Direct Modulators of K-Ras-Membrane Interactions

ACS Chem Biol. 2023 Sep 15;18(9):2082-2093. doi: 10.1021/acschembio.3c00413. Epub 2023 Aug 14.

Abstract

Protein-membrane interactions (PMIs) are ubiquitous in cellular signaling. Initial steps of signal transduction cascades often rely on transient and dynamic interactions with the inner plasma membrane leaflet to populate and regulate signaling hotspots. Methods to target and modulate these interactions could yield attractive tool compounds and drug candidates. Here, we demonstrate that the conjugation of a medium-chain lipid tail to the covalent K-Ras(G12C) binder MRTX849 at a solvent-exposed site enables such direct modulation of PMIs. The conjugated lipid tail interacts with the tethered membrane and changes the relative membrane orientation and conformation of K-Ras(G12C), as shown by molecular dynamics (MD) simulation-supported NMR studies. In cells, this PMI modulation restricts the lateral mobility of K-Ras(G12C) and disrupts nanoclusters. The described strategy could be broadly applicable to selectively modulate transient PMIs.

Publication types

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

MeSH terms

  • Cell Membrane / metabolism
  • Lipids
  • Molecular Dynamics Simulation
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Signal Transduction*
  • ras Proteins* / metabolism

Substances

  • ras Proteins
  • Lipids
  • Proto-Oncogene Proteins p21(ras)