RAS G12C Inhibitors: Three Birds with One Stone

Cancer Discov. 2024 May 1;14(5):698-700. doi: 10.1158/2159-8290.CD-24-0175.

Abstract

In this issue, Rubinson, Tanaka, and colleagues demonstrate that differences among G12C inhibitors rely on their ability to covalently bind not only G12C mutant KRAS but also NRAS and HRAS, proposing sotorasib as a potent NRAS G12C inhibitor. See related article by Rubinson et al., p. 727 (6).

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • GTP Phosphohydrolases / genetics
  • Humans
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / genetics
  • Mutation
  • Piperazines*
  • Proto-Oncogene Proteins p21(ras)* / antagonists & inhibitors
  • Proto-Oncogene Proteins p21(ras)* / genetics
  • Pyridines*
  • Pyrimidines*

Substances

  • Proto-Oncogene Proteins p21(ras)
  • Membrane Proteins
  • KRAS protein, human
  • GTP Phosphohydrolases
  • sotorasib
  • NRAS protein, human
  • Antineoplastic Agents
  • Piperazines
  • Pyridines
  • Pyrimidines