Dynamic regulation of GDP binding to G proteins revealed by magnetic field-dependent NMR relaxation analyses

Nat Commun. 2017 Feb 22:8:14523. doi: 10.1038/ncomms14523.

Abstract

Heterotrimeric guanine-nucleotide-binding proteins (G proteins) serve as molecular switches in signalling pathways, by coupling the activation of cell surface receptors to intracellular responses. Mutations in the G protein α-subunit (Gα) that accelerate guanosine diphosphate (GDP) dissociation cause hyperactivation of the downstream effector proteins, leading to oncogenesis. However, the structural mechanism of the accelerated GDP dissociation has remained unclear. Here, we use magnetic field-dependent nuclear magnetic resonance relaxation analyses to investigate the structural and dynamic properties of GDP bound Gα on a microsecond timescale. We show that Gα rapidly exchanges between a ground-state conformation, which tightly binds to GDP and an excited conformation with reduced GDP affinity. The oncogenic D150N mutation accelerates GDP dissociation by shifting the equilibrium towards the excited conformation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • GTP-Binding Protein alpha Subunits / chemistry
  • GTP-Binding Protein alpha Subunits / metabolism*
  • Guanosine Diphosphate / metabolism*
  • Humans
  • Magnesium / pharmacology
  • Magnetic Fields*
  • Magnetic Resonance Spectroscopy*
  • Mutant Proteins / metabolism
  • Peptides / metabolism
  • Protein Conformation

Substances

  • GTP-Binding Protein alpha Subunits
  • Mutant Proteins
  • Peptides
  • Guanosine Diphosphate
  • Magnesium