9-Cis retinoic acid stereoisomer binds and activates the nuclear receptor RXRα
- 1 January 1992
- journal article
- Published by Springer Science and Business Media LLC in Nature
- Vol. 355 (6358), 359-361
- https://doi.org/10.1038/355359a0
Abstract
Vitamin A (retinol) and its natural derivatives are required for many physiological processes. The activity of retinoids is thought to be mediated by interactions with two subfamilies of nuclear retinoic acid receptors, RAR and RXR. The RARs bind all-trans retinoic acid (t-RA) with high affinity and alter gene expression as a consequence of this direct ligand interaction. RXR alpha is activated by t-RA, yet has little binding affinity for this ligand. t-RA may be converted to a more proximate ligand that directly binds and activates RXR alpha, and we have developed a method of nuclear receptor-dependent ligand trapping to test this hypothesis. Here we report the identification of a stereoisomer of retinoic acid, 9-cis retinoic acid, which directly binds and activates RXR alpha. These results suggest a new role for isomerization in the physiology of natural retinoids.Keywords
This publication has 31 references indexed in Scilit:
- 6′-Substituted naphthalene-2-car☐ylic acid analogs, a new class of retinoic acid receptor subtype-specific ligandsBiochemical and Biophysical Research Communications, 1991
- Characterization of DNA binding and retinoic acid binding properties of retinoic acid receptor.Proceedings of the National Academy of Sciences of the United States of America, 1991
- Retinoic acid and synthetic analogs differentially activate retinoic acid receptor dependent transcriptionBiochemical and Biophysical Research Communications, 1990
- A third human retinoic acid receptor, hRAR-gamma.Proceedings of the National Academy of Sciences of the United States of America, 1989
- Identification of a second human retinoic acid receptorNature, 1988
- Identification of a receptor for the morphogen retinoic acidNature, 1987
- A human retinoic acid receptor which belongs to the family of nuclear receptorsNature, 1987
- Identification and spatial distribution of retinoids in the developing chick limb budNature, 1987
- Cellular Biology and Biochemistry of the RetinoidsPublished by Elsevier BV ,1984
- The retinol requirements of rats for spermatogenesis and visionBritish Journal of Nutrition, 1969