2-Methoxyestradiol as a Chemotherapeutic for Prostate Cancer

Abstract

2-Methoxyestradiol (2-ME) is an endogenous metabolite of estradiol with promise for cancer chemotherapy including advanced prostate cancer. Our hypothesis is one of the cancer-specific mechanisms whereby 2-ME exerts its anti-prostate cancer activity is the deregulated activation of cyclin BI/cdkl kinase during the cell cycle which results in the induction of apoptotic cell death. Several experimental results support this hypothesis: 1) there is a positive correlation between the levels of cyclin BI protein and the ability of 2-ME to increase apoptosis in prostate cancer cells; 2) overexpression of cyclin BI increases 2-ME-mediated apoptosis while inhibition of cdkl activity lowers 2-ME-mediated apoptosis; 3)10w doses of 2-ME and docetaxel can increase G2/M cell cycle arrest and apoptosis in prostate cancer cell lines and in the GyIT transgenic mouse model of prostate cancer greater than either drug alone. We conclude that 2-ME can increase apoptosis in prostate cancer cells because of the expression of cyclin BI prntein which is minimally expressed in normal cells.

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Document Details

Document Type
Technical Report
Publication Date
Apr 01, 2007
Accession Number
ADA472868

Entities

People

  • Carlos Perez-stable

Organizations

  • University of Miami

Tags

DTIC Thesaurus Topics

  • Androgen Receptors
  • Antineoplastic Agents
  • Apoptosis
  • Cancer
  • Cell Line
  • Cell Physiological Processes
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Chemotherapy
  • Diseases And Disorders
  • Epithelial Cells
  • Neoplasms
  • Programmed Cell Death
  • Prostate Cancer
  • Proteins
  • Therapy

Fields of Study

  • Biology
  • Medicine

Readers

  • Mathematics or Statistics
  • Molecular Biology and Genetics
  • Prostate Cancer Biology.