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Zhang et al screened three thousand compounds library and
2023-06-13

Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeffe
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Curcumol br HIF Blockade in AA Therapy In
2023-06-07

HIF-α Blockade in AA Therapy In lieu of the evidence supporting a central role for HIF-α signaling in tumor angiogenesis and CC pathobiology, significant efforts have focused on the discovery of small-molecule HIF-α inhibitors (for exhaustive compendia, see [28,44,45]). In brief, inhibitors vary
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We designed SSOs that block APP exon splicing and induce
2023-06-06

We designed SSOs that block APP exon 17 splicing and induce the production of an alternatively spliced APP mRNA lacking exon 17 (APPΔex17). APPΔex17 mRNA encodes an APP protein isoform that lacks 49 Gastrodin receptor including the γ-secretase cleavage sites that give rise to the toxic, AD-associat
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The enzyme mediated ATP sensing mechanism in zebrafish
2023-06-01

The enzyme-mediated ATP-sensing mechanism in zebrafish can be compared with previous studies in other animal species reporting that enzymatic conversion of chemicals in the peripheral olfactory organ results in either “activation” or “inactivation” of odorants and pheromones. In male silkmoth, the a
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The enzyme mediated ATP sensing mechanism in zebrafish
2023-06-01

The enzyme-mediated ATP-sensing mechanism in zebrafish can be compared with previous studies in other animal species reporting that enzymatic conversion of chemicals in the peripheral olfactory organ results in either “activation” or “inactivation” of odorants and pheromones. In male silkmoth, the a
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br Perspectives and challenges Previously the main focus of
2023-06-01

Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascula
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br Conflict of interest br Financial support
2023-05-31

Conflict of interest Financial support Acknowledgments This work was supported by the Japanese Millennium project. We thank all members of the Center for Genomic Medicine of RIKEN and Dainippon-Sumitomo Pharma Co., Ltd. for supporting this study. We are also grateful to members of the Hiros
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Direct inhibition of LO activity by BRP is
2023-05-30

Direct inhibition of 5-LO activity by BRP-187 is clearly evident in cell-free assays using PMNL homogenates and isolated human recombinant 5-LO as enzyme source. In such assays, pure FLAP inhibitors like MK886 are inactive [9], [10], [29], [44]. Wash-out experiments and studies using the nonionic de
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In earlier experiments on snails a
2023-05-30

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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In the pituitary of R quelen
2023-05-30

In the pituitary of R. quelen mRNA levels of cyp19a1b were found to be higher in males than females, suggesting a sex-specific function, and perhaps a local action to regulate gonadotropins or other pituitary hormone secretion (Olivereau and Callard, 1985; Zhang et al., 2014). Interestingly, the hig
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Another interesting aspect of neutralizing AP
2023-05-29

Another interesting aspect of neutralizing AP-1 is the inhibition of interactions between AP-1 and Smad proteins, which synergize to activate the TGF-β1-responsive genes involved in hypertrophic growth of the heart muscle and in the development of cardiac fibrosis. Through preventing AP-1 activation
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Since primitive societies plants herbs and seeds rich in phy
2023-05-29

Since primitive societies, plants, herbs and seeds, rich in phytochemicals, were used due to their benefits in human health. These molecules were shown to present a diverse array of action mechanisms, including antioxidant activity, enzyme stimulation, hormones mimicking and by interfering with DNA
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br Experimental section br Acknowledgements This work was fu
2023-05-29

Experimental section Acknowledgements This work was funded by the Italian Association for Cancer Research (AIRC IG18590 to A.A.), by “Fondi di Ateneo-University of Pisa” years 2009 and 2010 (E. N., S. N., E. O., and A. R.) and partially by the Unipi project P.R.A.2016_27 (E. N., E.O. and A. R.
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br Pathophysiology of Alzheimer disease Alzheimer disease is
2023-05-29

Pathophysiology of Alzheimer disease Alzheimer disease is characterized by severe neurodegeneration, neuroinflammation, and progressive loss of cognitive abilities. The diagnostic criteria for dementia released by the National Institute on Aging-Alzheimer's Association define dementia as the deve
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SCH 39166 hydrobromide In earlier experiments on snails a be
2023-05-29

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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