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Targeting Ras with Macromolecules

Dehua Pei1, Kuangyu Chen1, Hui Liao1

  • 1Department of Chemistry and Biochemistry, The Ohio State University, Columbus, Ohio 43210.

Cold Spring Harbor Perspectives in Medicine
|August 6, 2017
PubMed

Insights

Activating Ras mutations drive ~30% of cancers, making Ras proteins key anticancer targets. New macromolecular inhibitors, including peptides and antibodies, are being developed to overcome challenges in targeting these difficult proteins.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Activating mutations in Ras proteins are implicated in approximately 30% of human cancers.
  • Ras proteins are challenging drug targets due to their intracellular function and lack of binding pockets for small molecules.

Purpose of the Study:

  • To provide an overview of developing macromolecular inhibitors targeting oncogenic Ras mutants.
  • To explore various modalities for Ras-targeted anticancer drug discovery.

Main Methods:

  • Review of emerging strategies for Ras protein inhibition.
  • Analysis of macromolecular inhibitor classes including peptides, macrocycles, antibodies, non-immunoglobulin proteins, and nucleic acids.

Main Results:

  • Significant research efforts are focused on developing novel therapeutic approaches against Ras.
  • Macromolecular inhibitors offer promising alternatives to conventional small molecules for Ras targeting.

Conclusions:

  • Targeting Ras proteins, particularly oncogenic mutants, remains a critical area in cancer therapy.
  • Diverse macromolecular strategies are being investigated to overcome the inherent challenges of Ras drug discovery.

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