The cationic porphyrin 5,10,15,20-tetrakis (diisopropyl-guanidine)-21H,23H-porphine (DIGPor) selectively binds to DNA containing O -methylguanine (O -MeG) and inhibits the DNA repair enzyme O -methylguanine-DNA methyltransferase (MGMT). The O -MeG selectivity and MGMT inhibitory activity of DIGPor were improved by incorporating Zn 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.
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| http://dx.doi.org/10.1002/cbic.201600652 | DOI Listing |
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