Estrogen Receptor Microarrays: Subtype-Selective Ligand Binding

Sung Hoon Kim, Anobel Tamrazi, Kathryn E. Carlson, Jonathan R. Daniels, In Young Lee, John A. Katzenellenbogen

Research output: Contribution to journalArticlepeer-review

Abstract

We present the first example of a nuclear hormone receptor microarray, using for illustration the ligand-binding domains of the two estrogen receptors, ERα-LBD and ERβ-LBD. The proteins are printed and allowed to attach to aldehyde slides; the efficiency of attachment depends on whether the LBD is liganded with agonists (low attachment) versus liganded with antagonists or unliganded (high attachment). This suggests that attachment is orientation specific and involves principally a single lysine residue. The attached ERs retain good ligand-binding activity that can be assessed using an estradiol-fluorophore conjugate, and specific and ER subtype-selective binding of ligands can be determined conveniently in competitive binding assays. This powerful new, high-throughput technique to study ligand binding to ER-LBDs can be extended to other nuclear hormone receptors and adapted to assay the recruitment of coregulator proteins.

Original languageEnglish (US)
Pages (from-to)4754-4755
Number of pages2
JournalJournal of the American Chemical Society
Volume126
Issue number15
DOIs
StatePublished - Apr 21 2004

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry

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