Insights for the design of protein lysine methyltransferase G9a inhibitors

Mariasoosai Ramya Chandar Charles, Arunkumar Dhayalan, Hsing Pang Hsieh, Mohane Selvaraj Coumar

Research output: Contribution to journalReview articlepeer-review

23 Citations (Scopus)


The epigenetic control of gene expression could be affected by addition and/or removal of post-translational modifications such as phosphorylation, acetylation and methylation of histone proteins, as well as methylation of DNA (5-methylation on cytosines). Misregulation of these modifications is associated with altered gene expression, resulting in various disease conditions. G9a belongs to the protein lysine methyltransferases that specifically methylates the K9 residue of histone H3, leading to suppression of several tumor suppressor genes. In this review, G9a functions, role in various diseases, structural biology aspects for inhibitor design, structure-activity relationship among the reported inhibitors are discussed which could aid in the design and development of potent G9a inhibitors for cancer treatment in the future.

Original languageEnglish
Pages (from-to)993-1014
Number of pages22
JournalFuture Medicinal Chemistry
Issue number9
Publication statusPublished - 2019

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery


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