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Our observation of LPS induced increase in the sensitivity o
2022-04-11

Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary CGP 54626 hydrochloride towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary arteries. However, th
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br Prostaglandins meet Hippo The prostaglandins lie at
2022-04-11

Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic Exendin-3 (9-39) amide sale by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects agains
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br General aspects of HDACs
2022-04-11

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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A more quantitative view of kinase specificity suggests a
2022-04-11

A more quantitative view of kinase specificity suggests a continuum of phosphorylation rates for the various substrates of a particular kinase (Figure 4A). Such differences in ‘substrate quality’ can arise from variations in phosphorylation site or docking sequences and may explain why the timing or
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For the study described herein analogues of CID were
2022-04-11

For the study described herein, analogues of CID1792197 (2) were selected for exploration. There are a variety of reasons for this decision. First, the synthetic approach, described hereafter, is modular in nature to rapidly enable the independent modification of either end of the molecule. Second,
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GPR A a G protein coupled receptor located mainly on
2022-04-11

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic Antagonist G mg [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-me
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Even though for almost years GnRH was considered the main
2022-04-11

Even though for almost 30 years GnRH was considered the main neuropeptide regulating gonadotropin release in vertebrates, Tsutsui et al. (2000) discovered, in the Japanese quail, Coturnix japonica, a hypothalamic neuropeptide that directly inhibits gonadotropin release, and thus named as gonadotropi
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No compounds in this series showed
2022-04-11

No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in ma
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To maintain low Glu concentrations in the synaptic
2022-04-11

To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino Thalidomide 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 astroc
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br Ghrelin and energy balance To characterize
2022-04-09

Ghrelin and exactly balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact appear identical to t
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ddhGTP br Materials and methods br Results
2022-04-09

Materials and methods Results Discussion Several peripheral hormones that are involved in the central regulation of energy homeostasis, such as leptin, insulin, and amylin [34], [35], [36], [37], [38], cross the BBB by saturable and unsaturable mechanisms. Whether these transport processes
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In conclusion we show to our
2022-04-09

In conclusion, we show, to our knowledge for the first-time, compelling evidence for functional OTR and GHSR crosstalk, which is likely via the formation of a novel OTR/GHSR heterocomplex with important downstream signalling consequences. This OTR/GHSR interaction is poised to play an important phys
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Next we studied the effects of the
2022-04-09

Next, we studied the effects of the compounds PA-Glu, PA-hSuc, and PA-hPim on the IGly of rat hippocampal neurons. As in the experiments with IGABA, IGly was affected by steroids with a pregnane skeleton, but not those with an androstane skeleton. At the same time, androstane steroids were shown to
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d mannitol Studies have indicated that formylated peptides F
2022-04-09

Studies have indicated that formylated peptides, FPRs, and in particular FPR-1 may be principal conductors in inflammatory processes in sterile-24, 26 and infection-related diseases. FPR-1 and formylated peptides, which are active components of CS, have been involved in smoking-induced lung damage,
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Ning et al showed that
2022-04-09

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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