Skip to main content
padlock icon - secure page this page is secure

Open Access Identification of Endocrine-Disrupting Compounds Using Nanoelectrospray Ionization Mass Spectrometry

Download Article:
(PDF 1,186.1 kb)
A method using chip-based nanoelectrospray mass spectrometry (nanoESI-MS) is described to detect noncovalent ligand binding to the human estrogen receptor alpha ligand-binding domain (hERα LBD). This system represents an important environmental interest, because a wide variety of molecules, known as endocrine-disrupting compounds (EDCs), can bind to the estrogen receptor (ER) and induce adverse health effects in wildlife and humans. An efficient analytical method is therefore required to identify EDCs and characterize their solution-phase binding affinity and character (i.e. agonist or antagonist). Using proper experimental conditions, the nanoESI-MS approach allowed the detection of specific ligand interactions with hERα LBD. The best approach to evaluate solution-binding affinity by nanoESI-MS was to perform competitive binding experiments with 17β-estradiol (E2) as a reference ligand. Among the ligands tested, the relative binding affinity for hERα LBD measured by nanoESI-MS was 4-hydroxytamoxifen ≈ diethylstilbestrol > E2 ≫ genistein ≫ bisphenol A, consistent with the order of the binding affinities in solution. To discern agonist from antagonist, we used the specificity of a coactivator peptide for agonist-bound receptor. A specific coactivator-hERα LBD complex was detected only in the presence of an agonist ligand. Therefore, the specificity of nanoESI-MS combined with its speed (1 min/ligand), low sample consumption (90 pmol protein/ligand), and its sensitivity for ligand (30 ng/ml) demonstrates that this method is promising for the identification and characterization of suspected ER ligands in a high-throughput manner.

46 References.

No Supplementary Data.
No Article Media
No Metrics


Document Type: Research Article

Publication date: May 1, 2008

More about this publication?
  • International Journal for Chemistry and Official Membership Journal of the Swiss Chemical Society (SCS) and its Divisions

    CHIMIA, a scientific journal for chemistry in the broadest sense, is published 10 times a year and covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.

  • Editorial Board
  • Information for Authors
  • Subscribe to this Title
  • Information for Advertisers
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more