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GSK343 br Short Communication Free fatty acid receptors FFAR
2022-05-19

Short Communication Free fatty GSK343 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 increases lipid accre
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Compound and several additional FPR
2022-05-19

Compound 10 and several additional FPR1 antagonists identified here specifically blocked fMLF-induced responses mediated via FPR1 in FPR1-HL60 Micafungin and human neutrophils, but not responses mediated via FPR2 or FPR3 (in human neutrophils and transfected HL60 cells) or Fpr1 (murine neutrophils
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We next investigated whether pharmaceutical inhibition of th
2022-05-19

We next investigated whether pharmaceutical inhibition of the PI3K pathway was synergistic with FGFR inhibition using BKM120, a pan-PI3K inhibitor with modest antitumor activity in cancer patients, as a single agent. We found that RT112 (- translocation) and JMSU1 ( amplification) were not signifi
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FXa is a vitamin K dependent serine protease consisting of
2022-05-19

FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 Oxamic acid and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The ac
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The concentration of rapamycin that gave half maximal
2022-05-19

The concentration of rapamycin that gave half-maximal induction of the expression of HO-1 and Prx-1 mRNA in normal hepatocytes was 0.05 μM, with maximal induction at about 0.1 μM rapamycin. While, at rapamycin concentrations higher than 0.1 μM, the degree of enzyme induction decreased, elevated expr
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br Materials and methods br Results br Discussion Serum HBsA
2022-05-18

Materials and methods Results Discussion Serum HBsAg is not only an important serological marker for the screening and diagnosis of HBV infection but also an important indicator for the treatment of hepatitis B [15]. Jaroszewicz et al. [4] and Nguyen et al. [8] reported that the HBsAg level
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Organisms can adapt to increasing ROS production by up
2022-05-18

Organisms can adapt to increasing ROS production by up-regulating antioxidant defences, such as the activities of antioxidant enzymes (Livingstone, 2003). Failure of antioxidant defences to detoxify excess ROS production can lead to significant oxidative damage including enzyme inactivation, protein
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l glycine br For some time it was
2022-05-18

For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor l glycine in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on the regul
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br All platelet agonists acting through specific receptors a
2022-05-18

All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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br Conclusion In this report we describe the
2022-05-18

Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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Boc-D-FMK To apply the recently developed GPR ligands to CNS
2022-05-18

To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the Boc-D-FMK and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end, the
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Previously we reported that the inhibition of PKC and
2022-05-18

Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl
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Recently a receptor for nicotinic acid named GPR A also
2022-05-18

Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f
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Kifunensine GlxI is a member of the
2022-05-18

GlxI is a member of the βαβββ superfamily of proteins, consisting of fosfomycin resistance protein (FosA), methylmalonyl-CoA epimerase (MMCE), extradiol dioxygenase (DIOX), mitomycin C resistance protein (MRP) and bleomycin resistance protein (BRP) [29], [30], [31]. These proteins are believed to ha
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br Clinical trials testing GLP mimetics in AD
2022-05-18

Clinical trials testing GLP-1 mimetics in AD or PD patients GIP analogues show good neuroprotective effects in animal models of AD and PD Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino everolimus incretin growth factor which activates pancreatic islets to enhance insulin secr
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