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The aim of our study was to investigate the polymorphisms
2022-04-12
The aim of our study was to investigate the polymorphisms of RAGE and glyoxalase I gene and sRAGE serum levels in patients with pathological pregnancy trying to describe the genetic background of pathological pregnancy or to find a new biochemical marker (sRAGE) of these pathological states in pregn
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The aim of this study is to explore new
2022-04-12
The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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Given that we planned to isolate the GluN GluN
2022-04-12
Given that we planned to isolate the GluN1/GluN3A receptor by immunoaffinity chromatography using a Myc epitope tag on GluN3A, we first checked that the tag does not affect the functional properties of the receptor. To do this we co-transfected HEK-293 cells with DNA encoding WT GluN1 and either WT
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tetraethylammonium synthesis To maintain low Glu concentrati
2022-04-12
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino tetraethylammonium synthesis is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic
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The previous study demonstrated that the
2022-04-12
The previous study demonstrated that the main CYP isoforms present in the human Boceprevir synthesis included CYP46A1, 2J2, 2U1, 1B1, 2E1 and 2D6 (Dutheil et al., 2009b, 2010). CYP1B1 and CYP2U1 were found in the mitochondrial and microsomal fractions of astrocytes in the human frontal lobe, hippoca
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br Do the actions of GLP R agonists on the
2022-04-12
Do the actions of GLP-1R agonists on the vascular endothelium account for GLP-1R agonist-mediated cardioprotection? The previous section highlighted the recent clinical evidence from cardiovascular outcomes studies supporting the notion that GLP-1R agonists confer cardioprotective actions in pati
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br Indirect GLI antagonists br Direct GLI antagonists br
2022-04-12
Indirect GLI antagonists Direct GLI antagonists Concluding remarks Targeting GLI effectors represents a promising therapeutic strategy for cancer treatment. This is particularly relevant for certain tumors, such as MB, since, although classified into four distinct molecular groups (Hh- or W
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br Role of ghrelin in
2022-04-12
Role of ghrelin in reward and addiction In addition to its well-known effects on AF 12198 homeostasis regulation at the hypothalamic level [reviews in (Al Massadi et al., 2017, Muller et al., 2015)], ghrelin also has the ability to increase food motivation acting on hypothalamic and extra-hypoth
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br Materials and methods br Conflicts of interest Some of
2022-04-12
Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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Introduction br Channel activity Since initial reports of th
2022-04-12
Introduction Channel activity Since initial reports of the Ca2+-activated K+ permeability of erythrocytes (see Gardos, 1958), several ‘criteria’ have been established to certify K+ fluxes as being due to the Gárdos channel. For example, the requirement for Ca2+ at the intracellular face of the c
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With rare exceptions the biological role of secretase cleava
2022-04-12
With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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We next investigated whether pharmaceutical inhibition of th
2022-04-12
We next investigated whether pharmaceutical inhibition of the PI3K pathway was synergistic with FGFR inhibition using BKM120, a pan-PI3K inhibitor with modest antitumor activity in cancer patients, as a single agent. We found that RT112 (- translocation) and JMSU1 ( amplification) were not signifi
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Clinical data showed TAK was rapidly
2022-04-12
Clinical data showed TAK-875 was rapidly absorbed with a half-life of 28-30h and clearance primarily through glucouronidation in the liver with minimal urinary clearance [30]. TAK-875 made the glycosylated hemoglobin (HbA1c) levels fall significantly from baseline after 24-week administration in onc
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On the contrary the benzhydrol
2022-04-12
On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the Topiroxostat sale tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to t
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We also intended to determine
2022-04-11
We also intended to determine the possible mechanism underlying EZH2 upregulation in the PC. Although no recurrent mutations of EZH2 have been described in CLL [27, 28, 29], we aimed to rule out the possibility of activating mutations in the background of EZH2 overexpression. We detected no mutation
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