Retinoids selective for retinoid X receptor response pathways.

J M Lehmann; L Jong; A Fanjul; J F Cameron; X P Lu; P Haefner; M I Dawson; M Pfahl

doi:10.1126/science.1335166

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PubMed · 1335166

Retinoids selective for retinoid X receptor response pathways.

J M Lehmann·L Jong·A Fanjul·J F Cameron·X P Lu·P Haefner·M I Dawson·M Pfahl

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Abstract

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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Animals Cell Line Chloramphenicol O-Acetyltransferase Kinetics Macromolecular Substances Molecular Structure Receptors, Cell Surface Receptors, Retinoic Acid Recombinant Fusion Proteins Retinoid X Receptors Retinoids Structure-Activity Relationship Transcription Factors Transcription, Genetic Transfection Tretinoin Comparative Study Journal Article Research Support, U.S. Gov't, P.H.S.

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J M Lehmann, L Jong, A Fanjul, J F Cameron, X P Lu, P Haefner, M I Dawson, M Pfahl. 1992-12-18. Retinoids selective for retinoid X receptor response pathways.. https://doi.org/10.1126/science.1335166

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