Inhibition of glutaminyl cyclase alters pyroglutamate formation in mammalian cells

Biochim Biophys Acta. 2006 Oct;1764(10):1618-25. doi: 10.1016/j.bbapap.2006.08.003. Epub 2006 Aug 16.

Abstract

Mammalian cell lines were examined concerning their Glutaminyl Cyclase (QC) activity using a HPLC method. The enzyme activity was suppressed by a QC specific inhibitor in all homogenates. Aim of the study was to prove whether inhibition of QC modifies the posttranslational maturation of N-glutamine and N-glutamate peptide substrates. Therefore, the impact of QC-inhibition on amino-terminal pyroglutamate (pGlu) formation of the modified amyloid peptides Abeta(N3E-42) and Abeta(N3Q-42) was investigated. These amyloid-beta peptides were expressed as fusion proteins with either the pre-pro sequence of TRH, to be released by a prohormone convertase, or as engineered amyloid precursor protein for subsequent liberation of Abeta(N3Q-42) after beta- and gamma-secretase cleavage during posttranslational processing. Inhibition of QC leads in both expression systems to significantly reduced pGlu-formation of differently processed Abeta-peptides. This reveals the importance of QC-activity during cellular maturation of pGlu-containing peptides. Thus, QC-inhibition should impact bioactivity, stability or even toxicity of pyroglutamyl peptides preventing glutamine and glutamate cyclization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoacyltransferases / analysis
  • Aminoacyltransferases / antagonists & inhibitors*
  • Amyloid beta-Peptides / chemistry
  • Amyloid beta-Peptides / genetics
  • Amyloid beta-Peptides / metabolism*
  • Animals
  • Cell Line
  • Chromatography, High Pressure Liquid
  • Humans
  • Mice
  • Peptide Fragments / chemistry
  • Peptide Fragments / genetics
  • Peptide Fragments / metabolism*
  • Pyrrolidonecarboxylic Acid / analysis
  • Pyrrolidonecarboxylic Acid / metabolism*

Substances

  • Amyloid beta-Peptides
  • Peptide Fragments
  • Aminoacyltransferases
  • glutaminyl-peptide cyclotransferase
  • Pyrrolidonecarboxylic Acid