DNA-Targeted Inhibition of MGMT.

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DNA-Targeted Inhibition of MGMT.

Chembiochem. 2017 May 18;18(10):894-898

Authors: Marsoner T, Schmidt OP, Triemer T, Luedtke NW

Abstract
The cationic porphyrin 5,10,15,20-tetrakis (diisopropyl-guanidine)-21H,23H-porphine (DIGPor) selectively binds to DNA containing O(6) -methylguanine (O(6) -MeG) and inhibits the DNA repair enzyme O(6) -methylguanine-DNA methyltransferase (MGMT). The O(6) -MeG selectivity and MGMT inhibitory activity of DIGPor were improved by incorporating Zn(II) 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.

PMID: 28177192 [PubMed - indexed for MEDLINE]

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