Targeting protein lysine methylation and demethylation in cancers

Area of Science:

• Biochemistry
• Molecular Biology
• Oncology

Background:

• Recent research highlights the critical role of lysine methylation/demethylation in regulating protein function.
• These post-translational modifications, catalyzed by protein lysine methyltransferases (PKMTs) and protein lysine demethylases (PKDMs), affect key proteins like p53, NF-kappaB, and E2F1.
• Aberrant regulation of these methylation processes is increasingly linked to tumorigenesis.

Purpose of the Study:

• To review recent advancements in understanding the function of protein lysine methylation.
• To summarize the discovery of small molecule inhibitors targeting PKMTs and PKDMs.
• To discuss the therapeutic potential and challenges of targeting protein lysine methylation in cancer treatment.

Main Methods:

• Literature review of studies on protein lysine methylation and demethylation.
• Analysis of the roles of PKMTs, PKDMs, and their substrates in cancer.
• Examination of small molecule inhibitors developed against PKMTs and PKDMs.

Main Results:

• Protein lysine methylation/demethylation are vital 'Ying-Yang' modifications fine-tuning protein activity.
• PKMTs, PKDMs, and their substrates are implicated in various cancers.
• Growing evidence connects dysregulated methylation to cancer development.

Conclusions:

• Targeting protein lysine methylation pathways offers potential for novel cancer therapies.
• Further research is needed to fully elucidate the mechanisms and overcome challenges in developing effective inhibitors.
• Understanding these modifications is key to advancing cancer treatment strategies.