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Screening a selection of analogues
2024-04-09

Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to SAR-302503 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonstrated >5
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br Aurora A Aurora B and Aurora C small molecule
2024-04-09

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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Findings of the present study provide a molecular
2024-04-09

Findings of the present study provide a molecular mechanism for the elevated ASK1 expression in obesity and how it may be functionally linked to whole-body insulin resistance. The role our findings assign to increased E2F1 in upregulating ASK1 parallels the capacity of this transcription factor to r
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br Funding The present study
2024-04-09

Funding The present study was funded by The Scientific and Technological Research Council of Turkey (TUBITAK) within Research Program 1001, unique project number: 214S349. Introduction The apelin receptor, also called APJ or angiotensin receptor-like 1 was first cloned in 1993 due to its stro
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The zinc transporter proteins are members of the SLC
2024-04-08

The zinc transporter proteins are members of the SLC superfamily of metal transporters, and comprise two structurally and functionally different groups, the zinc-importer (ZIP; Zrt-, Irt-like proteins) family (SLC39A), which regulate zinc transport into the cytoplasm from outside the cell and from i
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Breast Cancer Although androgens have been considered to be
2024-04-08

Breast Cancer: Although androgens have been considered to be a risk factor in prostate cancer they have been recommended to treat breast cancers. Even before the discovery of SERMs and aromatase inhibitors, steroidal androgens such as medroxyprogesterone and fluoxymesterone were used to treat breast
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br Introduction It is well known
2024-04-08

Introduction It is well known that when epithelial cells are deprived of anchorage, they undergo detachment-induced apoptosis, also known as anoikis. Cancer cells, by contrast, are able to suppress anoikis and survive under anchorage -independent conditions in the circulating system, which is tho
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br Acknowledgements br Introduction Microbial enzymes have g
2024-04-08

Acknowledgements Introduction Microbial enzymes have gained interest for their widespread uses in industries and medicine owing to their stability, catalytic activity, and ease of production and optimization than plant and animal enzymes (Singh et al., 2016). Microbial aminopeptidases (amino-a
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br Introduction Alzheimer s disease AD
2024-04-08

Introduction Alzheimer's disease (AD) is a neurodegenerative disorder and the leading cause of dementia. It is characterized by progressive and irreversible damage to different AZ505 areas, resulting in cognitive impairment and behavioral changes (O'Neill, 2013, De Strooper and Karran, 2016, Alz
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We found evidence of the interaction between AR and hemiacet
2024-04-08

We found evidence of the interaction between AR and hemiacetals by evaluating the effect of glucose on l-idose reduction. l-idose was recently proposed as the best AR substrate able to mimic glucose [38]. This aldose is structurally very closely related to d-glucose, from which it differs only in th
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There are some limitations and further experiments that
2024-04-08

There are some limitations and further experiments that are required. First, to our surprise, measurement of the cardiomyocyte cross-sectional area in Akt1−/−/iAkt2 KO mice showed comparable areas to WT mouse despite of reduced heart weight. In addition to measuring cardiomyocyte cross-sectional are
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In silico docking analysis performed in the current study
2024-04-08

In silico docking analysis performed in the current study indicated that TCDD strongly binds to AhR-LBD. Moreover, the formation of the TCDD/AhR-LBD complex was confirmed experimentally with the use of EMSA. We found that 10nM TCDD after 2 hours of incubation not only bound to the AhR in the porcine
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In addition to plasma membrane sites OCT was also observed
2024-04-08

In addition to plasma membrane sites, OCT3 was also observed associated with endomembranes, including mitochondrial membranes, with particularly strong expression in the outer nuclear membranes of both neurons and astrocytes (Gasser et al., 2017), indicating that, in addition to regulating extracell
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Although the effects of adenosine receptor signaling in acut
2024-04-08

Although the effects of adenosine receptor signaling in acute renal IRI have been attributed to the generation of high concentrations of adenosine, we have recently reported an increase in kidney levels of both AMP and adenosine, with a concomitant fall in ATP and ADP. We have also previously demons
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We investigated the role of ABT treatment in MAPKinase activ
2024-04-08

We investigated the role of ABT 702 treatment in MAPKinase activation in mouse microglia in vitro. In Fig. 7D immunocytochemistry results revealed that Iba1 and p-ERK1/2 co-localized in LPS induced mouse microglia. In our previous study we have reported that LPS activates ERK1/2 phosphorylation (Ahm
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