A stromelysin assay for the assessment of metalloprotease inhibitors on human aggregated proteoglycan

Agents Actions. 1993:39 Spec No:C151-3. doi: 10.1007/BF01972750.

Abstract

Human proteoglycan was aggregated to an immobilized hyaluronan solid phase on a 96-well ELISA plate. This complex was then degraded by recombinant human stromelysin. The remaining proteoglycan fragments were detected using a monoclonal antibody probe directed against the chondroitin sulfate (CS) region of the core protein. Stromelysin degraded the aggregate in a time and dose dependent manner as reflected by the loss of the CS epitope. Assay sensitivity was 0.125 U/well with total loss of the CS epitope occurring at 4 U/well. o-phenanthroline (IC50 = 52 microM) and U24522 (IC50 = 9 microM) inhibited degradation, while phosphoramidon did not. Serine and cysteine protease inhibitors had no effect. A comparative analysis of this assay with a reference method, substance P assay, gave similar inhibitor profiles. The use of aggregated human proteoglycan (native conformation) as a substrate, may better reflect how stromelysin inhibitors behave in the presence of complex substrates such as cartilage matrix.

MeSH terms

  • Animals
  • Antibodies, Monoclonal
  • Cartilage, Articular / metabolism
  • Chondroitin Sulfates
  • Enzyme-Linked Immunosorbent Assay
  • Femur
  • Glycopeptides / pharmacology
  • Humans
  • Hyaluronic Acid / chemistry
  • Hyaluronic Acid / immunology
  • Matrix Metalloproteinase 3
  • Metalloendopeptidases / antagonists & inhibitors
  • Metalloendopeptidases / metabolism*
  • Mice
  • Phenanthrolines / pharmacology
  • Proteoglycans / chemistry
  • Proteoglycans / immunology
  • Proteoglycans / metabolism*
  • Recombinant Proteins / metabolism
  • Substance P / metabolism

Substances

  • Antibodies, Monoclonal
  • Glycopeptides
  • Phenanthrolines
  • Proteoglycans
  • Recombinant Proteins
  • Substance P
  • Hyaluronic Acid
  • Chondroitin Sulfates
  • Metalloendopeptidases
  • Matrix Metalloproteinase 3
  • phosphoramidon
  • 1,10-phenanthroline