Targeting the cancer epigenome for therapy

PA Jones, JPJ Issa, S Baylin - Nature Reviews Genetics, 2016 - nature.com
Nature Reviews Genetics, 2016nature.com
Next-generation sequencing has revealed that more than 50% of human cancers harbour
mutations in enzymes that are involved in chromatin organization. Tumour cells not only are
activated by genetic and epigenetic alterations, but also routinely use epigenetic processes
to ensure their escape from chemotherapy and host immune surveillance. Hence, a growing
emphasis of recent drug discovery efforts has been on targeting the epigenome, including
DNA methylation and histone modifications, with several new drugs being tested and some …
Abstract
Next-generation sequencing has revealed that more than 50% of human cancers harbour mutations in enzymes that are involved in chromatin organization. Tumour cells not only are activated by genetic and epigenetic alterations, but also routinely use epigenetic processes to ensure their escape from chemotherapy and host immune surveillance. Hence, a growing emphasis of recent drug discovery efforts has been on targeting the epigenome, including DNA methylation and histone modifications, with several new drugs being tested and some already approved by the US Food and Drug Administration (FDA). The future will see the increasing success of combining epigenetic drugs with other therapies. As epigenetic drugs target the epigenome as a whole, these true 'genomic medicines' lessen the need for precision approaches to individualized therapies.
nature.com