• To investigate the potential molecular mechanism of FXR medi

  2022-07-16

  

  To investigate the potential molecular mechanism of FXR-mediated regulation of liver cancer cell proliferation, gene expression profiles were determined using Agilent arrays in SK-Hep-1-FXR and NC after treatment with the FXR agonist GW4064. The results indicate that mTOR and S6k are involved in div

• We next determined the selectivity profile of

  2022-07-16

  

  We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty KB SRC 4 receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinity to medium-

• br Materials and methods br Results br Discussion

  2022-07-15

  

  Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own

• S/GSK1349572 sale A subsequent modeling study by a different

  2022-07-15

  

  A subsequent modeling study by a different group was based on the bovine rhodopsin homology model using the 1L9H construct [38]. However, the site-directed mutagenesis data and docking suggested that the niacin-binding pocket is different to that described in the aforementioned report, but similar t

• Resolving the molecular details of glyco proteome variation

  2022-07-15

  

  Resolving the molecular details of (glyco)proteome variation in different tissues and organs of the human body is critical for the understanding of human biology and disease [59]. Glycoproteomic analysis of disease-related tissues and cells has provided valuable information to identify promising tar

• There were significant differences in mRNA expression levels

  2022-07-15

  

  There were significant differences in mRNA expression levels observed for 7 out of 15 analyzed genes. This observation suggests, that selection of a reference/control group may influence interpretation of gene expression studies performed in liver pathologies. This study directly evidenced that anal

• AKR D is very highly

  2022-07-14

  

  AKR1D1 is very highly expressed in human liver and based upon the observations outlined above, with respect to other steroid hormone pre-receptor metabolising enzymes, it is entirely plausible that AKR1D1 could represent a critical regulatory step in the control of metabolic phenotype within the liv

• To directly address whether pharmacological

  2022-07-14

  

  To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N

• br Acknowledgements This work was supported by a

  2022-07-14

  

  Acknowledgements This work was supported by a fellowship to C.H. under the ‘100 Foreign Expert’ scheme of the Shanxi province government(R100456). Conflict of interest: Dr. Holscher is a named inventor on a patent submitted by Lancaster University on the use of dual GLP-1/GIP analogues in neurode

• The regulation of gap junction connexin mediated activities

  2022-07-14

  

  The regulation of gap junction-connexin-mediated activities may be achieved through action on the channel gating properties (membrane voltage, pH, interaction with junctional and cytoskeletal proteins, Ca2+ and K+ concentrations, etc) or on the trafficking, turnover and localization of connexins. Sh

• By association a possible mechanism which

  2022-07-14

  

  By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et

• jak stat inhibitor br Declarations of interest br Acknowledg

  2022-07-14

  

  Declarations of interest Acknowledgements This work was supported by the National Natural Science Foundation of China (81673321, 21506099), the State Key Laboratory of Drug Research (SIMM1705KF-13), the Natural Science Foundation of Jiangsu Province (Grant No. BK20151541), and the Jiangsu Syn

• Interestingly transgenic mice that constitutively express ac

  2022-07-14

  

  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

• In a follow up study

  2022-07-14

  

  In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c

• uPAR promotes cell associated proteolysis by binding to

  2022-07-14

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

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