Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor

Bioorg Med Chem Lett. 2003 Aug 18;13(16):2655-8. doi: 10.1016/s0960-894x(03)00575-4.

Abstract

Anti-androgens were designed based on the principle of inhibiting the folding of helix 12 of the nuclear androgen receptor. The prepared anti-androgens exhibited full antagonistic activity toward human prostate tumor LNCaP cells with T877A point-mutated nuclear androgen receptor, as far as examined, towards which other known anti-androgens, including hydroxyflutamide, are inactive or act as androgen agonists.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androgen Antagonists / chemical synthesis*
  • Androgen Antagonists / pharmacology
  • Binding, Competitive
  • Drug Design
  • Humans
  • Isoxazoles / chemical synthesis
  • Isoxazoles / pharmacology
  • Male
  • Molecular Structure
  • Point Mutation
  • Prostate-Specific Antigen / analysis
  • Protein Folding
  • Receptors, Androgen / biosynthesis
  • Receptors, Androgen / drug effects*
  • Receptors, Androgen / genetics
  • Testosterone
  • Tumor Cells, Cultured

Substances

  • Androgen Antagonists
  • Isoxazoles
  • Receptors, Androgen
  • Testosterone
  • Prostate-Specific Antigen