Methyltransferase Inhibitors: Competing with, or Exploiting the Bound Cofactor

@article{Freitas2019MethyltransferaseIC,
  title={Methyltransferase Inhibitors: Competing with, or Exploiting the Bound Cofactor},
  author={Renato Ferreira de Freitas and Danton Ivanochko and Matthieu Schapira},
  journal={Molecules},
  year={2019},
  volume={24}
}
Protein methyltransferases (PMTs) are enzymes involved in epigenetic mechanisms, DNA repair, and other cellular machineries critical to cellular identity and function, and are an important target class in chemical biology and drug discovery. Central to the enzymatic reaction is the transfer of a methyl group from the cofactor S-adenosylmethionine (SAM) to a substrate protein. Here we review how the essentiality of SAM for catalysis is exploited by chemical inhibitors. Occupying the cofactor… CONTINUE READING

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