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Science 18 December 1992:
Vol. 258. no. 5090, pp. 1944 - 1946
DOI: 10.1126/science.1335166

Articles

Science, Vol 258, Issue 5090, 1944-1946
Copyright © 1992 by American Association for the Advancement of Science


articles

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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Evidence that Retinoid X Receptors Mediate Retinoid-dependent Transcriptional Activation of the Retinoic Acid Receptor [IMAGE] Gene in S91 Melanoma Cells.
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Ligand-dependent Antagonism by Retinoid X Receptors of Inhibitory Thyroid Hormone Response Elements.
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A novel pathway for vitamin A signaling mediated by RXR heterodimerization with NGFI-B and NURR1..
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Evidence for the Involvement of Retinoic Acid Receptor RARalpha-dependent Signaling Pathway in the Induction of Tissue Transglutaminase and Apoptosis by Retinoids.
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J. Biol. Chem. 270, 3001-3011
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Similar Ligand-induced Conformational Changes of Thyroid Hormone Receptors Regulate Homo- and Heterodimeric Functions.
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Acute Promyelocytic Leukemia.
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Direct Functional Interactions between Insulin-like Growth Factor-binding Protein-3 and Retinoid X Receptor-alpha Regulate Transcriptional Signaling and Apoptosis.
B. Liu, H.-Y. Lee, S. A. Weinzimer, D. R. Powell, J. L. Clifford, J. M. Kurie, and P. Cohen (2000)
J. Biol. Chem. 275, 33607-33613
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