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Post-translational modification of KRAS: potential targets for cancer therapy

Wei-Hua Wang1, Tao Yuan1, Mei-Jia Qian1

  • 1Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.

Acta Pharmacologica Sinica
|October 22, 2020
PubMed

Insights

Aberrant activation of the KRAS (Kirsten rat sarcoma) oncoprotein, a key factor in cancer, is regulated by various post-translational modifications. Targeting these modifications shows promise for potent anti-tumor activities.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Aberrant activation of the RAS superfamily, particularly KRAS mutations, is a critical driver of carcinogenesis.
  • KRAS is the most frequently mutated oncogene, making it a significant target for cancer intervention strategies.
  • While KRAS function is extensively studied, its regulation by post-translational modifications is an evolving area of research.

Purpose of the Study:

  • To review the regulatory roles of diverse post-translational modifications on KRAS activation and localization.
  • To highlight recent therapeutic strategies targeting these KRAS modifications for cancer treatment.

Main Methods:

  • Literature review of studies on KRAS post-translational modifications.
  • Analysis of recent research on targeting these modifications for anti-tumor effects.

Main Results:

  • Post-translational modifications including prenylation, palmitoylation, ubiquitination, phosphorylation, SUMOylation, acetylation, and nitrosylation significantly regulate KRAS activity.
  • Targeting these specific KRAS modifications has demonstrated potent anti-tumor activities in preclinical studies.

Conclusions:

  • Post-translational modifications are crucial regulators of KRAS aberrant activation in cancer.
  • Developing therapeutic interventions that target KRAS post-translational modifications offers a promising avenue for effective cancer treatment.
Keywords:
KRASSUMOylationacetylationcancer therapynitrosylationoncogenepalmitoylationphosphorylationpost-translational modificationpostprenylationprenylationubiquitination

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