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Recently two distinct small molecule
2025-02-20
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer pituitary adenylate cyclase-activating peptide with high SSP flux [50,51]. The inhibitor NCT-503, which has
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The number of times an animal reared was the
2025-02-20
The number of times an animal reared was the only emotional behavior that was significantly higher in the young mice than in the middle-aged group. This may be explained by diminished curiosity or augmented ambulation with aging (Lalonde and Strazielle, 2008). A recent study showed that middle-aged
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Although several ARIs have reached various phases of clinica
2025-02-20
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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In contrast to the beneficial treatment of skin
2025-02-20
In contrast to the beneficial treatment of skin-inflammation with PAH containing coal tar, epidemiology showed that environmental pollution, containing AHR-activating PAH, lead to more eczema [80]. Of note, other epidemiological data suggested that Th17 cell polarization may be enhanced air pollutio
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Taken together the results reveal a
2025-02-20
Taken together, the results reveal a complex feedback and feedforward signaling network between the tryptophan metabolic enzymes IDO1/TDO2, the KP metabolite KYN, and the ligand-activated transcription factor AhR (Figure 2). Cancer dihydrofolate reductase inhibitor antibacterial highjack this signa
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br Material and methods br
2025-02-20
Material and methods Results Discussion GRK2 activity has increasingly been shown to contribute to the progression of numerous diseases and organ dysfunction [5], [6]. For instance, a large body of work over the last two decades has identified GRK2 as a major regulator of cardiac dysfunctio
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The anorexic effect observed when AR is infused into
2025-02-20
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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Since the cloning of ARs
2025-02-20
Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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br Expression of ADK in the normal brain
2025-02-20
Expression of ADK in the normal brain In adult brain, ADK is primarily expressed in astrocytes. Immunocytochemical analysis of adult rat and mouse Concanavalin A glycan binding revealed predominant astrocytic expression throughout the hippocampus and cortex. Two isoforms of ADK have been identif
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The assay performance was estimated
2025-02-20
The assay performance was estimated using Z′-factors (plotted in Fig. 2A) according to Zhang et al. calculated for each plate comparing positive (in the absence of an inhibitor) and negative controls (in the presence of an AdK inhibitor). The mean Z′-factor±SD was determined to be 0.7±0.1, indicativ
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br Conclusion br Conflicts of Interest
2025-02-20
Conclusion Conflicts of Interest/Disclosures Acknowledgement This study was funded by the Ministry of Science of the Republic of Serbia (grant #175083). Introduction Myasthenia gravis (MG) is an antibody-mediated, neuromuscular transmission disorder, where the targets are postsynaptic p
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br Experimental section br Results and discussion br Conclus
2025-02-20
Experimental section Results and discussion Conclusion In the present study, 3a,8a-dihydroxy-8-oxo-1,3,3a,8a-tetrahydroindeno[1,2-d]imidazol-2(1H)-iminium chloride (3) has been synthesized and characterized by spectral studies and single crystal X-ray crystallography. DFT calculations have
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In fact serotonin is a
2025-02-20
In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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For the TSH receptor signaling at the Golgi
2025-02-20
For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as 5-Methyl-UTP depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Continued s
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Plant defensins are cysteine rich cationic peptides of kDa
2025-02-19
Plant defensins are cysteine-rich cationic peptides of 5–8 kDa whose mature domain comprises 45 to 54 amino Depression treatment residues, with an isoelectric point around 9. The global fold of plant defensins consists of a cysteine-stabilized motif (CSα/β) made up of an α-helix and a triple-strand
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