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We conducted the largest drug screen to date
2024-01-19
We conducted the largest drug screen to date in HPV-positive cancers and identified Aurora kinase inhibitors as effective and understudied drugs in HNSCC and CESC. These drugs cause apoptosis and cell cycle arrest in vitro and decrease tumor size in vivo. This is the first published study to demonst
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Ryoichi et al modified potent clinical candidate VX with
2024-01-19
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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The tumor suppressor function of LOX in normal prostate
2024-01-19
The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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How does the ATM to ATR switch
2024-01-19
How does the ATM-to-ATR switch occur at DSBs? The progressive attenuation of ATM activation could be attributed to the loss of DNA structures that activate ATM, or to the generation of DNA structures that interfere with ATM activation. Our finding that SSOs do not directly affect the binding of puri
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Neuropathic animals display increased sensitivity to the
2024-01-19
Neuropathic animals display increased sensitivity to the anti-nociceptive effect of baclofen and whilst the number and affinity of GABAB 6-Bnz-cAMP sodium salt mg in the dorsal horn are not altered (Smith et al., 1994; Zemoura et al., 2016), GABAB receptors subunits (B1 and B2) are both down-regula
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Human hepatocyte transplantation resulted in some
2024-01-19
Human hepatocyte transplantation resulted in some animals with relatively sparse repopulation while others had >90% of their liver containing human hepatocytes. The presence of circulating human albumin varied based on the amount of repopulation as the degree of humanization is reported to correlate
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br Materials and methods br Results
2024-01-18
Materials and methods Results and discussion Conclusion Introduction Free radicals produced by normal oxidative metabolism in the human body can cause chain oxidation of food, accelerate food deterioration and cause serious problems of food safety (Choe & Min, 2006). Excess free radicals
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br Acknowledgements br Introduction Microbial enzymes have g
2024-01-18
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 The lipoxygenase pathway and microvascular
2024-01-18
The 12/15-lipoxygenase pathway and microvascular complications of diabetes The 12/15-lipoxygenase pathway in adipose tissue Only recently has adipose tissue been recognized as a highly metabolically active endocrine organ imparting profound local and systemic inflammatory effects. Adipose tiss
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GSK2269557 A unique finding in this study is that
2024-01-18
A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic GSK2269557 for substrate, can regulate CREB phosphoryation in the context of Alzheimer's
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The aldehyde reductase AKR A
2024-01-18
The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.
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Fructose Colorimetric/Fluorometric Assay Kit br There are th
2024-01-18
There are three types of 5-HT2 receptors. 5-HT2A, 5-HT2B and 5-HT2C receptors Exhibit 46–50% overall sequence identity and couple preferentially to Gq/11 to increase inositol phosphates and cytosolic [Ca2+] and in agreement with their long known role in muscle contraction and stimulation in the br
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Metabolism Compound Library While A Rs communicate mainly wi
2024-01-18
While A1Rs communicate mainly with the D1R subtype [36], A2AR and D2R interaction occurs mainly in basal ganglia. D2Rs colocalizes with A2ARs in this Metabolism Compound Library area where they are preferentially localized postsynaptically in the soma and dendrites of GABAergic striatopallidal neur
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br Acknowledgments The authors would like to thank
2024-01-18
Acknowledgments The authors would like to thank Ms. Ashley Davis for her administrative assistance in preparing this article and Mr. Dan Beck for his artistic contributions to Fig. 1. Introduction Acetylcholine is the most abundant neurotransmitter in the central nervous system (CNS) of insec
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Matthew et al synthesized and carried out SAR
2024-01-17
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that IL-18, human recombinant protein sale 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphor
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