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bace inhibitors In this study in an
2023-04-20
In this study, in an effort to explore the possible role of 5-HT6 receptors in mediating the memory-enhancing effects of YL-0919, we first assessed the memory-enhancing effects of YL-0919 in the Morris water maze, object recognition test and step-down passive avoidance task. In addition, we then inv
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The role of DHT in
2023-04-20
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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In this scenario the receptor
2023-04-20
In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; Pits PIK-90
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The enzyme Arginase ARG plays a role in the hepatic
2023-04-20
The enzyme Arginase 1 (ARG1) plays a role in the hepatic urea cycle by hydrolyzing L-arginine to L-ornithine and urea [13]. In the context of macrophages and MDSCs, ARG1 expression redirects L-arginine metabolism to abolish cytotoxic nitric oxide production [14], suppress T-cell function [15], [16],
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Protein arrays provide a new approach for the identification
2023-04-20
Protein arrays provide a new approach for the identification of substrates for several protein-modifying enzymes. For example, protein kinase substrate identification, which constitutes an important aspect of pathway mapping because of the prevalence of these substrates in biological pathways. MacBe
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Imatinib was first approved for the treatment
2023-04-20
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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To guide our attempts at achieving AKT potency
2023-04-20
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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br Discussion Here we show
2023-04-20
Discussion Here, we show opposing effects of iontophoretically administered phenylephrine,aselective α1-AR agonist, on firing of putatively DAergic and non-DAergic neurons recorded in vivo in the VTA of urethane anaesthetized rats. Phenylephrine application caused a relatively weak decrease in fi
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The reduced IFN production seen
2023-04-19
The reduced IFNγ production seen with BPAL10-primed splenocytes could potentially be attributed to the impaired intracellular survival of B. pertussis, thereby leading to a weakened induction of cell-mediated immunity. Earlier studies have suggested an antimicrobial role of IFNγ in mediating the eli
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br Results and discussion br
2023-04-18
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic Necrosulfonamide synthesis group extending from the C-3 position of the aniline and
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Nowadays more than kinases have been identified of
2023-04-18
Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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Aurora B is also known as chromosomal passenger protein
2023-04-18
Aurora-B is also known as chromosomal passenger protein and localizes at the chromosome arms and at centromeres during prophase. As cell cycle continues, Aurora-B moves towards the inner centromere region followed by the central spindle and cortex during 1478 and finally accumulates in the midbody
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Crystal structures were obtained of sulfonamide and amide as
2023-04-18
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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Autophagy is a self protecting
2023-04-18
Autophagy is a self-protecting cellular catabolic pathway that degrades and recycles cytoplasmic contents for the maintenance of cellular homeostasis (Shao et al., 2016b). Macrophage autophagy plays an essential role in atherosclerosis by safeguarding Disuflo Cy3 azide against oxidative stress, red
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pathways cu australia br Materials and Methods br Results br
2023-04-18
Materials and Methods Results Discussion XHP is a traditional Chinese anti-cancer medicine that is widely used for the treatment and adjuvant treatment of breast cancer. XHP has been shown to induce apoptosis in various breast cancer pathways cu australia in vitro, including Hs578T, MCF-7,
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