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In order to postulate its binding mode in APN compound
2024-07-29

In order to postulate its binding mode in APN, bcrp transporter 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupied
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In view of the ubiquitous distribution
2024-07-29

In view of the ubiquitous distribution of the arachidonate 12S-lipoxygenase isoforms and the variety of cellular reactions influenced by the resulting arachidonate metabolites, these products widely play important roles in many biological systems. The development of new type-specific inhibitors of t
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When arachidonic acid is used as a substrate the platelet
2024-07-29

When arachidonic tipiracil synthesis is used as a substrate, the platelet-type 12S-lipoxygenase produces predominantly the 12S-hydroperoxy derivative. In contrast, the leukocyte-type 12S-lipoxygenases generate substantial amounts of the 15-lipoxygenase product in addition to the 12S-hydroperoxy der
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br Results and discussion br Conclusion The tyrosine kinase
2024-07-29

Results and discussion Conclusion The tyrosine kinase ALK represents one of the most successful molecular targets for the development of precise medicine to treat stratified subgroups of cancer patients. Three generations of ALK inhibitors have been awarded the FDA's approval or are being exte
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Accumulating evidence suggest that patients with
2024-07-29

Accumulating evidence suggest that patients with advanced -positive NSCLC are at increased risk of VTE or coagulation disorders during the course of their disease, indicating that cancer genotype might play a role in the occurrence of cancer-related thromboembolism . Here we report the case of a pat
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The binding of TQ to hsALDH
2024-07-29

The binding of TQ to hsALDH changes the characteristic Ellipticine spectrum of the enzyme. Therefore, TQ forms a complex with hsALDH and changes its absorption properties [39]. Ksv and Kb values indicate that the binding of TQ to hsALDH is very strong and of the order of static binding (complex form
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Through systematic deletion of AhR in
2024-07-29

Through systematic ion channels of AhR in specific cell types, Di Meglio et al. (2014) revealed that AhR in keratinocytes and fibroblasts are key to the exacerbated psoriatic phenotype induced by IMQ in AhR-deficient mice. This emphasizes the crosstalk between keratinocytes and the immune system to
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A number of studies suggest
2024-07-29

A number of studies suggest that adiponectin promotes osteoblast differentiation and bone formation by directly targeting GSK-3β and β-Catenin signaling [64], [65], favoring bone marrow mesenchymal stem cell (BMSC) differentiation toward the osteoblastic lineage [66], [67], decreasing sympathetic to
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br Functional consequences of ADK regulation on astrocyte
2024-07-29

Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in cysteine protease (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation of AD
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Some alterations in the integrity of cell membranes caused b
2024-07-29

Some alterations in the integrity of cell membranes caused by toxic agents can be determined by measuring certain enzymes released by damaged cells [8]. The cholinesterases, for example, catalyze the hydrolysis of bromodomain inhibitor (ACh) in choline and acetic acid. Theses enzymes are divided in
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Autophagy is a highly conservative intracellular bulk degrad
2024-07-29

Autophagy is a highly conservative intracellular bulk degradation process including three major forms namely microautophagy, chaperone-mediated autophagy and macroautophagy. A large number of evidence has depicted a pivotal role for autophagy in the maintenance of cardiac geometry and contractile fu
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Although several different membrane estrogen receptors have
2024-07-26

Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec
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br Current limitations and future directions There are sever
2024-07-26

Current limitations and future directions There are several limitations associated with PET imaging of aromatase using carbon-11 labeled aromatase inhibitors. Due to the very short half-life of carbon 11 (20min), PET studies with currently available, validated tracers can only be performed in med
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It is reported that calpain plays a
2024-07-26

It is reported that calpain-2 plays a critical role in BDNF-induced signaling and memory formation, and knockdown of calpain-2, but not calpain-1, completely suppresses BDNF-induced pathway activation and protein translation (Briz et al., 2013). BDNF prevents neuronal apoptosis or death (Ferrer et a
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Additional support for a role of HMGN in enhancing DNA
2024-07-26

Additional support for a role of HMGN1 in enhancing DNA repair comes from studies of transcription-coupled repair (TCR) in human cells. Lesions in the template strand of DNA induced by UV light stall the movement of RNA polymerase II (RNAPII) and interrupt transcription. Removal of these transcripti
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