GEFs and GAPs: Critical Elements in the Control of Small G Proteins

Cell. 2007 Jun 1;129(5):865-77. doi: 10.1016/j.cell.2007.05.018.

Abstract

Guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs) regulate the activity of small guanine nucleotide-binding (G) proteins to control cellular functions. In general, GEFs turn on signaling by catalyzing the exchange from G-protein-bound GDP to GTP, whereas GAPs terminate signaling by inducing GTP hydrolysis. GEFs and GAPs are multidomain proteins that are regulated by extracellular signals and localized cues that control cellular events in time and space. Recent evidence suggests that these proteins may be potential therapeutic targets for developing drugs to treat various diseases, including cancer.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • GTPase-Activating Proteins / antagonists & inhibitors
  • GTPase-Activating Proteins / chemistry
  • GTPase-Activating Proteins / metabolism*
  • Guanine Nucleotide Exchange Factors / antagonists & inhibitors
  • Guanine Nucleotide Exchange Factors / chemistry
  • Guanine Nucleotide Exchange Factors / metabolism*
  • Humans
  • Models, Molecular
  • Monomeric GTP-Binding Proteins / chemistry
  • Monomeric GTP-Binding Proteins / metabolism*
  • Neoplasms / drug therapy
  • Signal Transduction

Substances

  • GTPase-Activating Proteins
  • Guanine Nucleotide Exchange Factors
  • Monomeric GTP-Binding Proteins