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The G protein coupled receptor GPR also
2021-11-08

The G protein-coupled receptor, GPR40 (also called FFAR1) responds to medium and long chain unsaturated fatty acids, resulting in increase of insulin secretion during elevated glucose levels. The glucose dependency of insulin secretion makes this receptor a very good target for developing therapies
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br Anti Factor Xa methods for DiXaIs measurement in plasma
2021-11-08

Anti-Factor Xa methods for DiXaIs measurement in plasma Concerning Anti-Factor Xa methods, there is an excellent correlation between the 1-stage and 2-stage Anti-assays as shown in Fig. 6, and the concentrations measured are very similar with all methods. These methods and the DiXaI concentration
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Several observations about structure activity relationships
2021-11-08

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic Fmoc-Arg(Pbf)-OH class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether l
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A large body of literature have reported that various
2021-11-08

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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Fmoc-Gln(Trt)-OPfp Several lines of evidences suggest
2021-11-08

Several lines of evidences suggest that the biological features of PCs are different from other CLL/SLL Fmoc-Gln(Trt)-OPfp in the lymph node: the tumor cells in the PCs have been shown to accumulate cytogenetic abnormalities [1, 4] and aberrant expression of oncogene and tumorsuppressor microRNAs (
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Nowadays it is accepted that ligands
2021-11-08

Nowadays, it is accepted that ligands which have been classically described as inverse agonists, due to their negative efficacy at modulating the G protein pathway, could also display some positive efficacy regarding receptor desensitization, internalization, or even signaling though another pathway
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Another level of complexity within the TGF
2021-11-08

Another level of complexity within the TGF-ß/SMAD and Hippo/YAP/TAZ pathway crosstalks was recently uncovered. TGF-ß induces robust TAZ, but not YAP, protein expression in both mesenchymal and epithelial PD 0332991 through a SMAD3-independent, p38/MAPK-dependent mechanism that triggers myocardin-re
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Biological evaluations of the compounds were done both using
2021-11-08

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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Acknowledgments Financial support from the National
2021-11-06

Acknowledgments Financial support from the National Natural Science Foundation of China (81730094, 81473262 and 81573299) is gratefully acknowledged. This project was also supported by the “111 Project” from the Ministry of Education of China, the State Administration of Foreign Expert Affairs of C
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To examine the possible role of mGluRs in the LH
2021-11-06

To examine the possible role of mGluRs in the LH/PFA in the hypercapnic ventilatory response, a nonspecific antagonist of mGluRs, MCPG, was microinjected into the LH/PFA. MCPG elicited a significantly increased hypercapnic ventilatory response in awake rats, but not during sleep, in the light and da
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Notch signaling maintains the balance between neural stem
2021-11-06

Notch signaling maintains the balance between neural stem cells and neural progenitors (Aguirre et al., 2010, Basak and Taylor, 2007, Mizutani et al., 2007). Conditional knock out of Notch causes depletion in the progenitor pool, showing that Notch is required for the maintenance of neural stem cell
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In the last thirty years accumulating data have addressed
2021-11-06

In the last thirty years, accumulating data have addressed a role for GABA in the modulation of gastrointestinal (GI) functions via its possible involvement in the circuitry of the enteric nervous system (ENS). The ENS is a complex neuronal network located within the gut wall, capable of regulating,
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Analysis of the i motif structures during
2021-11-06

Analysis of the i-motif structures during biased unfolding of G-quadruplexes leads to the conclusion that at acidic pH the i-motif is absolutely unaffected by that process. The hydrogen bonds within the i-motif are intact (Fig. 3D) and they only fluctuate around mean values. On the other hand, the i
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br Introduction GPR also known as free fatty acid receptor
2021-11-06

Introduction GPR40 (also known as free fatty dub ubiquitin receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and long-ch
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Introduction of a chloropyridine group onto the
2021-11-06

Introduction of a chloropyridine group onto the fluoro derivative (→) leads to a similarly potent compound that exhibits a lower /, and as was observed with (), was rapidly cleared. However, the high clearance of () did not prevent the increase in the concentrations of FAAs even as its plasma levels
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