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Celiac disease occurs in the small intestine due to the
2020-12-24
Celiac disease occurs in the small intestine due to the ingestion of gluten and triggers an immune response by T-cells resulting in tissue remodelling and malnutrition [6]. Earlier studies by many researchers have shown that the prolamins of gluten are the toxic agent for celiac disease, since they
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br Prospect of DDR antagonist
2020-12-24
Prospect of DDR2 antagonist DDR2, a receptor of tyrosine kinase has been found now to be reported to play a significant role in onset of osteoarthritis at the early stage of diseases progression. The DDR2 are the receptor for extracellular collagen and activated upon the binding of collagen resul
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Z-YVAD-FMK Our previous studies indicate that EBI is involve
2020-12-24
Our previous studies indicate that EBI2 is involved in the regulation of pro-inflammatory responses and inter-cellular communication under pathophysiological conditions such as LPS challenge (Rutkowska et al., 2016b). The data showed that media taken from LPS stimulated astrocytes induces macrophage
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The expression of cytokine inducible genes is
2020-12-23
The expression of cytokine-inducible genes is mediated by a number of components within the cell. It has been shown that Jak2 and the Ras/Raf/MAP kinase signaling cascades are required for the expression of DUB-1[9], [29]. However, the enhancer domain of DUB-1 lacks a consensus sequence for Stat bin
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br Effect of DPP Inhibitors on the
2020-12-23
Effect of DPP-4 Inhibitors on the Clinical Course of Heart Failure Four large-scale cardiovascular outcomes trials with DPP-4 inhibitors have been completed, and their findings have been published (Table 1) 31, 32, 33, 34. In 2 studies (with saxagliptin and alogliptin), DPP-4 inhibition was accom
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The first ones class A receptors found as heterodimers
2020-12-23
The first ones class A receptors found as heterodimers were reported by Gomes et al. (2000), who identified a heteromer constituted by two subtypes of opioid receptors (μ and δ) in heterologous cells. The same year, Ginés et al. (2000) showed the first heteromer composed of two different receptors,
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DGK is a key enzyme in glucose uptake
2020-12-23
DGKδ is a key enzyme in glucose uptake in skeletal muscle. Chibalin et al. demonstrated that a decrease in DGKδ expression increases the severity of type 2 diabetes [20]. Additionally, DGKδ expression was increased in people who exhibited enhanced insulin sensitivity after exercise training [56]. Fr
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br Conformational properties of DGK br Interaction of DGK
2020-12-23
Conformational properties of DGKϵ Interaction of DGKϵ with its lipid substrate A major component of the interaction between DGKϵ and lipid bilayers is the insertion of the hydrophobic segment comprising residues 20–42 into the membrane, as discussed above. However, this is not the only interac
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Inhibition of DHODH is reflected by
2020-12-23
Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear thymidine phosphorylase (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few sel
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Our finding that activating DDR
2020-12-23
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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We report here that DAPK signaling pathways play significant
2020-12-23
We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the melanocortin receptor to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by inactiva
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br Fragment based drug discovery FBDD is a powerful
2020-12-23
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical palmitoylethanolamide reviews space with libraries which are smaller in size, producing drug leads with high ligand-bindi
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Oral antipsychotics are substrates of CYP enzymes which
2020-12-23
Oral antipsychotics are substrates of CYP450 enzymes, which are crucial to their metabolism and elimination (Fig. 1). The efficacy and toxicity of antipsychotic agents is affected by factors that induce or inhibit CYP450 expression and function, such as drug–drug interactions. Additionally, the mult
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Drug drug interactions are frequently attributed to function
2020-12-23
Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is th
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van Linden et al developed a comprehensive guide
2020-12-23
van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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