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While previously reported optimizations on compound focused
2019-12-26

While previously reported optimizations on Spironolactone receptor focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to e
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br Activatable photoacoustic probes Photoacoustic PA imaging
2019-12-26

Activatable photoacoustic probes Photoacoustic (PA) imaging is a recently developed technique [47]. The imaging approach uses probes that absorb a pulsed laser beam and convert light energy into acoustic signals. It combines the advantages of the high sensitivity offered by optical imaging and th
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dihydroxycholesterol OHC was recently identified by
2019-12-26

7α,25-dihydroxycholesterol (7α,25-OHC) was recently identified by classic analytical methods as a high-affinity ligand for EBI2 (Hannedouche et al., 2011; Liu et al., 2011). 7α,25-OHC was previously identified as an intermediate in the alternate pathway of hepatic bile sr 75 synthesis (Russell, 200
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E ubiquitin ligases are key players
2019-12-26

E3 ubiquitin ligases are key players in the ubiquitin-proteasome pathway because they catalyse ubiquitination of substrate proteins.39, 40, 41 As important regulators of cellular ubiquitination, E3 ligases are emerging as attractive drug targets, particularly in cancer.42, 43, 44 However, E3 ligases
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Multi subunit RING type E ligases
2019-12-26

Multi-subunit RING-type E3 ligases are exemplified by the CULLIN-RING-ligase (CRL) and the anaphase-promoting complex/cyclosome (APC/C) [19]. CRLs constitute the biggest family of other multi-component E3 ligases. These consist of a cullin scaffold protein (CULLIN 1, 2, 3, 4A, 4B, 5, 7), a substrate
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br Diacylglycerol kinases and T cell responses
2019-12-26

Diacylglycerol kinases and T cell responses Diacylglycerol kinases and cancer Several studies implicate DGKα in tumor progression, but its function is debated, as it might also have roles as a tumor suppressor. Diminished DGKα expression is linked to malignant transformation in epithelia. Hig
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br Acknowledgments br Introduction Heterocyclic chemistry ha
2019-12-26

Acknowledgments Introduction Heterocyclic chemistry has become one of the most important fields of research in pharmaceutical industry due to their many fold applications. Amongst all, heterocyclic orexin containing nitrogen and oxygen have shown most potent biological activities. It follows f
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br Introduction Lycium barbarum also
2019-12-26

Introduction Lycium barbarum, also known as wolfberry, belongs to the plant family Solanaceae. Red-coloured fruits of L. barbarum are used as traditional Chinese herbal medicine to promote health and longevity and as a food supplement for thousands of years [1]. They possess many biological activ
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In summary our findings show that LPS can activate CysLT
2019-12-26

In summary, our findings show that LPS can activate CysLT2R on microglial FITC, Fluorescein isothiocyanate to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity
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Compounds and administered orally to fasted Harlan Sprague D
2019-12-26

Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinica
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The presence of H PPases in parasitic
2019-12-24

The presence of H+-PPases in parasitic protists raises the question of the physiological role of these proteins. So far, they had been extensively characterized mainly in higher plants, and some prokaryotes [1], [2], [3], [4], [5], [6], [7], [16], [20]. A common feature to all these organisms is tha
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We also found a significantly inverse correlation
2019-12-24

We also found a significantly inverse correlation of OPRM1 CpG2-4 methylation level with HDL-C in Han male controls. Lipids are known to involve the inflammation pathway, Aβ formation and stability of neuron, whereby their abnormalities have been shown to increase the risk of AD [39], [40], [41]. HD
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This study focused on NPC L
2019-12-24

This study focused on NPC1L1 because it is critical for intestinal 5\'-Iodoresiniferatoxin of both dietary and biliary cholesterol.1, 7, 8 Overall, regulation in the intestine of cholesterol, BAs, and lipids by FGF19 and SHP may involve the combined actions of regulation of other genes that were id
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To further investigate mechanisms of rXCI we
2019-12-24

To further investigate mechanisms of rXCI, we generated female ESCs with a homozygous RlimKO. We found that these ampk inhibitors undergo XCI in vivo but that XCI in vitro is strongly influenced by culture conditions, including both method of differentiation and O2 levels. Our results demonstrate R
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Interestingly global EGFR depletion increased the rate of ce
2019-12-24

Interestingly, global EGFR depletion increased the rate of cell elimination everywhere in the notum (Figures 2B–2D), irrespective of the deformation status of the cells. Accordingly, we found that peptide receptors are not any more sensitive to stretching upon EGFR depletion (Figures S6A–S6C; Video
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