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In the a first in vitro indication of modulation
2022-02-10

In the 2003, a first in vitro indication of modulation of FXR expression in CRC showed that FXR expression was absent in undifferentiated colon carcinoma cell line SW480, while it was progressively increasing along with the degree of cell differentiation in Caco2 and HT29 cells, and its transcriptio
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Colorectal cancer CRC is the leading cause of
2022-02-10

Colorectal cancer (CRC) is the leading cause of cancer deaths in Taiwan and is also a most common cancer in the world (Huang et al., 2012, Jemal et al., 2011). With early detection and treatment in the initial stage, CRC can be recognized as curable in comparison with other malignant tumors (Levin e
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Consideration must be given to
2022-02-10

Consideration must be given to both the tissues themselves and to infiltrating immune cells. As highlighted by Maxwell and Eckardt [88], clinical trials of compounds targeting these pathways will require large numbers of participants and prolonged follow-up to identify rare and late complications or
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br Trifluoromethylketones This group of
2022-02-10

Trifluoromethylketones This group of compounds was demonstrated to bind the zinc LY2801653 in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core motif for
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br Discussion Using HBV transgenic mice Kim et al first
2022-02-10

Discussion Using HBV transgenic mice, Kim, et al. first reported that the HBx gene caused HCC [34]. Since then, transgenic mice have become a useful experimental model for defining the molecular events of HBV hepatitis, and HBV-related hepatocarcinogenesis. In the present study, we first confirme
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The ketone body receptor HCA is most likely not active
2022-02-10

The ketone body receptor HCA2 is most likely not active under normal conditions, since local levels and plasma levels of ketone bodies such as β-HB are too low to activate the receptor. However, overnight fasting or prolonged starvation results in plasma levels of the ketone body in the millimolar r
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It appears that not all GPR agonists require
2022-02-10

It appears that not all GPR119 agonists require a high dose to elicit acceptable 2,4-Diacetylphloroglucinol receptor control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those
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As disclosed in our preceding
2022-02-10

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, Thalidomide lacks an e
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G protein coupled receptor GPCR
2022-02-10

G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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br Materials and methods br Results br Discussion
2022-02-10

Materials and methods Results Discussion DNA repair pathways have evolved for a long time to act independently of one another. However, over the past decade several overlaps and crosstalks between these pathways were identified, showing that the DNA repair system is more complex than previo
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A high fat maternal diet during the pregestation
2022-02-10

A high-fat maternal diet during the pregestation period and extending throughout gestation (including the period of conception) has the propensity of affecting early embryonic development and placentation. Previous investigations have revealed that the preimplantation embryos are generally exposed t
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The results obtained here in
2022-02-09

The results obtained here in int-Gr+/+ and int-Gr−/− mice suggested that Gr is required to maintain basal level of Fgf15 expression in the ileum, whereas DEX treatment is able to reduce Fgf15 mRNA in a Gr-independent manner. In previous in vitro studies we have already shown that GC are able to affe
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MG 149 In addition to the four classical FGFRs there
2022-02-09

In addition to the four classical FGFRs there is an additional receptor, FGFR like-1 (FGFRL1, also known as FGFR5) (Ornitz and Itoh, 2015, Trueb et al., 2003). FGFRL1 gene was discovered in a cartilage specific cDNA library in 2000 (Trueb, 2011, Trueb et al., 2003) and thereafter it has been found
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Receptor interactions and binding mode of in
2022-02-09

Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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Relative to the impact of moderate PAE on markers
2022-02-09

Relative to the impact of moderate PAE on markers of histaminergic neurotransmission, there were four salient observations from the studies reported here. First, it does not appear that moderate PAE affects the number of HDC-positive neurons in the tuberomammillary nucleus of the ventral hypothalamu
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