• The isoenzyme hGSTP is an attractive drug target due

  2022-09-06

  

  The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t

• The recently de orphaned G protein

  2022-09-06

  

  The recently de-orphaned G-protein coupled receptor (GPCR), GPR55, is activated endogenously by L-α-lysophosphatidylinositol (LPI), a lipid signaling molecule, as well as N-arachidonoyl glycine (NAGly) and numerous endo, phyto, and synthetic cannabinoids (Oka et al., 2007, Henstridge et al., 2010, H

• TGR is a class A GPCR

  2022-09-06

  

  TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological act

• br Acknowledgments This work was funded

  2022-09-03

  

  Acknowledgments This work was funded by NIH Grant 2R01 MH066958 (JGT) and NSF CAREER award IOS- 1053716 (NV). We thank Dr. Greti Aguilera for the generous gift of the GRE-Luciferase construct and Dr. Louis Muglia for the generous gift of the GR-GFP construct. Introduction Prostate cancer (PCa

• Different responses in feed intake have been noticed followi

  2022-09-03

  

  Different responses in feed intake have been noticed following administration of exogenous GHRL (peripherally or centrally) depending on animal species. In mammals, injection of GHRL stimulates food intake (orexigenic effect) (reviewed in Kaiya et al., 2013b). In contrast, in domestic birds, exogeno

• Bile acids BAs are critical for facilitating

  2022-09-03

  

  Bile acids (BAs) are critical for facilitating the kv1.3 inhibitor of dietary lipids and lipid-soluble vitamins in the intestines [6], [7]. At physiological levels, BAs function as signaling molecules and activate specific nuclear receptors [farnesoid X receptor (FXR), pregnane X receptor, and vita

• br Short Communication Free fatty acid

  2022-09-03

  

  Short Communication Free fatty p-nitro-Cyclic Pifithrin-α receptors (FFAR) play significant roles in energy metabolism (Brown et al., 2005; Ichimura et al., 2009). The receptor FFAR1 is involved in insulin secretion in humans (Meidute Abaraviciene et al., 2013). Activation of the receptor FFAR2 i

• The typical pharmacophore for GPR agonists contains

  2022-09-03

  

  The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors

• br Introduction GPR also known as

  2022-09-03

  

  Introduction GPR40 (also known as free fatty egfr inhibitor receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and long-c

• In regards to animals several studies have reported the

  2022-09-03

  

  In regards to animals, several studies have reported the peroxisomal localization of FPS (Krisans et al., 1994, Olivier et al., 2000, Kovacs et al., 2007). Transfections of mammalian cells with the rat short FPS isoform followed by immunodetection localized the enzyme to the peroxisome (Olivier et a

• There have already been many reports on

  2022-09-03

  

  There have already been many reports on the AFS gene (Beuning et al., 2010, Green et al., 2007, Li et al., 2006, Pechous and Whitaker, 2004, Pechous et al., 2005, Yuan et al., 2007, Yuan et al., 2010) and HMGR gene (Pechous and Whitaker, 2002, Rupasinghe et al., 2001). The recent advances concerning

• EZH affects cancer by regulating the expression

  2022-09-03

  

  EZH2 affects cancer by regulating the expression of target genes [22]. EZH2, together with SUZ12 and EED, forms the polycomb repressive complex 2 (PRC2), which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) [23,24]. PRC2 may recruit other polycomb complexes, DNA methyltransferases, and

• br Materials and methods br Results and

  2022-09-03

  

  Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka

• LSD also contributes to the regulation of

  2022-09-03

  

  LSD1 also contributes to the regulation of specific programs of gene expression in postmitotic, fate-committed neurons. Perhaps its most specialized role is in the complex series of epigenetic regulatory events that permit each olfactory sensory neuron to express one and only one of the thousands of

• Materials and methods br Results

  2022-09-03

  

  Materials and methods Results and discussion Acknowledgments This work was supported in part by the Japan Society for the Promotion of Science KAKENHI Grants JP21300174 and JP25282144 (H.K.). Introduction Epigenetic modifications of histones, such a lysine acetylation, play a key role in

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