@article{6e2011ad251c4aae9356cc790c0e63d3,
title = "9-cis retinoic acid is a high affinity ligand for the retinoid X receptor",
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.",
author = "Heyman, {Richard A.} and Mangelsdorf, {David J.} and Dyck, {Jacqueline A.} and Stein, {Robert B.} and Gregor Eichele and Evans, {Ronald M.} and Christina Thaller",
note = "Funding Information: Mike McClurg, Steve Lazarchik, and Peter Syka for expert technical assistance; David Clemm for providing baculoviral-expressed retinoid receptors; Drs. Charles Pathiranaand Marcus Boehm for their insights on retinoid chemistry; Dr. Tina Berger and members of New Leads Discovery for their assistance with the transfection assays; Drs. J. Wesley Pike, Henry Sucov, and Mike McKeown for their discussions of this research; and Elaine Stevens and Cynthia Foster for manuscript preparation. R. A. H. was a Salk Institute Staff Scientist and is Senior Research Manager at Ligand Pharmaceuticals, D. J. M. is a Staff Scientist at the Salk Institute, and R. M. E. is an Investigator of the Howard Hughes Medical Institute at the Salk Institute for Biological Studies. This work was supported by HHMI, NIH, NCI, the Mathers Foundation, and a f&Knight Development Award to G. E.",
year = "1992",
month = jan,
day = "24",
doi = "10.1016/0092-8674(92)90479-V",
language = "English (US)",
volume = "68",
pages = "397--406",
journal = "Cell",
issn = "0092-8674",
publisher = "Cell Press",
number = "2",
}