Exploiting IR-Inducible NQ01 Levels Using B-Lapachone, A Novel Apoptotic Agent

Abstract

We theorize that Beta-lapachone is an effective agent against prostate cancer (CaP) cells/tumors. It kills cells by targeting elevated NQ01 levels in CaP tissue. Beta-Lapachone targets ionizing radiation (IR)-inducible NQ01. Normal cells with little or no NQ01 levels are spared, while IR-treated CaP cells expressing NQ01 are killed by apoptosis. Beta-Lapachone killing of CaP tumors is independent of p53, pRb, cell cycle status, or hormone (non)responsiveness and involves calpain activation. We are testing this theory using NQ01-deficient LNCaP cells, and comparing these cells to constitutively expressing NQ01 cells, with or without inhibitors of the enzyme (i.e., dicoumarol) . We are examining whether constitutive or inducible NQ01 levels are required for radiosensitization by Beta-lapachone. In Aim 1, in vitro responses and mechanisms of cell death after Beta-lapachone are examined, with or without IR, using cultured human CaP cells. In Aim #2, we will examine the efficacy of radiosensitization by Beta-lapachone in vivo using human CaP xenografts in male nude mice. Preclinical animal studies to move Beta-lapachone, from the bench to clinical trials against CaP have started.

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Document Details

Document Type
Technical Report
Publication Date
Apr 01, 2002
Accession Number
ADA405451

Entities

People

  • David A. Boothman

Organizations

  • Case Western Reserve University

Tags

DTIC Thesaurus Topics

  • Body Weight
  • Breast Cancer
  • Cell Membrane
  • Cell Physiological Processes
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Confocal Microscopy
  • Drug Abuse
  • Indicator Dyes
  • Neoplasms
  • Oncology
  • Pharmacology
  • Programmed Cell Death
  • Tumor Cell Line

Fields of Study

  • Biology
  • Medicine

Readers

  • Cellular and Molecular Pathways of Apoptosis.
  • Oncology (Cancer Research).