The G protein signaling regulator RGS3 enhances the GTPase activity of KRAS

Science. 2021 Oct 8;374(6564):197-201. doi: 10.1126/science.abf1730. Epub 2021 Oct 7.

Abstract

Recently reported to be effective in patients with lung cancer, KRASG12C inhibitors bind to the inactive, or guanosine diphosphate (GDP)–bound, state of the oncoprotein and require guanosine triphosphate (GTP) hydrolysis for inhibition. However, KRAS mutations prevent the catalytic arginine of GTPase-activating proteins (GAPs) from enhancing an otherwise slow hydrolysis rate. If KRAS mutants are indeed insensitive to GAPs, it is unclear how KRASG12C hydrolyzes sufficient GTP to allow inactive state–selective inhibition. Here, we show that RGS3, a GAP previously known for regulating G protein–coupled receptors, can also enhance the GTPase activity of mutant and wild-type KRAS proteins. Our study reveals an unexpected mechanism that inactivates KRAS and explains the vulnerability to emerging clinically effective therapeutics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Extracts
  • Cell Line, Tumor
  • Enzyme Activation
  • GTP Phosphohydrolases / metabolism*
  • Guanosine Triphosphate / metabolism*
  • Humans
  • Hydrolysis
  • Lung Neoplasms / drug therapy
  • Lung Neoplasms / enzymology*
  • Lung Neoplasms / genetics
  • Mice
  • Mice, Nude
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Proto-Oncogene Proteins p21(ras) / metabolism*
  • RGS Proteins / genetics
  • RGS Proteins / metabolism*
  • Signal Transduction
  • Xenograft Model Antitumor Assays

Substances

  • Cell Extracts
  • KRAS protein, human
  • RGS Proteins
  • RGS3 protein, human
  • Guanosine Triphosphate
  • GTP Phosphohydrolases
  • Proto-Oncogene Proteins p21(ras)