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br Alzheimer s disease AD
2024-06-07
Alzheimer’s disease (AD) is an irreversible, age-associated neurodegenerative disorder that is characterized by progressive memory loss and cognitive decline. AD is also the leading cause of dementia, accounting for 5 million cases in the United States and 44 million cases worldwide. In 2015, AD c
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Epidermal growth factor EGF has been shown to increase
2024-06-07
Epidermal growth factor (EGF) has been shown to increase the 12S-lipoxygenase mRNA level by about two-fold in human epidermoid carcinoma A431 cells [71]. This enzyme was shown to be of the platelet-type and associated with the microsomal fraction of the cells [71], [72]. A requirement for EGF recept
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The diversity of metabolic adaptations employed by
2024-06-07
The diversity of metabolic adaptations employed by cancer cells in response to rapidly changing conditions, contributes to their biological aggressiveness and therapeutic resistance by enabling them to proliferate when nutrients are plentiful and to shift their resources to survival when nutrients a
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br Introduction Alzheimer s disease AD is a
2024-06-07
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 vegfr areas, resulting in cognitive impairment and behavioral changes (O'Neill, 2013, De Strooper and Karran, 2016, Alzh
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Activation of AhR is also known to upregulate the expression
2024-06-07
Activation of AhR is also known to upregulate the expression of AhRR (AhR repressor), an inhibitor protein of AhR [29]. However, the exact mechanism by which AhRR represses AhR signaling is not well understood. The initial study by Mimura and colleagues suggested that AhRR is capable of directly com
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Aberrant or a sustained activation of AhR signaling pathway
2024-06-07
Aberrant or a sustained activation of AhR signaling pathway, triggered by exogenous toxic ligands such as dioxins, PAHs or polychlorinated biphenyls (PCBs), is a well-described biological process engaged during tumor initiation and/or promotion in various tissues (e.g. liver, lung, skin)(reviewed i
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A high throughput small molecule ACK biochemical inhibition
2024-06-07
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found 4-Methylhistamine dihydrochloride to be both ATP-competitive and reversible. Early structure-activity relati
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In conclusion two novel series of
2024-06-07
In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas
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A similar circuit between pyramidal neurons
2024-06-07
A similar circuit between pyramidal neurons and SST interneurons is also prevalent in layers 2/3 of the cortex. The synapses onto SST interneurons, however, are functionally weak, raising questions about their computational power. In the first set of experiments, Urban-Ciecko et al. (2018) show that
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prostaglandin agonist synthesis Having taken a step back fro
2024-06-07
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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Various cardiovascular diseases show a high occurrence
2024-06-07
Various cardiovascular diseases show a high occurrence of autophagosomes. Whereas basal autophagy is required for the proper functioning of cardiomyocytes [82], the deletion of Atg5 gene in myocardium shows a high risk of cardiomyopathy [83]. Hamacher et al. observed that an upregulation of Bnip3, a
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IC values were obtained for an expanded version of the
2024-06-07
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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Treatment of all of the GYN cancer cells in
2024-06-07
Treatment of all of the GYN cancer INCB-024360 receptor in this study with ATRi not only reduced phosphorylation of Chk1 at Ser345 following genotoxic stress, but also phosphorylation of ATM. Loss of phospho-ATM following ATRi treatment is not likely due to non-specific targeting of ATM by ETP-4646
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Autophagy and apoptosis have a very complex relationship and
2024-06-07
Autophagy and apoptosis have a very complex relationship, and the precise mechanism remains to be determined. At present, a large amount of research has confirmed that autophagy can protect the cell from apoptosis in special conditions such as nutrient deficiency or growth factors deprivation; the e
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The radiographic correlate will be
2024-06-06
The radiographic correlate will be similarly important for the success of other non-VEGF TKIs, such as those targeting the epidermal growth factor receptor expressed in 50% of high-grade primary AP26113 neoplasms. It has been reported that icotinib and gefitinib, epidermal growth factor receptor–TK
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