• br Modulators of the GUCY C cGMP

  2022-02-08

  

  Modulators of the GUCY2C/cGMP/PDEs signaling pathways for CRC prevention and therapy (pre-clinical and clinical development) Several modulators of the GUCY2C/cGMP/PDEs signaling pathways, including GUCY2C agonists and PDEs inhibitors, have been developed and explored as chemopreventive agents for

• br Material and methods br Results The search for proteins

  2022-02-08

  

  Material and methods Results The search for proteins selectively expressed in pancreatic islet β-Sitosterol in the Human Protein Atlas (HPA) yielded 27 hits, including well-known islet cell markers such as insulin, glucagon and pancreatic polypeptide (Table 1). The search algorithm excluded i

• Adenosine triphosphatase ATP is a

  2022-02-07

  

  Adenosine triphosphatase (ATP) is a signaling molecule in acute pain and chronic pain(Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). It is also known that presynaptic A1 receptors are involved in the inhibition of transmitter release (Vizi and Knoll, 1976). Extracellular

• br Acknowledgments This research was supported by

  2022-02-07

  

  Acknowledgments This research was supported by a grant from the Korea Health Technology R&D Project through the Korean Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI17C0616). Dr. Jun-Mo Yang was supported by the Natio

• br Introduction Conversion of visual input into electrical i

  2022-02-07

  

  Introduction Conversion of visual input into electrical information and routing this information to the brain is the main function of the eye (Levin et al., 2011). These processes require a microenvironment that offers adequate supply with oxygen and nutrients and also removal of all unwanted and

• In total strains with relatively rapid

  2022-02-07

  

  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

• The typical pharmacophore for GPR agonists

  2022-02-07

  

  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

• Multi targeting agents are of major

  2022-02-05

  

  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;

• Interestingly the rabbit cornea exhibited a more than

  2022-02-05

  

  Interestingly, the rabbit cornea exhibited a more than two-fold higher level of total GST activity compared with that of the porcine cornea, whereas their levels of GSTO1‐1 and GSTP1‐1 activity were similar (Fig. 4). Because members of the GST Alpha, Mu, Pi and Omega 516 3 receptor primarily utiliz

• br Discussion CHO K cell lines stably expressing

  2022-02-04

  

  Discussion CHO-K1 cell lines stably expressing each of the NH2-terminal isoforms of the human glycine reuptake transporter GlyT1 have been developed. GlyT1 uptake assays have been validated for two lines for each isoform, one low and high expressor. Expression levels in the lines have been confir

• NEIL interacts with many DNA replication

  2022-02-04

  

  NEIL1 interacts with many DNA replication proteins including flap-endonuclease 1 (FEN-1), proliferating cell nuclear antigen (PCNA), and Werner RecQ helicase (WRN) through its disordered C-terminal part. One study showed that in in vitro condition, NEIL1 binds to the damaged SC-514 in an RPA-coated

• Previously we have shown that ghrelin and cannabinoids

  2022-02-03

  

  Previously, we have shown that ghrelin and cannabinoids stimulate hypothalamic AMPK activity (Kola et al., 2005). In contrast, both the orexigenic compounds have inhibitory effects on AMPK activity in the liver and visceral fat (Kola et al., 2005). In this study, we were able to reproduce our previo

• Zn is the second most abundant trace metal in many

  2022-02-03

  

  Zn2+ is the second most abundant trace metal in many cells and neurons in the brain. It regulates cellular functions such as gene expression, epigenetic enzymatic activity, protein structural stability, and neuronal plasticity. Zn2+ is particularly abundant in the cortex and limbic system, including

• 69 9 receptor br FXR FGF in the control of BAs synthesis The

  2022-02-03

  

  FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, 69 9 receptor and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-synt

• The fibroblast growth factor receptor FGFRs

  2022-02-03

  

  The fibroblast growth factor receptor (FGFRs), including four highly conserved proteins (FGFR1-4), are important membrane sensors for extracellular signals [4]. By binding to their ligands, FGFRs are activated and can trigger various downstream intracellular signaling cascades, which is required for

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