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Given the overexpression of HO in some tumors such
2022-02-24

Given the overexpression of HO-1 in some tumors, such as CML, and its potential involvement in chemoresistance to classical chemotherapeutic agents, compounds 4 and 8f were tested in CML cell lines resistant to IM, a classical TK inhibitor used in CML. Compounds 4 and 8f, in combination with IM, sho
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In summary we propose a model that explains the possible
2022-02-24

In summary, we propose a model that explains the possible mechanism the HULC mediates activation of HBV in liver cancer egfr inhibitors (Fig. 8). In the model, HULC promotes the expression of miR-539 by stimulating HBx-co-activated STAT3. Then, miR-539 down-regulates APOBEC3B, leading to an increase
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The intracellular signaling that mediates the adipogenesis i
2022-02-24

The intracellular signaling that mediates the adipogenesis induced by GPR120 still remains largely unknown. In the present study we showed that TUG-891 induced the activation of [Ca2+]i and ERK1/2 signaling in 3T3-L1 cells. Moreover, incubation of TUG-891 combined with BAPTA-AM or U0126 abolished TU
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The occurrence of MDR in
2022-02-23

The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer a cool way to improve in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems inclu
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Previous studies have shown that zinc interacts with other
2022-02-23

Previous studies have shown that zinc interacts with other allosteric modulators at the glycine receptor (Kirson et al., 2013, McCracken et al., 2010, McCracken et al., 2013). Of note, the chelation of zinc via tricine decreases the effects of alcohol at α1-, α2-, and α3-containing glycine receptors
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Epidemiological evidence indicates that neuroinflammation pl
2022-02-23

Epidemiological evidence indicates that neuroinflammation plays a pivotal role in pathogenesis of AD (Heneka et al., 2015, Heneka et al., 2013, Holmes et al., 2009, Liu et al., 2016). For example, prolonged treatment with nonsteroidal anti-inflammatory drugs reduces the risk of developing AD (In et
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br Material and methods br Results br
2022-02-23

Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a
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Since the Gardos channel Ca sensor have been
2022-02-23

Since the Gardos channel Ca2+ sensor have been shown to be constitutively bound calmodulin [16] and the PMCA is activated by association to a calcium–calmodulin complex, it seems probable that the NS309 agonist effect is caused by direct interaction with the Gardos channel, and not by an action on c
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br Results and discussion br
2022-02-23

Results and discussion Conclusion In conclusion, twenty-one 4-monocyclic aryl-5-carbamoyl-3-isoxazolols have been synthesized and evaluated for their antagonistic activities against housefly and common cutworm GABARs expressed in Xenopus oocytes. The TEVC results indicated that Prednisone syn
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br Promotion of GLS expression Glutamine metabolism is anoth
2022-02-23

Promotion of GLS2 expression Glutamine metabolism is another target for alteration in ferroptosis. Glutamine is required for the induction of ferroptosis during serum-induced injury after amino g-quadruplex starvation [72]. The first step of glutamine catabolism is its conversion to glutamate, wh
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In spite of decades of research the mechanisms of
2022-02-23

In spite of decades of research the mechanisms of SV endocytosis and recycling remain controversial. Accumulating evidence suggests that SV endocytosis occurs by more than one mechanism (e.g. clathrin-independent endocytosis, clathrin-mediated endocytosis, bulk endocytosis; reviewed in (Dittman and
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The present study was therefore
2022-02-23

The present study was therefore conducted with three aims; (1) we tested the effect of IRL-1620, a selective ETB receptor agonist, on the analgesic tolerance to morphine and oxycodone in mice; (2) we determined the expression of ETA receptors and ETB receptors in the HOBt of morphine and oxycodone
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br Drugs approved or in development To date
2022-02-23

Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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Dithiodipyridine also known as aldrithiol
2022-02-23

2,2′-Dithiodipyridine , also known as aldrithiol, is a known zinc ejector, targeting for instance the zinc finger in nucleocapsid protein of human immunodeficiency BAPTA-AM australia type 1. inhibited G9a activity with IC = 0.65 µM and GLP with IC = 2.6 µM. We also tested disulfide cysteamine dihyd
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br Histamine H R The
2022-02-23

Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other perifosine receptor receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al.,
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