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Science 18 December 1992: Vol. 258. no. 5090, pp. 1944 - 1946 DOI: 10.1126/science.1335166
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Articles
Science, Vol 258, Issue 5090, 1944-1946
Copyright © 1992 by American Association for the Advancement of Science
Retinoids selective for retinoid X receptor response pathways
JM Lehmann,
L Jong,
A Fanjul,
JF Cameron,
XP Lu,
P Haefner,
MI Dawson,
and
M Pfahl
Cancer Center, La Jolla Cancer Research Foundation, La Jolla, CA 92037.
Retinoids have a broad spectrum of biological activities and are useful therapeutic agents. Their physiological activities are mediated by two types of receptors, the retinoic acid receptors (RARs) and the retinoid X receptors (RXRs). RARs, as well as several related receptors, require heterodimerization with RXRs for effective DNA binding and function. However, in the presence of 9-cis-retinoic acid, a ligand for both RARs and RXRs, RXRs can also form homodimers. A series of retinoids is reported that selectively activates RXR homodimers but does not affect RAR-RXR heterodimers and thus demonstrates that both retinoid response pathways can be independently activated.
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