The TWEAK receptor Fn14 is a therapeutic target in melanoma: immunotoxins targeting Fn14 receptor for malignant melanoma treatment

J Invest Dermatol. 2013 Apr;133(4):1052-62. doi: 10.1038/jid.2012.402. Epub 2012 Nov 29.

Abstract

Fibroblast growth factor-inducible protein 14 (Fn14), the cell surface receptor for tumor necrosis factor-like weak inducer of apoptosis (TWEAK), is overexpressed in various human solid tumor types and can be a negative prognostic indicator. We detected Fn14 expression in ∼60% of the melanoma cell lines we tested, including both B-Raf WT and B-Raf(V600E) lines. Tumor tissue microarray analysis indicated that Fn14 expression was low in normal skin, but elevated in 173/190 (92%) of primary melanoma specimens and in 86/150 (58%) of melanoma metastases tested. We generated both a chemical conjugate composed of the recombinant gelonin (rGel) toxin and the anti-Fn14 antibody ITEM-4 (designated ITEM4-rGel) and a humanized, dimeric single-chain antibody of ITEM-4 fused to rGel (designated hSGZ). Both ITEM4-rGel and hSGZ were highly cytotoxic to a panel of different melanoma cell lines. Mechanistic studies showed that both immunotoxins induced melanoma cell necrosis. In addition, these immunotoxins could upregulate the cellular expression of Fn14 and trigger cell-signaling events similar to the Fn14 ligand TWEAK. Finally, treatment of mice bearing human melanoma MDA-MB-435 xenografts with either ITEM4-rGel or hSGZ showed significant tumor growth inhibition compared with controls. We conclude that Fn14 is a therapeutic target in melanoma and the hSGZ construct appears to warrant further development as a therapeutic agent against Fn14-positive melanoma.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cell Death / drug effects
  • Cell Line, Tumor
  • Drug Design
  • Female
  • Humans
  • Immunologic Factors / genetics
  • Immunologic Factors / immunology
  • Immunologic Factors / pharmacokinetics*
  • Immunotoxins / genetics
  • Immunotoxins / immunology
  • Immunotoxins / pharmacokinetics*
  • Melanoma / drug therapy*
  • Melanoma / immunology
  • Mice
  • Mice, Inbred BALB C
  • NF-kappa B / metabolism
  • Protein Binding / immunology
  • Receptors, Tumor Necrosis Factor / immunology*
  • Receptors, Tumor Necrosis Factor / metabolism
  • Signal Transduction / drug effects
  • Signal Transduction / immunology
  • Skin Neoplasms / drug therapy*
  • Skin Neoplasms / immunology
  • TWEAK Receptor
  • Up-Regulation / drug effects
  • Up-Regulation / immunology
  • Xenograft Model Antitumor Assays

Substances

  • Immunologic Factors
  • Immunotoxins
  • NF-kappa B
  • Receptors, Tumor Necrosis Factor
  • TNFRSF12A protein, human
  • TWEAK Receptor
  • Tnfrsf12a protein, mouse