of funding source Conflict of interest Acknowledgements We thank F. Blaskovits and P. Kesner for technical assistance. This project was supported by operating grants from the Canadian Institutes of Health Research (CIHR) to X. Zhang (MOP123249) and the National Natural Science Foundati
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In conclusion we have shown that the brain penetrating
2022-06-09
In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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TAK-715 A large body of literature have reported
2022-06-09
A large body of literature have reported that various cellular pathways are dysregulated in NPC [19]. Among these pathways, Akt is frequently hyperactivated in NPC and regulates diverse cellular processes including tumor cell growth, proliferation, metabolism, survival and invasion, as well as angio
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A small number of patients had accessory
2022-06-09
A small number of patients (11%) had accessory integrase mutations (E157Q, G163R, L74IM, and/or V151I) that confer potential or low-level resistance and generally only when they occur in combination with other high/intermediate level resistance mutations. This is a somewhat higher incidence than tha
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Not only does G a GLP complex
2022-06-09
Not only does G9a/GLP complex appear to play a role (albeit a seemingly conflicting one) in LTP maintenance, it may also be involved in long-term depression (LTD) (). At hippocampal CA1 synapses, LTD can be induced by pharmacological or synaptic stimulation of Group 1 metabotropic glutamate receptor
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BMP signals play pivotal roles in the various processes
2022-06-09
BMP signals play pivotal roles in the various processes of chondrogenesis [12], [13]. At early stages of chondrogenesis, BMP signaling regulates the differentiation of mesenchymal UNC669 into chondrocytes via the induction of Sox9[29]. The loss of Noggin, a BMP antagonist, results in the overgrowth
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Thus while there is ample evidence to rule out a
2022-06-08
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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Biological evaluations of the compounds were done
2022-06-08
Biological evaluations of the compounds were done both using HCV protease and replicon assays. Results are shown in . The protease inhibitory IC’s were determined using a FRET assay with HCV NS3/4A 1a protease domain. The replicon EC’s were determined using a replicon luciferase cell-based assay. Th
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Under most circumstances NO is a potent endogenous vasodilat
2022-06-08
Under most circumstances, NO is a potent endogenous vasodilator. Therefore, its involvement in an endothelium-dependent contraction seems paradoxical, to say the least. Soluble guanylyl cyclase (sGC) is the major downstream target of NO; its inhibition results in the lack of vasoconstrictor response
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NPxY was recognized as the first short signal
2022-06-08
NPxY was recognized as the first short signal sequence motif in the cytoplasmic domain of membrane receptors and proteins with critical roles in internalization and trafficking of receptor molecules [130]. Including LDL receptor, beta-1 integrin, megalin, beta-amyloid precursor protein, EGF receptor
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