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Neurotransmitter transporters are rapidly recycled from and
2022-01-14
Neurotransmitter transporters are rapidly recycled from and to the membrane. For instance, the GABA transporter GAT1 is recycled in a calcium and depolarization dependent manner. GAT1 located in the plasma membrane is internalized to a subpopulation of small vesicles different from the classical neu
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To maintain low Glu concentrations in the synaptic cleft
2022-01-14
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino Caspase-6, human recombinant protein is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of peri
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To confirm the in vitro findings atorvastatin
2022-01-14
To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g
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Type diabetes mellitus is characterised by two
2022-01-14
Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta Syringin [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to insulin resistance in per
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br Conclusions Temporally controlled disruption of
2022-01-14
Conclusions Temporally-controlled disruption of Gcgr reveals a lack meaningful contribution to the improvement of glycemic control in insulinopenic conditions attributable to the intrinsic loss of GCGR signaling. On the other hand, these data highlight the importance of compensatory systems, incl
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The fine interplay among post
2022-01-14
The fine interplay among post-translational modifications and intersection with other pathways, such as PI3K–AKT, has a crucial role in the regulation of GLI activity and in the generation of their repressor forms 40, 41, 42. In addition to β-TrCP, for example, other E3 ligases belonging to the real
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Gap junctions mediate electrical coupling
2022-01-13
Gap junctions mediate electrical coupling between cells by conducting direct ionic currents and thereby modulate their electrical activity (Hormuzdi et al., 2004). In the nervous system, electrical coupling organizes network activity by amplifying and synchronizing neuronal firing (Galarreta and Hes
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Hydantoin in region F bridging the phenoxybenzene and benzim
2022-01-13
Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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br General aspects of HDACs br General aspects of
2022-01-13
General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai
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PLP has been found to be
2022-01-13
PLP has been found to be effective inhibitor of many enzymes that have 5 aza 2 deoxycytidine australia for phosphate-containing substrates or effectors, including RNA polymerase [14], [15], reverse transcriptase [16], and DNA polymerase [17], [18]. Oka et al. [19], [20] reported that vitamin B6 def
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As natural ligands of GPR several long chain polyunsaturated
2022-01-13
As natural ligands of GPR120, several long chain polyunsaturated fatty acids (Lc-PUFAs) have been demonstrated to modulate the 3T3-L1 adipogenic differentiation. However, the effects of the Lc-PUFAs are inconclusive. DHA is shown to inhibit, promote or even not affect the differentiation of preadipo
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Acarbose and voglibose the classic glucosidase inhibitors we
2022-01-12
Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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We identified three genes KEAP NAA
2022-01-12
We identified three genes—KEAP1, NAA38, and ABCC1/MRP1—as negative regulators of glutathione abundance in human cells. Like KEAP1, NAA38 appears to regulate NRF2 stability, as NAA38 deletion increased NRF2 protein levels and the expression of NRF2 target genes. NAA38 is a component of the NatC N-ter
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In principle an ideal Fenton reaction element should have
2022-01-12
In principle, an ideal Fenton reaction element should have multiple oxidation states to form a redox cycle in the process of H2O2 decomposition to HO•. Although iron is very effective in catalyzing Fenton reaction, it requires a low pH value (pH 2-4) to reach the optimal catalytic efficiency, which
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The subcellular redistribution of some
2022-01-12
The subcellular redistribution of some metabolic enzymes is dynamic and responsive to metabolic conditions. In the absence of glucose, Glucokinase (GK) is bound to its regulatory protein in the nucleus of the hepatocyte and translocates to the cytoplasm when sugar levels increase [12]. Muscle glycog
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