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To understand the kinase selectivity profile of
2024-02-18
To understand the kinase selectivity profile of this series, GSK2606414 , as a representative analog from this series, was profiled against 216 purified protein kinases representing the tyrosine and serine/threonine kinase families using an in-house Caliper EZ Reader mobility shift assay. Assays wer
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Despite hydrolysis with commercial enzymes like
2024-02-18
Despite hydrolysis with commercial enzymes like trypsin, pepsin, Alcalase, Flavourzyme and Thermolysin have been used to digest parent proteins and generate peptides, microbial fermentation by proteolytic species has also proved to be a successful strategy (Fakhfakh et al., 2013, Jemil et al., 2016,
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A promising target that is involved in the
2024-02-18
A promising target that is involved in the biosynthesis of the precursor LTA4 is the 5-LO-activating protein (FLAP), which in vivo is seemingly indispensable for LT formation [8], [9]. FLAP, a member of the MAPEG family (membrane-associated proteins in eicosanoid and glutathione metabolism), is an i
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In our studies of leucine and BCH in pancreatic
2024-02-18
In our studies of leucine and BCH in pancreatic islets and clonal insulin cell lines, we noticed that leucine was a slightly stronger stimulant of insulin release. Previous studies showed that leucine can be metabolized to CO2[11], [12], [13], [14] and can increase acetoacetate in pancreatic islets
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Mitochondria are key organelles involved in the
2024-02-18
Mitochondria are key organelles involved in the mechanism of apoptosis (Xiong et al., 2014), and loss of ΔΨm is an important marker associated with mitochondrial dysfunction and cell death. We found that Mino induced ΔΨm impairment and nuclear fragmentation in Jurkat IOX4 in a concentration-depende
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br Conclusion br Competing interests br
2024-02-18
Conclusion Competing interests Funding The Bolger Prostate Cancer Research Fund (no grant number), the National Institute of General Medical Sciences of the National Institutes of Health (1-R01-GM58553, G. B. Bolger, principal investigator), and the National Cancer Institute of the NIH to t
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The mechanisms that control Ahr transcription are poorly
2024-02-14
The mechanisms that control Ahr transcription are poorly understood, especially when considering cell type-specific regulation. A recent report suggested that the Ahr transcription might be directly promoted by RORγt [retinoic braf inhibitors receptor (RAR)-related orphan receptor γt] based on ChIP-
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br Discussion With recently improved understanding of the ro
2024-02-14
Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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Moreover an increase of extracellular calcium
2024-02-14
Moreover, an increase of extracellular calcium stimulates BMP-2 expression of pulp fak inhibitor via L-type calcium channel and ERK signaling, which can be attenuated by PD98059 and nifedipine . Dental pulp cells expressed little calcium-sensing receptors . immunohistochemistry staining also shows t
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It is worth pointing out that phenotypes of
2024-02-14
It is worth pointing out that phenotypes of in vivo HSP90β inhibition were not identical to those observed in rapsyn mutant mice (Gautam et al., 1995). Postsynaptically, junctional AChR clusters appeared fragmented, in addition to expected reduction in AChR intensity, in muscles injected with 17-AAG
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At present drugs that specifically inhibit YAP activity
2024-02-14
At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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Our sample is representative of
2024-02-14
Our sample is representative of mRCC treated with sunitinib. However, the results from CCC setting have limited inference due to small exploratory sample (n = 51). Additionally, the significance of survival differences in CCC according to AXL staining is tangential. Unfortunately, we were unable to
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Previously using a P lacZ reporter gene
2024-02-10
Previously, using a P-lacZ reporter gene system, it has been shown that the β-galactosidase activity was 9-fold higher in the stationary phase ER 50891 when compared with those of the exponential phase [15]. Furthermore, inositol supplementation did not have a major effect on the expression of β-gal
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CPI-455 mg Thymoquinone TQ is the major active compound deri
2024-02-10
Thymoquinone (TQ) is the major active CPI-455 mg derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005, Badr et al., 2
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phenanthroline Another heroic set of studies combining retro
2024-02-10
Another heroic set of studies combining retrodialysis with electrophysiological recording at two distinct brain sites further indicated that the estradiol-induced increase in auditory-evoked firing in NCM also enhanced the selectivity of auditory-evoked responses in the downstream sensorimotor nucle
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