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This crosstalk may be responsible for the
2021-10-13

This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on thymidine phosphorylase pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of hig
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Acknowledgements We appreciated the contributions
2021-10-13

Acknowledgements We appreciated the contributions of Ana Carolina Galha, Selma XSL Pinheiro and Islene Azevedo for technical assistances. In addition, we wish to thank Adilson José de Almeida (in memoriam), Moyra M Portilho, Vanessa A Marques and Letícia P Scalioni, for data analysis during the set
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The characterization of Da CTSL shows that it
2021-10-13

The characterization of Da-CTSL1 shows that it preferentially cleaves Z-FR-AFC (Fig. 8), which has a syk inhibitors phenylalanine at P2 and Da-proCTSL1 is autocatalyzed at pH 8.0 releasing an activated Da-CTSL1 that exhibits optimal activity at pH 8 indicating that the enzyme when secreted by the fo
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Urinary hydroxypyrene OHP is a widely used biological marker
2021-10-13

Urinary 1-hydroxypyrene (1-OHP) is a widely used biological marker of exposure to PAHs and indicator for internal dose of activated PAHs (Jongeneelen, 1987, Adonis et al., 2003). PAH metabolites may be excreted either as free or as conjugated compounds. When 1-OHP is measured after treating the urin
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Lipid sensing GPCRs as therapeutic targets G protein coupled
2021-10-13

Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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Some biguanides can cross the mitochondrial membrane
2021-10-13

Some biguanides can cross the mitochondrial membrane and increase L-lactate formation by inhibiting oxidative Decanoyl-RVKR-CMK [34]. On the other hand, it has also been reported that levels of fasting plasma lactate in T2DM patients are similar regardless of whether or not metformin is administere
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In conclusion we have designed and characterized a
2021-10-13

In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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In order to elucidate the reasons of
2021-10-13

In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen filgotinib synthesis of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12 μM)
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Animal studies have shown that various antidepressant treatm
2021-10-13

Animal studies have shown that various antidepressant treatment are capable of upregulating GR protein and mRNA in key Imeglimin synthesis regions including the hippocampus and decreasing basal and/or stress-induced glucocorticoid secretion [37]. Changes in the level or function of GR regulate the n
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Azidobutyric acid NHS ester sale When PKC was applied alone
2021-10-13

When PKC19–31 was applied alone, it attenuated the activity run-down following excision. Furthermore, the activity induced by addition of PKC19–31 during PMA treatment in many cases was higher than in controls. Accordingly, in our experimental conditions, the mechanism which underlays channel inhibi
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Based on the previous report that
2021-10-12

Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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Recent research has focused on identifying key
2021-10-12

Recent research has focused on identifying key agonists and receptors mediating nutrient-induced GLP-1 and insulin secretion. The long-chain fatty phenethyl receptor receptor GPR40 is the most abundant GPCR expressed in islet β cells and is also expressed on intestinal L-cells, where it contributes
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By measuring the accumulation of unprenylated Rap a as a
2021-10-12

By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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Colorectal cancer CRC is the
2021-10-12

Colorectal cancer (CRC) is the leading cause of cancer deaths in Taiwan and is also a most common cancer in the world (Huang et al., 2012, Jemal et al., 2011). With early detection and treatment in the initial stage, CRC can be recognized as curable in comparison with other malignant tumors (Levin e
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TLRs were originally identified as pathogen associated molec
2021-10-12

TLRs were originally identified as pathogen-associated molecular pattern recognition receptors that recognized exogenous ligands in response to infection [31]. In cirrhotic mice or patients, the gastrointestinal tract produces and absorbs considerable bacterial LPS with increased permeability of the
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