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Compounds were profiled for their inhibitory activity agains
2023-08-17
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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The first rationally designed dual mPGES LO
2023-08-17
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic dibromide - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesi
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In earlier experiments on snails
2023-08-17
In earlier experiments on snails, a behavioral model was employed of certain food rejection to study the mechanisms of the reconsolidation of long-term associative memory. It was found that conditioned food stimuli (reminder) presentation, combined with injections of NMDA glutamate receptor antagoni
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Stroke also known as a cerebrovascular accident
2023-08-17
Stroke, also known as a cerebrovascular accident or Oxytocin attack, is one of the leading causes of death and disability worldwide (Haley et al., 2017; Hankey, 2017; Lie et al., 2017). According to the data released by the World Health Organization (WHO), stroke occurs every 5 s worldwide (WHO, 20
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Recent studies have indicated that
2023-08-17
Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ 5'-Iodoresiniferatoxin have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the p
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In Rainey et al published the
2023-08-17
In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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br Results Of the U S jurisdictions surveyed
2023-08-17
Results Of the 51 U.S. jurisdictions surveyed (Table 1), 33 reported that hyperargininemia is one of the conditions for which all newborns are required to be screened, with the earliest screening reported in Massachusetts in 1999. Of the 18 other jurisdictions, an additional 5 reported that hyper
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br Model Fig demonstrates the block scheme
2023-08-16
Model Fig. 1 demonstrates the block-scheme of main interactions between variables of the model under investigation. These interactions are described below in details and are expressed in mathematical form as well, where all variables are the functions of space and time coordinates, r and t, which
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Our observation that squalestatin caused
2023-08-16
Our observation that squalestatin caused only small differences in the production of Aβ40 and Aβ42 was in contrast to prior reports of the effects of other cholesterol synthesis inhibitors. This may be due to using squalestatin, a more specific cholesterol synthesis inhibitor that does not affect is
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In this study high concentrations mM of thuringiensin
2023-08-16
In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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To date more than different mutations
2023-08-16
To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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In this scenario the receptor tyrosine kinase inhibitors TKI
2023-08-16
In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; PPNU 37883 hy
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Over the past decade extensive research has been directed to
2023-08-16
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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br Disclaimer Statement br Acknowledgments br
2023-08-16
Disclaimer Statement Acknowledgments Introduction Metabolic changes are a common feature of cancerous tissues. Mutations in oncogenes and tumor suppressor genes cause alterations to multiple intracellular signaling pathways that rewire tumor cell metabolism and re-engineer it to allow enhan
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Human lipoxygenase exists in two
2023-08-16
Human 15-lipoxygenase exists in two forms, named 15-LOX-1 (also named 12/15-LOX, 15-LO-1) and 15-LOX-2. Several reports indicate that 15-LOX-1 has a pathophysiological role in respiratory inflammatory diseases, in particular asthma. Increased activity of 15-LOX-1 is displayed in the respiratory trac
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