• Recent studies in our laboratory demonstrated that

  2022-06-10

  

  Recent studies in our laboratory demonstrated that several histamine H1 receptor antagonists induce apo A-I gene expression while histamine itself represses it [20]. In humans, there are three histamine receptor genes (H1, H2, and H3) that code for G-protein-coupled receptors (GPCR's) which bind his

• Multi targeting agents are of major

  2022-06-10

  

  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;

• Bile acids synthesized in the liver are

  2022-06-10

  

  Bile acids synthesized in the liver are secreted into the intestinal tract to facilitate the digestion and Deacetylase Inhibitor Cocktail 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 b

• br Acknowledgements This research was

  2022-06-10

  

  Acknowledgements This research was supported by the Natural Sciences and Engineering Council of Canada (NSERC) Discovery Grant awarded to RGM. LMW was supported in part by fellowships from the University of Regina and the Government of Saskatchewan Fish and Wildlife Development Fund (FWDF). We wo

• Indeed GSTP mRNA appears to

  2022-06-10

  

  Indeed GSTP1-1 mRNA appears to be already highly stable in K562 leukemia CH 223191 synthesis with a half-live of more then 40h which is even further increasing to 92h after hemin treatment and erythroid differentiation. Previous reports quantified GST mRNA half-lives which depend on the cellular mo

• br S NO signalling during the

  2022-06-10

  

  (S)NO signalling during the plant immune response Redox signalling molecules must exhibit specificity for their target substrate. Moreover, a given redox-based modification must be reversible to ensure transient signalling. Oxidative cysteine (Cys) modifications are integral to a variety of redox

• Epidemiological evidence indicates that neuroinflammation

  2022-06-09

  

  Epidemiological evidence indicates that neuroinflammation plays a pivotal role in pathogenesis of AD (Heneka et al., 2015, Heneka et al., 2013, Holmes et al., 2009, Liu et al., 2016). For example, prolonged treatment with nonsteroidal anti-inflammatory drugs reduces the risk of developing AD (In et

• Insulin de sensitization has been observed in

  2022-06-09

  

  Insulin de-sensitization has been observed in the brains of people with AD [51], [52], [53] and we previously demonstrated that the GLP-1 analogue liraglutide was able to reverse this [54]. Importantly, Malotilate insulin de-sensitization correlates well with cognitive decline [15], [55] and with t

• In the liver ghrelin has opposite effects

  2022-06-09

  

  In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty β-Tocotrienol oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a GH-independe

• In total strains with relatively rapid acid producing

  2022-06-09

  

  In total, 5 strains with relatively rapid acid-producing ability (MA14, 15M2, DQHXNQ38–12, 5G2, and 6G5) were selected for further analysis. Compared with the strains ATCC19435, ZN8, and D-XJ4–12, which were used as controls, these 5 strains exhibited significantly different growth and titratable ac

• Interestingly transgenic mice that constitutively express

  2022-06-09

  

  Interestingly, transgenic mice that constitutively express active FXR in the intestine (iVP16FXR) are protected from chemically-induced and genetically-induced cholestasis. This protective effect is attributed to the induction of intestinal FGF15 and repression of hepatic Cyp7a1 expression, downregu

• The recent identification of new mechanisms for triggering f

  2022-06-09

  

  The recent identification of new mechanisms for triggering ferroptosis, by compounds termed FIN56 and FINO2, provided new insights into regulation of ferroptosis. FINO2 acts through a distinct mechanism: it promotes lipid peroxidation by oxidizing iron and indirectly inactivating GPX4 [180]. FIN56 w

• Recently considerable effort has been invested

  2022-06-09

  

  Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most

• Next we were interested in replacing the

  2022-06-09

  

  Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva

• Mitochondrial binding by HK prevents mortality by inhibiting

  2022-06-08

  

  Mitochondrial binding by HK prevents mortality by inhibiting pro-apoptotic factor (Bcl-2 family)-mediated opening of the mitochondrial permeability transition pore (mPTP) (Arora and Pedersen, 1988, Calmettes et al., 2016, Kodde et al., 2007, Pedersen et al., 2002, Rosano, 2011, Schindler and Foley,

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