CHAPTER 10: Dosing - When less is more

Kurinji Pandiyan, Peter A. Jones, Stephen B. Baylin

Research output: Chapter in Book/Report/Conference proceedingChapter


Epigenetic mechanisms control the expression of both canonical coding genes and non-coding regulatory RNA species. Such mechanisms include DNA methylation changes at predominantly CpG sites in humans, modification of histone tails, packaging of DNA into nucleosomes, and control of nucleosome positioning or nucleosome remodelling. These steps ultimately impact upon gene expression and therefore cell state definition. It has been established that a variety of epigenetic aberrations seen in cancers can complement genetic abnormalities in tumorigenesis and some are almost certainly driving events for malignant potential. Epigenetic abnormalities are potentially reversible with respect to pharmacological intervention for cancer management. In this chapter we will discuss the evolution of epigenetic therapy over the last approximately 40 years, our current understanding of clinically available agents and future approaches towards drug development, regulatory studies and clinical efficacy assessment.

Original languageEnglish (US)
Title of host publicationPrivileged Scaffolds in Medicinal Chemistry
Subtitle of host publicationDesign, Synthesis, Evaluation
EditorsNessa Carey
PublisherRoyal Society of Chemistry
Number of pages18
StatePublished - 2016

Publication series

NameRSC Drug Discovery Series
ISSN (Print)2041-3203
ISSN (Electronic)2041-3211

ASJC Scopus subject areas

  • Drug Discovery


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