9-cis retinoic acid is a high affinity ligand for the retinoid X receptor

Richard A. Heyman, David J. Mangelsdorf, Jacqueline A. Dyck, Robert B. Stein, Gregor Eichele, Ronald M. Evans, Christina Thaller

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Abstract

All-trans retinoic acid (RA) has previously been shown to modulate the transcriptional properties of the retinoic acid receptor (RAR) and retinoid X receptor (RXR). The inability of all-trans RA to bind to RXR suggests that it may be metabolized to a more active high affinity ligand. We report here an experimental approach that has identified 9-cis RA as an RXR ligand. It is up to 40-fold more potent than all-trans RA in transfection assays and binds with high affinity. The production of 9-cis RA in cultured cells and the identification of this molecule in liver and kidney demonstrates the existence of this molecule in living organisms. The discovery of this novel hormone points to the key role retinoid metabolism may have in generating new signaling pathways.

Original languageEnglish (US)
Pages (from-to)397-406
Number of pages10
JournalCell
Volume68
Issue number2
DOIs
StatePublished - Jan 24 1992

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ASJC Scopus subject areas

  • Cell Biology
  • Molecular Biology

Cite this

Heyman, R. A., Mangelsdorf, D. J., Dyck, J. A., Stein, R. B., Eichele, G., Evans, R. M., & Thaller, C. (1992). 9-cis retinoic acid is a high affinity ligand for the retinoid X receptor. Cell, 68(2), 397-406. https://doi.org/10.1016/0092-8674(92)90479-V