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Analogous to all GPCRs the
2022-03-04
Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva
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Although in in vitro analyses GANT sensitized
2022-03-04
Although in in vitro analyses GANT61 sensitized Daoy Bufexamac 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 var
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br Conclusion br Ethics statements file
2022-03-04
Conclusion Ethics statements file Conflict of interest Acknowledgements This study was supported by the National Research Foundation of Korea (NRF) Grant funded by the Korean Government (MSIP) (Nos. 2011-0030074 and 2018R1D1A3B07050361) and Sookmyung Women’s University Specialization Pro
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The highest metabolic stability observed
2022-03-04
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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GSK 2837808A Some malignant human tumors cells also express
2022-03-04
Some malignant human tumors GSK 2837808A also express FPRs and respond to bacterial or endogenous agonists by increased motility and growth. For instance, FPRs expressed by human gastric cancer cells, mediate epithelial–mesenchymal transition, cell proliferation, migration, and resistance to apopto
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br Results The RAS MEK ERK pathway is a potential
2022-03-04
Results The RAS/MEK/ERK pathway is a potential target of FGFR signaling. Indicative for its activation is the presence of double phosphorylated (activated) ERK (dpERK), which is generated in a series of phosphorylation events downstream of FGFR (op. cit. (Lemmon and Schlessinger, 2010)). Followin
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MST are involved in signalling pathways following
2022-03-03
MST1/2 are involved in signalling pathways following along the canonical and noncanonical Hippo pathway. The canonical pathway is highly conserved between D. melanogaster and mammals and a master regulator of tissue growth. During development and within the canonical pathway, MST1/2 seem to have red
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xanthine oxidase inhibitors Kinases belonging to the Thousan
2022-03-03
Kinases belonging to the Thousand and one (Tao) family are conserved throughout evolution. Three Tao proteins are encoded in the human genome (TAO1, TAO2, and TAO3), while D. melanogaster possesses a single ancestral Tao kinase (Tao-1). Like Hpo and GckIII, Tao kinases belong to the Sterile 20-like
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Upon LPS stimulation ERK and
2022-03-03
Upon LPS stimulation, ERK and STAT3 signaling pathways were activated in a time-dependent manner, and the phosphorylation of Y705 occurred later than that of S727 (Supplementary Fig. S5B). STAT3 is known to be phosphorylated on serine 727 (S727) by the mitogen-activated protein (MAP) kinase pathway
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P corneus is a freshwater
2022-03-03
P. corneus is a freshwater hermaphroditic gastropod that is distributed all over the world (Jopp, 2006). In previous works of our laboratory, we have characterized the activities of B-esterases and we have also reported that the exposure for 48h to chlorpyrifos inhibits ChE and CES of whole Luzindol
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It is an open question if
2022-03-03
It is an open question if these in vitro findings have implications for the use of sGC activators in the in vivo situation and in patients. Assuming that incorporation in de novo synthesised enzyme occurs during therapy, one might speculate that the duration of drug administration has an influence o
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In this study we also investigated the
2022-03-03
In this study, we also investigated the role of GST Tideglusib in relation to ASD. In univariable analyses, where the role of each GST gene (i.e., GSTM1, GSTT1, GSTP1) was individually assessed, we did not observe any significant associations between the GST genotypes and ASD. In contrast, a previo
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br Materials and methods br Results br
2022-03-03
Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the Ivacaftor benzenesulfonate sale coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by
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The ability of FFA to elevate intracellular levels
2022-03-03
The ability of FFA4 to elevate intracellular levels of Ca2+5, 38, 39, 40 provided early predictions of a key role of the phosphoinositidase C-linked G proteins Gq and/or G11 in transduction of signals from this receptor, while later studies that examined production of inositol phosphates [41] provid
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In order to elucidate the mechanisms behind the
2022-03-03
In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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