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Molecular docking quantitative structure activity
2024-11-25
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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br Materials and methods br Results br
2024-11-25
Materials and methods Results Discussion Japanese encephalitis caused by JEV is characterized by TCEP HCl reagent neuron death. However, the underlying mechanism is not fully understood. We and other researchers have demonstrated that JEV induces apoptosis by ER stress-mediated IRE1/JNK an
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Glycosylphosphatidylinositol GPI cell wall anchor synthesis
2024-11-25
Glycosylphosphatidylinositol (GPI) oicr synthesis anchor synthesis pathway is another promising antifungal target. Novel inhibitors of Gwt1 and Mcd4, two enzymes in the GPI anchor pathway were identified by the chemical-genomics-based screening platform CaFT (Candida albicans fitness test) [89]. Sc
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am580 br Natriuretic peptides and neprilysin Left ventricula
2024-11-25
Natriuretic peptides and neprilysin Left ventricular systolic function, most commonly due to myocardial damage as a consequence of coronary artery disease, hypertension or both, and leading to sustained, pathological activation of the renin angiotensin am580 system (RAAS) and sympathetic nervous
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hydroxycarboxylic acid receptors Based on their different so
2024-11-25
Based on their different sources, the APN inhibitors (APNIs) can be divided into the natural products and synthetic compounds. Bestatin (1, Fig. 1), isolated from the Streptomyces oliuoreticuli by Umezawa et al., is the first reported and only marketed natural dipeptidomimetic inhibitor of APN. Afte
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br Acknowledgements br Introduction Microbial enzymes have g
2024-11-25
Acknowledgements Introduction Microbial enzymes have gained interest for their widespread uses in industries and medicine owing to their stability, catalytic activity, and ease of production and optimization than plant and animal enzymes (Singh et al., 2016). Microbial aminopeptidases (amino-a
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Iberiotoxin br Discussion The present understanding is that
2024-11-25
Discussion The present understanding is that patients suffering from AD are at a higher risk for epilepsy than individuals without AD [[1], [2]]. The clinical diagnostic accuracy of AD has improved significantly during the last decades. However, most of the epidemiological studies on these two of
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However although in vitro studies
2024-11-25
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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br Acknowledgements This work was
2024-11-25
Acknowledgements This work was supported by grants from the Program for Changjiang Scholars and Innovative Research Team in University (IRT_14R28), the National Basic Research Program of China (973) (Grant No.: 2013CB733602), the Major Research Plan of the National Natural Science Foundation of C
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The AR signalling pathways play important roles in several
2024-11-25
The AR signalling pathways play important roles in several physiopathological processes associated with ischaemia, inflammation, and tumourigenesis [35]. Moreover, A3AR is overexpressed in different tumour Ionomycin calcium salt and seems implicated in pro- or anti-apoptotic effects [36]. In partic
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Although our data failed to reproduce the robust enhancement
2024-11-25
Although our data failed to reproduce the robust enhancement of LTP in the rat dentate with nicotine that was previously reported, our results with NS6740 suggest a more fundamental role for α7 receptor signaling in modulation of synaptic tone in the LTP pathway. The discovery of the cholinergic ant
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Subsequently Palvimaki et al corroborated Ni and
2024-11-23
Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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In the current study we provide
2024-11-23
In the current study, we provide evidence that enhanced ATX activity correlates well with increased ATX protein concentration during cholestasis and pregnancy (Fig. 1). Hereby we have ruled out the possibility of ATX enzyme activation in these conditions, e.g. by circulating cholephiles. ATX clearan
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Recent studies have indicated that V
2024-11-23
Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ cas chemical have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pah1Δ cells'
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A high throughput screening campaign led to the
2024-11-23
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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