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Oltipraz has been shown to inhibit the growth of HCC
2022-06-18

Oltipraz has been shown to inhibit the growth of HCC gsk3 inhibitor and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver cells with oltipraz
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Biochemical assays have provided evidence that prolonged
2022-06-17

Biochemical assays have provided evidence that prolonged exposure to GPR35 agonists can induce GPR35 internalization [2], [4], [11], [13]. Our finding that neuronal excitability decreased regardless of whether the slices were superfused for a few minutes or incubated for a few hours with GPR35 agoni
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GW 6471 To assess the roles of GPR and GPR
2022-06-17

To assess the roles of GPR120 and GPR40 in malignant properties of pancreatic cancer cells, we generated GPR120 and GPR40 knockdown (PANC-sh120 and PANC-sh40, respectively) GW 6471 from PANC-1 (Fig. 2A). While no difference of cell growth rate between control PANC-RFP cells and PANC-sh120 cells was
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br Several reports have shown
2022-06-17

Several reports have shown an anti-proliferative effect of type I IFNs on CD4+ T That means activated in vitro either upon anti-CD3 antibody treatment [28,29] or upon cognate antigen stimulation [29]. However, the in vivo setting is a lot more complex, since the final outcome is the net effect of
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Neurotransmitter transporters are rapidly recycled from and
2022-06-17

Neurotransmitter transporters are rapidly recycled from and to the membrane. For instance, the GABA transporter GAT1 is recycled in a calcium and depolarization dependent manner. GAT1 located in the plasma membrane is internalized to a subpopulation of small vesicles different from the classical neu
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br Flavonoid function Antioxidants are
2022-06-17

Flavonoid function Antioxidants are compounds - when present at a lower concentration compared oxidizable substrate - that delay or prevent oxidation of the substrate [14], [106]. Antioxidants act as nucleophiles to reduce an oxidative molecule to prevent its interaction with another molecule [14
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Using data from a large population based cohort study in
2022-06-17

Using data from a large population-based cohort study in Finnish males and females, Suchankova et al. [97] looked at a subset of the aforementioned SNPs, namely one SNP on GHSR (rs2948694) and two SNPs on GHRL (rs4684677 and rs696217), in relation to alcohol use disorders identification test (AUDIT)
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Bile acids BAs are critical for facilitating the absorption
2022-06-17

Bile acids (BAs) are critical for facilitating the MLCK inhibitor peptide 18 sale 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 rec
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The PK profile and tissue distribution
2022-06-17

The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an
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Tianeptine sodium Recently a lot of synthetic FFA agonists
2022-06-17

Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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uPAR promotes cell associated proteolysis by binding to uPA
2022-06-17

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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Preliminary explorations focused on the linker of
2022-06-17

Preliminary explorations focused on the linker of 2 (Table 1). Lilly reported that the methylene between the phenyl and the piperidyl group was metabolically susceptible to N-dealkylation, so we replaced the methylene with a carbonyl moiety to block the metabolic site [23,48] (Fig. 2). In addition,
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In a recent study Neelaveni
2022-06-17

In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported
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Free fatty acids FFAs which are obtained from
2022-06-17

Free fatty acids (FFAs), which are obtained from dietary fat or endogenous synthesis, function as nutrients and signaling molecules. Studies have shown that free fatty L-Arabinose receptors 1–4 which are G-protein coupled receptors, bind free fatty acids and serve as receptors for these FFAs. Short
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As for all DOACs measurement
2022-06-17

As for all DOACs, measurement of DiXaIs activity requires the use of dedicated specific calibrators and controls. Each drug needs its own calibration and control material in a like to like manner. In no case can a drug concentration be extrapolated with the use of a calibrator established for anothe
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