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T lymphocytes play an important role in cellular
2022-01-06
T lymphocytes play an important role in cellular and humoral immunity and immune responses (Shin and Iwasaki, 2013; Schenkel and Masopust, 2014). T OSI-420 mature after complex selection and differentiation in the thymus. They can express various membrane proteins, such as CD3, CD4, and CD8 molecule
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We also demonstrated that inhibition
2022-01-06
We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express
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We confirmed a decrease in extracellular glutamate
2022-01-06
We confirmed a decrease in extracellular glutamate uptake and the presence of efflux in an endothelial cell model of oxygen-glucose deprivation (OGD), which effectively simulates the inefficient energy supply after brain injury [15], and analysed the function of endothelial EAATs and explored the ro
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The in vivo biological activity
2022-01-06
The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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br The Farnesoid X receptor FXR identification
2022-01-06
The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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Growing evidence supporting the anti inflammatory and
2022-01-06
Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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All of the designed compounds
2022-01-06
All of the designed compounds – was synthesized from -cyclopropane aldehyde , which was prepared following a procedure we reported previously. Treatment of with 4-chlorobenzene-1,2-diamine in pyridine constructed benzimidazole structure of , which was subjected to deprotection and subsequent oxidat
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The other possibility for the lack of
2022-01-06
The other possibility for the lack of effects of H1 receptor agonists, e.g. histamine, on the NMDAR-mediated responses is that other neurotransmitters may cause more profound effects than histamine on the gliotransmitter release from astrocytes. For example, recent studies showed that noradrenaline,
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Polyunsaturated fatty acid components of brain are
2022-01-05
Polyunsaturated fatty TAME 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 overwhelmed antiox
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Organisms can adapt to increasing ROS production by up regul
2022-01-05
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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It appears that not all GPR
2022-01-05
It appears that not all GPR119 agonists require a high dose to elicit acceptable BLZ945 control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg sitaglip
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br Introduction Few decades after
2022-01-05
Introduction Few decades after of HIV/AIDS diagnosis, it has been still a health problem and impact will continue in the next decades. In 2015, HIV/AIDS was the 12th cause of death in the world and it's estimated that 1.2 million people was died of HIV/AIDS this year. In the global epidemiologica
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One difficulty in studying gp is that
2022-01-05
One difficulty in studying gp120 is that it binds to more than one receptor. Understanding how fccp sale respond to gp120 is complex because of this promiscuity. In an attempt to establish the contribution of CXCR4 in the antagonistic effect of gp120 on morphine-induced antinociception, AMD3100 was
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In order to elucidate the reasons
2022-01-05
In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen bromocriptine mesylate of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12 μ
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br Funding sources This work was supported
2022-01-05
Funding sources This work was supported, in part, by NIH GM115388 to BGM. Acknowledgements Introduction Glucokinase (GCK) plays a central role in the regulation of glucose metabolism. Its activity is restricted to 17-ODYA with important roles in whole-body glucose homeostasis [1]. In panc
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