Role of the C-terminus in the activity, conformation, and stability of interleukin-6

Protein Sci. 1993 Sep;2(9):1472-81. doi: 10.1002/pro.5560020911.

Abstract

Two murine interleukin-6 (mIL-6) variants were constructed using the polymerase chain reaction (PCR), one lacking the last five residues (183-187) at the C-terminus (pMC5) and another with the last five residues of mIL-6 substituted by the corresponding residues of human IL-6 (pMC5H). The growth stimulatory activity of pMC5 on the mouse hybridoma cell line 7TD1 was < 0.05% of mIL-6, whereas pMC5H and mIL-6 were equipotent. The loss of biological activity of pMC5 correlated with its negligible receptor binding affinity on 7TD1 cells, while the binding of pMC5H was comparable to that of mIL-6. Both pMC5 and pMC5H, like mIL-6, failed to interact with recombinant soluble human IL-6 receptor when assayed by surface plasmon resonance-based biosensor analysis. These studies suggest that the C-terminal seven amino acids of human IL-6, alone, do not define species specificity for receptor binding. A variety of biophysical techniques, as well as the binding of a conformational-specific monoclonal antibody, indicated that the global fold of the mIL-6 variants was similar to that of mIL-6, although small changes in the NMR spectra, particularly for pMC5, were observed. Some of these changes involved residues widely separated in the primary structure. For instance, interactions involving Tyr-22 were influenced by the C-terminal amino acids suggesting that the N- and C-termini of mIL-6 are in close proximity. Equilibrium unfolding experiments indicated that pMC5 was 0.8 kcal/mol less stable than mIL-6, whereas pMC5H was 1.4 kcal/mol more stable. These studies emphasize the structural importance of the C-terminal amino acids of IL-6 and suggest that truncation or mutation of this region could lead to small but significant alterations in other regions of the molecule.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antibodies, Monoclonal / metabolism
  • Base Sequence
  • Drug Stability
  • Escherichia coli / genetics
  • Humans
  • Interleukin-6 / chemistry*
  • Interleukin-6 / metabolism
  • Interleukin-6 / pharmacology
  • Magnetic Resonance Spectroscopy
  • Mice
  • Molecular Sequence Data
  • Mutagenesis
  • Peptide Fragments / chemistry*
  • Polymerase Chain Reaction
  • Protein Conformation
  • Receptors, Interleukin / metabolism
  • Receptors, Interleukin-6
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • Structure-Activity Relationship
  • Thermodynamics

Substances

  • Antibodies, Monoclonal
  • Interleukin-6
  • Peptide Fragments
  • Receptors, Interleukin
  • Receptors, Interleukin-6
  • Recombinant Proteins