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To this end we evaluated novel D analogs for selectivity
2021-10-28
To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell 5046 sale systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-substitute
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br Materials and methods br Results br Discussion The
2021-10-28
Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast AS1842856 by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs within minutes an
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A majority of investigations of
2021-10-28
A majority of investigations of the GCK-PFK-2/FBPase-2 interaction have taken place within cells. Immunofluorescence studies in several fixed cell lines indicate that GCK colocalizes with PFK-2/FBPase-2 in the cytoplasm following overexpression [[68], [69], [70]]. Live cell imaging conducted on 69 9
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LXRs are physiological regulators of cholesterol and lipid
2021-10-28
LXRs are physiological regulators of cholesterol and lipid metabolism and influence glucose metabolism. In addition, they have been shown to repress transcription of certain pro-inflammatory genes (Jakobsson et al., 2012; Ogawa et al., 2005; Terasaka et al., 2005). Thus, LXRs can either activate or
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We next determined the selectivity profile of the most
2021-10-28
We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty Palifosfamide 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 med
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br Discussion and concluding remarks FPR is considered
2021-10-28
Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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LPCs have been previously described as potential
2021-10-28
LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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Evidence suggests that phosphorylation increases synaptotagm
2021-10-28
Evidence suggests that phosphorylation increases synaptotagmin affinity for the SNARE complex [15], [128]. It is, however, unclear how this might affect release. Synaptotagmin has been identified as part of the minimal vesicle docking machinery in chromaffin GW 6471 [129]. Thus, phosphorylation of
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The effects of C on the NF B pathway
2021-10-28
The effects of C646 on the NF-κB pathway could be explained by the role for p300 that has been described in the regulation of the NF-κB pathway [5]. For instance, acetylations of the p65 NF-κB subunit on lysines 218, 221 and 310 are mediated by the HATs p300 and PCAF [11] and increase transcriptiona
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Tumor specific CD cytolytic T lymphocytes CTLs recognizing t
2021-10-27
Tumor-specific CD8+ cytolytic T lymphocytes (CTLs) recognizing tumor antigenic peptide/major histocompatibility complexes-I (pMHC-I) presented on tumor cells play an important role in antitumor immunity [12]. However, immune tolerance including central (natural) or peripheral (acquired) tolerance be
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Interestingly systemic circulating levels of NOx
2021-10-27
Interestingly, systemic circulating levels of NOx were not dramatically increased by treatment with isosorbide mononitrate or sodium nitrite at a dose which exerted beneficial effects on the progression of PH. In line with our results, Mathew et al. [13] demonstrated that the long-acting NO donor mo
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The rat model was validated with another agonist of GPR
2021-10-27
The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L
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To characterize the binding receptor for HIV
2021-10-27
To characterize the binding receptor for HIV-1 gp120 in autophagy, we used the CXCR4 inhibitor AMD3100 and NMDA receptor inhibitor MK801 along with gp120 to treat the cardiomyocytes. Our data demonstrated that inhibition of the NMDA receptor significantly blocked the increase of gp120 induced autoph
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br Conclusion br Conflict of interest statement br
2021-10-27
Conclusion Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as Introduction Over the past decade, more than a hundred new biopharmaceutical products have been approved and market
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Polyunsaturated fatty acids PUFAs represent a class of lipid
2021-10-27
Polyunsaturated fatty acids (PUFAs) represent a class of lipids that contain two or more carbon double (unsaturated) bonds (CC) and classified as n-3, n-6 and n-9 fatty acids. PUFAs including n-3 such as docosahexaenoic 2-APB (DHA), eicosapentaenoic acid (EPA) and n-6 such as arachidonic acid (AA)
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