Role of glycosylation on the secretion and biological activity of erythropoietin

Biochemistry. 1992 Oct 20;31(41):9871-6. doi: 10.1021/bi00156a003.

Abstract

The erythropoietin (EPO) molecule contains four carbohydrate chains. Three contain N-linkages to asparagines at positions 24, 38, and 83, and one contains an O-linkage to a serine at position 126. We constructed human EPO variants that eliminated the three N-glycosylation sites by replacing the asparagines with glutamines singly or in combination. The O-linked carbohydrate chain was removed by replacing the serine with glutamine, valine, histidine, or alanine. A variant with a double mutation (Gln38,83) and another with a triple mutation (Gln24,38,83) were secreted poorly from COS1 and CHO cells even though RNA encoding these variants was present. All other variants with mutations in N-linked glycosylation sites were secreted normally. Removal of any of the N-glycosylation sites reduced the in vivo but not the in vitro biological activity of the EPO molecule. All the mutations at Ser126, the O-glycosylation site, were secreted normally. In vitro activity was also unaffected except for Ala126 which had a 50-fold decrease. The Val126 variant was tested in vivo, and its specific activity was only slightly less than that of the native EPO, which indicates that the O-linked carbohydrate is not essential for activity.

MeSH terms

  • Animals
  • Asparagine / chemistry
  • CHO Cells
  • Carbohydrate Conformation
  • Carbohydrates / chemistry*
  • Cell Line
  • Cricetinae
  • Erythropoietin / chemistry
  • Erythropoietin / genetics
  • Erythropoietin / physiology*
  • Glutamine / chemistry
  • Glycosylation
  • Immunoblotting
  • Mutagenesis, Site-Directed
  • Protein Conformation
  • Structure-Activity Relationship
  • Transfection

Substances

  • Carbohydrates
  • Glutamine
  • Erythropoietin
  • Asparagine