Background Although the role of epigenetic abnormalities has been studied for several
years in cancer genesis and development, epigenetic-targeting drugs have historically failed
to demonstrate efficacy in solid malignancies. However, successful targeting of chromatin
remodeling deficiencies, histone writers and histone reader alterations has been achieved
very recently using biomarker-driven and mechanism-based approaches. Epigenetic
targeting is now one of the most active areas in drug development and could represent …

Recurrent chromosomal rearrangements leading to the generation of oncogenic fusion
proteins are a common feature of many cancers. These aberrations are particularly
prevalent in sarcomas and haematopoietic malignancies and frequently involve genes
required for chromatin regulation and transcriptional control. In many cases, these fusion
proteins are thought to be the primary driver of cancer development, altering chromatin
dynamics to initiate oncogenic gene expression programmes. In recent years, mechanistic …