Determining the ERK-regulated phosphoproteome driving KRAS-mutant cancer

Science. 2024 Jun 7;384(6700):eadk0850. doi: 10.1126/science.adk0850. Epub 2024 Jun 7.

Abstract

To delineate the mechanisms by which the ERK1 and ERK2 mitogen-activated protein kinases support mutant KRAS-driven cancer growth, we determined the ERK-dependent phosphoproteome in KRAS-mutant pancreatic cancer. We determined that ERK1 and ERK2 share near-identical signaling and transforming outputs and that the KRAS-regulated phosphoproteome is driven nearly completely by ERK. We identified 4666 ERK-dependent phosphosites on 2123 proteins, of which 79 and 66%, respectively, were not previously associated with ERK, substantially expanding the depth and breadth of ERK-dependent phosphorylation events and revealing a considerably more complex function for ERK in cancer. We established that ERK controls a highly dynamic and complex phosphoproteome that converges on cyclin-dependent kinase regulation and RAS homolog guanosine triphosphatase function (RHO GTPase). Our findings establish the most comprehensive molecular portrait and mechanisms by which ERK drives KRAS-dependent pancreatic cancer growth.

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cyclin-Dependent Kinases / genetics
  • Cyclin-Dependent Kinases / metabolism
  • HEK293 Cells
  • Humans
  • MAP Kinase Signaling System
  • Mice
  • Mitogen-Activated Protein Kinase 1* / metabolism
  • Mitogen-Activated Protein Kinase 3* / metabolism
  • Mutation
  • Pancreatic Neoplasms* / genetics
  • Pancreatic Neoplasms* / metabolism
  • Phosphoproteins* / genetics
  • Phosphoproteins* / metabolism
  • Phosphorylation
  • Proteome*
  • Proto-Oncogene Proteins p21(ras)* / genetics
  • Proto-Oncogene Proteins p21(ras)* / metabolism

Substances

  • Cyclin-Dependent Kinases
  • KRAS protein, human
  • MAPK1 protein, human
  • MAPK3 protein, human
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3
  • Phosphoproteins
  • Proteome
  • Proto-Oncogene Proteins p21(ras)