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KU55933 Treatment and control for IBD are targeted
2021-09-30

Treatment and control for IBD are targeted to identify and eliminate the cause if possible, decrease intestinal inflammation, reduce diarrhea and vomiting, improve appetite, and promote weight gain. Methods include dietary manipulation with or without concurrent medical therapy such as corticosteroi
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NVP-AEE788 Eastern Guangdong is a Teochew dialect area
2021-09-30

Eastern Guangdong is a Teochew dialect area. We found that subtype 1b (3.1%) in this region was significantly lower than in other areas. Subtype 1b began its spread from the central part of China out into the whole country through illegal blood donation in the mid-1990s (Lu et al., 2013) and is now
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SB431542 While published data around the functional signific
2021-09-30

While published data around the functional significance of GPR84 are quite sparse, details of signaling pathways initiated by the receptor are even more limited, including in recombinant systems. In recombinant cells, GPR84 activation reportedly leads to Gi pathway activation, resulting in pertussis
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auda br Conclusion and future perspectives The
2021-09-30

Conclusion and future perspectives The nicotinic auda receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic acid and lact
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In summary through medicinal chemistry design and computer
2021-09-30

In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on d
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ATP is essential for maintaining
2021-09-30

ATP is essential for maintaining the ionic balance of the lens (Michael and Bron, 2011). Without sufficient ATP there is an ionic imbalance due to Na+K+ATPase dysfunction. Previous studies have shown that rabbit lenses incubated ex vivo without glucose rapidly lost ATP in their lens epithelium and f
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The usefulness of GIP R antagonism for the treatment of
2021-09-30

The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig
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br Results br Discussion Our studies highlight MUFAs as key
2021-09-29

Results Discussion Our studies highlight MUFAs as key lipid modulators of both non-apoptotic and apoptotic cell death. Recent studies show that a more mesenchymal phenotype, de-differentiation, and acquired resistance to targeted inhibitors, can all promote a ferroptosis-sensitive cell state (
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It has been shown that mice lacking SMAD
2021-09-29

It has been shown that mice lacking SMAD2 in T cells do not develop spontaneous lymphoproliferative autoimmunity (Malhotra et al., 2010). Further, FOXO1 is known to activate proinflammatory MCP-1 and IL-6 (Ito et al., 2009). To this end, we also validated the downstream target FOXO1 and SMAD2 after
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Multi targeting agents are of major
2021-09-29

Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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Bile acids synthesized in the liver are secreted into
2021-09-29

Bile acids synthesized in the liver are secreted into the intestinal tract to facilitate the digestion and Plumbagin receptor of nutrients. Most bile acids are reabsorbed by the ileum and are transported back to the liver via the portal blood circulation. Recently, bile acids have also been conside
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Importantly each conformational state in the SRP SR dimer
2021-09-29

Importantly, each conformational state in the SRP–SR dimer provides a distinct point of regulation at which these GTPases can directly sense and respond to different biological cues in the pathway. For example, assembly of a stable ‘closed’ complex between SRP and SR is intrinsically very slow (kon
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We show that pharmacological inactivation of GSTP over
2021-09-29

We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I
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br Molecular mechanisms underpinning GSNOR function in
2021-09-29

Molecular mechanisms underpinning GSNOR1 function in the defence response Recently, Arabidopsis GSNOR1 has been shown to govern the extent of S-nitrosylation of two key regulatory proteins, Non-Expresser of Pathogenesis-Related Genes 1 (NPR1) and SA binding protein 3 (SABP3), which are integral t
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The intracellular signaling that mediates the adipogenesis i
2021-09-29

The intracellular signaling that mediates the adipogenesis induced by GPR120 still remains largely unknown. In the present study we showed that TUG-891 induced the activation of [Ca2+]i and ERK1/2 signaling in 3T3-L1 cells. Moreover, incubation of TUG-891 combined with BAPTA-AM or U0126 abolished TU
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