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br Conflict of interest br Transparency document
2022-04-01

Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr.
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br Introduction Farnesoid X receptor FXR is a
2022-04-01

Introduction Farnesoid X receptor (FXR) is a bile Licarbazepine regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) that
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The overall very satisfactory potency profile of compounds a
2022-04-01

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic 2768 australia core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularl
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br The potential of EPA
2022-04-01

The potential of EPA-Ffar4 signaling as a novel intervention for HFpEF Conclusions and future directions Optimization of ω3-PUFA/EPA-therapy based upon titration to achieve therapeutic levels: A pressing clinical challenge is to continue to define the benefit of ω3-PUFA/EPA-therapy. Recent ana
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Due to the presence of all FGFRs
2022-04-01

Due to the presence of all FGFRs in the epithelium, there are several FGFs ligands that could be binding to these FGF receptors, namely FGFs 1–4, 8–10, 16 and 18–20. By evaluating the known roles of FGFs in epithelial-mesenchymal interactions and in bone development, this list can be reduced. For ex
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geldanamycin Previous research has suggested that difference
2022-04-01

Previous research has suggested that differences in spatiotemporal regulation of intracellular signaling pathways can confer specificity to cellular responses (Marshall, 1995). Conventional approaches based on gain- or loss-of-function genetic manipulations or small-molecule inhibitors, however, lac
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The lack of biological activity
2022-04-01

The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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br Anandamide signaling and cardiovascular function The card
2022-04-01

Anandamide signaling and cardiovascular function The cardiovascular effects of cannabinoid compounds have been known for a long time. Studies in humans indicate that chronic use of marijuana causes long lasting decrease in blood pressure and heart rate, whereas the acute use increases heart rate
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FXa is a vitamin K
2022-04-01

FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 pathways cu and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The ac
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Over recent decades there were three breakthroughs
2022-03-31

Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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Due to the importance of gene regulation in cancers HDAC
2022-03-31

Due to the importance of gene regulation in cancers, HDAC inhibitors have been studied extensively in cancer biology and are in current clinical use as anti-tumor therapies [17]. The HDAC inhibitors vorinostat, romidepsin, and belinostat have been approved for certain T-cell lymphomas, and panobinos
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Based on pharmacophore modeling a good HDAC inhibitor
2022-03-31

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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Several lines of evidence suggest that thermosensation in AF
2022-03-31

Several lines of evidence suggest that thermosensation in AFD is unlikely to be mediated by thermosensitive ion channels. AFD exhibits a steep temperature dependence with a reported Q of >1015 for temperature-evoked current, implying a strong amplification step in the thermotransduction process (Ram
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br Structural studies of GCAP Recoverin was the first member
2022-03-31

Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding R 59-022 receptor to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-terminal domains. T
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The difference in the expression of functional FFARs
2022-03-31

The difference in the expression of functional FFARs between neutrophils and monocytes/macrophages suggests that the role of FFA2R may be restricted to the very early phase of acute inflammation where neutrophils are dominating players called into action, whereas GPR84 may have a broader functional
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