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Enlarging the ligand binding pocket by reduction of the
2021-08-17

Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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br Materials and methods br Results br Discussion
2021-08-17

Materials and methods Results Discussion Here we show expression of the EP1 receptor in the hippocampus of mice and the functional influence of the EP1 receptor on kainic p2y receptor induced seizures. Mice lacking a functional EP1 receptor gene displayed a lower tendency to enter status e
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Glycolysis is important to maintain the vital functions of T
2021-08-17

Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its Sulfasalazine metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egress from host
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In conclusion we for the first
2021-08-17

In conclusion, we for the first time demonstrated the enzyme activity and immunoprotective traits of bioactive recombinant SjCE-2b, which was successfully recovered by protein refolding from inclusion bodies. The results address two essential questions that were undocumented in previous investigatio
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Ponesimod sale Despite a high affinity for progesterone
2021-08-17

Despite a high affinity for progesterone and a relatively high affinity for testosterone [7], the binding of progesterone and testosterone to CBG is often disregarded [1], [2], [3]. However, the concentrations of these two hormones varies considerably under both normal physiological and pathophysiol
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The development of novel approaches to study GPCR
2021-08-17

The development of novel approaches to study GPCR-mediated transactivation in live STF 083010 is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Gr
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In the absence of ligand RNA CARD of
2021-08-17

In the absence of ligand RNA, 2CARD of RIG-I is masked by the intramolecular interaction with the helicase domain, showing auto-repressed state [33], [34]. But upon viral RNA binding, 2CARD of RIG-I is exposed to interact with the CARD domain of MAVS (also known as Cardif, IPS-1 or VISA) on mitochon
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br Discussion Several DPP inhibitors are
2021-08-17

Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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The presence of external NAD P H
2021-08-16

The presence of external NAD(P)H dehydrogenases (NDE) on the outer surface of the inner mitochondrial membrane enables the mitochondria to oxidize cytosolic NAD(P)H (Moller 2001). A porin (a voltage-dependent anion-selective channel, VDAC) that is abundant in the outer mitochondrial membrane permit
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We report here that DAPK signaling pathways play significant
2021-08-16

We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the Y-27632 to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by inactivating ERK1/2 and
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br Materials and methods br
2021-08-16

Materials and methods Results The i.v. administration of urocortin 2 reduced the mean arterial blood pressure in a dose-dependent manner (Fig. 1). The ED50 for the urocortin 2 cumulative dose–response effect on mean arterial blood pressure was 0.014±0.004 mg kg−1. Urocortin 2 administration h
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AON successfully alleviated the myotonic phenotype
2021-08-16

AON successfully alleviated the myotonic phenotype in DM model mice [18], [23]. To screen for an optimal AON sequence, we used 25-mer phosphorothioate 2′ O-methyl RNA molecules that covered the exon 6B or exon 7A. Unexpectedly, AON 7A (+63−8) which covers the boundary of intron 7A and exon 7A enhanc
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Several CHK inhibitors have been reported in the
2021-08-16

Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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br Acknowledgements br Introduction L
2021-08-16

Acknowledgements Introduction α-L-Rhamnosidases (EC 3.2.1.40) are glycosyl hydrolases (GHs) that cleave terminal α-l-rhamnose from a large number of natural products [1]. The action of α-L-rhamnosidases (α-RHAs) has been reported, among others, on different complex substrates such as heteropol
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Another important new result that has expanded the
2021-08-16

Another important new result that has expanded the range of functions of iPLA2-VIA in physiology and pathophysiology is its implication in macrophage polarization under stimulation conditions. Ashley et al. [129] described in peritoneal macrophages from Pla2g6−/− mice that the absence of iPLA2-VIA f
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