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Thiols add across to the multiple bond of unsaturated compounds, either under catalysis by light or acid or, in the case of unsaturated compounds activated by adjacent carbonyl groups, under catalysis by base.
Thus, this suggests that some of the target compounds activated by NQO1 are novel prodrug candidates potential for selective anticancer therapy.
This "communication" between hepatocytes and LSECs is very specific for vinyl chloride and not observed for many other genotoxic compounds activated by hepatocytes (Cohen et al. 2009).
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Catechol and trihydroxybenzene (activated by CYP2E1) induced micronuclei most strongly at 6 h/18 h, whereas somewhat longer exposures were optimal for hydroquinone, another compound activated by CYP2E1.
Some of these compounds activated a p53 response by increasing p73 expression, and knockdown of p73 with siRNA reduced their ability to activate p53 reporter activity while other compounds acted in a p73-independent fashion [ 35].
Such compounds are activated by the enzyme to the corresponding radicals.
Photodynamic therapy, in which systemically administered photosensitive compounds are activated by an external light source, can be considered a related strategy to drug delivery and is under investigation for the treatment of superficial breast tumors.
The strong activating effect of compounds 991 and A769662 and the inhibitory effects of mutating an αC-binding residue from the C-interacting helix therefore suggests that these compounds activate AMPK by stabilizing a selective αC position.
The choice of tumour types and relevant patient population selection would be the key in the evaluation of the success of these compounds activating WT p53 by controlling its degradation and stability.
In those studies, nine of the 25 Tas2R bitter taste receptors were activated by quinine, while many other bitter compounds activate only one or a small number of receptors.
These compounds are generally activated by reduction in hypoxic conditions and work in a similar way to oxygen by causing DNA double strand breaks in the presence of irradiation as a result of the fixation of free radical damage (Katz et al. [2009]).
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com