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Gap junctions mediate electrical coupling
2022-09-03
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 He
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Our own search towards aryl imidazole derived GSMs led to
2022-09-03
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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br FXR expression in normal intestine and cancer Of note
2022-09-03
FXR LCL161 in normal intestine and cancer Of note, there are several question marks about FXR post-translational modifications (such as acetylation or SUMOylation) and their involvement in the pathogenesis of metabolic and inflammatory disease (Balasubramaniyan et al., 2013, Kemper et al., 2009,
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br ACKNOWLEDGMENTS br Introduction Odorant receptors ORs are
2022-09-03
ACKNOWLEDGMENTS Introduction Odorant receptors (ORs) are the largest subfamily of G protein-coupled receptors (GPCRs) and are mainly expressed by olfactory sensory neurons in the nose for the detection of various odorants [1]. However, more recent reports suggest that ORs are also expressed a
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We characterized the enzyme corresponding to N FPP was the
2022-09-03
We characterized the enzyme corresponding to N1. FPP was the most effective substrate as allylic diphosphate, and the activities with GPP and DMAPP were 50% and 11% that with FPP, respectively. The analysis of the prenols resulting from the treatment of prenyl diphosphates with Go 6983 receptor pho
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The ETA receptor has a higher affinity for
2022-09-03
The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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The molecular mechanisms underlying VSMC ETB receptor upregu
2022-09-03
The molecular mechanisms underlying VSMC ETB receptor upregulation have been studied after 24–48h organ culture in both coronary and cerebral arteries. The increased expression of contractile ETB receptor at these time points has been shown to depend on transcriptional mechanisms and PKC and the ext
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Accumulating evidence suggests that the NGF
2022-09-03
Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, BCA Protein Quantitation Kit derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [3
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Prolonged sGC oxidative inhibition occurs in many
2022-09-02
Prolonged sGC oxidative inhibition occurs in many diseases [46,[86], [87], [88]]. Keeping sGC membrane-bound and functional under conditions of high oxidative stress requires a mechanism for restoring oxidized sGC (Fe3+) heme iron to its reduced (Fe2+) state. Without this redox regulation, the sGC
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br S NO signalling during
2022-09-02
(S)NO signalling during the plant immune response Redox signalling molecules must exhibit specificity for their target substrate. Moreover, a given redox-based modification must be reversible to ensure transient signalling. Oxidative cysteine (Cys) modifications are integral to a variety of redox
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br FFA GPR was deorphanised
2022-09-01
FFA4 GPR120 was deorphanised as the second receptor for long-chain fatty acids in 2005 [5]. Initial focus highlighted expression in the lower gut, the capacity of unsaturated fatty acids to promote release of the incretin glucagon-like peptide-1 (GLP-1) from the enteroendocrine cell line STC-1, a
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Thyroid Hormone Receptor Antagonist (1-850) br GPR is a clas
2022-09-01
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine Thyroid Hormone Receptor Antagonist (1-850) which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated invol
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In previous work we showed that benzophenanthridines do not
2022-09-01
In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in t
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In the present study participants reported a significant
2022-09-01
In the present study, participants reported a significant decrease in symptoms of anxiety and depression along with other symptoms of psychological distress and PTSD. These results are in agreement with a study in which hospitalized patients diagnosed with psychotic and mood disorders demonstrated s
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Although the overall structures of mGlu and mGlu
2022-09-01
Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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