O-GlcNAcase targets pyruvate kinase M2 to regulate tumor growth

Oncogene. 2020 Jan;39(3):560-573. doi: 10.1038/s41388-019-0975-3. Epub 2019 Sep 9.

Abstract

Cancer cells are known to adopt aerobic glycolysis in order to fuel tumor growth, but the molecular basis of this metabolic shift remains largely undefined. O-GlcNAcase (OGA) is an enzyme harboring O-linked β-N-acetylglucosamine (O-GlcNAc) hydrolase and cryptic lysine acetyltransferase activities. Here, we report that OGA is upregulated in a wide range of human cancers and drives aerobic glycolysis and tumor growth by inhibiting pyruvate kinase M2 (PKM2). PKM2 is dynamically O-GlcNAcylated in response to changes in glucose availability. Under high glucose conditions, PKM2 is a target of OGA-associated acetyltransferase activity, which facilitates O-GlcNAcylation of PKM2 by O-GlcNAc transferase (OGT). O-GlcNAcylation inhibits PKM2 catalytic activity and thereby promotes aerobic glycolysis and tumor growth. These studies define a causative role for OGA in tumor progression and reveal PKM2 O-GlcNAcylation as a metabolic rheostat that mediates exquisite control of aerobic glycolysis.

Publication types

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

MeSH terms

  • Acetylation
  • Acetylglucosamine / metabolism
  • Animals
  • Antigens, Neoplasm / metabolism*
  • Carrier Proteins / metabolism*
  • Cell Line, Tumor
  • Datasets as Topic
  • Disease Progression
  • Female
  • Gene Expression Profiling
  • Glycolysis
  • HEK293 Cells
  • Histone Acetyltransferases / metabolism*
  • Humans
  • Hyaluronoglucosaminidase / metabolism*
  • Male
  • Membrane Proteins / metabolism*
  • Mice
  • N-Acetylglucosaminyltransferases / metabolism*
  • Neoplasm Grading
  • Neoplasm Staging
  • Neoplasms / metabolism
  • Neoplasms / pathology*
  • Protein Processing, Post-Translational
  • Thyroid Hormone-Binding Proteins
  • Thyroid Hormones / metabolism*
  • Tissue Array Analysis
  • Up-Regulation
  • Xenograft Model Antitumor Assays

Substances

  • Antigens, Neoplasm
  • Carrier Proteins
  • Membrane Proteins
  • Thyroid Hormones
  • Histone Acetyltransferases
  • N-Acetylglucosaminyltransferases
  • OGT protein, human
  • OGA protein, human
  • Hyaluronoglucosaminidase
  • Acetylglucosamine