RAS Function in cancer cells: translating membrane biology and biochemistry into new therapeutics

Biochem J. 2020 Aug 14;477(15):2893-2919. doi: 10.1042/BCJ20190839.

Abstract

The three human RAS proteins are mutated and constitutively activated in ∼20% of cancers leading to cell growth and proliferation. For the past three decades, many attempts have been made to inhibit these proteins with little success. Recently; however, multiple methods have emerged to inhibit KRAS, the most prevalently mutated isoform. These methods and the underlying biology will be discussed in this review with a special focus on KRAS-plasma membrane interactions.

Keywords: RAS; cancer; phospholipids; plasma membrane; small molecule inhibitors; therapeutics.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Cell Membrane / metabolism*
  • Humans
  • Molecular Targeted Therapy
  • Mutation
  • Neoplasms / genetics*
  • Neoplasms / metabolism
  • Protein Isoforms
  • Protein Processing, Post-Translational
  • Proto-Oncogene Proteins p21(ras) / antagonists & inhibitors
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Proto-Oncogene Proteins p21(ras) / metabolism
  • ras Proteins / chemistry
  • ras Proteins / genetics
  • ras Proteins / metabolism*

Substances

  • Antineoplastic Agents
  • KRAS protein, human
  • Protein Isoforms
  • Proto-Oncogene Proteins p21(ras)
  • ras Proteins