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The preferential expression of ALOX B
2024-07-19

The preferential expression of ALOX15B in human macrophages may explain why human genetic studies investigating the association of ALOX15 with cardiovascular disease did not show consistent results. Two rare functional polymorphisms have been characterized in the ALOX15 gene, which leads to increase
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br Current therapies for metabolic diseases Inborn errors
2024-07-19

Current therapies for metabolic diseases Inborn errors of metabolism caused by deficiency of particular enzymes due to loss of function mutations or deletions have been treated by decreasing the intake of the enzymatic substrate, supplementation with an essential cofactor or vitamin, increasing m
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Kasugamycin hydrochloride synthesis The results of cell cult
2024-07-19

The results of cell culture models were further supported by in vivo studies in mice treated with PXR and/or AhR agonists, PCN and β-NF. In these mice, AhR-regulated cyp1a1, and cyp1a2 were suppressed by PXR activation as determined by real time Q-PCR (Fig. 3). The level of PXR mRNA was not changed
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Molecular docking is widely used to predict
2024-07-19

Molecular docking is widely used to predict the interaction between an enzyme and its inhibitors. This is a computational simulation approach that can be used as a tool to investigate the structure-activity relationship of ACE inhibitory peptides (Goodsell, 2009). It has been recently shown that ACE
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PF also a dual Aurora A and Aurora B
2024-07-19

PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly phenanthroline for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was
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The phylogenetic relationship demonstrates that both bovine
2024-07-19

The phylogenetic relationship demonstrates that both bovine and porcine 12/15-LO is more related to the human enzyme than the rabbit enzyme, despite the fact that the rabbit reticulocyte enzyme is a 15-lipoxygenase. The rabbit is one single species that expresses a 12/15 LO with 15-LO activity while
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We demonstrated clearly that the overexpression of sFlt sign
2024-07-18

We demonstrated clearly that the overexpression of sFlt-1 significantly increased arginase MMP-2/MMP-9 Inhibitor I sale and enhanced arginase activity in HUVECs (Fig. 3). NO formation is related inversely to serum levels of sFlt-1 in preeclampsia [11]. The disorder of NO formation, which was involve
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br Angiotensin receptor neprilysin inhibitors
2024-07-18

Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu
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br Acknowledgements br Introduction Autoantibodies directed
2024-07-18

Acknowledgements Introduction Autoantibodies directed at neurotransmitter receptors and ion channels are pathogenic and/or biomarkers in several autoimmune neurological diseases [1]. For example, autoantibodies directed against voltage-gated potassium channels, the P/Q-type (α1A) voltage-gated
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The nAChR has been considered an interesting potential
2024-07-18

The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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PPM-18 In fact serotonin is a major modulator of dopaminergi
2024-07-17

In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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Despite functional studies demonstrating the role of HT
2024-07-17

Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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Here we show that the co
2024-07-17

Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC 5'-Iodoresiniferatoxin and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhib
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By performing knockdown of AXL once HER
2024-07-17

By performing knockdown of AXL once HER2+ cancer NS3694 receptor have achieved lung colonization, we demonstrated that AXL contributes to the establishment of macrometastases. While inhibition of AXL impairs the efficiency of metastasis, the later finding has major clinical implications since pharm
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Besides Arg overexpression our data
2024-07-17

Besides Arg2 overexpression, our data revealed that AGEs could decrease eNOS mRNA levels, which is considered a significant cause for attenuated NO production and vasodilation. It was found recently that AGEs significantly reduce eNOS expression levels and NO bioavailability in human carotid artery
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