Issue 9, 2022

Harnessing an emissive guanine surrogate to design small-molecule fluorescent chemosensors of O6-methylguanine-DNA-methyltransferase (MGMT)

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.

Graphical abstract: Harnessing an emissive guanine surrogate to design small-molecule fluorescent chemosensors of O6-methylguanine-DNA-methyltransferase (MGMT)

Associated articles

Supplementary files

Article information

Article type
Communication
Submitted
31 1 2022
Accepted
09 2 2022
First published
11 2 2022

Org. Biomol. Chem., 2022,20, 1888-1892

Harnessing an emissive guanine surrogate to design small-molecule fluorescent chemosensors of O6-methylguanine-DNA-methyltransferase (MGMT)

A. Fillion, J. Franco Pinto and A. Granzhan, Org. Biomol. Chem., 2022, 20, 1888 DOI: 10.1039/D2OB00208F

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