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During the tests in vitro SHP showed
2022-02-18

During the tests in vitro, SHP289-04 showed the beneficial effect on both two important aspects. In human liver carcinoma cell line HepG2, it was found to improve glucose consumption significantly. Otherwise, in pancreas cell line NIT1, it could only promote insulin secretion significantly at high g
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br Introduction G protein coupled receptors GPCRs represent
2022-02-18

Introduction G-protein coupled receptors (GPCRs) represent one of the largest family of receptors involved in cell membrane signal transduction and have become one of the leading therapeutic targets worldwide (Chakraborty and Chattopadhyay, 2015; Bouvier, 2001; Sriram and Insel, 2018). GPCRs sign
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GHSR A s have high levels of
2022-02-18

GHSR-1A's have high levels of constitutive activity and recent investigations show that constitutively active GHSR-1As in the absence of ligand (ghrelin) binding can have effects on feeding and energy balance (Mear et al., 2013, Petersen et al., 2009). Furthermore, GHSR-1As are capable of dimerizing
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Some but not all GSIs
2022-02-18

Some, but not all, GSIs inhibit signal peptide peptidases as well, though this has not been systemically studied [36], [41]. When considering biological activities of various GSIs this is an important and understudied caveat that could influence both biological response as well as potential toxiciti
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Conclusions br Author information The obtained models of
2022-02-18

Conclusions Author information The obtained models of complexes of FPR2 with most of the described compounds are freely available at the author’s web site: http://www.biomodellab.eu/models/. Acknowledgements This work was partly done at the Interdisciplinary Centre for Mathematical and Compu
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Recently we indicated that cell motility was regulated
2022-02-18

Recently, we indicated that cell motility was regulated by the different induction of GPR120 and GPR40 in liver epithelial WB-F344 mi2 treated with chemical agents. The cell motility of WB-F344 cells was stimulated by phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) which is a potent tumor
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On the other hand Li Zhang et al and
2022-02-18

On the other hand, Li+ (Zhang et al., 1996) and Ca2+ (Gizak et al., 2004) cations inhibit FBPases. However, in the case of Ca2+, the inhibition is attributed solely to the muscle isozyme which is over 100 times more susceptible to the cation action than the liver isoform (Gizak et al., 2004). At the
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This SAR work led to the
2022-02-18

This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c
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br Materials and methods br Results and discussion To analyz
2022-02-18

Materials and methods Results and discussion To analyze the dependence of lysosomal exocytosis on Cu we exposed HeLa BMS265246 to fresh buffer containing normal levels of free Ca (1mM) and measured β-hex levels in the extracellular medium, followed by measuring β-hex content in the total cellu
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Evidence demonstrating the interplay between hypoxia
2022-02-18

Evidence demonstrating the interplay between hypoxia and the dynamics of histone methylation is mounting [15], [43]. For example, hypoxia leads to an increase in H3K4me3 by inhibiting their responsible demethylase [44]. Hypoxia also leads to an increase in H3K9me2 by upregulating the methyltransfera
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Polyunsaturated fatty acid components of
2022-02-17

Polyunsaturated fatty lasofoxifene receptor components of brain are more prone to oxidative attack, an event called lipid peroxidation. Consistent with previous findings on neurotoxicity [58,59], colistin sulphate increased the level of MDA in the brain of rats. The elevated MDA, a consequence of o
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RNase Inhibitor Failure of antioxidant defenses to remove ex
2022-02-17

Failure of antioxidant defenses to remove exogenous ROS produced by redox cycling chemicals either by being inhibited by those compounds or overwhelmed by an excess ROS, will disrupt the balance between antioxidant/prooxidant system within the organisms leading to oxidative damage (Livingstone, 2003
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PDEs block GUCY C associated second messenger signaling
2022-02-17

PDEs block GUCY2C-associated second messenger signaling by degrading cyclic nucleotides, whereas inhibition of PDEs activity prevents cyclic nucleotide degradation (Fig. 1). Several researchers have described the pathophysiological roles of various PDEs in numerous tumor cell types, including CRC MD
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Recently higher grade varicoceles have
2022-02-17

Recently, higher-grade varicoceles have been reported to be associated with higher nocturia levels [20], and we observed an interesting phenomenon in which the urine volume/water intake ratio dramatically increased in the rat model of experimental left varicocele (ELV); the decreases in hypothalamic
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br Methods and materials br Results and discussion
2022-02-17

Methods and materials Results and discussion Conclusions This is the first study that attempted to isolate, purify and identify the characteristics of somatostatin receptor from ginseng. In vitro studies have demonstrated that PGL-1 efficiently suppressed SH-SY5Y cell apoptosis induced by
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