Recent advances in developing degraders & inhibitors of lysine methyltransferases

Julia Velez, H. Ümit Kaniskan, Jian Jin

Research output: Contribution to journalReview articlepeer-review

2 Scopus citations

Abstract

Over the last several decades, there has been continued interest in developing novel therapeutic approaches targeting protein lysine methyltransferases (PKMTs). Along with PKMT inhibitors, targeted protein degradation (TPD) has emerged as a promising strategy to attenuate aberrant PKMT activity. Particularly, proteolysis targeting chimeras (PROTACs) effectively eliminate PKMTs of interest, suppressing all enzymatic and non-enzymatic functions. PROTACs and other TPD approaches add new depth to PKMT research and novel therapeutics discovery. This review focuses on recent advances in PKMT degrader and inhibitor development over the last several years.

Original languageEnglish
Article number102356
JournalCurrent Opinion in Chemical Biology
Volume76
DOIs
StatePublished - Oct 2023

Keywords

  • Degraders
  • Inhibitors
  • Lysine Methyltransferases
  • PROTACs

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