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. 2017 May 18;18(10):894-898.
doi: 10.1002/cbic.201600652. Epub 2017 Apr 7.

DNA-Targeted Inhibition of MGMT

Theodor Marsoner  1 , Olivia P Schmidt  1 , Therese Triemer  1 , Nathan W Luedtke  1
Affiliations

DNA-Targeted Inhibition of MGMT

Theodor Marsoner et al. Chembiochem. .

Abstract

The cationic porphyrin 5,10,15,20-tetrakis (diisopropyl-guanidine)-21H,23H-porphine (DIGPor) selectively binds to DNA containing O6 -methylguanine (O6 -MeG) and inhibits the DNA repair enzyme O6 -methylguanine-DNA methyltransferase (MGMT). The O6 -MeG selectivity and MGMT inhibitory activity of DIGPor were improved by incorporating ZnII into the porphyrin. The resulting metal complex (Zn-DIGPor) potentiated the activity of the DNA-alkylating drug temozolomide in an MGMT-expressing cell line. To the best of our knowledge, this is the first example of DNA-targeted MGMT inhibition.

Keywords: MGMT; O6-methyl- guanine; drug discovery; inhibitors; porphyrin; temozolomide.

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