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In addition several other considerations were made for the
2021-10-18
In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty pramiracetam receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization efforts were c
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br Acknowledgments br The study was
2021-10-18
Acknowledgments The study was funded by the European Commission FP7-project Beta-JUDO (Grant 279153), and Swedish Diabetes Association (Grant DIA 2013-043) and Family Ernfors Foundation (Grant 150430). Free fatty PF-4708671 receptors (FFARs) represent a family of G-protein coupled receptors
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The minimal segment of the SIM
2021-10-18
The minimal segment of the SIM appears to be a core of Tolvaptan residues, which frequently matches the consensus sequences ΨΨΨΨ, ΨxΨΨ, or ΨΨxΨ (where Ψ is V, I, or L and x is typically D, E, S, or T) [29,31,32]. In a subset of SIMs, this hydrophobic core is flanked by serine residues and a stretch
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To address this we developed
2021-10-18
To address this, we developed approaches to image at high spatial and temporal resolution live WPB fusions as well as the release of VWF and other WPB cargo by spinning disk microscopy and combined laser ablation and total internal reflection fluorescence (TIRF) microscopy. Our live cell imaging re
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Pexmetinib br Although there are growing
2021-10-18
Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a
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The first suggestion that the Hh pathway might be
2021-10-18
The first suggestion that the Hh pathway might be involved in the pathogenesis of chronic liver disease was reported at the beginning of this millennium by Shackel et al. who noted that Patch and Gli were upregulated in their microarray analysis of liver tissues from patients with primary biliary ch
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br Hedgehog pathway The Hedgehog pathway
2021-10-18
Hedgehog pathway The Hedgehog pathway (Fig. 1) derives its name from Hh gene mutant Drosophila, which presents a spiked phenotype resembling the animal “hedgehog” [13]. The Hh proteins control embryonic development in vertebrates, where the signaling mechanisms mediated by the proteins are multip
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The HCV Ag immunoassay has been shown
2021-10-18
The HCV-Ag immunoassay has been shown from previous studies to be an adequate alternative to the two-stage diagnostic process [6], [9], [16]. Kesli et al. reported a high correlation coefficient of 0.864 when comparing HCV core antigen levels with HCV RNA levels (detected using Qiagen HCV RNA test;
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Substrate affinity and specificity can be enhanced by dockin
2021-10-18
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of emodin bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of short li
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The ketone body receptor HCA is most likely
2021-10-18
The ketone body receptor HCA2 is most likely not active under normal conditions, since local levels and plasma levels of ketone bodies such as β-HB are too low to activate the receptor. However, overnight fasting or prolonged starvation results in plasma levels of the ketone body in the millimolar r
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br Experimental br Results and discussion br Conclusion
2021-10-18
Experimental Results and discussion Conclusion In the current work, a novel method for separation and preparation of flavonoid glycosides from L. chinensis was successfully developed using a 2 D-HILIC × RPLC system based on a zwitterionic Click XIon column and a polar-modified Atlantis T3 c
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br According to WHO estimates
2021-10-18
According to WHO 2014 estimates, diabetes continues to present an increasing health risk to the global population, affecting 422 million individuals worldwide. Type 2 diabetes (T2D), which affects the vast majority (ca. 90%) of the diabetic population, occurs when the body cannot effectively utili
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In fact changes in mitochondrial dynamics
2021-10-18
In fact, changes in mitochondrial dynamics directly affects many things including cellular metabolism [127], mitochondrial mass and turnover [128], mitochondrial transport, and calcium buffering [129]. Nigrostriatal DA neurons seem to have a preferential susceptibility to loss of Mfn2 when compared
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br HO regulation and physiology The catabolism
2021-10-16
HO-1: regulation and physiology The catabolism of cellular heme in humans and other species is mediated by the heme oxygenase (HO) family of enzymes (E.C. 1:14:99:3; heme-hydrogen donor:oxygen oxidoreductase). The HOs localize primarily to the endoplasmic reticulum (ER) where they serve, in conce
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Starting from the hypothesis that
2021-10-16
Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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