Antineoplastic ribonucleases selectively kill thyroid carcinoma cells via caspase-mediated induction of apoptosis

J Clin Endocrinol Metab. 2003 Jun;88(6):2900-7. doi: 10.1210/jc.2002-020373.

Abstract

Bovine seminal ribonuclease (BS-RNase), a natural dimeric homolog of bovine pancreatic RNase (RNase A), and HHP2-RNase, an engineered dimeric form of human pancreatic RNase (HP-RNase), are endowed with powerful antitumor effects. Here we show that BS- and HHP2-RNases, but not monomeric RNase A, induce apoptosis of human thyroid carcinoma cell lines. RNase-induced apoptosis was associated with activation of initiation caspase-8 and -9. This was followed by activation of executioner caspase-3, leading to the proteolytic cleavage of poly(ADP-ribose) polymerase. The caspase inhibitor Z-Val-Ala-Asp-(OMe)-fluoromethylketone protected thyroid cancer cells from BS-RNase-induced apoptosis. RNase-triggered apoptosis and caspase activation were accompanied by reduced phosphorylation of Akt/protein kinase B (PKB), a serine-threonine kinase that when phosphorylated is able to deliver survival signals to cancer cells. BS-RNase antitumor effects in nude mice were accompanied by caspase activation and apoptosis. Because of the high selectivity of apoptotic effects for malignant cells, BS- and HHP2-RNase are promising tools for the treatment of aggressive thyroid cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Chloromethyl Ketones / pharmacology
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Apoptosis*
  • Carcinoma / physiopathology*
  • Caspase Inhibitors
  • Caspases / metabolism*
  • Cysteine Proteinase Inhibitors / pharmacology
  • Endoribonucleases / pharmacology*
  • Humans
  • Mice
  • Mice, Nude
  • Phosphorylation / drug effects
  • Protein Serine-Threonine Kinases*
  • Proto-Oncogene Proteins / metabolism
  • Proto-Oncogene Proteins c-akt
  • Ribonuclease, Pancreatic / pharmacology*
  • Thyroid Neoplasms / physiopathology*
  • Tumor Cells, Cultured

Substances

  • Amino Acid Chloromethyl Ketones
  • Antineoplastic Agents
  • Caspase Inhibitors
  • Cysteine Proteinase Inhibitors
  • Proto-Oncogene Proteins
  • benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone
  • AKT1 protein, human
  • Protein Serine-Threonine Kinases
  • Proto-Oncogene Proteins c-akt
  • Endoribonucleases
  • ribonuclease SPL
  • Ribonuclease, Pancreatic
  • pancreatic RNase 2, human
  • Caspases