EZH2, a histone methyltransferase, has been associated with various kinds of cancers. Specifically, mutations and and/or overactivity of EZH2 are found in a range of cancers, such as lymphomas, leukemias and breast cancer. There is an ongoing need for new agents as EZH2 inhibitors for use in anticancer treatment.
EZH2 inhibition has been described as being effective in mesothelioma cells with BAP1 loss [LaFave et al., 2015, Nat Med 21: 1344-1349]. while a subgroup of mesothelioma cells with BAP1 loss may be sensitive to FGFR inhibition [Quispel-Janssen et al., 2018. Clin Cancer Res 24: 84-94].
kinds of building blocks for EZH2 targets as below:
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