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Targeting WEE1 Kinase in Cancer.
Formation of 17-allylamino-demethoxygeldanamycin (17-AAG) hydroquinone by NAD(P)H:quinone oxidoreductase 1: role of 17-AAG hydroquinone in heat shock protein 90 inhibition.
TLDR
Low-performance liquid chromatography analysis of the metabolism of 17-AAG by recombinant human NQO1 revealed the formation of a more polar metabolite17-AAGH2, a relatively stable hydroquinone that exhibits superior Hsp90 inhibition.
Modification of Akt2 by 4-hydroxynonenal inhibits insulin-dependent Akt signaling in HepG2 cells.
TLDR
The inhibition of Akt by 4-HNE provides a novel mechanism for increased insulin resistance in ALD and provides a potential mechanism of dysregulation ofAkt2 during events associated with sustained hepatocellular oxidative stress.
Strategies and Approaches of Targeting STAT3 for Cancer Treatment.
TLDR
This review summarizes the development of STAT3 inhibitors organized by the approach used to inhibit STAT3, the current inhibitors of each class, and the assay systems used to evaluate STAT3 inhibition and offers an insight into future approaches for small molecule STAT3 inhibitor development.
Acrolein Inhibits Cytokine Gene Expression by Alkylating Cysteine and Arginine Residues in the NF-κB1 DNA Binding Domain*
TLDR
Aldehydes in cigarette smoke can regulate gene expression by direct modification of a transcription factor by blocking DNA binding to an NF-κB consensus sequence.
Enzymatic Reduction and Glutathione Conjugation of Benzoquinone Ansamycin Heat Shock Protein 90 Inhibitors: Relevance for Toxicity and Mechanism of Action
Two-electron reduction of benzoquinone ansamycin (BA) heat shock protein (Hsp) 90 inhibitors by NAD(P)H:quinone oxidoreductase 1 (NQO1) to hydroquinone ansamycins (BAH2s) leads to greater Hsp90
The Bioreduction of a Series of Benzoquinone Ansamycins by NAD(P)H:Quinone Oxidoreductase 1 to More Potent Heat Shock Protein 90 Inhibitors, the Hydroquinone Ansamycins
TLDR
An extensive study with a series of benzoquinone ansamycins, which includes gel-danamycin, 17-(amino)-17-demethoxygeldanamycin), shows that the reduction of this series by NQO1 generates the corresponding hydroquinones, which exhibit enhanced Hsp90 inhibition.
The role of glutathione in brain tumor drug resistance.
Manganese superoxide dismutase regulates a metabolic switch during the mammalian cell cycle.
TLDR
Results support the hypothesis that manganese superoxide dismutase regulates a "metabolic switch" during progression from quiescent through the proliferative cycle and propose MnSOD as a new molecular player contributing to the Warburg effect.
Inhibition of Wee1 Sensitizes Cancer Cells to Antimetabolite Chemotherapeutics In Vitro and In Vivo, Independent of p53 Functionality
TLDR
Inhibition of Wee1 sensitizes hematologic and solid tumor cell lines to antimetabolite chemotherapeutics, whether p53 is functional or not, suggesting that the use of p53 mutation as a predictive biomarker for response to Wee1 inhibition may be restricted to certain cancers and/or chemotherAPEutics.
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