Dysregulation of protein methyltransferases in human cancer: An emerging target class for anticancer therapy

Area of Science:

• Biochemistry
• Molecular Biology
• Cancer Research

Background:

• Protein methylation is a critical post-translational modification involved in cellular processes and epigenetic regulation.
• Initially thought irreversible, protein methylation is now understood to be dynamically regulated by methyltransferases and demethylases.
• This modification plays a significant role in both histone and non-histone protein regulation, impacting cancer development.

Purpose of the Study:

• To review the biological and physiological significance of protein methylation in human cancer.
• To highlight the role of protein methyltransferases and demethylases in cancer progression.
• To emphasize the potential of targeting these enzymes for novel anticancer therapies.

Main Methods:

• Literature review of studies on protein methylation, methyltransferases, and demethylases.
• Analysis of the role of protein methylation in epigenetic regulation and cancer.
• Examination of current therapeutic strategies targeting protein methylation pathways.

Main Results:

• Protein methylation is integral to epigenetic mechanisms and influences cancer development and progression.
• Dysregulation of protein methylation is frequently observed across various cancer types.
• Small-molecule inhibitors targeting protein methyltransferases and demethylases are under active development for cancer treatment.

Conclusions:

• Protein methylation is a vital regulatory mechanism with profound implications in human cancer.
• Protein methyltransferases represent promising therapeutic targets for developing innovative anticancer drugs.
• Ongoing clinical trials indicate the potential clinical utility of targeting protein methylation in oncology.