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At present drugs that specifically inhibit YAP activity are
2024-04-18
At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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Song et al reported series
2024-04-18
Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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Maduramicin is a polyether ionophore antibiotic that has
2024-04-17
Maduramicin is a polyether ionophore antibiotic that has the smallest margin of safety between the maximum authorized dosage and the minimum toxic concentration. Clinical signs of maduramicin intoxication are similar to that of other ionophores, often causing feed refusal, anorexia, respiratory dist
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As an internal control this study validated
2024-04-17
As an internal control, this study validated many of the known associations between GATA3 and predictive markers. GATA3 was shown to be associated with ER and PR, which are both well-known correlations. GATA3 was also negatively correlated with nuclear grade, which is consistent with our knowledge
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br Experimental procedures br Results br Discussion
2024-04-17
Experimental procedures Results Discussion Our biophysical and cellular analyses of mutant Aβ1–42 peptides support a role of the N-terminus of Aβ in peptide aggregation and toxicity. We demonstrate that double mutations constructed to humanize the rodent Aβ1–42 sequence result in a signific
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br Introduction AMP activated protein kinase AMPK
2024-04-17
Introduction AMP-activated protein kinase (AMPK) has been found to be a key character against cardiovascular diseases and cellular stress. When activated by certain stress, AMPK regulates sugars and fatty acids that are good or detrimental to the heart. For example, targeting AMPK phosphorylation
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br Aldehyde sensors to monitor substrate levels
2024-04-17
Aldehyde sensors to monitor substrate levels Previous efforts to ameliorate metabolic diseases frequently relied on biochemical methods which could measure the levels of toxic substrates in Desformylflustrabromine hydrochloride or bodily fluids (blood and serum or plasma, urine, cerebrospinal fl
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br Conclusions The present data suggest that homeostatic bal
2024-04-17
Conclusions The present data suggest that homeostatic balance of the cortical/hippocampal adenosinergic tone is necessary for normal working memory function and any deviation appears to impair performance – either as a consequence of A2AR under-activation when adenosine levels are reduced or due
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An alternative approach to the administration of ADO agonist
2024-04-17
An alternative approach to the administration of ADO agonists is to amplify the actions of endogenous ADO by inhibiting the ADO-metabolizing enzyme, ADO kinase (AK). Inhibition of AK has the net effect of potentiating the local concentration and the effects of ADO in the extracellular compartment. T
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br Introduction Stroke is a devastating condition that cause
2024-04-16
Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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Imatinib is a well known anticancer drug
2024-04-16
Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing gstp1 (K562 cell line
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br Introduction Lipoxygenases LOXs are a heterogeneous
2024-04-16
Introduction Lipoxygenases (LOXs) are a heterogeneous family of enzymes that catalyze the peroxidation of polyunsaturated fatty acids (PUFAs). By oxidizing free PUFAs, they were shown to contribute to the generation of various bioactive lipid mediators. However, LOX-mediated oxidation of PUFAs es
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Rottlerin receptor ATM dependent initiation of radiation ind
2024-04-16
ATM-dependent initiation of radiation-induced G2/M checkpoint arrest is well established [11], [34], [35]. However, the ATR pathway may also be involved [36], [37]. Brown and Baltimore generated Cre/lox-conditional cell lines or Rottlerin receptor with a kinase inactive allele of ATR (ATRkd) to eval
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It is well known that neurosteroids such as
2024-04-16
It is well-known that neurosteroids such as testosterone and their metabolites endogenously modulate neural excitability in animals and humans. Testosterone has protective effects against seizures induced by KA and PTZ (Frye et al., 2001b; Reddy, 2004b). Estrogens, on the other hand, have proconvuls
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Several MAP kinases are involved in the signal transduction
2024-04-16
Several MAP kinases are involved in the signal transduction pathways that lead to the upregulations of inflammatory mediators. Moreover, transcriptional activations of STATs are regulated by MAP kinases, as evidenced by reports that p38 MAPK is necessary for the S727 phosphorylation of STATs (Kovari
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