GEFs and GAPs: critical elements in the control of small G proteins

Johannes L Bos; Holger Rehmann; Alfred Wittinghofer

doi:10.1016/j.cell.2007.05.018

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.

Authors

Johannes L Bos¹, Holger Rehmann, Alfred Wittinghofer

Affiliation

¹ Department of Physiological Chemistry and Centre of Biomedical Genetics, UMC Utrecht Universiteitsweg 100, 3584 CG Utrecht, The Netherlands. j.l.bos@umcutrecht.nl

PMID: 17540168
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