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With the nitrogen containing heterocycle
2022-07-16
With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic LP533401 hcl (, and ), followed by deprotection by TFA, smoothly provided th
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In a recent study Neelaveni et al
2022-07-16
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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In enzyme assays it is convenient to quantify the product
2022-07-15
In enzyme assays, it is convenient to quantify the product formed in the enzyme reaction, where a decrease in the concentration of product indicates enzyme inhibition [35], [36], [37], [38]. In the present study, substrates were carefully chosen so that they are specific to each enzyme. Known natura
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GNE-617 We thus asked whether enhanced AEA levels
2022-07-15
We thus asked whether enhanced AEA levels in the GNE-617 reduce the level of age-related inflammatory changes and slow down brain ageing. To answer this question we compared the morphology of microglia and level of pro-inflammatory cytokines in the hippocampus of young and old wild-type and FAAH−/−
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Whether histamine receptor distribution is altered in
2022-07-15
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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br Conclusion The hub gene KIBRA and the Hippo signaling
2022-07-15
Conclusion The hub gene KIBRA and the Hippo signaling pathway were downregulated and miR-21 was upregulated in LAD. MiR-21 promoted the viability and mobility of LAD cells, reduced apoptosis and suppressed the Hippo signaling pathway in LAD through targeting KIBRA. Funding The study was appro
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br Acknowledgement The authors are grateful
2022-07-15
Acknowledgement The authors are grateful for financial support provided from specific university research (MSMT No 21-SVV/2018). Introduction Several recent studies have demonstrated that planaria, flatworms notable for their regenerative capabilities, can develop conditioned place preference
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In hypoxic breast cancer cells BNIP mediated autophagy activ
2022-07-15
In hypoxic breast cancer cells, BNIP3-mediated autophagy activation and elevation of amino MDL 12330A hydrochloride levels were notable. BNIP3, a BCL-2 family protein, is known to be transcriptionally regulated by HIF-1α and to be involved in cancer cell death in hypoxic conditions [51]. As a link t
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angiotensin receptor blockers br Discussion br Conflict of i
2022-07-15
Discussion Conflict of interest Acknowledgements We thank Rosetta Barkley for expert technical assistance. We thank Robin Maser, James Calvet, Darren Wallace, and Jovanka Koo for many helpful discussions and expert technical advice. This work was supported by National Institutes of Health,
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The beta catenin TCF complex is an
2022-07-15
The beta-catenin/TCF complex is an important target in the Wnt/beta-catenin pathway. This complex has proven challenging to target. However, natural inhibitors of this complex have been identified. One group of inhibitors is called the inhibitors of Wnt response (IWR-1/2). IWR-1/2 targets Axin and s
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br Amino acids The role of leucine
2022-07-15
Amino acids: The role of leucine Amino TBB metabolism plays a central role in brain physiology, as several amino acids serve as biosynthetic precursors for neurotransmitter synthesis [36]. In addition, the amino acids L-leucine and L-lysine may participate in ketogenesis. For these reasons, supp
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br Materials and methods br
2022-07-15
Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 chir99021 has been identified within discrete regions of the nervous
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br Conflict of interest statement br Acknowledgments The aut
2022-07-15
Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). GPR35 is an orphan G protein-coupled receptor (GPCR) implicat
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Compounds and were tested for pharmacodynamic
2022-07-15
Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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TGR is a class A GPCR
2022-07-15
TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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