A selective assay for endooligopeptidase A based on the cleavage of fluorogenic substrate structurally related to enkephalin

Biochem Biophys Res Commun. 1990 Dec 14;173(2):647-52. doi: 10.1016/s0006-291x(05)80084-1.

Abstract

A novel quenched fluorescence substrate, QF-ERP7 (Abz-G-G-F-L-R-R-V-EDDn), structurally related to enkephalins, proved to be suitable for assaying the endooligopeptidase A (E.C.3.4.22.19) activity. The enzyme only splits the L-R bond (Km 1.75 microM, Kcat 8.25 s-1), a reaction efficiently blocked by anti-endooligopeptidase A antibodies and by inhibitor and alternative substrates of the enzyme. Evidences based on the action of inhibitors and on the analysis of QF-ERP7 fragments demonstrated that endooligopeptidase A contributes with 100% of the QF-ERP7 cleaving activity found in the cytosol of rabbit brain homogenates and with 85% of that recovered in the membrane fraction. Homologous substrates, Abz-G-G-F-L-R-R-EDDn and Abz-G-G-F-L-R-EDDn, were resistant to hydrolysis. The convenience and sensitivity of the fluorimetric assay based on the QF-ERP7 moiety offers several advantages compared with previously described painstaking procedures for endooligopeptidase A activity measurements, what will certainly contribute to further our understanding of the role of this enzyme on the peptide hormone metabolism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antibodies / immunology
  • Chromatography, High Pressure Liquid
  • Cysteine Endopeptidases / analysis*
  • Cysteine Endopeptidases / immunology
  • Enkephalins*
  • Ethylenediamines*
  • Fluorescence*
  • Hydrolysis
  • Metalloendopeptidases*
  • Molecular Sequence Data
  • Oligopeptides*
  • Rabbits

Substances

  • Antibodies
  • Enkephalins
  • Ethylenediamines
  • Oligopeptides
  • QF-ERP7
  • Cysteine Endopeptidases
  • Metalloendopeptidases
  • thimet oligopeptidase