Abstract
The fluorescence properties of an emissive guanine surrogate, thienoguanine (thGN, 2-aminothieno[3,4-d]pyrimidin-4(3H)-one), were exploited to design two real-time chemosensors of O6-methylguanine-DNA-methyltransferase (MGMT), a key DNA repair enzyme involved in the resistance to DNA-alkylating anti-cancer drugs though direct reversal of O6-alkylated guanine adducts.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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DNA Modification Methylases / metabolism*
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DNA Repair Enzymes / metabolism*
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Drug Design*
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Fluorescent Dyes / chemical synthesis
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Fluorescent Dyes / chemistry
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Fluorescent Dyes / metabolism*
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Guanine / analogs & derivatives
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Guanine / chemistry
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Guanine / metabolism*
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Humans
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Molecular Structure
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Small Molecule Libraries / chemical synthesis
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Small Molecule Libraries / chemistry
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Small Molecule Libraries / metabolism*
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Tumor Suppressor Proteins / metabolism*
Substances
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Fluorescent Dyes
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Small Molecule Libraries
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Tumor Suppressor Proteins
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Guanine
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DNA Modification Methylases
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MGMT protein, human
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DNA Repair Enzymes