GTP-specific fab fragment-based GTPase activity assay

Anal Chem. 2015 Mar 17;87(6):3527-34. doi: 10.1021/acs.analchem.5b00117. Epub 2015 Mar 3.

Abstract

GTPases are central cellular signaling proteins, which cycle between a GDP-bound inactive and a GTP-bound active conformation in a controlled manner. Ras GTPases are frequently mutated in cancer and so far only few experimental inhibitors exist. The most common methods for monitoring GTP hydrolysis rely on luminescent GDP- or GTP-analogs. In this study, the first GTP-specific Fab fragment and its application are described. We selected Fab fragments using the phage display technology. Six Fab fragments were found against 2'/3'-GTP-biotin and 8-GTP-biotin. Selected antibody fragments allowed specific detection of endogenous, free GTP. The most potent Fab fragment (2A4(GTP)) showed over 100-fold GTP-specificity over GDP, ATP, or CTP and was used to develop a heterogeneous time-resolved luminescence based assay for the monitoring of GTP concentration. The method allows studying the GEF dependent H-Ras activation (GTP binding) and GAP-catalyzed H-Ras deactivation (GTP hydrolysis) at nanomolar protein concentrations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibody Specificity*
  • Enzyme Activation
  • Enzyme Assays / methods*
  • Enzyme Inhibitors / pharmacology
  • GTP Phosphohydrolases / antagonists & inhibitors
  • GTP Phosphohydrolases / metabolism*
  • GTPase-Activating Proteins / metabolism
  • Guanosine Triphosphate / immunology*
  • Guanosine Triphosphate / metabolism*
  • Humans
  • Hydrolysis
  • Immunoglobulin Fab Fragments / immunology*

Substances

  • Enzyme Inhibitors
  • GTPase-Activating Proteins
  • Immunoglobulin Fab Fragments
  • Guanosine Triphosphate
  • GTP Phosphohydrolases