Nuclear-receptor ligands and ligand-binding domains

Ross V. Weatherman, Robert J. Fletterick, Thomas S. Scanlan

Research output: Contribution to journalReview article

266 Scopus citations

Abstract

The determination of several structures of nuclear receptor ligand binding domains (LBD) has led to new insights into the mechanism of action of this very important class of receptors. This review describes and compares the different LBD structures and their relationship to the function of the nuclear receptors. The role of the ligand in the LBD structures and the implications of ligand structure on receptor activity are also discussed. Structural information regarding interactions between the LBD and coactivator proteins and the potential role of these interactions in ligand agonism and antagonism is reviewed. Different pathways for nuclear receptor signaling and the use of new ligands to investigate these pathways are also described.

Original languageEnglish (US)
Pages (from-to)559-581
Number of pages23
JournalAnnual Review of Biochemistry
Volume68
DOIs
StatePublished - Oct 4 1999

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Keywords

  • Hormone agonists/antagonists
  • Intracellular receptors
  • Intracellular signaling
  • Steroid/thyroid hormone receptors
  • Transcriptional regulation

ASJC Scopus subject areas

  • Biochemistry

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