Interleukin 6 receptor superantagonists are potent inducers of human multiple myeloma cell death

Cancer Res. 1996 Sep 15;56(18):4213-8.

Abstract

Interleukin-6 (IL-6) plays a central role in the pathogenesis of multiple myeloma, acting as both a growth and a survival factor for myeloma cells. A series of IL-6 receptor antagonists that are IL-6 variants has been recently obtained, the affinity of which for the ligand-specific receptor chain IL-6R alpha has been maintained or even increased, but the signaling of which is impaired by not being able to bind and/or dimerize the signaling chain gp130. Although IL-6 antagonists have been shown to inhibit the growth of IL-6-dependent myeloma, no information has been gathered on their ability to induce myeloma cell death. We show here that IL-6 receptor antagonists are pro-apoptotic factors for the IL-6-dependent human myeloma cell line XG-1. Their capacity to induce cell death is in direct relation to their affinity for IL-6R alpha, degree of gp130 binding impairment, and efficiency to inhibit intracellular signaling events. Interestingly, the most potent pro-apoptotic molecule, Sant7, counteracts the protective autocrine effect exercised by the limited amounts of IL-6 produced by XG-1 cells and is thus able to induce cell death at higher rate than just IL-6 deprivation. These findings are particularly relevant for the therapy of multiple myeloma.

MeSH terms

  • Antigens, CD / biosynthesis
  • Antigens, CD / chemistry
  • Antigens, CD / physiology*
  • Apoptosis* / drug effects
  • Cell Line
  • Flow Cytometry
  • Humans
  • Immunotherapy
  • Interleukin-6 / biosynthesis
  • Interleukin-6 / pharmacology*
  • Multiple Myeloma / immunology*
  • Multiple Myeloma / pathology*
  • Multiple Myeloma / therapy
  • Receptors, Interleukin / biosynthesis
  • Receptors, Interleukin / chemistry
  • Receptors, Interleukin / physiology*
  • Receptors, Interleukin-6
  • Recombinant Proteins / biosynthesis
  • Recombinant Proteins / pharmacology
  • Signal Transduction
  • Tumor Cells, Cultured

Substances

  • Antigens, CD
  • Interleukin-6
  • Receptors, Interleukin
  • Receptors, Interleukin-6
  • Recombinant Proteins