9-cis retinoic acid is a high affinity ligand for the retinoid X receptor
RA Heyman, DJ Mangelsdorf, JA Dyck, RB Stein… - Cell, 1992 - cell.com
RA Heyman, DJ Mangelsdorf, JA Dyck, RB Stein, G Eichele, RM Evans, C Thaller
Cell, 1992•cell.comAll-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 …
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 …
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.
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