Chemical synthesis, purification and folding of the human monocyte chemotactic proteins MCP-2 and MCP-3 into biologically active chemokines

Cytokine. 1995 Feb;7(2):97-104. doi: 10.1006/cyto.1995.1013.

Abstract

Monocyte chemotactic proteins 2 and 3 (MCP-2 and MCP-3) are chemokines structurally and functionally related to MCP-1. In contrast to MCP-1, they are produced in low amounts by stimulated leukocytes or tumour cells. As an alternative method to generate sufficient protein for in vitro and in vivo characterization of MCP-2 and MCP-3, we have synthesized both 76-residue chemokines using Fmoc chemistry. After automated solid phase peptide synthesis at a 0.05 to 0.25 mmol scale, and purification to homogeneity by C-8 RP-HPLC, correct disulfide bridges were formed in a mixture of oxidized and reduced glutathione. The synthesis was biochemically controlled by peptide sequencing of intermediate products and proteolytic fragments of the 76-residue chemokines and by mass analysis. Purified synthetic MCP-2 and MCP-3 coeluted and comigrated with their natural counterparts on analytical reverse phase columns and SDS-PAGE, respectively. Purified and folded MCP-2 and MCP-3 were chemotactic for monocytes at 7.5 ng/ml and 5 ng/ml, respectively. These minimal effective concentrations are comparable to those of the natural chemokines. Synthetic MCPs did not induce neutrophil chemotaxis. Automated Fmoc peptide synthesis is thus a useful method, allowing fast production of chemokines and analogues thereof.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Biological Assay
  • Chemokine CCL7
  • Chemokine CCL8
  • Chemotactic Factors / chemical synthesis*
  • Chemotactic Factors / chemistry*
  • Chemotactic Factors / pharmacology
  • Chemotaxis, Leukocyte / drug effects*
  • Chromatography, High Pressure Liquid
  • Cytokines*
  • Disulfides
  • Electrophoresis, Polyacrylamide Gel
  • Endopeptidases
  • Humans
  • Molecular Sequence Data
  • Monocyte Chemoattractant Proteins*
  • Monocytes / drug effects
  • Monocytes / physiology
  • Neutrophils / physiology
  • Peptide Fragments / chemistry
  • Peptide Fragments / isolation & purification
  • Protein Folding*

Substances

  • CCL7 protein, human
  • CCL8 protein, human
  • Chemokine CCL7
  • Chemokine CCL8
  • Chemotactic Factors
  • Cytokines
  • Disulfides
  • Monocyte Chemoattractant Proteins
  • Peptide Fragments
  • Endopeptidases