Rapid on-line profiling of estrogen receptor binding metabolites of tamoxifen

J Med Chem. 2006 Jun 1;49(11):3287-92. doi: 10.1021/jm0507936.


Here we present a high-resolution screening (HRS) methodology for postcolumn on-line profiling of metabolites with affinity for the estrogen receptor alpha (ERalpha). Tamoxifen, which is metabolized into multiple metabolites, was used as the model compound. Most of the 14 metabolites detected exhibited affinity for the ERalpha. The HRS methodology shows great potential for metabolite bio-affinity profiling and application in drug discovery and development.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / metabolism*
  • Antineoplastic Agents / pharmacokinetics
  • Chromatography, High Pressure Liquid / instrumentation
  • Estrogen Antagonists / metabolism*
  • Estrogen Antagonists / pharmacokinetics
  • Estrogen Receptor alpha / metabolism*
  • In Vitro Techniques
  • Ligands
  • Microsomes, Liver / metabolism
  • Rats
  • Spectrometry, Mass, Electrospray Ionization
  • Swine
  • Tamoxifen / metabolism*
  • Tamoxifen / pharmacokinetics


  • Antineoplastic Agents
  • Estrogen Antagonists
  • Estrogen Receptor alpha
  • Ligands
  • Tamoxifen