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The Endeavours in RAS Inhibition - the Past, Present, and Future

Javeena Hussain1, Sivapriya Kirubakaran1, Srimadhavi Ravi1

  • 1Discipline of Chemistry, Indian Institute of Technology Gandhinagar, Palaj Campus, Gandhinagar, Gujarat - 382355, India.

Current Topics in Medicinal Chemistry
|September 5, 2020
PubMed

Insights

Targeting KRAS mutations, a key driver in many cancers, is a major focus in drug discovery. Novel inhibitors targeting RAS proteins show promise for future clinical trials in cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • KRAS mutations are prevalent gain-of-function alterations in human cancers.
  • RAS proteins, small GTPases, regulate critical cellular functions and are implicated in cancer pathogenesis.
  • Targeting mutant RAS is a significant challenge and a foremost goal in cancer research.

Purpose of the Study:

  • To review the role of RAS in cancer drug discovery.
  • To describe methodologies for developing direct and indirect RAS inhibitors.
  • To highlight recent accomplishments in novel RAS inhibitor development.

Main Methods:

  • Review of existing literature on RAS biology and cancer drug discovery.
  • Analysis of diverse strategies for developing RAS inhibitors.
  • Focus on targeting specific RAS attributes: membrane localization, active form, downstream binding, and nucleotide exchange.

Main Results:

  • Significant progress has been made in discovering RAS inhibitors.
  • Several approaches targeting different RAS attributes are under investigation.
  • Emerging RAS inhibitors are nearing clinical trials, indicating a potential breakthrough.

Conclusions:

  • RAS proteins are critical targets for cancer therapy.
  • Advancements in understanding RAS biology have enabled the development of novel inhibitors.
  • The development of RAS inhibitors represents a promising new avenue for cancer treatment.
Keywords:
CancerGTP-binding proteinInhibitorRAS mutationSmall GTPaseSmall molecule

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