Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease

Area of Science:

• Biochemistry
• Molecular Biology
• Epigenetics

Background:

• Protein lysine methylation is a key post-translational modification regulating protein function.
• Dysregulation of lysine methyltransferases (KMTs) is linked to various diseases, including cancer and developmental disorders.
• KMTs are critical enzymes involved in epigenetic regulation and other cellular processes.

Purpose of the Study:

• To highlight advances in developing drugs targeting KMTs.
• To explore KMTs as emerging therapeutic targets beyond chromatin modification.
• To underscore the potential of KMT inhibitors in treating diverse diseases.

Main Methods:

• Review of recent advancements in KMT inhibitor development.
• Analysis of KMTs involved in histone methylation and epigenetic regulation.
• Exploration of KMTs regulating protein synthesis and other biological processes.

Main Results:

• Significant progress has been made in developing KMT inhibitors.
• Tazemetostat, a KMT inhibitor, is approved for specific cancers.
• Multiple KMT inhibitors are in clinical and preclinical development.

Conclusions:

• Targeting KMTs represents a promising therapeutic strategy for various diseases.
• KMTs involved in non-histone protein regulation are emerging as valuable drug targets.
• Continued research into KMT inhibitors holds potential for novel disease treatments.